SUPER PHARMA TABLE

Maria Yña Eluisia T. Pereyra RPh, MD, MBA

DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES

1. AUTONOMIC DRUGS
Cholinomimetics
A. Direct Acting Choline Esters
i. Acetylcholine Muscarinic agonist; activates M1 through M3 receptors in CNS stimulation, miosis, cyclospasm, very short lived DOA: 5-30sec,
all peripheral tissues. Results to increased secretion, brochoconstriction, excessive GI and GU smooth apidly hydrolyzed by AChE; acts on
smooth muscle contraction (except in vascular smooth muscle contraction, increased secretory activity both M and N receptors
muscles where it causes relaxation) and changes in heart of sweat gland, airways etc, vasodilation
rate
ii.Betanechol Muscarinic agonist; activates M1 through M3 receptors in Cylospasm, diarrhea, urinary urgency, Results in smooth muscle
all peripheral tissues (same as Ach) ; for Bladder and bowel vasodilation, reflex tachycardia, sweating contraction except in vascular
atony smooth muscles where it causes
relaxation; resistant to AChE, orally
active, act on M receptors only
iii. Carbachol Nonselective muscarinic and nicotinic agonist; similar to Cylospasm, diarrhea, urinary urgency, acts on both M and N receptors,
betanechol; used topically for glaucoma treatment vasodilation, reflex tachycardia, sweating DOA: 30mins-2hrs

B. Direct Acting Muscarinic Alkaloids

i. Pilocarpine Partial muscarinic agonist; used for treatment of Miosis, blurring of vision good lipid solubility compared to
Glaucoma, Sjogren's syndrome and Sicca syndrome choline esters

C. Direct Acting Nicotinic Agonists

i. Nicotine Agonist at both NN and NM receptos; activates autonomic Generalized ganglionic stimulation (hypertension, Able to enter the CNS and activates
post ganglionic neurons (both sympathetic and tachycardia, nausea, vomiting, diarrhea) NN receptors ; DOA: 1-6h only
parasympathetic) and skeletal muscle neuromuscular end
plates ; for Smoking Cessation
ii. Varenicline Selective partial agonist at nicotinic receptors; used Generalized ganglionic stimulation (hypertension, longer DOA than nicotine: 12-24h
exclusively for smoking cessation tachycardia, nausea, vomiting, diarrhea)
D. Short Acting Cholinesterase Inhibitor (Alcohol)
i. Edrophonium Binds briefly to active site of acetylcholinesterase (AChE) Miosis, salivation, nausea, vomiting, diarrhea, parenteral, very short lived DOA: 5-
and prevents access of acetylcholine (Ach); Amplifies all bradycardia 15min
actions of Ach; increases parasympathetic activity and
somatic neuromuscular transmission ; for Myasthenia
gravis diagnosis (Tensilon test)
E. Intermediate Acting Cholinesterase Inhbitors (Carbamates)
i. Neostigmine Forms covalent bonds with AChE, but is hydrolyzed and Miosis, salivation, nausea, vomiting, diarrhea, poor lipid solubility, oral, DOA:
released; Longer acting than Edrophonium ; for bradycardia 30min-2h
Myasthenia gravis treatment; reversal of nondepolarizing
muscular blockade, Ogilvie syndrome
ii. Pyridostigmine Longer acting effect compared to Neostigmine Miosis, salivation, nausea, vomiting, diarrhea, poor lipid solubility, oral, DOA: 4-8h
bradycardia
iii. Physostigmine Natural alkaloid tertiary amine, similar to neostigmine Miosis, salivation, nausea, vomiting, diarrhea, good lipid solubility: able to enter
bradycardia the CNS, DOA: 4-8h
F. Long Acting Cholinesterase Inhibitors (Organophosphates)
i. Echothiophate Similar to neostigmine but with slower release Miosis, salivation, nausea, vomiting, diarrhea, moderate lipid solubiliy, DOA: 2-
bradycardia 7days
ii. Malathion, Parathion malathion: scabicide, parathion: insecticide Miosis, salivation, nausea, vomiting, diarrhea, high lipid solubiliy, DOA: 7-30 days
bradycardia
Cholinoceptor Blocking Drugs
i. Scopolamine Competitively blocks all muscarinic receptors, antagonizes Drowsiness, blurring of vision, dry eyes, known as Hyoscine-N-Butyl-
histamine and serotonin ; for motion sickness, dec. acid constipation, dry mouth, urinary retention Bromide (Buscopan)
secretion in the GIT
ii. Atropine Nonselective competitive antagonism at all muscarinic Tachycardia, mydriasis, cyloplegia, skin flushing, DOC for organophosphate
receptors in the CNS and peripheral tissues; causes delirium, hallucinations, urinary retention, poisoning; notorious for causing
mydriasis and cycloplegia; mandatory antidote for severe constipation hyperthermia
cholinesterase inhibitor poisoning ; Mydriatic, cycloplegic,
antidote for organophosphate poisoning (DOC), for
bradycardia, hypersalivation and to decrease airway
secretion during general anesthesia
iv. Homatropine Similar to atropine but with a shorter duration of action Mydriatic, cycloplegic
(12-24h) ; Mydriatic, cycloplegic in eye examinations
v. Cyclopentolate Similar to atropine but with a shorter duration of action (3- Mydriatic, cycloplegic
6h), Mydriatic, cycloplegic in eye examinations
vi. Tropicamide Similar to atropine but with the shortest duration of action shorter DOA among cholineceptor
(15-60min); Mydriatic, cycloplegic in eye examinations blockers (15-60min)
vii. Ipratropium Competitive nonselective antagonist at muscarinic Dry mouth, cough, nasal dryness not as effective as SABAs but less
receptors ; for BA and COPD tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
viii. Tiotropium Similar to Ipratropium but with longer duration of action Dry mouth, cough, nasal dryness not as effective as SABAs but less
tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
ix. Oxybutinin Nonselective muscarinic antagonist which reduces Tachycardia, mydriasis, cyloplegia, skin flushing, for urinary urgency and
detrussor smooth muscle tone spasms ; for decreasing delirium, hallucinations, urinary retention, incontinence
urgency in mild cystitis and dec. bladder spasm after constipation
urologic surgery
x. Pralidoxime Regenerates active acetylcholinesterase; can relieve muscle weakness Must be administered before 6-8
skeletal muscle and endplate block ; Usual antidote for hours of organophosphate bond
early stage cholinesterase inhibitor poisoning with cholinesterase occurs ; has
oxime group which has high affinity
for phosphorus

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 xi. Hexamethonium, Competitively blocks all Nn nicotinic Ach receptors ; for Postural hypotension, dry mouth, blurred vision, first successful agents in treating
Mecamylamine, Trimethaptan Hypertensive emergencies (obsolete) constipation, sexual dysfunction HTN
Sympathomimetics
i. Epinephrine Non-selective, direct acting sympathomimetic; activates A Hypertension, tachycardia, ischemia, DOC for Anaphylaxis ; inactive per
and B adrenergic receptors; A1 - vasoconstriction and hyperglycemia orem ; do not enter CNS
increased BP; B1 - increased HR, conduction and significantly ; short DOA
contractility; B2 - bronchodilatation ; used for Cardiac
arrest, anaphylaxis, asthma, COPD, Hemostasis
ii. Norepinephrine Non-selective, direct acting sympathomimetic; activates A Extreme vasospasm, tissue necrosis, excessive BP Compensatory vagal reflexes tend
and B adrenergic receptors; A1 - vasoconstriction and increase, arrhythmias, infarction, reflex to overcome the direct postive
increased BP; B1 - increased HR, conduction and bradycardia chronotropic effects ; alpha activity
contractility; B2 - bronchodilatation ; used for Neurogenic > beta activity; inactive per orem ;
shock, cardiogenic shock do not enter CNS significantly ;
short DOA
iii. Dopamine Non-selective, direct acting sympathomimetic; activates A, Cardiovascular disturbances, arrhythmias inactive per orem ; do not enter
B and D1 adrenergic receptors; A1 - vasoconstriction and CNS significantly ; short DOA; very
increased BP; B1 - increased HR, conduction and effective in renal failure associated
contractility; D1 - vasodilation in splanchnic and renal with shock
blood vessels ; for cardiogenic Shock and heart failure
iv. Isoproterenol Beta nonselective sympathomimetic; nonselectively Cardiovascular disturbances, arrhythmias synthetic catecholamine, not
activates B adrenergic receptors; B1 - increased HR, readily taken up into nerve endings
conduction and contractility; B2- bronchodilatation ; for
Asthma
vi. Phenylephrine A1 agonist used for short term maintenance of BP in acute Rebound nasal congestion (Rhinitis Mydriasis without cycloplegia
hypotension; also used intranasally to produce local medicamentosa), hypertension, stroke, MI
vasoconstriction as a decongestant ; mydriatic, for drug-
induced hypotension, spinal shock
vii. Clonidine A2 agonist that inhibits adenylyl cyclase and interacts with Sedation, rebound hypertension, dry mouth When taken per orem, there is
other intracellular pathways; marked vasodilation by initial inc in BP then will go down
central sympatholytic effect ; for Hypertension, Cancer once the drug enters the CNS
pain, opioid withdrawal
viii. Methyldopa, Guanfacine and Central sympatholytics analogous to clonidine ; Sedation, positive Coomb's test (Hemolytic Methyldopa - positive Coomb's test
Guanabenz Methyldopa is used for Pre-eclampsia anemia) (Hemolytic anemia)
xi. Apraclonidine, Brimonidine A2 agonist; reserved for ophthalmologic use in glaucoma eye discomfort, hyperemia and pruritus, blurred NONE
for reduction of intraocular pressure vision
xii. Dobutamine B1 agonist that activates adenylyl cyclase, increasing Tachyarrhythmia, Hypertension, Eosinophilic Beta1 selective
myocardial contractility; with positive inotropic effect ; myocarditis, Premature ventricular beats, Angina,
Clinically used for cardiogenic shock and acute heart Dyspnea, Fever, Headache, Nausea, Palpitation
failure
xiii. Albuterol/Salbutamol B2 agonist with adenylyl cyclase activation; results to Nausea , Fever, Bronchospasm, Vomiting, Rapid development of tolerance;
bronchial smooth muscle dilation ; for Bronchial Asthma Headache, Dizziness, Cough, Allergic reactions DOC as Asthma reliever
xiv. Fenoldopam D1 agonist that activates adenylyl cyclase; results to Angina, Cardiac dysrhythmia, Dizziness, Flushing, D1 agonist
vascular smooth muscle relaxation ; for Hypertension Heart failure, Hypotension, Myocardial
infarction, Tachycardia
xv. Bromocriptine D2 agonist that inhibits adenylyl cyclase and interacts with Nausea, Hypotension, Headache, Dizziness D2 agonist
other intracellular pathways; restores dopamine actions in
the CNS for Parkinson's disease, prolactinemia
Sympatholytics
i. Phenoxybenzamine Irreversibly blocks A1 and A2 receptors resulting to indirect Orthostatic hypotension, Reflex tachycardia, GI Irreversible blockade
baroreflex activation. Decreases blood pressure but irritation
increases heart rate due to baroreflex activation ; for
Pheochromocytoma
ii. Phentolamine Reversible A1 and A2 receptor antagonist with low half life Orthostatic hypotension, Reflex tachycardia, GI Reversible blockade
; for Pheochromocytoma and Rebound hypertension irritation
iii. Prazosin, Doxazosin, Terazosin Blocks A1 but not A2 receptors; leads to reduction in blood Dizziness, Drowsiness, Headache, Weakness, Used in patients with HTN and BPH
pressure ; for Benign Prostatic Hyperplasia, Hypertension Asthenia, Nausea, Palpitation, Edema, at the same time
Orthostatic hypotension
iv. Tamsulosin Slightly selective A1a blockade causing relaxation of Headache, Orthostatic hypotension, Rhinitis, Slightly selective A1a blockade
prostatic smooth muscles > vascular smooth muscle ; for Abnormal ejaculation, Dizziness, Arthralgia, causing relaxation of prostatic
BPH Infection smooth muscles > vascular smooth
muscle
vi. Labetalol Beta blockade > A1 blockade; still with BP depressant Bronchospasm, cardiac depression, AV block, safe in pregnant patients
effects and limited HR increase hypotension, dizziness, headache; Use in caution
vii. Propranolol, Nadolol, Timolol Blocks B1 and B2 receptors; lowers both HR and BP and with DM Px: Masks symptoms of hypoglycemia in Propranolol has local anesthetic
reduces the release of renin ; for Angina prophylaxis, diabetics effect
hypertension, arrhythmias, migraine, performance anxiety,
hyperthyroidism
viii. Metoprolol, Atenolol, B1 > B2 blockade; lowers both HR and BP, reduces the Nebivolol has vasodilating effect ;
Alprenolol, Betaxolol, Nebivolol release of renin BUT is considered safer for patients with metoprolol reduce moratlity in
asthma ; for Angina prophylaxis, hypertension, heart failure
arrhythmias, migraine, performance anxiety,
hyperthyroidism
x. Pindolol, Acebutolol, Carteolol, B1, B2 with intrinsic sympathomimetic (partial agonist) Pindolol is a partial agonist,
Bopindolol, Oxprenolol, Celiprolol, effect; lowers BP with modest reduction in HR therefore safer in bronchial asthma
Penbutolol
xi. Carvedilol, Medoxalol, Beta blockade > A1 blockade; still with BP depressant Carvedilol reduce mortality in heart
Bucindolol, Labetalol effects and limited HR increase ; for Heart Failure failure
xii. Esmolol B1 > B2 blockade; for rapid control of BP and arrhythmias, Used in for perioperative thyroid
thyrotoxicosis and myocardial ischemia intraoperatively ; storm
for Supraventricular tachycardia

2. CARDIOVASCULAR-RENAL DRUGS
Antihypertensives
lower BP by decreasing volume and a direct vascular effect
A. Diuretics that is not yet fully understood

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 Inhibit Na/Cl transporter in distal convoluted tubule. Cause Hypokalemic metabolic alkalosis, Dilutional causes hypercalcemia in contrast
i.Thiazide: Hydrochlorothiazide, moderate diuresis and reduced excretion of calcium; for hyponatremia, Potassium wasting, with loop diuretics which cause
Chlorthalidone, Metolazone, mild to moderate hypertension (FIRST LINE), Heart failure, hyperlipidemia, hyperuricemia, sulfa allergy, hypocalcemia ; FIRST LINE for mild
Indapamide Nephrogenic Diabetes Insipidius, Renal calcium stones hyperglycemia, hypercalcemia to moderate hypertension
Inhibit Na/K/2Cl transporter in thick ascending limb of loop Hypokalemic metabolic alkalosis, Potassium
of Henle, Cause powerful diuresis and increased CA wasting, ototoxicity, hyperuricemia, causes hypocalcemia in contrast
ii. Loop: Furosemide, Torsemide, excretion; for heart failure, hypertension, acute renal nephrotoxicity, dehydration, hypomagnesemia, with thiazide diuretics which cause
Bumetanide, Ethacrynic Acid failure, Pulmonary edema, hypercalcemia, Anion overdose sulfa allergy hypercalcemia
decrease venous return, decrease HR, decrease contractile
B. Sympathoplegics force, decrease cardiac output, decrease TPR
dry mouth, sedation, rebound hypertension, Taper use prior to discontinuation
i.Sympathetic Outflow Blocker: activates a2 adrenergic receptors ; for hypertensive hemolytic anemia: (+) Coomb's test to avoid rebound hypertension ;
Clonidine, Methyldopa urgency (clonidine), pre eclampsia (methyldopa) (methyldopa), sedation readily enter the CNS
ii. Ganglion blockers: competetively blocks Nn nicotinic Ach receptors; for Postural hypotension, blurred vision,
Hexamethonium,Trimethaphan hypertension (obsolete), hypertensive emergencies constipation, dry mouth, sexual dysfunction NONE
Reserpine Irreversibly blocks the vesicular monoamine
iii. Nerve terminal blockers: transporter (VMAT) while Guanethidine and Guanadrel
Reserpine, Guanethidine, inhibit the vesicular release of NE from the presynaptic Sedation, suicidal ideation, severe psychiatric
Guanadrel neuron; for Hypertension (obsolete) depression NONE
Tamsulosin is most selective for
iv. Adrenergic antagonists: prostatic smooth muscle ;
Prazosin,Doxazosin, Terazosin, selectively blocks a1 adrenergic receptors; for Reflex tachycardia (less chance), first dose Doxazosin and Terazosin has longer
Tamsulosin, Silodosin hypertension, benign prostatic hyperplasia orthostatic hypotension duration of action than prazosin
C. Vasodilators
Release NO from endothelial cells, Relaxes arteriolar combination treatment with ISDN
smooth muscle, causing vasolidation. Decreases afterload ; Edema, myocardial ischemia, drug induced lupus for heart failure is more effective
i. Oral Vasolidator: Hydralazine for pre-eclampsia, hypertension, heart failure (hydralazine), reflex tachycardia than ACEIs in blacks
Opens K+ channels in vascular smooth muscle, causing Edema, Angina, Reflex tachycardia, Pulmonary require concomitant use of
hyperpolarization, muscle relaxation and vasolidation; for hypertension, Pericarditis, Hirsutism, salt and diuretics and BBs to block
Minoxidil alopecia / male pattern baldness, hypertension water retention compensatory responses
ii. Calcium Channel Blockers
Non-dihydropyridine calcium block voltage-gated L-type calcium channels (cardiac > Constipation, Nausea, flushing,gingival
channel blocker: Verapamil, vascular); for Angina, Supraventricular tachycardia, hyperplasia, AV block, sinus node depression, excessive cardiac depression may
Diltiazem migraine, hypertension Pretibial edema, dizziness occur
Dihydropyridine calcium
channel blocker: Nifedipine,
Amlodipine, Nicardipine, block voltage-gated L-type calcium channels (vascular > Nausea, Flushing, dizziness, pretibial edema, greater vasodilator effect that
Nisoldipine, Isradipine, Felodipine cardiac); for Angina, hypertension constipation cardiodepressant effect
iii. Parenteral Vasodilators
not commonly used because it is
relaxes venous and arteriolar smooth muscle; for acute very light sensitive, has short
heart failure, controlled hypotension, cardiogenic shock, Duration of action ; given as
Nitroprusside hypertensive emergency hypotension, headache, CN toxicity continuous infusion
a thiazide derivative without a
diuretic effect ; also reduces insulin
Opens K+ channels in vascular smooth muscle, causing release (can be used to treat
hyperpolarization, muscle relaxation and vasolidation; for hypoglycemia in insulin-producing
Diazoxide hypertension hypotension, headache tumors)
causes arteriolar vasolidation of the afferent and efferent
arterioles. Increases renal blood flow; for hypertensive
Fenoldopam emergency hypotension, hypokalemia short duration of action: 10mins
D. Angiotensin antagonists and renin inhibitor
cough, hyperkalemia, rash, hypotension,
palpitations, renal damage in patients with slows down the progression of DM
i. ACE inhibitors: Captopril, inhibit angiotensin converting enzyme ; for hypertension, preexisting renal vascular disease but is nephropathy and cardiac
Enalapril, Lisinopril, Benazepril heart failure protective for DM nephropathy ; CI in pregnancy remodelling in heart failure
ii. Angiotensin receptor blocker:
Losartan, Valsartan, Irbesartan, competetively blocks Angiotensin 1 receptor site ; for fatigue / weakness, hypoglycemia, anemia,
Candesartan hypertension diarrhea, cough, CI in pregnancy as effective as ACEi but less cough
no reproductive toxicity but is also
diarrhea, cough, rash, hyperkalemia, increase in CI because of the toxicity of ACEi
iii. Renin inhibitor: Aliskerin inhibitor of renin's action on its substrate angiotensinogen serum creatinine, renal impairment, angioedema and ARBs
Vasodilators and anti-Angina Pectoris
A. Nitrates
releases nitric oxide (NO), relaxes smooth muscle,
i. Ultrashort-acting nitrate: Amyl especially vascular, increases cGMP (cyclic guanosine Reflex tachycardia, Orthostatic hypotension, inhalational route, but now rarely
Nitrite monophosphate); for cyanide poisoning methemoglobinemia used
Dangerous hypotension with PDE
ii. Short-acting nitrate: releases nitric oxide (NO), increases cGMP (cyclic inhibitors such as Sildenafil ; First
Nitroglycerin, Isosorbide Dinitrate, guanosine monophosphate) and relaxes smooth muscle Reflex tachycardia, orthostatic hypotension, Pass effect is ~90% (NTG), NTG also
Isosorbide Mononitrate especially vascular; for Angina, acute coronary syndromes headache, tolerance (transdermal) decrease platelet aggregation
B. Calcium Channel Blockers
i. Non-dihydropyridine calcium block voltage-gated L-type calcium channels (cardiac > Constipation, Nausea, flushing,gingival
channel blocker: Verapamil, vascular); for Angina, Supraventricular tachycardia, hyperplasia, AV block, sinus node depression, excessive cardiac depression may
Diltiazem migraine, hypertension Pretibial edema, dizziness occur
ii. Dihydropyridine calcium
channel blocker: Nifedipine,
Amlodipine, Nicardipine, block voltage-gated L-type calcium channels (vascular > Nausea, Flushing, dizziness, pretibial edema, greater vasodilator effect that
Nisoldipine, Isradipine, Felodipine cardiac); for Angina, hypertension constipation cardiodepressant effect
Drugs used in Heart Failure

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 Other drugs for heart failure include Diuretics (Furosemide
is the DOC for acute heart failure), Angiotensin Antagonists
(ACEi is the DOC for chronic heart failure), Beta1 blockers
(dopamine and dobutamine), Non-selective Beta Blockers
(Carvedilol, Labetalol, Metoprolol), PDEi (Inamrinone,
A. Cardiac Glycoside Milrinone), Vasodilators (Nitroprusside, Nitroglycerin)
Arrhythmogenesis increased by
inhibits Na/K ATPase; increases intracellular Ca, increasing Narrow therapeutic index, Arrhythmias, diarrhea, hypokalemia, hypercalcemia,
i. Digoxin cardiac contractility; for heart failure, Nodal arrythmias vomiting, visual changes hypomagnesemia
Anti-Arrhythmics
A. Class 1 Antiarryhtmics
Use- and state-dependent block of INa channels; some Arrhythmias, lupus-like syndrome
block of Ik channels. Slowed conduction velocity and (procainamide), hypotension, cinchonism
pacemaker activity; prolonged action potential duration (quinidine), thrombocytopenia (quinidine),
i. Class 1A: Procainamide, and refractory period; for atrial and ventricular antimuscarinic effect (disopyramide), quinidine Hyperkalemia exacerbates cardiac
Disopyramide, Quinidine, arrhythmias especially after myocardial infarction reduces digoxin clearance toxicity
Hyperkalemia, exacerbates cardiac
toxicity. Lidocaine is the least
highly selective use and state-dependent INa block; cardiotoxic among conventional
minimal effect in normal tissue; no effect on IK; DOC for anti-arrhythmics ; only affect
ventricular arrhythmia post-myocardial infarction, Digoxin- ischemic tissue; lidocaine is never
ii. Class 1B: Lidocaine, induced arrhythmia ; Mexilitine can be used for CNS stimulation, Allergy, Arrhythmias, given P.O due to significant first
Mexiletene, Tocainide, Phenytoin neuropathic pain depression, Agranulocytosis pass effect
iii. Class 1C: Flecainide, Selective use and state-dependent block of INa; slowed hyperkalemia exacerbates cardiac
Propafenone, Encainide, conduction velocity and pacemaker activity; for refractory Increased arrhythmias (proarrhythmic effect), toxicity contraindicated for post MI
Moricizine arrhythmias CNS excitation arrhythmias
B. Class 2 Antiarrythmics
Block of beta-receptors, decrease in cAMP results to In CHF, reduces progression and
decreased Na and Ca current and suppression of cardiac decreases incidence of potentially
pacemaker activity; for Post MI prophylaxis against fatal arrhythmias. Sotalol is a beta-
sudden death, thyrotoxicosis, acute perioperative and Bronchospasm, AV block, Hypotension, Cardiac blocker anti arrhythmic that has
i. Propranolol, Esmolol thyrotoxic arrhythmias, Supraventricular tachycardia depression class 3 properties
C. Class 3 Arrhythmics Group with the greatest risk for TDP
Selective Ik block ; prolonged action potential and QT
i. Dofetilide, Ibutilide, interval;
Ik for treatment
block and and prophylaxis
beta-adrenoceptor of ventricular
block; for atrial fibrillation Torsade de pointes NONE
arrhythmias, Supraventricular tachycardia, Atrial Dose-related torsade de pointes, excessive beta-
ii. Sotalol fibrillation blockade (sinus bradycardia, asthma) NONE

Strong Ik block produces marked prolongation of action Amiodarone has Class 1, 2 3 and 4
potential and refractory period. Group 1 activity slows activity therefore is the MOST
conduction velocity; groups 2 and 4 activity confer Microcrystalline deposits in cornea and skin, EFFICACIOUS of all anti-arrhythmics,
additional anti arrhythmic activity; for refractory paresthesias, Pulmonary fibrosis, Tremor, Thyroid amiodarone has longest among all
iii. Amiodarone, Dronedarone arrhythmia, used off label in many arrhythmia dysfunction (hyper- or hypo-) anti-arrhythmics (1-10 weeks)
D. Class 4 Antiarrythmatics
Block voltage-gated L-type calcium channels (cardiac
i. Non-dihydropyridine calcium >vascular), decreased AV conduction velocity ; for Angina, Constipation, Pretibial edema, Nausea, Flushing,
channel blocker: Verapamil, Hypertension, Supraventricular tachycardia, migraine, Gingival hyperplasia, heart failure, AV block, should be avoided in Ventricular
Diltiazem Raynaud's Phenomenon, Vasospasm dizziness, sinus node depression tachycardia
E.Miscellaneous Antiarrythmics
Increase in diastolic Ik of AV node that causes marked
hyperpolarization and conduction block; reduced ICa; For DOC for paroxysmal
AV nodal arrhythmias, DOC for paroxysmal Flushing, Transient chest pain, Dyspnea, supraventricular tachycardia,
i. Adenosine supraventricular tachycardia Hypotension Duration of action is only 15sec
Diuretics
A. Carbonic Anhydrase Inhibitors
Inhibits carbonic anhydrase. In proximal tubule, In
glaucoma, secretion of aqueous humor is reduced and in Drowsiness, Sulfa Allergy, Renal calcium stones,
i. Acetazolamide, Dorzolamide, mountain sickness, metabolic acidosis increases Paresthesias, hyperchloremic metabolic acidosis,
Brinzolamide, Dichlorphenamide, respiration; for glaucoma, diuresis for edema with hepatic encephalopathy in cirrhotic patients, diuresis is self-limiting after 2-3
Methanolamide alkalosis. potassium wasting days
B. Loop Diuretic

Inhibit Na/K/2Cl transporter in thick ascending limb of loop Synergistic ototoxicity with
of Henle, Cause powerful diuresis and increased Ca Hypokalemic metabolic alkasis, dehydration, aminoglycosides. Efficacy decreased
excretion; for Heart failure, Hypertension, Pulmonary Ototoxicity, Potassium wasting, Sulfa allergy, by NSAIDs ; causes hypocalcemia in
i.Furosemide, Bumetanide, Edema, Hypercalcemia, Acute renal failure, Anion Hyperuricemia, Hypocalcemia, Hypomagnesemia, contrast with thiazide diuretics
Torsemide overdose Nephritis which cause hypercalcemia
C. Thiazide Diuretics
Synergistic effect with loop
Inhibit Na/Cl transporter in distal convolutes tubes. Causes diurectics. Efficacy decreased by
i. Hydrochlorothiazide, moderate diuresis and reduced excretion of calcium; For Hypokalemic metabolic alkalosis, Potassium NSAIDs ; causes hypercalcemia in
Chlorthalidone, Indapamide, hypertension Hypercalciuria, Heart failure, Nephrogenic wasting, dilutional hyponatremia, Hyperglycemia, contrast with loop diuretics which
Metolazone diabetes insipidius, renal calcium stones hyperuricemia, sulfa allergy, hyperlipidemia cause hypocalcemia
D. Potassium-Sparing Diuretics
Steroid inhibitors of cytoplasmic aldosterone receptor in
cortical collecting ducts. Reduce K excretion; for Hyperkalemia, impotence, Benign prostatic Eplerenone reduces progression of
i. Spironolactone, Eplerenone Hyperaldosteronism, Heart failure, Hypokalemia, hyperplasia, Hyperchloremic metabolic acidosis, DM nephropathy and reduces
(Aldosterone Antagonist) Hypertension anti-androgenic effect (Spironolactione) mortality post MI
Inhibitor of ENaC (Epithelial sodium channels) in cortical Hyperkalemia, kidney stones, metabolic acidosis,
ii. Amiloride, Triamterene (Na collecting duct, reduces Na reabsorption and K excretion; Acute renal failure (with indomethacin), should should never be given with
channel Blocker) for hypokalemia never be given with potassium supplements potassium supplements
E. Osmotic Diuretics

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 Osmotically retains water in tubule by reducing
reabsorption in proximal tubule, descending limb of
Henle's loop, and collecting ducts; in the periphery,
mannitol extracts water from cells; for Rhabdomyolysis, Transient volume expansion (hyponatremia,
i. Mannitol, Glycerin, Isosorbide, Hemolysis, Increased intracranial pressure, Acute pulmonary edema; followed by hypernatremia)
Urea glaucoma nausea, headache, dehydration, vomiting used to maintain high urine flow
F. ADH Agonists/ Antagonists
Agonists at V1 and V2 ADH receptors. Activate insertion of
aquaporin water channels in collecting tubule. Increases the factor VIII activity of
i. Antidiuretic hormone, Vasoconstriction; For central diabetes insipidus, patients with mild hemophilia A or
Desmopressin, Vasopressin hemophilia, Nocturnal enuresis, von Willebrand's disease Hypertension, Hyponatremia von Willebrand disease
Infusion site reactions, hyperkalemia,
G. ADH Antagonists: Conivaptan, Nephrogenic diabetes insipidus, Bone and Teeth Central Pontine Myelinosis may
Tolvaptan, Lixivaptan, Antagonist at V1, V2 receptors; for SIADH and abnormalities(demeclocycline), Renal failure occur with rapid correction of
Demeclocycline, Lithium Hyponatremia (Lithium, demeclocycline) hyponatremia

3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES

Histamine, Serotonin and the Ergot Alkaloids
A. H1 antagonists diminish or abolish the major actions of histamine in the Sedation, should not be given to neonates Possess antimuscarinic, adrenaline-
body by competitive, reversible blockade of histamine H1- because they are more susceptible to antagonising, serotonin
receptor sites on tissues ; used primarily for the alleviation antimuscarinic effects antagonising, and local anaesthetic
of conditions such as urticarial rashes and nasal allergy effects. Some have calcium-channel
that are characterised by type I hypersensitivity ; are of blocking activity ; Sedating
value in preventing urticaria and are used to treat urticarial antihistamines may enhance the
rashes and mild angioedema sedative effects of CNS depressants
including alcohol, barbiturates,
hypnotics, opioid analgesics,
anxiolytic sedatives, and
antipsychotics ; all are PO but can
be given topical (nose and eyes) ;
i. 1st Generation: Reversible blockade of histamine H1-receptor sites on negligible
Anticholinergic effects, orthostatic hypotension more likelyeffect on H2
to block receptors
autonomic
Diphenhydramine, tissues ; anti-nausea and antiparkinsonism effect, for (promethazine), sedation receptors, also has alpha1 blocking
Dimenhydrinate, allergic reactions, for sedation and motion sickness and local anesthetic effect ;
Chlorpheniramine, Meclizine, (Diphenhydramine Dimenhydrinate, Cyclizine, Meclizine, Cyclizine (more anti-motion
Promethazine Promethazine), for chemotherapy-induced vomiting sickness action less sedative and
(Diphenhydramine) and autonomic effects);
Promethazine (less anti-motion
sickness, more sedative and
autonomic effects ; Usual half-life: 4-
12h
ii. 2nd Generation: Loratadine, Reversible blockade of histamine H1-receptor sites on headache, dry mouth, hyperkinesia, malaise, may No sedation and antimuscarinic
Desloratadine, Cetirizine, tissues ; for allergic reactions cause arrhythmia due to blockade of cardiac effects ; usual half-life: 12-24h
Levocertirizine, Fexofenadine potassium channels (acrivastine, astemizole,
cetirizine, loratadine, and terfenadine)
B. H2 antagonists No blocking action on H1 receptor
i. Cimetidine, Ranitidine, Surmountable competitive pharmacologic block of H2 CYP450 inhibitor, antiandrogen effects, used in the ICU setting to prevent
Famotidine, Nizatidine receptors, reduction of nocturnal acid secretion in gastirc decreased hepatic blood flow (cimetidine), weak gastric erosion and hemorrhage ;
and duodenal ulcer, accelerate healing and prevent enzyme inhibitory effect (Ranitidine) usual half-life: 1-3h
recurrences ; for PUD, GERD and ZES

C. Serotonin Agonists
i. 5HT1D receptor agonist: Agonist at the 5HT1D receptor in the blood vessels causing Injection site reaction, paresthesia, dizziness, all are per orem only except for
Sumatriptan, Naratriptan, vasocontriction ; 1st line treatment for Acute migraine and warm/hot sensation, chest pain, coronary Sumatriptan which can also be
Almotriptan, Eletriptan, cluster headache attacks vasospasm given intranasally, transdermal and
Frovatriptan, Rizatriptan, IV ; All has 2-27hrs DOA exc for
Zolmitriptan sumatriptan DOA: 2-4h

D. Serotonin Antagonists
i. 5HT3 receptor antagonist: Selectively block 5HT3 receptors ; For antiemesis in Constipation, headache, malaise Dolasetron can increase QRS and
Ondansetron, Granisetron, patients post-chemotherapy or post-operation QT (proarrhythmic effect) duration
Dolasetron, Alosetron so never use in patients with heart
disease
E. Ergot Alkaloids most are partial agonists at alpha receptors and 5HT
receptors but some are potent agonist at dopamine
receptors
i. Vasoselective: Ergotamine Mixed partial agonist effects at 5-HT2 and a- gangrene (secondary to ischemia) in overdose, can cause epinephrine reversal due
adrenoceptors, causes vasoconstriction; For Migraine unusual hyperplasia of the retroperitoneal, to partial agonist effect on alpha
attacks (but 5HT1D are preferred) retropleural or subendocardial cavity --> receptors (REMEMBER: All partial
hydronephrosis, cardiac valvular and conduction agonist will act as antagonist in the
system malfunction present of a full agonist)
ii. Uteroselective: Ergonovine Mixed partial agonist effects at 5-HT2 and a- marked uterine contraction, GI upset (nausea, uterus becomes more sensitive to
adrenoceptors, causes vasoconstriction; For control of post- vomiting, diarrhea) ergots during pregnancy, produce
partum bleeding very powerful and long-lasting
contraction leading to decreased
bleeding, Never give before delivery
of placenta
The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds
A. Prostaglandin E1 analog
i. Misoprostol, Gemeprost PGE1 analogue, activated EP receptor, causes increased Abdominal pain, Uterine cramping, teratogen, Misoprostol's intended use is for
HCO3 and mucus secretion in stomach and uterine miscarriage NSAID-induced gastritis, may also
contraction; For prevention of ulcer in patients who take be used together with Mifepristone
high doses of NSAIDs due to arthritis, abortifacient or Methotrexate as safe
abortifacient
ii. Alprostadil PGE1 analogue, causes vascular smooth muscle relaxation Apnea, hypotension, priapism, lightheadedness, given as injection into the
and vasolidation; For Maintenance of patent ductus arrhythmia cavernosa for erectile dysfunction
arteriosus (PDA), Erectile dysfunction
B. Prostaglandin E2 analog

5
 i. Dinoprostone, Sulprostone Low concentrations contract, higher concentrations relax Cramping, Fetal trauma approved abortifacient in the 2nd
uterine and cervical smooth muscle, soften cervix at term trimester, although effective in
before induction with oxytocin; For cervical ripening, inducing labor, it produces more SE
induction of labor, abortifacient than other oxytocics
C. Prostaglandin F2a analog
i. Latanoprost, Arboprost, PGF2a analogue, increases outflow of aqueous humor thus vomiting, diarrhea, transient bronchoconstriction Latanoprost may cause changes in
Bimatoprost, Travoprost, reduces intraocular pressure; For glaucoma the color of the iris and may
Unoprostone lengthen eyelashes
D. Prostaglandin I2 analog
i. Epoprostenol, Beraprost, PGI2 analogue, activates IP receptor, causes vasolidation Hypotension, headache, flusing used primarily for pulmonary
Iloprost, Treprostinil and reduces platelet aggregation; For severe pulmonary hypertension (esp Treprostinil IV)
Hypertension and reducing platelet aggregation in dialysis
machines
E. Leukotriene antagonists
i. Lipoxygenase inhibitor: see entry on Drugs used for Asthma
Zileuton
ii. LT receptor blocker: see entry on Drugs used for Asthma
Montelukast, Zafirlukast
F. Corticosteroids see entry on Drugs used for Asthma
G. Non-steroidal anti- see entry on Analgesics
inflammatory drugs
Drugs used in Asthma
A. Beta2-selective agonist (short-acting)
i. Albuterol/Salbutamol, Activates beta2-receptors in bronchial smooth muscle Tachycardia, Nervousness, tremors, restlessness, Increase toxicity when used for
Levalbuterol, Terbutaline, leading to bronchodilation ; DOC for acute asthma attacks arrhythmias when used excessively, loss of COPD (May precipitate arrythmias)
Metaproterenol, Pirbuterol, responsiveness (tolerance, tachyphylaxis) and in patients with heart disease;
Procaterol, Fenoterol usual DOA: 2-4hrs, all are given
inhalational, Salbutamol and
terbutaline is also available PO,
terbutaline can also be given IV

B. Beta2-selective agonist (long acting)

ii. Salmeterol, Formoterol, Activates beta2-receptors in bronchial smooth muscle Tachycardia, Nervousness, tremors, restlessness, Increase asthma mortality when
Cleneterol, Bambuterol leading to bronchodilation, potentiates corticosteroid arrhythmia when used excessively, loss of used alone; May precipitate
action; For Asthma prophylaxis responsiveness (tolerance, tachyphylaxis) arrhythmias; usual DOA: 12hrs

C. Muscarinic receptor agonist

i. Ipratropium, Tiotropium Blocks muscarinic receptors in bronchial smooth muscle anti-muscarinic effects (dry mouth, blurred vision More effective and less toxic than
and prevent bronchoconstriction mediated by vagal etc.) beta agonists for COPD, Tiotropium
discharge; For acute BA attack and COPD has longer DOA than Ipratropium,
Ipratropium given as aerosol has
little systemic effects, has no effect
on the chronic inflammation aspect
of BA
C. Methylxanthine
i. Theophylline, Aminophylline, Phosphodiesterase inhibitor, Adenosine receptor CNS stimulation (Insomnia, seizure, Anorexia), Antidote in overdosage is BB.
Pentoxifylline antagonist, causes bronchodilation and increased strength Cardiac stimulation (Arrhythmias), Tremors, Higher clearance in adolescents and
of contraction of diaphragm; For asthma especially in increased BP, diuresis, inc GI motility smokers. Narrow therapeutic
nocturnal attacks, Intermittent claudication window; usual DOA: 12hrs
(pentoxifylline), very useful in COPD
D. Mast cell Stabilizer
i. Cromolyn, Nedocromil, Prevents calcium influx and stabilizes mast cells, Cough, Airway irritation No bronchodilator action but can
Lodoxamide preventing degranulation and release of histamine, prevent bronchoconstriction caused
leukotrienes and mediators; for Asthma prophylaxis and by antigens (both in the early and
allergies (oral, nasal and ophthalmic drops) late BA responses), unusually
insoluble chemicals so rarely used
E. Corticosteroid
i. Fluticasone, Beclomethasone, Inhibit synthesis of arachidonic acid by inhibiting Oropharyngeal candidiasis, mild growth For status asthmaticus: use IV
Budesonide, Flunisolide, Phospholipase A2, Reduces expression of COX and LT, inc retardation observed in children, Minimal prednisolone or hydrocortisone ;
Mometasone, Triamcinolone, responsiveness of Beta receptors in the airway, bind to systemic steroid steroid toxicity (eg, adrenal prednisolone is the active
Ciclosenide intracellular receptors and activate Glucocorticoid suppression), Mild growth retardation metabolite of prednisone
response elements in the nucleus leading to synthesis of
substances that prevent full expression of inflammation
and allergy ; DOC for Asthma prophylaxis, First line
treatment for moderate to severe BA, COPD, Allergic
rhinitis, also used as anti-inflammatory for other
conditions such as auto-immune diseases and cancer, also
F. Leukotriene synthesis inhibitor
i. Zileuton Inhibitor of 5-lipoxygenase. Reduces synthesis of Flulike syndrome, headache, drowsiness, No bronchodilator action, not
leukotrienes. Prevents airway inflammation and dyspepsia, hepatitis, elevation of liver enzymes recommended for acute BA attack
bronchoconstriction; For asthma prophylaxis (more than LT receptor blockers)
G. Leukotriene Antagonist
i. Montelukast, Zafirlukast, Blocks leukotriene-1 receptor, prevents airway Gastrointestinal upset, Insomnia, elevation of No bronchodilator action, not
Pranlukast inflammation and bronchoconstriction; For asthma liver enzymes recommended for acute BA attack
prophylaxis
H. Anti-IgE antibody
i. Omalizumab Binds IgE antibodies on sensitized mast cells and prevents Long term toxicity not yet well documented humanized murine monoclonal
activation by BA triggers and subsequent release of antibody, very expensive and only
inflammatory mediators; For prophylaxis of severe, administered IV
refractory asthma not responsive to all other drugs

4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM

Sedative-Hypnotics

6
A. Short-acting benzodiazepines
additive CNS depression if used
bind GABA-A receptor subunits to increase frequency of with ethanol, antihistamines,
chloride channel opening which causes membrane causes anterograde amnesia, decreased antipsychotics, opioids and TCAs,
hyperpolarization ; For acute anxiety, panic attacks, psychomotor skills, unwanted daytime sedation, decreased REM sleep, use lower
i. Midazolam, brotizolam, anesthesia induction and preoperative sedation (esp tolerance, dependence liability and rebound doses in the elderly when used for
triazolam, oxazepam, etizolam Midazolam), insomnia (Triazolam) insomnia or anxiety. insomnia
B. Intermediate-acting benzodiazepines additive CNS depression if used
with ethanol etc, decreased REM
sleep, High dose BZD and Barbs may
suppress seizure but at the
bind GABA-A receptor subunits to increase frequency of expenses of marked sedation
chloride channel opening which causes membrane EXCEPT Clonazepam and
hyperpolarization; For anxiety disorders even panic Phenobarbital, Lorazepam is
disorders (Alprazolam and Clonazepam), insomnia preferred over Diazepam in Status
i. Lorazepam, Alprazolam, (Estazolam), skeletal muscle relaxation, seizure disorders causes anterograde amnesia, decreased Epilepticus due to its long
Estazolam, Clonazepam, (Clonazepam), status epilepticus (Lorazepam), psychomotor skills, unwanted daytime sedation, distribution halflife, use lower
Lormetazepam, Nitrazepam, tranquilizers, Bipolar disorder (Clonazepam), infantile tolerance, dependence liability and unwanted doses in the elderly when used for
Temazepam spasm (Clonazepam) daytime sedation. insomnia
C. Long-acting Benzodiazepine
bind GABA-A receptor subunits to increase frequency of
chloride channel opening which causes membrane
hyperpolarization; For anxiety disorders, insomnia causes anterograde amnesia, decreased additive CNS depression if used
(Flurazepam), skeletal muscle relaxation (e.g. cerebral psychomotor skills (esp Diazepam and with ethanol etc., decreased REM
i. Diazepam, chlorazepate, palsy - Diazepam), seizure disorders, tranquilizers, for Flurazepam), unwanted daytime sedation, sleep, Flunitrazepam is used as a
chlordiazepoxide, flurazepam, status epilepticus (Diazepam), anesthesia (Diazepam), tolerance, dependence liability and rebound date-rape drug, use lower doses in
quazepam, flunitrazepam alcohol withdrawal (Diazepam and Chlordiazepoxide) insomnia or anxiety. the elderly when used for insomnia
D. Benzodiazepine antagonist
Seizures and arrhythmias may occur
agitation, confusion, and precipitates when administered in patients who
antagonist at benzodiazepine sites on GABA-A receptor ; benzodiazepine withdrawal syndrome for those took both TCAs and
i. Flumazenil for benzodiazepine overdose. with benzodiazepine dependence. benzodiazepines
E. Ultrashort-acting barbiturates
bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride channel additive CNS depression if used
opening, block glutamic acid neurotransmission, at high with ethanol etc., CYP450 inducer,
i. Thiopental, Methohexital, doses can block NA channels ; For anesthesia induction dependence liability is greater than Thiopental has highest lipid
Thiamylal (esp Thiopental) benzodiazepine, acute intermittent porphyria. solubility
F. Short and intermediate-acting barbiturates
bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride channel
opening, block glutamic acid neurotransmission, at high
i. Pentobarbital, secobarbital, doses can block Na channels ; For insomnia and
amobarbital, butalbital, preoperative sedation (Secobarbital), for status epilepticus dependence liability is greater than additive CNS depression if used
butabarbital, talbutal, aprobarbital (Phenobarbital) benzodiazepine, acute intermittent porphyria. with ethanol etc., CYP450 inducer
G. Long-acting barbiturate
additive CNS depression if used
with ethanol, CYP450 inducer,
bind to GABA-A receptor sites (distinct from Phenobarbital may be excreted
benzodiazepines) to increase duration of chloride channel unchanged in the urine, High dose
opening, block glutamic acid neurotransmission, at high BZD and Barbs may suppress
doses can block Na channels ; For insomnia, seizure dependence liability is greater than seizure but at the expenses of
i. Phenobarbital, mephobarbital, disorders (Phenobarbital), status epilepticus benzodiazepine, acute intermittent porphyria, marked sedation EXCEPT
primidone (Phenobarbital) severe respiratory and cardiovascular depression Clonazepam and Phenobarbital
H. Imidazopyridine sedative-hypnotics
lack anti-convulsant, anti-anxiety
and muscle relaxant effects, effects
are reversed with Flumazenil, very
rapid onset of action, may dec. REM
sleep, rebound inc on withdrawal
bind selectively to a subgroup of GABA-A receptors, acting from chronic use, increasing use
like benzodiazepines to enhance membrane day-after psychomotor depression, few amnestic due to rapid onset with minimal
hyperpolarization, only interact with GABA-A receptors effects; tolerance, dependence liability and effects on the sleep pattern and
i. Zolpidem, Zaleplon, with alpha-1 subunit ; For insomnia and sleep disorder esp. withdrawal symptoms is less than that of cause less daytime cognitive
Eszopiclone when sleep onset is delayed benzodiazepines impairment as compared to BZD
I. Atypical Sedative-Hypnotics
minimal abuse liability, minimal
CNS depressant effects, tolerance
and withdrawal ; no anticonvulsant
non-specific chest pain, tachycardia, palpitations, or muscle relaxant property ; slow
partial agonist at 5-HT1A receptors and possibly D2 dizziness, nervousness, tinnitus, GI distress, onset of action (>1week),
i. Partial Serotonin Agonist: receptors, precise MOA of anxiolytic effect is unkown ; For paresthesias, dose-dependent pupillary metabolized by CYP3A4, safe for
Buspirone generalized anxiety disorders constriction pregnant patients

minimal rebound insomnia or

withdrawal symptoms, minimal
abuse liability, metabolized by
activates melatonin receptors (MT1 and MT2 receptors) in CYP450 (increased levels in the
ii. Melatonin receptor agonist: the suprachiasmatic nuclei in the CNS --> decreased Dizziness, fatigue, decreased testosterone, presence of CYP1A2 or CYP2D6
Ramelteon latency of sleep onset increased prolactin inhibitors
Antiseizure Drugs

7
 CYP450 inducer , metabolism is non-
linear (elimination shift from 1st
order to zero order at moderate to
high dose levels) , Fosphenytion is a
nystagmus, diplopia, sedation, gingival water-soluble prodrug of phenytoin
hyperplasia, hirsutism, anemias, peripheral ; phenytoin is preferred in
block voltage-gated Na channel ; DOC for generalized tonic- neuropathy (absent DTRs), osteoporosis, fetal prolonged therapy for status
i. Phenytoin, Fosyphenytoin, clonic seizures, DOC for partial seizures, status epilepticus, hydantoin syndrome, abnormalities in Vit D epilepticus because it is less
Mephenytoin, Ethotoin arrhythmias, migraine metabolism sedating.
CYP450 inducer, Oxcarbazepine has
less drug interactions, metabolism
diplopia, cognitive dysfunction, drowsiness, may be inhibited by other drugs
block voltage-gated Na channels and decreases glutamate ataxia, blood dyscrasias, Stevens-Johnson such as Propoxyphene and valproic
release ; DOC for trigeminal neuralgia, DOC for generalized syndrome, erythematous rash, teratogen (spina acid ; may be used for acute manic
ii. Carbamazepine, tonic-clonic seizures, DOC for partial seizures, for bipolar bifida and craniofacial anomalies), hyponatremia phase and as prophylaxis in the
Oxcarbazepine disorders (Oxcarbazepine) depressive phase
CYP450 inhibitor ; also have the
same effect on Ca currents like
blocks high-frequency firing of neurons which modifies Ethosuximide ; Other MOA include
amino acid metabolism ; DOC for bipolar disorder (acute enhancing K channel permeability ;
mania), DOC for generalized tonic-clonic seizures and drowsiness, nausea, tremor, alopecia, weight BZDs are commonly required at
absence seizure, partial seizures, myoclonic seizures, also gain, hepatotoxicity (esp in infants), neural tube initiation therapy of valproic acid ;
iii. Valproic acid used for Bipolar disorders defects DOC for acute manic illness
May also act on Na channels and as
antagonist at some glutamate
receptors ; primary anticonvulsant
in infants, children and pregnant
iv. Phenobarbital see notes above ; For status epilepticus in children cognitive dysfunction, dependence patients
v. Ethosuximide, Phensuximide, inhibit low threshold (T-type) Ca currents esp in thalamic GI distress, lethargy, headache and behavioural
Methsuximide neurons ; DOC for absence seizure changes. Long half-life
vi. Diazepam see entry on Sedative-Hypnotics
eliminated in the kidneys in their
unchanged form ; structural
analogues of GABA but does not
blocks Ca++ channels, increases GABA release ; For activate GABA receptor directly ;
neuropathic pain such as postherpetic neuralgia, partial also have the same effect on Ca
vii. Gabapentin, Pregabalin seizures, migraine dizziness, sedation, ataxia, nystagmus, tremor currents like Ethosuximide
blocks Na and Ca++ channels and decreases glutamate , primarily undergoes
Zonisamide only blocks Na channels ; For generalized tonic- glucuronidation reaction ;
clonic seizures, DOC for partial seizures, myoclonic dizziness, ataxia, nausea, rash, SJS / TEN Lamotrigine may be used for acute
viii. Lamotrigine, Zonisamide seizures, absence seizures, bipolar disorder. (lamotrigine), severe skin reaction (Zonisamide) manic phase and as prophylaxis in
Bind synaptic protein selectively inhibiting It is not metabolized by CYP450
hypersynchronization of epileptiform burst firing ; For dizziness, sedation, weakness, irritability, enzymes, eliminated in the kidneys
ix. Levetiracetam generalized tonic-clonic seizures, partial seizures hallucinations, psychosis in their unchanged form
Antiseizure drugs with the most
multiple actions on synaptic function, probably via actions number of MOA, undergo both
on phosphorylation (Na, Ca, GABA, AMPA-glutamate, hepatic and renal metabolism,
carbonic anhydrase), Felbamate also facilitate the drowsiness, dizziness, ataxia, psychomotor Topiramate can also block Na
inhibitory actions of GABA but its exact MOA is still slowing, memory impairment, paresthesias, channels and potentitae action of
unknown ; For generalized tonic-clonic seizures, partial weight loss, acute myopia, glaucoma, myopia, GABA and block glutamate
seizures, absence seizures, migraine ; Felbamate is only for urolithiasis ; felbamate causes hepatic failure and receptor, Felbamate may also block
x. Topiramate, Felbamate severe refractory seizure states hematotoxic (can cause ITP, aplastic anemia) glutamate receptors
Irreversibly inactivates GABA aminotransaminase (GABA-T)
xi. Vigabatrin which terminates the action of GABA ; For GTC seizure visual field defects None
Inhibits GABA transporter (GAT-1) in neurons and glia thus
inhibiting its reuptake, leading to prolongation of GABA
xii. Tiagabine effects ; For partial seizures asthenia or weakness, dizzines None
General Anesthetics
A. Inhalational General Anesthetics This group in general increase the threshold for firing of CNS neurons
Lowest Potency (highest MAC) and
least cardiotoxic; additive CNS
Facilitates GABA-mediated inhibition, block brain NMDA depression with many agents
and Ach-N receptors; used as anesthesia for minor surgery megaloblastic anemia on prolonged exposure; especially opioids and sedative-
i. Nitrous Oxide and dental procedures Euphoria (laughing gas), bronchodilation hypnotics
additive CNS depression with many
agents especially opioids and
sedative-hypnotics ; all inhaled
Facilitates GABA-mediated inhibition, block brain NMDA anesthetcis cause bronchodilation
ii. Desflurane and Ach-N receptors ; For general anesthesia bronchospasm, peripheral vasodilation except Desflurane
additive CNS depression with many
Facilitates GABA-mediated inhibition, block brain NMDA peripheral vasodilation, renal insufficiency (due agents especially opioids and
iii. Sevoflurane and Ach-N receptors; For general anesthesia to Flourine release), bronchodilation sedative-hypnotics
additive CNS depression with many
Facilitates GABA-mediated inhibition, block brain NMDA catecholamine-induced arrhythmias, peripheral agents especially opioids and
iv. Isoflurane and Ach-N receptors ; For general anesthesia vasodilation, bronchodilation sedative-hypnotics
spike-and-wave activity in EEG, muscle twitching, additive CNS depression with many
breath-holding, myocardial depression, renal agents especially opioids and
Facilitates GABA-mediated inhibition, block brain NMDA insufficiency (due to Flourine release), dec sedative-hypnotics ; has pungent
v. Enflurane and Ach-N receptors ; For general anesthesia cardiac output, bronchodilation odor which limits its use
catecholamine-induced arrhythmias, myocardial additive CNS depression with many
Facilitates GABA-mediated inhibition, block brain NMDA depression, post-operative hepatitis, dec cardiac agents especially opioids and
vi. Halothane and Ach-N receptors ; For general anesthesia output, bronchodilation sedative-hypnotics
Highest potency and lowest MAC
(very slow onset and recovery);
additive CNS depression with many
Facilitates GABA-mediated inhibition, block brain NMDA renal insufficiency (due to Flourine release), agents especially opioids and
vii. Methoxyflurane and Ach-N receptors ; For general anesthesia bronchodilation sedative-hypnotics
B. Intravenous General Anesthetics

8
 i. Barbiturates: Thiopental, are respiratory and circulatory depressants -->
Methohexital, Thiamylal see notes above dec cerebral blood flow --> dec ICP rapid entry into the brain (<1min)
Midazolam is a usual adjunct with
ii. Benzodiazepine: Midazolam, inhalational anesthetics and IV
Brotizolam, Triazolam, Oxazepam, opioids, has a slow onset but longer
Etizolam see notes above see notes above DOA
Blocks excitation by glutamate at NMDA receptors; For CV stimulation, hypertension, increased ICP, Reduces delirium by pretreatment
iii. Phencyclidine derivative: dissociative anesthesia (analgesia, amnesia and catatonia delirium, Dissociative anesthesia, post-op effects: with benzodiazepine, congener of
Ketamine but with retained consciousness) disorientation, hallucination, excitation Phencyclidine / angel dust
Modulates GABA-A receptors containing beta3 subunits; pain at injection site, myoclonus, postoperative Minimal effects on CV and
iv. Imidazole derivative: For general anesthesia to patients with limited cardiac or nausea and vomiting, adrenocortical suppression respiratory functions, no analgesic
Etomidate respiratory reserve (on prolonged administration) properties, short DOA
Antidote is Naloxone / Naltrexone ;
Neuroleptanesthesia (analgesia +
amnesia) happens when Fentanyl,
Droperidol and Nitrous oxide are
Interacts with mu, sigma, kappa receptors for endogenous given together ; faster recovery
v. Opioid analgesics: Fentanyl, opioid peptides ; For high risk patients who might not respiratory depression, chest wall rigidity (which with remifentanil ; these drugs have
morphine, alfentanil, remifentanil survive general anesthesia may cause impaired ventilation) and constipation fast onset of action
"milk of anesthesia", additive
effects with sedative-hypnotic
drugs ; as rapid as thiopental and
bradycardia, vasodilation, hypotension, negative also with fast recovery ; antiemetic
Potentiates GABA-A receptors, blocks Na channels; For inotropism, pain at injection site, anterograde action ; Fospropofol is the water-
prolonged sedation esp in ICU patients and also in OPD amnesia, dystonia, priapism, paresthesia soluble prodrug form of propofol
vi. Propofol, Fospropofol surgeries (Fospropofol) but with slower onset and recovery
Local Anesthetics
this group can cause antibody
A. Ester Local Anesthetics formation in some patients
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness, Shortest half-life among local
i. Procaine potential propagation; For local anesthesia nystagmus, seizures, respiratory, CV depression anesthetics
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, topical light-headedness, sedation, restlessness, Use cautiously in sunburns, Topical
ii. Benzocaine anesthesia nystagmus, seizures, respiratory, CV depression only
with intrinsic sympathomimetic
activity so it does not need an alpha
agonist (like epinephrine) to limit its
systemic absorption; causes mood
light-headedness, sedation, restlessness, elevation due to action on
Blockade of Na channels slows which prevents axon nystagmus, seizures, respiratory, CV depression, dopamine receptor ; All local
potential propagation, with intrinsic sympathomimetic abuse liability, severe hypertension, cerebral anesthetics are vasodilators EXCEPT
iii. Cocaine activity; For local anesthesia, topical anesthesia hemorrhage, cardiac arrhythmia, MI cocaine ; Topical only
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, spinal
anesthesia, epidural anesthesia, topical ophthalmic light-headedness, sedation, restlessness, also available as Ophthalmic
iv. Tetracaine anesthesia nystagmus, seizures, respiratory, CV depression solution
B. Amide Local Anesthetics
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, antiarrhythmia Frequently administered with
(group 1B activity), used for post-MI and for digitalis light-headedness, sedation, restlessness, Epinephrine to avoid systemic
i. Lidocaine toxicity nystagmus, seizures, respiratory, CV depression absorption
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, dental light-headedness, sedation, restlessness, causes methemoglobinemia
ii. Prilocaine anesthesia nystagmus, seizures, respiratory, CV depression (antidote: methylene blue)
Use with caution in pregnant
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness, women and patients with cardiac
potential propagation; For local anesthesia, epidural nystagmus, seizures, respiratory, CV depression, disease (may cause heartblock,
iii. Bupivacaine anesthesia, intrathecal anesthesia severe CV toxicity, hypotension and arrhythmias arrhyhtmia and hypotension)
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness,
potential propagation; For local anesthesia, epidural nystagmus, seizures, respiratory, CV depression, Longest half-life among local
iv. Ropivacaine anesthesia cardiotoxicity anesthesia
Skeletal Muscle Relaxant
A. Depolarizing Neuromuscular Blocker
muscle pain, hyperkalemia, increased intragastric Metabolized by
Agonist at Ach-N receptors causing initial twitch then pressure leading to regurgitation (aspiration), pseudocholinesterase ; may cause
persistent depolarization ; For skeletal muscle relaxation increased intraocular pressure, malignant malignant hyperthermia if given
i. Succinylcholine during intubation and general anesthesia hyperthermia together with inhaled anesthetics
effects are easily reversed by giving
AChE inhibitors such as
B. Non-Depolarizing Neuromuscular Blocker a common SE for this group is Histamine release Neostigmine
Metabolized by
i. Mivacurium (short-acting: 10- respiratory paralysis, apnea, and moderate pseudocholinesterase; reverse
20mins DOA) histamine release effects with Neostigmine
Undergoes Hoffman elimination
(rapid spontaneous breakdown);
reverse effects with Neostigmine ;
ii. Atracurium (intermediate- respiratory paralysis, apnea, and moderate converted to Laudanosine which
acting) histamine release and bronchospasm can cause seizures

iii. Vecuronium (intermediate- Undergoes elimination in bile;

acting) respiratory paralysis and apnea reverse effects with Neostigmine
reverse effects with Neostigmine;
Suggamadex is a novel reversal
iv. Rocuronium (intermediate- agent for rocuronium; most rapid
acting) respiratory paralysis and apnea, hypersensitivity onset time (60-120 sec)
Competitive antagonists at skeletal muscle nicotinic Relatively contraindicated in
acetylcholine receptors; For skeletal muscle relaxation respiratory paralysis, apnea, hypotension and myocardial ischemia; reverse
v. Tubocurarine (long-acting) during intubation and general anesthesia recurarization effects with neostigmine

9
 Competitive antagonists at skeletal muscle nicotinic
acetylcholine receptors; For skeletal muscle relaxation
during intubation and general anesthesia, euthanasia, respiratory paralysis, apnea, tachycardia, Reverse effects with Neostigmine,
vi. Pancuronium (long-acting) lethal injection, strychnine poisoning hypertension, recurarization may cause heart block
Anti-Parkinsonism and other drugs for movement disorders
A. Dopamine Precursor
Contraindicated in patients with
history of psychosis; hypertensive
crisis occurs when used with MAO
inhibitors, ameliorates signs of
GI upset (emesis), dyskinesia (choreoathetosis), parkinsonism and decreases
behavioural changes (anxiety, agitation, mortality rate ; patient response
Levodopa is a dopamine precursor, carbidopa inhibits confusion, delusion), on-off phenomena, wearing- decreases with time but is
peripheral metabolism via dopa decarboxylase; Drug of off phenomena, postural hypotension, improved when given together with
i. Levodopa-carbidopa choice for parkinson’s disease tachycardia COMT inhibitors
B. Dopamine Agonist
anorexia, nausea, vomiting, dyskinesia, postural
Partial agonist at dopamine D2 receptors in brain; For hypotension, behavioural changes,
Parkinson’s disease which is levodopa intolerance, erythromelalgia (Bromocriptine), pulmonary
i. Bromocriptine, Pergolide hyperprolactinemia infiltrate (Bromocriptine) Ergot alkaloids

Contraindicated for patients with

active peptic ulcer disease,
psychotic illnesss or recent MI ;
anorexia, nausea, vomiting, dyskinesia, postural decrease dose in renal dysfunction ;
Partial agonist at dopamine D3 receptors in brain, hypotension, behavioural changes (more Neuroprotective ; Ropirinole is
ii. Pramipexole, Ropinirole Roprinole is a D2 agonist; For Parkinson’s disease prominent compared to levodopa) metabolized by CYP1A2
Partial agonist at dopamine D3 receptors, antagonist at 5-
HT and alpha adrenoceptors; For off-periods of Parkinson’s Premedicate with
disease, alcoholism, opiate addiction, erectile dysfunction, severe nausea, dyskinesia, hypotension, Trimethobenzamide to prevent
iii. Apomorphine alzheimer’s disease drowsiness and sweating severe nausea
C. MAO type B inhibitor
Selective inhibitors of MAO type B leading to decreased serotonin syndrome occurs when
degradation of dopamine, increases response to used with SSRI and Meperidine ;
levodopa/carbidopa; Only as adjunct to levodopa for Selegiline is hepatically metabolized
parkinson’s disease but Rasigiline can be given alone insomnia, mood changes, dyskinesias, GI distress into desmethyl selegiline (which is
i. Selegiline, Rasagiline (more potent) and hypotension neuroprotective) and amphetamine
D. COMT inhibitor
Block L-dopa metabolism by inhibiting catechol-O- dyskinesias, GI distress, postural hypotension,
methyltransferase in periphery and CNS, prolongs sleep disturbance, orange discoloration of urine, Entacapone only acts in the
response to levodopa; used in the wearing-off phenomena hepatotoxicity (tolcapone only), neuroleptic periphery while Tolcapone acts
i. Entacapone, Tolcapone of parkinson’s disease, as adjuncts to levodopa malignant syndrome, rhabdomyolysis both in the periphery and CNS.
E. Antiviral
enhances dopaminergic transmission by unknown behavioural changes (restlessness, agitation,
mechanism, maybe by influencing the synthesis, release or insomnia, hallucination, psychosis), livedo May improve bradykinesia, rigidity
reuptake of dopamine; For Parkinson’s disease and reticularis, GI disturbances, urinary retention, and tremor ; has antimuscarinic
i. Amantadine influenza postural hypotension, peripheral edema action
F. Anticholinergic
Exacerbate tardive dyskinesias that
Decrease the excitatory actions of cholinergic neurons on result from prolonged use of
cells in the striatum by blocking muscarinic receptors; as antipsychotic drugs; improve
i. Benztropine, Biperiden, adjunct for parkinson’s disease and extrapyramidal drowsiness, inattention, confusion, delusions, tremor and rigidity with little effect
Trihexyphenidyl, Orphenadrine symptoms caused by antipsychotics hallucinations, atropine-like effects on bradykinesia
Antipsychotics and Lithium

A. Typical Antipsyhotics may also be used for pruritus and as sedatives has no effect on negative symptoms
extrapyramidal dysfunction, tardive dyskinesia,
hyperprolactinemia, atropine-like effects, failure
of ejaculation, postural hypotension, marked
Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia sedation, corneal and lens deposits, neuroleptic prototype of all typical
i. Phenothiazine: Chlorpromazine and other psychotic disorders malignant syndrome, contact dermatitis antipsychotics
Thioridazine has the Strongest
autonomic effects; only
antipsychotic with fatal overdose ;
extrapyramidal dysfunction, tardive dyskinesia, Fluphenazine and Trifluoperazine
ii. Other Phenothiazines: hyperprolactinemia, atropine-like effects, failure have very significant parkinson-like
Thioridazine, Fluphenazine, Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia of ejaculation, postural hypotension, retinal effect ; Fluphenazine has less
Perphenazine, Prochlorperazine, and other psychotic disorders, antiemesis deposits (thioridazine), cardiotoxicity sedation compared to other anti-
Trifluoperazine (prochlorperazine) (arrhythmias - thioridazine) psychotics
causes the most extrapyramidal
Blocks D2 receptors >> 5-HT2 receptors; For schizophrenia extrapyramidal dysfunction, tardive dyskinesia, symptoms of all typical anti-
iii. Butyrophenol: Haloperidol, and other psychotic disorders, huntington’s disease and hyperprolactinemia, neuroleptic malignant psychotics ; has the weakest
Droperidol tourette’s syndrome syndrome autonomic effects
may be used for mania and psychotic symptoms in cure both negative and positive
B. Atypical Antipsychotics Alzheimer's dementia and Parkinsons disease symptoms
Extrapyramidal dysfunction (less), Only antipsychotic that reduces the
hyperprolactinemia (less), postural hypotension, risk of suicide ; may be effective for
weight gain, hyperglycemia, hyperlipidemia, drug-resistant types ; weight gain,
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia myocarditis, agranulocytosis, seizures, ileus, agranulocytosis, seizure and
i. Clozapine (refractory, suicidal) and other psychotic disorders hypersalivation (sialorrhea) hyperglycemia is prominent
Extrapyramidal dysfunction (less),
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, hyperprolactinemia (less), postural hypotension, weight gain and hyperglycemia is
ii. Olanzapine bipolar disorders, anorexia nervosa and depression weight gain, hyperglycemia, hyperlipidemia prominent, safe in pregnancy
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural hypotension,
weight gain, somnolence, fatigue, sleep paralysis,
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, hypnagogic hallucinations, cataracts, priapism,
iii. Quetiapine bipolar disorders (manic) QT prolongation (TDP) can cause TDP, safe in pregnancy

10
 Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, Extrapyramidal dysfunction (less),
bipolar disorders, depression, intractable hiccups, tourette hyperprolactinemia (marked), insomnia, Only antipsychotic approved for
iv. Risperidone syndrome photosensitivity schizophrenia in the youth
Increased mortality in elderly
Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, Extrapyramidal dysfunction (less), postural patients with dementia-related
v. Ziprasidone bipolar disorders (acute mania) hypotension, QT prolongation (TDP) psychosis ; can cause TDP

Blocks 5-HT2 receptors >> D2 receptors; For schizophrenia, Extrapyramidal dysfunction (less), GI upset, Least sedating atypical
vi. Aripiprazole bipolar disorders, depression, autism, cocaine dependence tremor, hypersensitivity (rare) antipsychotics in sick sinus
Contraindicated
syndrome; treat overdose with
hemodialysis ; high volume of
distribution ; clinical benefit is seen
Tremor, sedation, ataxia, aphasia, thyroid only after weeks of use ;
Uncertain MOA but the proposed MOA is by inhibiting the enlargement, hypothyroidism, reversible antipsychotic agents or BZDs are
enzyme involved in the recycling of neuronal membrane nephrogenic diabetes insipidus, edema, commonly required at initiation
phosphoinositides which causes depletion of acneiform skin eruption, leukocytosis, teratogen therapy of Li and valproic acid ;
phosphatidylinositol bisphosphate, thus consequently (ebstein’s anomaly), bradycardia, some drugs Contraindicated in lactation ;
decreasing IP3 and DAG --> decrease in neurotransmission (NSAIDs, ACEi, diuretis etc) can increase Lithium Natriuresis stimulates reflex
; For bipolar disorder, recurrent depression, schizoaffective toxicity while caffeine and theophylline can increase in the reabsorption of Li
vii. Lithium (mood stabilizer) disorder decrease its toxicity and Na in the PCT
Antidepressants
A. Tricyclic Antidepressants
Additive depression of the CNS with
other central depressants ;
Imipramine is metabolized to
desipramine while amitriptyline is
metabolized to nortriptyline ;
longterm use may lead to down-
Block NE and 5-HT transporters leading to potentiation of regulation of Beta receptors leading
NT action at postsynaptic receptors; For MDD (most excessive sedation, fatigue, confusion, to a decrease in BP and depression
effective), bipolar disorder, acute panic attacks, ADHD, sympathomimetic effects, atropine-like effects, of cardiac conduction ; has
chronic pain states, as sleeping aid, OCD (Clomipramine) ; orthostatic hypotension, cardiomyopathies, significant muscarinic receptor
i. Imipramine, Clomipramine, this group is very useful for patients with psychomotor arrhythmias, tremors, paresthesias, weight gain ; blocking effect esp Amitriptyline ;
Desipramine, Amitryptyline, retardation, sleep disturbance, poor appetite and weight 3Cs of overdose: Coma, Cardiotoxicity, lower seizure threshold ; may
Nortryptiline loss Convulsions interfere with antihypertensive
B. SSRI Serotonin syndrome when used
with MAOIs ; minimal inhibitory
effect on cholinergic or adrenergic
receptors ; lower seizure threshold ;
this group can decrease appetite
leading to weight loss ; Increased
Inhibits neuronal reuptake of serotonin by inhibiting nausea, vomiting, headache, anxiety, agitation, risk for suicide in children and
i. Fluoxetine, Paroxetine, Serotonin Transporter (SERT); DOC for OCD, for MDD, drowsiness, insomnia, erectile dysfunction, EPS, adolescents ; Fluoxetine,
Citalopram, Escitalopram, anxiety, panic attacks, phobias, PTSD, GAD, bulimia, QT prolongation (citalopram), withdrawal Fluvoxamine and Paroxetine are
Sertraline, Fluvoxamine premenstrual dysphoric disorder, alcohol dependence syndrome CYP450 inhibitors
C. SNRI
venlafaxine has less affinity for NE
dizziness, insomnia, sedation, GI distress, transporter than desvenlafaxine
Inhibits neuronal reuptake of serotonin and hypertension (venlafaxine), hepatotoxicity and duloxetine ; differ from TCA in
norepinephrine by binding to transporters for both 5HT (duloxetine), withdrawal syndrome even in just lacking blockade of H1, M and alpha
i. Venlafaxine, Duloxetine, and NE; For MDD, fibromyalgia, neuropathic pain, one missed dose, CNS stimulation (Venlafaxine), receptors ; Increased risk for suicide
Desvenlafaxine menopausal symptoms liver dysfunction (Duloxetine) in children and adolescents
D. Serotonin antagonist
May cause arrhythmias in px with
pre-existing cardiac disease ; short
t1/2 so given BID to TID, has
significant muscarinic receptor
blocking effect esp Nefazodone ;
sedation, GI disturbance, orthostatic CYP450 inhibitors ; Trazodone also
Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT hypotension, priapism, hyperprolactinemia, liver has significant alpha1 and H1
i. Trazodone, Nefazodone transporters; For MDD, as sleeping aid (trazodone) dysfunction (nefazodone) blocking effect
Increased risk for suicide in children
E. Tetracyclics and adolescents
Strong norepinephrine reuptake inhibitor and weak autonomic effects, akathisia, parkinsonism (due Lowers seizure threshold, has
serotonin reuptake inhibitor, blocks dopamine D2 to dopamine receptor blockade), seizures, significant muscarinic receptor
i. Amoxapine receptors; For MDD cardiotoxicity blocking effect
Increases amine release from nerve endings by
antagonism of presynaptic a2 adrenoceptors, also blocks
serotonin 5-HT2A receptors; For MDD, appetite weight gain, marked sedation, dizziness, blurred has significant muscarinic receptor
ii. Mirtazapine stimulation, as sleeping aid vision and nightmares and alpha2 blocking effect
Inhibits neuronal reuptake of dopamine and Lowers seizure threshold, for
norepinephrine, increase dopamine and norepinephrine weight loss, agitation, anxiety, dizziness, dry smoking cessation ; no effect on
activity; For MDD and smoking cessation, alcohol mouth, aggravation of psychosis, seizures, 5HT or NE receptors or amine
iii. Bupropion dependence priapism transporters ; CYP450 inhibitor
F. MAO Inhibitors Hypertensive crisis when taken with
tyramine-rich food, serotonin
syndrome when taken with SSRI ;
this group is structurally related to
Inhibits MAO type A and type B, increases CNS levels of NE amphetamine ; CYP450 inhibitors ;
and serotonin, Phenelzine and Tranylcypromine are longterm use may lead to down-
nonselective MAO inhibitors while Selegiline is a MAO-B regulation of Beta receptors
selective inhibitor; For MDD unresponsive to other agents ; dizziness, insomnia, orthostatic hypotension, (leading to decrase in BP) ; lower
i. Phenelzine, tranylcypromine, useful in patients with significant anxiety, phobic features blurred vision, arrhythmia, diarrhea, seizure threshold ; selegiline may
selegiline and hypochondriasis hyperthermia, CNS stimulation, seizure be given as skin patch
Opioid Analgesics and Antagonists

11
 Additive CNS depression with other
A. Full Agonist TRIAD: miosis, coma, respiratory depression depressants
Exerts hemodynamic effects on the
pulmonary circulation ; significant
first-pass effect ; metabolized in the
miosis, restlessness, respiratory depression, body to morphine-6-glucuronide
Strong agonist at u receptors; For severe pain, pain increased ICP, postural hypotension, urinary which has equal analgesic activity
i. Morphine associated with acute MI, for pulmonary edema retention, pruritus, addiction liability as morphine
restlessness, respiratory depression, increased May be given transdermally or via
Strong agonist at u receptors; For severe pain, adjunct in ICP, postural hypotension, urinary retention, lollipop; ohmefentanyl is the most
ii. Fentanyl anesthesia, chronic pain and breakthrough cancer pain pruritus, addiction liability potent opioid
Only opioid that does not cause
miosis and biliary contraction ;
opioid of choice for pain relief in
pancreatitis ; metabolized to
normeperidine which can cause
seizure therefore contraindicated in
Strong agonist at u and k receptors, inhibits pain patients with seizure disorder ; if
neurotransmission, muscarinic blocking actions; For restlessness, respiratory depression, increased given with MAOi --> Hyperpyrexic
moderate to severe pain, labor analgesia, spasmodic pain ICP, postural hypotension, urinary retention, coma, if given with SSRI -->
iii. Meperidine (biliary, renal), preoperative sedation pruritus, addiction liability, seizures Serotonin syndrome
Used in methadone maintenance
Strong agonist at u receptors, inhibits pain therapy (MMT) for opioid
neurotransmission, binds NMDA receptors and miosis, restlessness, respiratory depression, dependence; currently being
antagonizes the effects of glutamate; For moderate to increased ICP, postural hypotension, urinary investigated as a novel treatment
iv. Methadone severe pain, opioid dependence, opioid withdrawal retention, pruritus, addiction liability for leukemia
B. Partial Agonist / Moderate Agonist
Strong agonist at u receptors, inhibits pain
neurotransmission, binds NMDA receptors and miosis, restlessness, respiratory depression, there is genetic variation in the
antagonises the effects of glutamate; For moderate to increased ICP, postural hypotension, urinary metabolism of codeine and its
i. Hydrocodone, oxycodone severe pain, opioid dependence, opioid withdrawal retention, pruritus, addiction liability derivatives
Decreases sensitivity of cough receptors, depressing the hallucination, confusion, excitation, increased or
medullary cough center through sigma receptors decreased pupil size, nystagmus, seizures, coma, codeine is metabolized by CYP2D6
ii. Dextrometorphan, codeine stimulation; For cough suppression respiratory depression, addiction liability to morphine
C. Weak Agonist
i. Propoxyphene, Weak agonist at u receptors, inhibits pain miosis, respiratory depression, increased ICP,
levopropoxyphene, neurotransmission; For mild to moderate pain, restless leg postural hypotension, urinary retention, pruritus, Withdrawn because of fatal
dextropropoxyphene syndrome addiction liability, fatal arrythmias cardiotoxicity
D. Mixed Agonist-Antagonist
Strong agonist at k receptors, weak antagonist activity at u Buprenorphine reduces craving in
receptors; For moderate to severe pain, opioid sedation, dizziness, sweating, nausea, anxiety, alcohol dependence,
i. Nalbuphine, buprenorphine, dependence, alcohol dependence, balance anesthesia, for hallucinations, nightmares, respiratory buprenorphine and nalbuphine is
butorphanol, pentazocine opioid withdrawal states (buprenorphine) depression (less), tolerance, dependence liability resistant to Naloxone
E. Opioid Antagonist
Precipitates abstinence syndrome
in Px with opioid dependence ;
Competitively blocks u, sigma and k receptors, rapidly Naloxone and Nalmefene is IV
i. Naloxone, naltrexone, reverses effects of opioid agonists; For opioid overdose, (DOA: 12-24 hrs) while Naltrexone is
nalmefene opioid and alcohol dependence (naltrexone) pruritus, nausea, vomiting PO (DOA: 48h)
F. Dual-acting
Weak agonist at u receptors, inhibits neuronal reuptake of Lower seizure threshold ; CI in Px
serotonin and norepinephrine; For moderate pain, chronic taking SSRI and those with history
i. Tramadol pain syndrome, neuropathic pain seizures, nausea, dizziness, pruritus, constipation of seizure

5. DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, & GOUT

Agents Used in Anemias and Hematopoietic Growth Factors
A. Hematopoietic growth factor
i. Ferrous sulfate, Ferrous
gluconate, Ferrous Fumarate, Iron Required for the biosynthesis of heme and heme Black stools, shock, lethargy, dyspnea, abdominal
dextran, Sodium Ferric Gluconate containing proteins, including hemoglobin and myoglobin; pain, necrotizing gastroenteritis, death, organ
complex, Iron sucrose For Iron deficiency anmia, iron supplementation failure, hemochromatosis, metabolic acidosis None
B. Heavy metal chelator
Hypotension, Neurotoxicity, ARDS, Increased
i. Deferoxamine, Deferasirox Chelates excess iron; For acute and chronic iron poisoning susceptibility to infections None
C. Hematopoietic growth factor
Cofactor required for essential enzymatic reactions that
form tetrahydrofolate, convert homocysteine to Hydroxocobalamin has a longer
i. Cyanocobalamin, methionine and metabolize methylmalonyl-CoA; For t1/2 than cyanocobalamin ; has a
Hydroxocobalamin vitamin B12 deficiency, megaloblastic anemia No significant toxicity storage of up to 5yrs in the liver
D. Hematopoietic growth factor
Precursor of an essential donor of methyl groups used for
synthesis of amino acids, purines and deoxynucleotide; For
i. Folic acid, Folacin Megaloblastic anemia, prevention of neutral tube defects only modest amounts are stored in
(Pteroylglutamic acid), Folinic acid (spina bifida), prevention of coronary artery disease No significant toxicity the body
E. Hematopoietic growth factor
Performance-enhancing drug in
athletes ; darbepoietin is once a
i. Epoetin Alfa, Darbepoetin alfa, Agonist of erythropoietin receptors expressed by red cell week administration, while
Methoxy Polyethylene Glycol- progenitors; For Anemia, associated with chronic renal Methoxy Polyethylene Glycol-
Epoetin Beta failure, cancer, HIV infection and prematurity Hypertension, Thrombosis, Pure red cell aplasia Epoetin Beta is 1-2x per month
F. Myeloid growth factor

12
 Binds receptors on myeloid progenitors and stimulates cell
maturation and proliferation ; Accelerates neutrophil
recovery and reduces incidence of infection; For
i. (G-CSF) Filgrastim, Sargamostim neutropenia associated with chemotherapy,
(GM-CSF), Pegfilgrastim myelodysplasia, and aplastic anemia Edema, Fever, Arthralgia Pegfilgrastim has longer t1/2
G. Megakaryocyte growth factor
Recombinant form of an endogenous cytokine; activates IL -
i. Oprelvekin(IL-11), 11 receptors ; For secondary prevention of fatigue, headache, anemia, fluid accumulation in
Thrombopoietin thrombocytopenia in patients undergoing chemotheraphy the lungs, dizziness, transient atrialarrythmias given SC OD
Agents Used in Dyslipidemia
has direct anti-atherosclerotic
effect, and can prevent bone loss ;
Increased risk of myopathy and
rhabdomyolysis when used with
fibrates ; Given before bedtime
because cholesterol synthesis
predominantly occurs at night ;
simvastatin and lovastatin are
prodrugs, all the rest are in their
active form already ; Rosuvastatin,
Atorvastatin and Simvastatin have
Inhibits rate-limiting enzyme in cholesterol biosynthesis greater maximal effect than other
A. HMG-CoA Reductase Inhibitors: (HMG-CoA reductase), Increased hepatic cholesterol statins ; if given together with resins
Simvastatin, Atorvastatin, uptake, Increased high affinity LDL receptors which leads give at least 1hr before or 4hrs after
Rosuvastatin, Fluvastatin, to decreased LDL levels ; DOC for hypercholesterolemia resin administration (resins
Pravastatin, Lovastatin, (high LDL), decreases risk of acute coronary syndromes, Hepatoxicity, Myopathy, Rhabdomyolysis, decrease the absorption of statins) ;
Pitavastatin, Cerivastatin, ischemic stroke Gastrointestinal distress, Teratogen has CYP450 dependent metabolism
non-absorbable polymers that bind bile acids and similar
steroids in the intestines preventing their reabsorption, Increases TGs and VLDL in patients
increases cholesterol utilization for replacement, modestly with high TGs and combined
B. Bile Acid Binding Resin: lowers LDL levels by increasing hepatic LDL receptors ; For Constipation, Bloating, Gritty taste, Gallstone hyperlipidemia ; Treat constipation
Colesevelam, Colestipol, hypercholesterolemia (high LDL), pruritus in cholestasis, formation, steatorrhea, malabsortion of fat with fiber supplements/psyllium ;
Cholestyramine digitalis toxicity soluble substances (vitamin k, folate) Avoid in patients with diverticulitis
Selective inhibitor of the NPC1L1 transporter decreasing
intestinal absorption of cholesterol and other phytosterols,
decreases cholesterol hepatic pool, increases hepatic LDL
C. NPC1L1 transporter inhibitor: receptors ; For Hypercholesterolemia (High LDL), Synergistic LDL-lowering effect with
Ezetimibe phytosterolemia Hepatoxicity (increased with statin use), Myositis statins ; is a prodrug
Cholesterol analog, takes the place of dietary and billiary
cholesterol, decreasing intestinal absorption of cholesterol
D. Sterol absorption blocker: and other phytosterols ; For Hypercholesterolemia (high Gastrointestinal upset, bloating, impotence
Sitosterol LDL), phytosterolemia (rare), coronary events NONE
decreases fibrinogen and increases
Decreases VLDL synthesis and LDL cholesterol t-PA ; NSAIDs pre-treatment
concentrations, decreases hormone-sensitive lipase reduces flushing ; Avoid in patients
activity leading to decreased LDL levels, Increases HDL Flushing, nausea, vomiting, Pruritus, Acanthosis with peptic ulcer disease ;
cholesterol by decreasing its catabolism ; DOC for nigricans, Rashes, Gastrointestinal irritation, Potentiates effects of
increasing HDL levels, for Hypercholesterolemia (low HDL, Hepatoxicity (mild), Hyperuricemia, Impaired antihypertensives (vasodilators,
E. Nicotinic Acid derivatives: Niacin high LDL/VLDL), hypertriglyceridemia glucose tolerance, Arrhythmias, Ambylopia ganglion blockers)
Increased risk of myopathy and
rhabdomyolysis when used with
statins ; Avoided in patients with
hepatic or renal dysfunction ; may
increase LDL in patients with
familial combined
Activates PPAR-α and increases expression of lipoprotein hyperlipoproteinemia ; has little or
lipase and apolipoproteins (apoA-I, apoA-II) leading to no effect on LDL ; higher risk of
F. Fibrates: Gemfibrozil, enhanced clearance of TG-rich lipoproteins, Lowers Nausea, Rashes, Leukopenia, nausea, vomiting, gallstone formation if given
Fenofibrate, Bezafibrate triglycerides, Increases HDL ; DOC for hypertriglyceridemia increased risk of cholesterol gallstones together with resins
Drugs for Coagulation
A. Antiplatelet For arterial thrombosis only
Nonselective, irreversible COX 1&2 inhibitor. Reduces
platelet production of thromboxane A2, temporarily inhibit
Prostacyclin synthesis ; For prevention or arterial Gastrointestinal toxicity, nephrotoxicity, tinnitus, Uncoupler of oxidative
thrombosis (MI, TIA, CVD), Inflammatory disorders hyperventilation, hypersensitivity, HAGMA, phosphorylation, associated with
(rheumatic fever, juvenile rheumatoid arthritis, kawasaki Increased bleeding time, Nephrotoxicity (AKI and Reye syndrome in children ; Do not
i. Aspirin disease) inhibits the binding of fibrin and other ligands
Reversbily Interstitial Nephritis) use as NSAID for gout
to the platelet GPIIb-IIIa receptor ; For antithrombosis
ii. GPIIb-IIIa inhibitor: Abciximab, during PCI, Acute coronary syndromes (unstable angina,
Eptifibatide,Tirofiban NSTEMI) Bleeding, Thrombocytopenia Adjunct to thrombolysis
Inhibits phosphodiesterase III and increases cAMP in
platelets and blood vessels, Inhibits platelet aggregation additional MOA: inhibit uptake of
and causes vasolidation ; For prevention of adenosine by endothelial cells and
thromboembolic complications of cardiac valve RBC, thus increasing adenosine
replacement (as adjunct to warfarin), secondary levels leading to inhibition of
iii. PDE III inhibitor: prevention of ischemic stroke (with aspirin), Intermittent platelet aggregation ; Cilostazol is
Dipyridamole, Cilostazol claudication (Cilostazol only) Headache, palpitations contraindicated in heart failure
Irreversibly inhibits binding of ADP to platelet
receptors,thus reducing platelet aggregation ; For
prevention and treatment of arterial thrombosis (stroke, Bleeding, nausea, hematologic (neutropenia, GI & Hematologic SE are more
iv. ADP inhibitor: TIA, unstable angina), Acute coronary syndromes, leukopenia), thrombotic thrombocytopenic common with ticlopidine. Additive
Clopidogrel,Ticlopidine, Prasugel Prevention of re-stenosis after PCI purpura (Ticlopidine), dyspepsia effects with aspirin
B. Anticoagulant For both venous and arterial thrombosis

13
 Activates antithrombin III which Inactivates thrombin or
factor IIa, factor IXa & factor Xa by forming stable
complexes with them ; For deep venous thrombosis,
myocardial dysfunction, Pulmonary embolism, adjuvant to
percutaneous coronary intervention (PCI) and
thrombolytics, Atrial fibrillation, Pulmonary embolism, DOC for anticoagulation during
given with thrombolytics for revascularization procedures, Bleeding, transient Heparin-induced pregnancy ; administered IV or SC ;
i. Heparin (indirect thrombin given with GPIIb-IIIa inhibitors for angioplasty and stent thrombocytopenia, Osteoporosis with chronic Monitor with aPTT, Antidote:
inhibitor) placement use Protamine Sulfate
Does not require aPTT monitoring,
Binds and potentiates effect of antithrombin III on factor Protamine sulfate is only partially
Xa (more selective for Xa); For Deep venous thrombosis, effective in reversing effects ;
ii. LMWH: Enoxaparin, Pulmonary embolism, unstable angina, myocardial advantage over regular heparin is
Dalteparin, Tinzaparin, infarction, adjuvant to percutaneous coronary intervention higher bioavailability and t1/2 ;
Fondaparinux (PCI) and thrombolytics, Atrial fibrillation Bleeding, less risk of thrombocytopenia Fondaparinux is given SC OD
Monitor with aPTT. No reversal
Binds to thrombin's ative site and inhibits its enzymatic agents exist ; Dabigatran is PO while
iii. Direct Thrombin Inhibitors: action; For anticoagulation in patients with heparin all the rest are parenteral ;
Lepirudin, Desirudin, Bivalirudin, induced thrombocytopenia (HIT), percutaneous coronary Bleeding, Anaphylactic reactions, Effect- Bivalirudin also inhibits platelet
Argatroban, Dabigatran angioplasty (Bivalirudin with aspirin) prolonging antibodies activation
iv. Direct Oral Factor Xa inhibitor: bind to free and bound factor Xa ; For prevention of
Rivaroxaban, Apixaban Venous thrombosis, in stroke patients with Afib bleeding No reversal agent
Inhibits vitamin K epoxide reductase (responsible for y-
carboxylation of the vitamin K- dependent clotting (factors Monitor effects with PT-INR.
II, VII, IX, X, Protein C & Protein S) ; For chronic Bleeding, Teratogen (bone defects, hemorrhage), Antidote is vitamin K or FFP. Narrow
anticoagulation (DVT, atrial fibrillation, valve replacement) warfarin-induced skin necrosis (transient therapeutic window ; 99% protein-
v. Warfarin, Dicumarol EXCEPT in pregnancy hypercoagulability) bound
C. Antidote
Chemical antagonist of heparin. Reverses excessive
anticlotting activity of unfractionated heparin; For heparin hypotension, flushing, bradycardia, dyspnea,
i. Protamine Sulfate overdosage hypersensitivity Partially reverses effect of LMWHs
Increases supply of reduced vitamin K, which is required
for synthesis of functional vitamin K-dependent clotting
ii. Endogenous Vitamin: Vitamin and anticlotting factors ; For Vitamin K deficiency, Antidote
K1, K2, K3 (Phytonadione, to warfarin, prevention of hemorrhagic diatheses in Severe infusion reaction when administered at a
Menaquinone, Menadione) newborns fast rate (dyspnea, chest and back pain) Vit K1 may be given PO or IV
Tx should be done within 6 hrs,
better if within 3hrs ; Antidote is
AMINOCAPROIC ACID ;
Streptokinase forms a complex with
endogenous plasminogen, thus
D. Thrombolytic: Alteplase, Tissue plasminogen activator analog. Converts catalyzing the conversion of
Anistreplase, Reteplase, plasminogen to plasmin, which degrades the fibrin and Bleeding, Reperfusion, Cerebral hemorrhage, plasminogen to plasmin ; tPA is
Streptokinase, Tenecteplase, fibrinogen, causing thrombolysis ; For acute myocardial Arrhythmias ; Loss of effectiveness (on 2nd use) selective for fibrin-bound
Urokinase infarction, pulmonary embolism, Ischemic stroke and allergic reactions (streptokinase) plasminogen
Competitively inhibits plasminogen activation thus
inhibiting fibrinolysis ; For prevention and treatment of
acute bleeding episodes in patients with high risk of Contraindicated in disseminated
E. Antiplasmin drug: Tranexamic bleeding (hemophilia, intracranial aneurysms, menstrual, intravascualr coagulation (DIC) and
acid obstetrics, thrombolytics, postperative) Thrombosis, hypotension, Myopathy, Diarrhea genitourinary bleeding
Vasopressin V2 receptor agonist, Increases factor VIII
activity of patients with mild hemophilia A or VWD; For
hemophillia A, von Willebrand's disease, central diabetes headaches, nausea, flushing, seizures, may cause immunologic reactions
F. ADH agonist: Desmopressin insipidus hyponatremia and infections
Non-steroidal Anti-Inflammatory Drugs, Disease-Modifying Anti-rheumatic Drugs, Non-opioid Analgesics & Drugs Used in Gout
A.Non-selective NSAID
low doses undergo first order
kinetics while high doses undergo
zero order reaction ; Long term use
i. Aspirin, Sodium Salicylate See entry on Drugs for caogulation Disorder See entry on Drugs for caogulation Disorder reduces the
Ibuprofen andriskIndomethacin
of colon cancer
can be
used to close PDA ; Ibuprofen and
naproxen have moderate
effectiveness ; Ibuprofen is
relatively safe but with short half-
life of 2hrs ; Naproxen and
ii. Ibuprofen, Diclofenac, Piroxicam have longer half-lives ;
Diflunisal, Etodolac, Fenoprofen, Ketorolac has significant analgesic
Flurbiprofen, Ketoprofen, effect but not anti-inflammatory
Meloxicam, Nabumetone, effect ; use Ketorolac only for 72hrs
Naproxen, Oxaprozin, Piroxicam, Nonselective reversible COX-1 and COX-2 inhibitor. Inhibits Gastrointestinal bleeding (less than aspirin), due to GI and renal damage ;
Sulinidac, Tolemtin, Mefenamic prostaglandin and thromboxane synthesis ; For analgesia, Nephrotoxicity (AKI and Interstitial Nephritis), NSAIDs may interfere with ASA's
acid, Ketorolac fever and as anti inflammatory Hypersensitivity reaction antithrombotic action
Nonselective reversible COX-1 and COX-2 inhibitor. Inhibits
prostaglandin synthesis and inhibit crystal phagocytosis by Gastrointestinal toxicity, pancreatitis, Indomethacin has greater anti-
macrophages ; For anti inflammatory (gout arthritis, Nephrotoxicity, Serious hematologic reactions, inflammatory effect compared to
iii. Indomethacin ankylosing spondylitis), for closing PDA BM suppression other NSAIDs
Gastrointestinal bleeding, Nephrotoxicity (same Rofecoxib and Valdecoxib
B. COX-2 Selective NSAID: Selective COX-2 inhibitor. Inhibits prostaglandin synthesis ; risk as nonselective NSAIDs), Myocardial withdrawn due to incereased
Celecoxib, Etoricoxib, Parecoxib For Analgesia, Anti inflammatory, Antipyretic infarction and stroke incidence of thrombosis
C. Non-opioid Analgesic (COX3 Selectively inhibits COX-3 in the CNS, Weak COX-1 and COX- Hepatoxicity (antidote: NAC), Renal papillary Preferred antipyretic in children
inhibitor) Paracetamol 2 inhibitor in the periphery, Inhibits prostaglandin necrosis and Interstitial nephritis, (does not cause reye's syndrome) ;
(Acetaminophen) synthesis ; For Analgesia and antipyretic Methemoglobinemia, Hemolytic anemia t1/2 is only 2-3h
D. Disease Modifying Anti-Rheumatic Drug
Inhibits AICAR transformylase and thymidylate synthase,
with secondary effects on polymorphonuclear chemotaxis Nausea, Mucosal ulcers, hepatoxicity, DMARD of choice for Rheumatoid
; For rheumatoid arthritis, SLE, JRA, psoriatic arthritis, hypersensitivty, Pseudolymphomatous reaction, arthritis, Rescue agent: Leucovorin
i. Methotrexate Ankylosing spondylitis, Polymyositis teratogen, hematotoxicity (Folinic acid)

14
 Bacterial infections (URTIs), reactivation of latent
tuberculosis, lymphoma, Demyelination,
Reactivation of Hepatitis B, Auto antibody
ii. TNF-alpha inhibitor: Infliximab, Binds or inhibits to TNF-a ; For Crohn's disease, rheumatoid formation (ANA, anti dsDNA), infusion reactions, Synergistic effects with
Adalimumab, Etanercept arthritis, other rheumatic disease hepatoxicity, hematotoxicity, cardiotoxicity methotrexate

Cannot give allopurinol with

azathioprine (allopurinol reduces
Forms 6-thioguanine, suppressing inosinic acid synthesis, B- xanthine oxidase catabolism of
cell and T-cell function, Immunoglobulin production and Bone marrow supression, increased risk of purine analogs, increasing 6-
interleukin-2 secretion ; For rheumatoid arthritis, psoriatic infections, increased incidence of lymphoma, thioguanine nucleotides, leading to
iii. Azathioprine arthritis, reactive arthritis, polymyositis, SLE Fever, rash, hepatotoxicity, allergic reactions severe leukopenia)

Suppression of T-lymphocyte leading to decreased

leukocyte chemotaxis, stabilization of lysosomal enzymes,
inhibition of DNA and RNA synthesis, trapping of free Ocular toxicity, Dyspepsia, Nausea, vomiting,
iv. Chloroquine, radicals ; For rheumatiod arthritis, SLE, Sjogren's abdominal pain, rashes, nightmares, myopathy,
Hydroxychloroquine syndrome, Malaria neuropathy, ocular toxicity safe for pregnant women

Forms phospharamide mustard, which cross links DNA to

prevent cell replication, Supresses T-cell and B-cell
function ; For Rheumatoid arthritis, SLE vasculitis, Hemorrhagic cystitis, Rescue agent
v. Cyclophosphamide Wegener's granulomatosis, severe rheumatic diseases Hemorrhagic cystitis is Mesna
Inhibits interleukin-1 and iterleukin-2 receptor production
and secondarily inhibits macrophage-T-cell interaction and
T-cell responsiveness ; For rheumatoid arthritis, SLE, Tissue Nephrotoxicity, hypertension, hyperkalemia,
vi. Cyclosporine transplantation hepatoxicity, Gingival hyperplasia, hirsutism NONE
active product inhibits inosine monophosphate
dehydrogenase and inhibits T-cell lymphocyte proliferation
; For SLE nephritis, vasculitis, Wegener's granulomatosis, Gastrointestinal disturbances, headache,
vii. Mycophenolate Mofetil rheumatoid arthritis hypertension, reversible myelosupression NONE

Nausea, vomiting headache,rash, hemolytic

anemia, methemoglobinemia, neutropenia,
active metabolite inhibits the release of inflammatory leukopenia, thrombocytopenia, pulmonary
bowel cytokines; For rheumatoid arthritis, inflammatory toxicity, autoantibody formation (anti dsDNA),
viii. Sulfasalazine bowel disease, JRA, ankylosing spondylitis Reversible infertility in men anti-IBD drugs
E. Antigout drugs

Diarrhea, nausea, vomiting, abdominal pain, a general mitotic poison, may also
hepatic necrosis, acute renal failure, be used for Familial Mediterranean
Inhibits microtubule assembly and LTB4 production disseminated intravascular coagulation, seizures, Fever ; diarrhea is the adverse
i. Microtubule assembly inhibtor: leading to decreased macrophage migration and hair loss, bone marrow depression, peripheral effect which signals toxicity from
Colchicine phagocytosis ; For gout neuritis, myopathy colchicine

May precipitate acute gout during

early phase of drug action (prevent
by coadministering with colchicine
or indomethacin) ; may be given
together with antimicrobial agents
(particularly Penicillins) to prolong
are weak acids that compete with uric acid for therapeutic effect by inhibiting
ii. Uricosuric agent: Probenecid, reabsorption in the PCT leading to increased uric acid Gastrointestinal irritation, rashes, nephrotic renal tubular secretion of
Sulfinpyrazone excretion ; For gout syndrome, aplastic anemia ; sulfa allergy antibiotics
Inhibits metabolism of
mercaptopurine and azathioprine.
Witheld for 1-2 wk after an acute
episode of gouty arthritis
(coadministered with colcichine or
indomethacin to avoid an acute
attack) ; Feboxustat is a newer non-
Active metabolite (alloxanthine) irreversibly inhibits Gastrointestinal upset, Rash, Peripheral neuritis, purine inhbitor of Xanthine Oxidase
iii. Xanthine oxidase inhibitor: xanthine oxidase and lowers production of uric acid; 1st Vasculitis, bone marrow dysfunction, Aplastic ; Febuxostat is more effective than
Allopurinol, Febuxostat line treatment of chronic gout, tumor lysis syndrome anemia, liver dysfunction (Febuxostat) Allopurinol

6. ENDOCRINE DRUGS
Hypothalamic and Pituitary Hormones

Recombinant Growth hormone, Increases release of IGF-1

in the liver and carilage, stimulates skeletal muscle growth,
amino acid transport, protein synthesis and cell
proliferation ; For GH deficiency in children and genetic
disease associated with short stature (Turner syndrome,
Prader-Willi syndrome), failure to thrive due to chronic Peripheral edema, Myalgia, Arthralgia,
renal failure or SGA, AIDS wasting, improve GI function in Intracranial hypertension, pseudotumor cerebri, used as Performance enhancing
patients who underwent intestinal resection that led to slipped capital femoral epiphysis, progression of drug since it increases muscle mass
i. Somatropin malabsorption syndrome scoliosis, hyperglycemia ; given SC

Recombinant IGF-1 ; For children unresponsive to GH remedy to hypoglycemia: give

ii. Mecasermin therapy Hypoglycemia, increased LFT, intracranial HTN patient some snacks prior to dose
Somatostatin analog, suppresses the release of growth
hormones, glucagon, insulin, gastrin, IGF-1, serotonin and regular release: given BID-QID SC, if
gastrointestinal peptides ; For Acromegaly, pituitary slow release: every 4wks IM ; are
adenoma, carcinoid, gastrinoma, glucagonoma, variceal GI upset, gallstone, cardiac condution long-acting synthetic analogs of
iii. Octreotide, Lanreotide bleeding abnormality somatostatin

15
 Diarrhea, nausea, flu-like syndrome, elevated onset of action is expected within
iv. Pegvisomant GH receptor antagonist ; For acromegaly LFTs, hypesensitivity
Headache, depression,reaction
edema, ovarian 2wks of usealfa and beta are
Follitropin
Gonadotropin analog (FSH analog); activates FSH receptors hyperstimulation syndrome (ovarian recombinant FSH forms while
and mimics effects of endogenous FSH ; For Controlled enlargement, ascites, hypovolemia, shock), Urofollitropin is a purified
v. Follitropin alfa, Follitropin ovarian hyperstimulation, infertility due to hypogonadism multiple pregnancies in women, gynecomastia in preparation from urine of
beta, Urofollitropin in men men postmenopausal women

menotropins are mixtures of FSH

and LH from postmenopausal
Gonadotropin analog (LH analog); activates LH receptors women ; Choriogondaotropin alfa
vi. Menotropins, Human and mimics effects of endogenous LH ; For Controlled Headache, depression, edema, ovarian is a recombinant hCG while
chorionic gonadotropin (HCG), ovarian hyperstimulation (ovulation induction), hyperstimulation syndrome, multiple Lutropin is a recombinant LH ; hCG
Choriogondaotropin alfa, Lutropin hypogonadotripic hypogonadism pregnancies in women, gynecomastia in men given IM
there is exacerbation of symptoms
in males with prostate CA and
GnRH analog, increased LH and FSH secretion with children with precocious puberty
intermittent administration , reduced LH and FSH secretion during the first few weeks of
with prolonged continuous administration (due to therapy (remedy: co-administer
downregulation of GnRH receptors in the pituitary cells Flutamide, an androgen receptor
vii. Leuprolide, Gonadorelin, that normally release LH and FSH ; For Controlled ovarian Hot flushes, sweats, headaches, osteoporosis, antagonist) ; Gonadorelin is a
Goserelin, Histrelin, Nafarelin, hyperstimulation, endometriosis, myoma uteri, precocious gynecomastia, reduced libido, decreased synthetic human GnRH ; Leuprolide
Triptorelin puberty, prostate CA hematocrit has a long agonist activity

Does NOT cause tumor flare-up

whe used for treatment of
advanced prostate cancer, also less
likely to cause ovarian
GnRH antagonist, blocks GnRH receptors, reduces hyperstimulation syndrome ;
endogenous production of LH and FSH ; For Controlled Nausea, headache, hypersensitivity, hot flushes, Degarelix is used for prostate CA
viii. Ganirelix, Cetrorelix, ovarian hyperstimulation (prevents premature LH surge), gynecomastia, decreased libido, decreased while Ganirelix prevent LH surge in
Degarelix advanced prostate CA hematocrit, osteoporosis controlled ovulation

Dopamine agonist, partial agonist at dopamine D2 Nausea, headache, lightheadedness, orthostatic

receptors in brain, inhibits prolactin release ; For hypotension, fatigue, behavioral changes, Slightly inhibits GH release if given
Hyperprolactinemia, Pituitary adenoma, acromegaly, erythromelalgia, Raynaud's phenomenon, in high doses ; CI in patients with
ix. Bromocriptine, Carbegoline Parkinson's disease pulmonary infiltrates history of psychotic illness
Activates oxytocin receptors, stimulates uterine
contraction and labor, stimulates mammary glands,
lactation and milk let-down ; For Labor induction, labor Fetal distress, placental abruption, uterine
augmentation, control of uterine hemorrhage post- rupture, fluid retention, hyponatremia, heart ATOSIBAN - an oxytocin antagonist
x. Oxytocin delivery failure, seizures, hypotension used in preterm labor

ADH agonist, Vasopressin V2 receptor agonist which

causes insertion of water channels in the collecting duct also contracts vascular smooth
leading to more water reabsoprtion, also regulates the muscles via V1 receptor leading to
release of factor VIII and VWF ; For Central DI, Hemophilia vasoconstriction, used as treatment
A, von Willebrand's disease, Variceal bleeding, colon Headaches, flushing, nausea, hyponatremia, for esophageal varices or colon
xi. Desmopressin, Vasopressin diverticula, primary nocturnal seizures seizures diverticula

Central pontine myelinolysis may

ADH antagonist, Antagonist at V1a and V2 receptors ; For occur with rapid correction of
xii. Conivaptan, Tolvaptan, SIADH, Hyponatremia, offset fluid retention in acute heart hyponatremia, tolvaptan is more
Lixivaptan failure and SIADH which causes hyponatremia (dilutional) Infusion site reactions, hyperkalemia selective for V2 receptors
Thryoid & Antithyroid Drugs

T4 dose must be lowered in

patients with cardiovascular disease
or longstanding hypothyroidism
Thryoid hormone, activation of nuclear receptors results in (increased cardiosensitivity) ;
i. Levothyroxine (T4), gene expression with RNA formation and protein synthesis Dry skin, sweatng, tachycardia, nervousness, Liothyronine has a faster onset but
Liothyronine (T3) ; For Hypothyroidism, myxedema coma tremor, weight loss, weakness, heat intolerance shorter half-life
Maculopapular pruritic rash, gastrointestinal
distress, fulminant hepatitis, agranulocytosis, Drug of choice for pregnant
urticaria, vasculitis, lupus-like syndrome, hyperthyroid patients (does not
Inhibits thyroid peroxidase reactions, blocks iodine lymphadenopathy, hypoprothrombinemia, eneter placenta and breastmilk);
organification, inhibits peripheral conversion of T4 into T3 ; Exfoliative dermatitis, polyserositis, arthralgia, slow onset of action (3-4 weeks for
ii. Propylthiouracil (PTU) For Hyperthyroidism, thyroid storm hypothyroidism full effect)
Maculopapular pruritic rash, gastrointestinal
distress, fulminant hepatitis, dose-dependent,
agranulocytosis, urticaria, vasculitis, lupus-like Methimazole and Carbimazole are
syndrome, lymphadenopathy, teratogens (causes Aplasia Cutis
Inhibits thyroid peroxidase reactions, blocks iodine hypoprothrombinemia, Exfoliative dermatitis, Congenita) ; given as once daily
iii. Methimazole, Carbimazole organification ; For Hyperthyroidism, thyroid storm polyserositis, arthralgia, hypothyroidism dosing

onset is more rapid (2-7 days) but

effect is transient (thyroid gland
escapes iodide block after several
Inhibit iodine organification and hormone release leading weeks of treatment) ; Should not be
to reduced size and vascularity of thyroid gland ; For Iodism, acneiform rash, swollen salivary glands, used alone (escape in 2-8 weeks);
Hyperthyroidism, thyroid storm, preparation for surgical mucous membrane ulcerations, conjunctivitis, prevents radiation induced thryoid
iv. Lugol Solution (Iodine in thyroidectomy to reduce the size and vascularity of the rhinorrhea, drug fever, metallic taste, bleeding damage; prenatal exposure causes
Potssium Iodide), Potassium Iodide thyroid gland, radiation prophylaxis disorders, anaphylactoid reactions fetal goiter
Beta blocker control HR and other cardiac abnormalities of Esmolol may be used to treat
severe thyrotoxicosis, slows pacemaker activity; inhibits thyrotoxicosis-related arrhythmias;
v. Propranolol, Esmolol, peripheral conversion of T4 into T3 ; For Hyperthyroidism, Bronchospasm, cardiac depression, AV block, causes clinical improvement
Metoprolol, Atenolol thyroid storm, post MI prophylaxis, hypertension hypotension WITHOUT altering thyroid hormone

16
 Preferred treatment for most
Iodide, emits beta rays causing destruction of thyroid patients due to ease of
parenchyma ; For hyperthyroidism, permanent cure of administration, effectiveness, low
thyrotoxicosis without surgery and no effect on other expense and absence of pain;
vi. Radioactive Iodine tissues Permanent hypothyroidism, sore throat contraindicated in pregnant women
Adrenocorticosteroids & Adrenocortical Antagonists
i. Low Potency: Desonide Effects: stimulate gluconeogenesis,
ii. Med Potency: Fluticasone, increased fat deposition, muscle
Mometasone protein and bone catabolism,
lymphoid connective tissue fat and
skin wasting inhibit cell-mediated
immunologic functions,
lymphotoxic, increased neutrophils,
decreased lymphocytes eosinophils
basophils and monocytes, inhibit
leukocyte migration, inhibit PLA2,
Glucocorticoid, activates glucocorticoid receptors, leading delay rejection in transplant
to altered gene transcription, Suppresses inflammation, patients, increased GI acid secretion
Replaces cortisol when deficient ; For Acute adrenal (ulcer) ; Biochemical effects:
insufficiency associated with life-threatening shock, induced synthesis of an inhibitor of
chronic adrenal insufficiency (Addison's disease), Adrenal suppression, growth inhibition, DM, PLA2, decreased mRNA for COX2,
iii. High Potency: congenital adrenal hyperplasia, insect bites, contact muscle wasting, osteoporosis, salt retention, decrease in IL-2 and IL-3 and
Desoximetasone, Clobetasol dermatitis, status asthmaticus, thyroid storm glucose intolerance, behavioral changes decrease in Platelet Activating

iv. Synthetic GCs: Prednisone, Glucocorticoid; For supressession of inflammation and

Prednisolone, immune response, hematopoeitic cancers, transplant prednisolone is the active
Methylprednisolone, rejection, collagen and rheumatic disease, lung maturation metabolite of prednisone ; this
Meprednisone, Dexamethasone, in preterm labor (betamethasone and dexamethasone), Adrenal suppression, growth inhibition, muscle group has a long t1/2, reduced salt-
Betamethasone, Triamcinolone, bronchial asthma, chemotherapy-induced vomiting, wasting, osteoporosis, salt retention, glucose retaining effect and better
Beclomethasone, Budesonide hypercalcemia, mountain sickness intolerance, behavioral changes (psychosis) penetration of lipid barriers

Additive hypokalemia with loop

diurectics and thiazides ;
Deoxycorticosterone is the
strong agonist of mineralocorticoid receptors and precursor of aldosterone ;
moderate activation of glucorticoid receptors, Increases Na Fludrocortisone also has significant
reabsorption, K and H excretion ; For Chronic adrenal glucocorticoid activity ; Aldosterone
v. Mineralocorticoid: insufficiency (Addison's disease), Congenital adrenal Salt and fluid retention, Hypokalemia, Congestive is implicated in myocardial and
Fludrocortisone, hyperplasia, adrenal replacement therapy post- heart failure, muscle wastng, osteoporosis, vascular fibrosis and baroreceptor
Deoxycorticosterone adrenalectomy glucose intolerance, behavioral changes dysfunction
Corticosteroid Antagonists

Glucorticoid synthesis inhibitor, inhibits desmolase

activity, blocking conversion of cholesterol to Also inhibits synthesis of all
vi. Aminoglutethimide pregnenolone ; For Breast
Glucorticoid synthesis CA, Cushing
inhibitor; syndrome inhibits
azole antifungal; Skin rash, hepatotoxicity, hypothyroidism hormonally active steroids
cholesterol side chain cleavage, cytochrome P450 enzymes
and other enzymes necessary for synthesis of all steroids ;
For Adrenal CA, Hirsutism, Breast CA, steroid-responsive
metastatic Prostate CA, Cushing's syndrome, Fungal Hepatotoxicity, many drug interactions,
vii. Ketoconazole infections, hirsutism androgenic effect Potent inhibitor of CYP450 enzymes
Glucorticoid synthesis inhibitor, selective inhibitor of
steroid-11 hydroxylation, interfering with cortisol and
viii. Metyrapone corticosterone synthesis ; As diagnostic test for adrenal DOC for pregnant patients with
function Dizziness, GI disturbances Cushing's syndrome

abdominal pain and cramping, uterine cramping, also used as an approved

ix. Mifepristone (RU486) competitive inhibitor at the GC receptor as well as nausea, headache, vomiting, diarrhea, dizziness, abortifacient for medical abortion
progesterone receptor ; For Cushing's syndrome vaginal bleeding (usually together with misoprostol)

x. Spironolactone, Eplerenone Aldoesterone antagonist ; For hypokalemia due to other Hyperkalemia, gynecomastia (spironolactone) - also with weak antagonist effect at
diuretics, for post-MI, hyperaldoteronism- see entry - see entry - the androgen receptor
Gonadal Hormones and Inhbitors
A. Estrogen compounds Increases risk of endometrial cancer
and breast cancer ; Ethinyl Estradiol
has low bioavailability,
PO/TD/IM/Intravaginal ; Estradiol
cypionate is IM with longer t1/2 ;
Premarin is a mixture of conjugated
estrogen used in HRT ; Ethinyl
estradiol undergoes enterohepatic
recirculation ; Effects of Estrogen:
i. Ethinyl Estradiol, Mestranol,
growth of genital structures and
Estradiol cypionate, Premarin
secondary sexual characteristics,
breakthrough bleeding, nausea, breast modifies serum protein levels and
tenderness, migraine, thromboembolism (DVTs), decrease bone resorption,
Activates etrogen receptors, leads to changes in rates of gallbladder disease, hypertriglyceridemia, enhances coagulability of blood,
trasncription of estrogen-regulated genes ; For Primary hypertension, premature closure of the epiphysis increases TG and HDL levels while
hypogonadism, Postmenopausal hormonal replacement in young females, increased risk of breast and decreasing LDL levels, if given as
therapy, Osteoporosis and prevention of bone loss, endometrial cancer (remedy: add progesterone continuous infusion will inhibt FSH
Contraception, Intractable dysmenorrhea to the preparation) and LH release

17
 breakthrough bleeding, nausea, breast
tenderness, migraine, thromboembolism (DVTs),
Synthetic estrogen (nonsteroid); activates estrogen gallbladder disease, hypertriglyceridemia,
ii. Diethylstilbestrol receptors; leads to changes in rates of transcription of hypertension, premature closure of the epiphysis associated with Infertility, ectopic
estrogen-regulated genes ; For Atrophic vaginitis, hormone in young females, increased risk of breast and pregnancy, clear cell vaginal
replacement therapy, prevention of adverse pregnancy endometrial cancer (remedy: add progesterone adenocarcinoma in daughters of
outcomes, metastatic prostate CA to the preparation) women treated with DES
B. Progestins Prevents estrogen induced
endometrial cancer when used in
combination with estrogens;
Megesterol is used as an appetite
stimulant ; given PO or as vaginal
cream ; Medroxyprogesterone has a
better oral bioavilability ; L-
Norgestrel and Norethindrone has
i. Norgestrel,
more androgenic effect ; Norgestrel
Medroxyprogesterone,
undergoes enterohepatic
Norethindrone, Norgestimate,
recirculation ; Effects of
Desogestrel, Megestrol
activates progesterone receptors, changes rate of progesterone: induces secretory
transcription of progesterone-regulated genes ; For changes in the endometrium,
Hormone replacement therapy (given together with stabilize the endometrium, affect
Estrogen, to prevent estrogen-induced endometrial carbohydrate metabolism and
cancer), contraception, assisted reproduction (for Hypertension, decreased HDL, weight gain, stimulate deposition of fat, high
maintenance of pregnancy), anovulation induction (given reversible decrease in bone mineral density, doses suppress FSH and LH
in high doses to suppress FSH and LH) delayed resumption of ovulation after use secretion

C. Combined Hormonal Contraceptives maybe

LifetimePO/IM/TD/vaginal rings/IUD
risk of breast cancer is NOT
i. Estradiol + Norethindrone changed; Norethindrone is a
testosterone derivative while
ii. Ethinyl Estradiol + Desogestrel Drospirenone is a spironolactone
iii. Ethinyl Estradiol + Combined oral contraceptive, activates estrogen and derivative that is antiandrogenic ;
Drospirenone progesterone receptors, inhibits ovulation, effects on breakthrough bleeding, nausea, breast Norgestimate and Desogestrel are
cervical mucus gland, uterine tubes and endometrium lead tenderness, migraine, thromboembolism (DVTs), newer progestins ; combined OCPs
to decreased fertility, inhibit ovulation when given before breast cancer (earlier onset), headache, skin may be used for androgen-induced
iv. Ethinyl Estradiol + the LH surge ; For Contraception, hypogonadism, acne, pigmentation, depression, weight gain acne and hirsutism ; Mestranol (Estrogen)
Noregistmate hirsutism, dysmenorrhea, endometriosis hirsutism for older OCPs may also be used in OCPs
Progestin-only contraceptive, activates progresterone
receptors, Prevents conception by altering cervical mucus
and creating a hostile endometrium ; For Contraception, Breakthrough bleeding, hair loss, dysmenorrhea,
v. Medroxyprogesterone Acetate hormone replacement therapy delayednausea,
Severe return of fertility,breast
vomiting, osteoporosis
tenderness, IM depot preparation
Postcoital contraceptive, activates estrogen and/or irregular bleeding, headache, dizziness (fewer SE
progesterone receptors, thickens cervical mucus, inhibits compared to estrogen alone and combi Must be taken within 72 hours of
vi. Levonorgestrel ovulation ; For Emergency contraception contraceptives) unprotected sexual intercourse
D. Selective Estrogen Receptor Modulators (SERMs)
Estrogen antagonist actions in breast tissue and CNS,
Estrogen agonist effects in uterus, liver and bone ; For prevent osteoporosis in post-
Hormone responsive breast CA, prophylaxis of breast CA Hot flushes, thromboembolism, endometrial menopausal women ; Torimefene is
i. Tamoxifen, Torimefene esp. in those with high risk hyperplasia, endometrial cancer structurally related to Tamoxifen
Estrogen antagonist actions in breast tissue, uterus, and
CNS, Estrogen agonist effects in liver and bone. Increases
bone mineral density ; For Osteoporosis esp on post No estrogenic effect on endometrial
ii. Raloxifene menopausal women, breast CA prevention Hot flushes, thromboembolism tissue unlike tamoxifen

may cause multiple pregnancies ;

FULVESTRANT: pure estrogen
Partial agonist in pituitary, reduces negative feedback by receptor anatgonist in all tissues
estradiol, increases FSH and LH output ; For Induction of Hot flushes, afterimages, headache, constipation, used in breast CA resistant to
iii. Clomiphene ovulation in women who want to become pregnant reversible hair loss, ovarian enlargement tamoxifen
Effective against brest CA that have
become tamoxifen-resistant ;
iv. Anastrozole, Letrozole, Reduces estrogen synthesis by inhibiting aromatase ; For Hot flushes, musculoskeletal disorders, Exemestane is an IRREVERSIBLE
Exemestane breast CA, precocious puberty osteoporosis, joint pains inhibitor
Ovarian inhibitor, weak cytochrome P450 inhibitor and
partial agonist of progestin and androgen receptors ; For
Endometriosis, Fibrocystic disease, Hemophilia, Acne, hirsutism, weight gain, menstrual May also act on Glucocorticoid
v. Danazol Angioneurotic edema disturbances, hepatic dysfunction receptors

Combined with misoprostol results

in abortion of 95% of early
pregnancies ; as abortifacient in
early pregnancy (may be used up to
Vaginal bleeding, abdominal pain, GI upset 49days after menses) ;
Glucocorticoid receptor antagonist, progesterone receptor (vomiting, diarrhea), uterine cramping, nausea, complication: failure to induce
vi. Mifepristone (RU486) antagonist ; For Medical abortion, Cushing's syndrome vomiting, headache, dizziness, diarrhea complete abortion
vii. Leuprolide and Ganirelix see entry see entry see entry
E. Androgens may be given IV or as TD

Effects of androgen: secondary

sexual characteristics, fertility and
libido, male pattern baldness,
increases muscle mass, increased
Activates androgen receptors, promotes development of RBC production, decreased urea
male characteristics, increases body muscle bulk and RBC nitrogen excretion, maintains
i. Testosterone, production ; For Male hypogonadism, delayed puberty, Virilization and menstrual irregularities in normal bone density ; used illegally
Fluoxymesterone, wasting syndromes (for weight gain), certain types of females, paradoxical feminization in males, by atheletes as performance
Methyltestosterone anemias cholestatic jaundice, elevated LFTs enhancer

18
 Activates androgen receptors, promotes development of
male characteristics, increases body muscle bulk and RBC Virilization in females, paradoxical feminization
ii. Oxandrolone, Stanozolol, production; increased ratio of anabolic-to-androgenic in males; cholestatic jaundice, elevated liver this group is called "anabolic
Nandrolone activity in animals enzymes, hepatocellular CA steroids"
For benign and malignant prostate disease, precocious
F. Anti-androgens puberty, hair loss and hirsutism

GnRH analogs must be

coadministered with flutamide to
prevent acute flareups of prostate
i. Flutamide, Bicalutamide, Competitive antagonist at androgen receptor ; For Prostate Gynecomastia, hot flushes, impotence, CA ; Bicalutamide and Nilutamide
Nilutamide CA, surgical castration hepatotoxicity have less heaptotoxicity

Antagonist at androgen receptor. Marked progestational

effect that suppresses the feedback enhancement of LH
and FSH ; for Hirsutism, component of combined oral Hepatotoxicity, Adrenal suppression, depression,
ii. Cyproterone contraceptives, decreased sexual drive in men gynecomastia, galactorrhea, thromboembolism Orphan drug status
Dutasteride is newer with longer
Androgen synthesis inhibitor, inhibits 5a reducase enzyme t1/2 ; this group is less likely to
that converts testosterone to dihydrotestosterone ; For cause impotence, infertility and
iii. Finasteride, Dutasteride BPH, Male pattern baldness. Hirsutism Impotence, gynecomastia, depression decreased libido

iv. GnRH agonist and antagonists see entry see entry see entry
v. Spironolactone for treatment of hirsutism in women
vi. Ketoconazole inhibit gonadal and adrenal steroid synthesis see entry see entry
P ancreatic Hormones & Antidiabetic Drugs
A. Insulins
Effects of insulin: increased
glycogen and protein synthesis,
decreased protein catabolism,
increased TG storage ; rapid acting
i. Rapid Acting Insulin: Lispro, insulins are injected a few mins
Aspart, Glulisine prior to meals and they are the
preferred insulin for continuous SC
ii. Short Acting Insulin: Regular infusion devices ; short-acting
iii. Intermediate Acting: NPH, Activates insulin receptors leading to a reducting of insulins are injected more than an
Lente circulating glucose: promotes glucose transport and hour before a meal ; intermediate
oxidation; glycogen, lipid, protein synthesis and regulation Hypoglycemia (antidote: sugar or candy, IV acting insulins are often combined
iv. Long Acting Insulin: Detemir, of gene expression ; For Diabetes mellitus, diabetic glucose, IM glucagon), insulin allergy, immune with regular and rapid acting
Glargine, Ultralente, Lantus emergencies like DKA, HHS (rapid-acting), Hyperkalemia insulin resistance, lipodystrophy at injection site insulins ; long acting insulins are
B. Sulfonylureas
2nd generation sulfonylurea, acts as an insulin
secretagogue, increases insulin secretion from pancreatic
i. Glipizide, Glibenclamide, beta cells by closing ATP sensitive K+ channels leading to Less hypoglycemia, weight gain, photosensitivity, Not effective in patients with
Glimepiride, Gliclazide, Glyburide depolarization of the B cell; For Type 2 Diabetes Mellitus cholestatic jaundice (glibenclamide) functional B cells
1st generation sulfonylurea, acts as an insulin tolbutamide and chlorpropamide
secretagogue; increases insulin secretion from pancreatic Hypoglycemia, weight gain, disulfiram reaction, are highly protein bound drugs,
ii. Tolazamide, Tolbutamide, beta cells by losing ATP sensitive K+ channels ; for Type 2 hyperemic flush, dilutional hyponatremia, which may also cause allergic
Chlorpropamide Diabetes Mellitus hematologic toxicity reactions and rash
C. Meglitinides
Insulin Secretagogue, similar to sulfonylureas with some
overlap in binding sites, reduces circulating glucose,
increases glycogen, fat and protein formation and gene Least Hypoglycemia, rapid onset
i. Repaglinide regulation ; For Type 2 Diabetes Mellitus Least hypoglycemia, headache, URTI and short DOA
Insulin Secretagogue, similar to sulfonylureas with some Has least incidence of
overlap in binding sites, reduces circulating glucose, hypoglycemia, may be used in CKD
increases glycogen, fat and protein formation and gene patients ; rapid onset and short
ii. Nateglinide regulation ; For Type 2 Diabetes Mellitus Least hypoglycemia, headache, URTI DOA
D. Biguanides DOC for obese diabetics ; may also
cause slowing of glucose absorption
from GIT, decreased plasma
glucagon ; causes a decrease in
endogenous insulin production by
Reduced hepatic and renal gluconeogenesis with increasing insulin sensitivity of
decreased endogenous glucose production, activates AMP- tissues "Insulin Sparing Effect"
stimulated protein kinase leading to inhibition of GI disturbance, weight loss, lactic acidosis (esp in therefore does not have weight
gluconeogenesis ; For Type 2 DM, Diabetes prevention, renally and hepatically impaired patients), Vit gain as a SE ; do NOT cause
i. Metformin PCOS B12 malabsorption hypoglycemia
E. Alpha Glucosidase Inhibitors
Inhibits intestinal alpha-glucosidases , reduces conversion relatively minor glucose lowering
of starch and disacchardies to monosaccharidea, reduces effects ; impaired absoprtion of
post prandial hyperglycemia ; For Type 2 DM, Diabetes GI disturbance, hypoglycemia, increased liver sucrose ; taken immediately before
i. Acarbose, Miglitol prevention enzymes, flatulence, diarrhea, abdominal pain a meal
F. Thiazolidinediones
Regulates gene expression by binding to PPAR-gamma and
PPAR-alpha which increases tissue sensitivity, increases binds to PPAR-gamma and PPAR-
glucose uptake in muscle and adipose tissue, inhibits alpha ; PPAR regulates transcription
hepatic gluconeogenesis, effects on lipid metabolism and of genes encoding proteins involved
distribution of body fat, control of fasting and postprandial Fluid retention, weight gain, congestive heart in carbohydrate and lipid
glucose, decreased risk of DM in high-risk patients ; For failure, fractures esp in women, cardiovascular metabolism ; may increase risk for
i. Pioglitazone Type 2 DM, Diabetes prevention events, hepatotoxicity (Troglitazone), macular developing Bladder Cancer
Regulates gene expression by binding to PPAR-gamma edema, dyslipidemia, increased risk of MI
ii. Rosiglitazone ONLY ; for Type 2 DM, Diabetes prevention (Rosiglitazone) binds to PPAR-gamma ONLY
G. Novel Antidiabetic Agents

19
 Analog of GLP-1, Binds to GLP-1 receptors which leads to
reducetion of post-meal glucose excursions, increases
glucose-mediated insulin release, lowers glucagon levels,
slows gastric emptying time, produces satiety ; For Type 2 Hypoglycemia, acute pancreatitis, GI upset, usually combined with SU or
i. Exenatide DM nausea, vomiting metformin ; long-acting injectables
Dipeptidyl Peptidase-4 Inhibitors, blocks degradation of
GLP-1, raises circulating GLP-1 levels, reduces post-meal
glucose excursions, increases glucose mediated insulin
release, lowers glucagon levels, slows gastric emptying
ii. Sitagliptin, Linagliptin time, decreases appetite ; For Type 2 DM Headache, nasopharyngitis, URTI often combined with metformin
Analog of amylin, Binds to amylin receptors, reduce post-
meal glucose excursions, lowers glucagon levels, slows used with insulin to control post-
iii. Pramlintide gastric emptying, decreases appetite ; For Type 2 DM Hypoglycemia, GI disturbances prandial glucose
Bile acid binder, lowers glucose through unknown
iv. Colesevelam hydrochloride mechanisms ; For Type 2 DM constipation, dyspepsia, myalgia, asthenia None
Agents That Affect Bone Mineral Homeostasis
A. Vitamin D Metabolites and Analogs
INACTIVE Vitamin D; Regulates gene tanscription via the
vitamin D receptor; stimulates intestinal calcium
absorption, bone resorption, renal calcium and phosphate
reabsorption, decreases PTH, promote innate immunity ;
For Vitamin D deficiency states (intestinal osteodystrophy, given topically for psoriasis ; given
CKD, chronic liver disease, hypoparathyroidism, nephrotic Hypercalcemia, hyperphosphatemia, with calcium supplements for
i. Cholecalciferol, Ergocalciferol syndrome) osteoporosis, psoriasis hypercalciuria osteoporosis
The active form Calcitriol is
preferred in patients with CKD,
chronic liver disease and
hypoparathyroidism ;
Doxercalciferol is a prodrug that is
converted in the liver to 1,25-
ACTIVE Vitamin D; Regulates gene tanscription via the dihydroxyvitaminD ; Paricalcitol,
vitamin D receptor; stimulates intestinal calcium Calcipotriene are analogs of
absorption, bone resorption, rena calcium and phosphate Hypercalcemia, hyperphosphatemia, calcitriol and are used topically for
reabsorption, decreases PTH, promote innate immunity ; hypercalciuria ; Doxercalciferol, Paricalcitol and psoriasis and are being investigated
ii. Calcitriol, Doxercalciferol, For Secondary hyperparathyroidism in CKD, hypocalcemia Calcipotriene cause less hypercalcemia and for malignancies and inflammatory
Paricalcitol, Calcipotriene in hypoparathyroidism, psoriasis hypercalciuria disorders
B. Bisphosphonates Pamidronate, Zoledronic acid and
Etidronate are used IV for
hypercalcemia in Paget's disease
and cancer ; all other preparations
and Etidronate can be given PO but
with low bioavailability (<10%) ;
Treatment regimen: oral OD
(alendronate, risedronate,
Suppress the activity of osteoclasts in part via inhibition of ibandronate), weekly PO
i. Alendronate, Risedronate, farnesyl pyrophosphate synthesis, inhibit resorption and Adynamic bone, Esophagitis, Osteonecrosis of (alendronate, risedronate), monthly
Ibandronate, Pamidronate, formation of bone by acting on the basic hydroxyapatite the Jaw, renal impairment, GI irritation (remedy: PO (ibandronate), quarterly
Zoledronate, Etidronate, crystal structure ; For Paget's disease of the bone, take lots of water and keep patient in an upright injection (ibandronate), annual IV
Tiludronate, Zoledronic acid Hypercalcemia esp in malignancies, Osteoporosis position for 30mins after intake of drug) (zoledronate)
C. Hormones
Recombinant PTH, Acts via cognate G protein coupled
receptors, stimulates bone formation when given in low hypercalcemia, arthralgia, rhinitis, nausea,
i. Teriparatide intermittent doses weakness, dizziness, pharyngitis, dyspepsia, rash used IV for osteoporosis
given as injection or as nasal spray ;
Acts via cognate G protein coupled receptors; suppresses used for osteoporosis but is less
bone resorption ; For Paget's disease of the bone, effective than bisphosphonates and
ii. Calcitonin hypercalcemia, osteoporosis, tumor marker for thyroid CA Rhinitis, Nausea, vomiting, facial flushing teriparatide
D. Selective Estrogen Receptor Modulators (SERMs)
Interacts selectively with estrogen receptors, inhibits PTH-
stimulated bone resorption without stimulating breast or
endometrial hyperplasia, delay bone loss in post-
i. Raloxifene menopausal women see entry see entry
E. Rank Ligand (RANKL) Inhibitor
Monoclonal antibody, binds to RANKL and prevents it from as potent as bisphosphonates ;
stimulating osteoclast differentiation and function, blocks given SC every 6months which
i. Denosumab bone resorption ; For postmenopausal osteoporosis increased risk of infection avoid the GI SE
F. Calcium Receptor Antagonist
Activates the calcium sensing receptors in the parathyroid
gland, inhibits PTH secretion ; For secondary
hyperparathyroidism in CKD, hypercalcemia in patients hypocalcemia, adynamic bone disease (profound considered a Calcimimetic
i. Cinacalcet with parathyroid CA decreae in bone cell activity) (decreases PTH)

7. CHEMOTHERAPEUTIC DRUGS
Beta-Lactam & Other Cell Wall-Active & Membrane-Active Antibiotics
Bactericidal ; excreted unchanged
A. Penicillin in the urine ; capable of entering
the blood brain barrier
Inactivated by beta-lactamase
i. Natural Penicillins: Penicillin G, Binds to penicillin-binding proteins, inhibits (penicillinase) ; given IM but Pen V
Penicillin V (narrow spectrum transpeptidation in bacterial cell walls ; DOC for syphillis, can be given PO ; increased activity
penicillin) for streptococcal, meningococcal, G+ bacilli, spirochete against enterococci when given
infection hypersensitivity, GI disturbances together with aminoglycosides
Resistant to inactivation by beta-
ii. Anti-Staphylococcal Penicillins: lactamase (penicillinase) ; all
Methicillin, nafcillin, oxacillin, Binds to penicillin-binding proteins, inhibits penicillins are excreted unchanged
cloxacillin (very narrow spectrum) transpeptidation in bacterial cell walls; For staphylococcal hypersensitivity, GI disturbances, interstitial in the urine EXCEPT for Nafcillin
infections nephritis (methicillin), neutropenia (nafcillin) which is excreted in the bile

20
 Inactivated by beta-lactamase
(penicillinase), enhanced effect
when used with beta-lactamase
iii. Extended Spectrum Penicillin: inhibitors (clavulanic acid,
Ampicillin, Amoxicillin sulbactam) ; ampicillin undergoes
Binds to penicillin-binding proteins, inhibits hypersensitivity, GI disturbances, enterohepatic recirculation ;
transpeptidation in bacterial cell walls ; For enterococci, pseudomembranous colitis (ampicillin), rash synergistic effect with
Listeria, E. coli, Proteus, H. influenza, Moraxella (ampicillin) aminoglycosides
Inactivated by beta-lactamase
(penicillinase), enhanced effect
iv. Antipseudomonal Penicillin: Binds to penicillin-binding proteins, inhibits when used with beta-lactamase
Piperacillin, ticarcillin, carbenicillin transpeptidation in bacterial cell walls ; For Pseudomonas, inhibitors (clavulanic acid,
Enterobacter, Klebsiella hypersensitivity, GI disturbances tazobactam)
Bactericidal ; mostly IV ; all have
B. Cephalosporins renal excretion EXCEPT
Cefoperazone and Ceftriaxone
Increases nephrotoxicity of
i.First Generation: Cefazolin, Binds to penicillin-binding proteins, inhibits aminoglycosides ; do not cross the
cefadroxil, cephalothin, transpeptidation in bacterial cell walls ; For surgical BBB ; minimal activity against G-
cephapirin, cephradine, cephalexin prophylaxis, bone infections, infections due to staph and hypersensitivity, injection site reactions, cocci, enterococci, MRSA and most
strep, E. coli, Klebsiella, G+ cocci phlebitis, GI upset G- rods

Increases nephrotoxicity of
aminoglycosides ; do not cross the
ii. Second Generation: BBB ; slight less activity against G+
Cefamandole, cefaclor, cefonicid, but extended G- activity ;
cefuroxime, cefprozil, loracarbef, Binds to penicillin-binding proteins, inhibits Cefuroxime has improved action
ceforanide, cefoxitin, cefmetazole, transpeptidation in bacterial cell walls ; For surgical against pneumococcus and H.
cefotetan prophylaxis, bone infections, infections due to staph strep influenzae ; Cefotetan and Cefoxitin
and E. coli, Enterobacter, Neisseria, infections against hypersensitivity, injection site reactions, have good activity against B. fragilis
anaerobes (Bacteroides), sinus ear and respiratory phlebitis, GI upset, Hypoprothrombinemia and and thus are used for abdominal
infections by Klebsiella andHemophilus Disulfiram rection (cefamandole, cefotetan) and pelvic infections

Synergistic effect with

aminoglycosides ; all have renal
excretion EXCEPT Cefoperazone and
Ceftriaxone ; all can penetrate the
iii. Third Generation: BBB EXCEPT Cefoperazone and
Cefoperazone, cefotaxime, Cefixime ; Ceftriaxone and
ceftizoxime, ceftriaxone, cefixime, Cefotaxime are the most active
cefpodoxime proxetil, cefdinir, Cephs against Penicillin resistant
ceftibuten Streptococcus pneumoniae ;
Ceftizoxime is commonly used
Binds to penicillin-binding proteins, inhibits against Bacteroides ; should be
transpeptidation in bacterial cell walls ; decreased gram + reserved against serious infection
coverage, increased gram – activity (pseudomonas, EXCEPT ceftriaxone and cefixime ;
bacteroides), against Providencia, Serratia, Neiserria, Ceftriaxone has very good CNS
Haemophilus ; DOC for gonorrhea (Ceftriaxone and hypersensitivity, GI upset, Hypoprothrombinemia penetration ; Ceftazidime has very
Cefixime) and Disulfiram rection (cefoperazone) good action on Pseudomonas

More resistant to beta-lactamase

produced by Enterobacter,
iv. Fourth Generation: Cefipime, Haemophilus, Neisseria and
Ceftaroline Binds to penicillin-binding proteins, inhibits Pneumococcal ; Has improved
transpeptidation in bacterial cell walls ; wide coverage stability to chromosomal lactamase
against gram + and gram - bacteria hypersensitivity, GI upset ; Ceftaroline used for MRSA
C. Other Beta-Lactams Reserved for serious ife-threatening
infections; cilastatin inhibits renal
metabolism of imipenem ; given IV ;
low susceptibility to B-lactamases ;
active against Pseudomonas and
Acinetobacter EXCEPT Ertapenem ;
i. Carbapenems: Imipenem-
Imipenem given with Cilastatin
cilastatin , ertapenem,
which acts as Dehydropeptidase
meropenem
Binds to penicillin-binding proteins, inhibits enzyme inhibitor ; Partial cross-
transpeptidation in bacterial cell walls, wide coverage allergenicity with Penicillins ;
against gram + gram - bacteria and anaerobes ; For Ertapenem has longer t1/2 but less
infections resistant to other antibiotics EXCEPT MRSA, DOC hypersensitivity, GI upset, CNS toxicity active against Enterococci and
for Enterobacter, Citrobacter and Serratia (confusion, encephalopathy, seizures) Pseudomonas
Resistant to beta-lactamase, no
activity against gram + bacteria or
ii.Monobactam: Aztreonam Binds to penicillin-binding proteins, inhibits anaerobes ; given IV ; synergistic
transpeptidation in bacterial cell walls ; used against Gram GI upset, superinfection, vertigo, headache, skin with AG ; renal excretion ; No cross-
– like klebsiella, pseudomonas and Serratia rash and hepatotoxicity allergenicity with Pens
Most active against plasmid
encoded B lactamases (Gonococci,
Streptococci, E coli and H.
iii. Beta-Lactamase Inhibitors: Influenzae ; not good inhibitor of
Clavulanic acid , sulbactam, inducible chromosomal B
tazobactam Inhibits inactivation of penicillins by bacterial beta- lactamases
lactamase (penicillinase); used against beta-lactamase (Enterobacter,Pseudomonas,
producing gonococci, streptococci, E. coli and H. influenza hypersensitivity and cholestatic jaundice Serratia)
D. Other Cell Wall Synthesis Inhibitors

21
 Narrow spectrum Treat red man
syndrome by slowing the rate of
infusion ; VRSA and VRE are due to
D-Ala-D-Lactate formation ;
i. Glycopeptides: Vancomycin, teicoplanin and telavancin are not
teicoplanin, telavancin, absorbed in the GIT thus used for
dalbavancin bacterial enterocolitis, they are also
eliminated unchanged in the urine ;
Inhibits cell wall synthesis by binding to the D-Ala-D-Ala decrease dose for renally impaired
terminus of nascent peptidoglycan --> inhibit patients ; Dalbavancin has very long
transglycosylation --> prevent elongation and cross-linking t1/2 (6-11 days) which permits once-
of peptidoglycan chain ; For MRSA, PRSP, as alternative for red man syndrome, nephrotoxicity, ototoxicity, weekly dosing and is more active
pseudomembranous colitis chills, fever, phlebitis than Vancomycin
Interferes with a late stage oin cell wall synthesis in gram + Reserved for topical use only due to
ii. Peptide Antibiotic: Bacitracin
organisms ; For gram + bacteria nephrotoxicity marked nephrotoxicity
Blocks incorporation of D-Ala into the pentapeptide side only used as a second-line agent in
iii. Antimetabolite: Cycloserine
chain of the peptidoglycan ; For drug-resistant TB neurotoxicity (tremors, seizures and psychosis) TB
inhibits cytosolic enolpyruvate transferase --> prevents renal excretion ; resistance emerges
iv. Antimetabolite: Fosfomycin formation of N-acetylmuramic acid (a peptidoglycan rapidly ; synergistic with Beta
precursor molecule) Diarrhea lactam and quinolones
monitoring of CPK is needed, NOT
v. Cyclic lipopeptide: Daptomycin same spectrum of activity as Vancomycin ; For VRE, VRSA, Bactericidal (only destabilizes
for G+ acitivity, against endocarditis and sepsis myopathy bacterial cell membrane)
Tetracyclines, Macrolides, Clindamycin, Chloramphenicol, Streptogramins & Oxazolidinones
Inhibits transpeptidation (catalyzed by peptidyl given PO and IV ; able to cross the
transferase) by blocking the binding of aminoacyl moiety placenta and BBB ; Inhibits hepatic
of the charged tRNA to the acceptor site o mRNA at 50S drug-metabolizing enzymes causing
subunit, basteriostatic ; For meningitis (Strep pneumonia, many drug interactions ; resistance
A. Chloramphenicol (broad H influenza, Neisseria meningitides), back up for is due to the formation of
spectrum protein synthesis Salmonella, Rickettsia, Bacteroides, Wide spectrum GI disturbance, aplastic anemia, gray baby acetyltransferase that inactivates
inhibitor) antibiotic syndrome drug ; usually used as topical agent

Tigecycline has the broadest

spectrum and has the longest t1/2
(30-36hrs); do not drink with milk
(decreased absorption with divalent
Binds 30s ribosomal subunit thus preveting the binding of cations like calcium) ; high Vd, cross
tRNA to mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ the placenta, enterohepatic
and G-), For infections caused by Mycoplasma pneumonia, recycling ; all are excreted renally
Chlamydia, Rickettsia, Vibrio, Spirochetes such as EXCEPT Doxycycline (bile) ;
Leptospira, Peptic ulcer disease, Lyme disease, Malaria Resistance is due to development of
prophylaxis, Amoebiasis, Acne, Doxycycline is an efflux pumps for active extrusion of
alternative to macrolides as initial treatment of CAP, tetracyclines and the formation of
Alternative in syphilis, treatment of respiratory infection ribosomal protection proteins that
caused by susceptible organism, prophylaxis against GI disturbances (enetrocolitis, nausea, diarrhea, interfere with tetracycline binding
infection in chronic bronchitis ; Selective uses: Tetracycline vomiting), teratogen (tooth enamel (but not present with Tigecycline
(H. Pylori PUD), Doxycycline (Lyme disease and malaria dysplasia/discoloration), hepatotoxicity, EXCEPT in Proteus and
prevention), Minocycline (Meningococcal carrier state), nephrotoxicity, photosensitivity n(esp. Pseudomonas) ; Tigecycline is given
B. Tetracyclines: Tetracycline, Demeclocycline (SIADH), Tigecycline (more broad spectrum demeclocycline), vestibulotoxicity, candidiasis, IV only and is unaffected by
doxycycline, minocycline, - MRSA, VRE, B-lactamase producing G- bacteria, bacterial superinfection with S. aureus and C. common tetracyclie resistace
tigecycline, demeclocycline anaerobes, Chlamydiae, Mycobacteria) difficile, Fanconi syndrome mechanisms
C. Macrolides
good oral bioavilability but
azithromycin absoprtion is impeded
by food ; All macrolides inhibit
Binds 30s ribosomal subunit, inhibit transpeptidation, CYP450 except azithromycin;
bacteriostatic ; For community-acquired pneumonia, azithromycin has highest Vd and
pertussis, diphtheria, chlamydial infections ; slowest elimination; telithromycin is
Eryhthromycin (Campylobacter, Chlamydia, Mycoplasma, used for macrolide-resistance ; Half-
Legionella, Corynebacterium, Chlamydophila, Legionella, lives: Erythromycin (2hrs),
Ureaplasma, Bordetella, G+ cocci, some G-), Clarithromycin Clarithromycin (6hrs), Azithromycin
and Azithromycin (coverage of Erythromycin plus greater (24-48hrs) ; Resistance is due to
activity against Chlamydia, Mycobacterium avium, development of efflux pumps and
Toxoplasma, Helicobacter, Haemophilus, Moraxella, production of methylase enzyme ;
i. Erythromycin, azithromycin, Neiserria) ; Azithromycin is used as an alternative GI disturbance, cholestatic hepatitis, QT Cross-resistance among macrolides:
clarithromycin, telithromycin Ceftriaxone in Gonorrhea and to Pen G in syphilis prolongation, drug interaction complete or partial resistance with
as effective as Vancomycin as
a narrow spectrum macrolide, for G+ and anaerobe, low GI upset, rashes, eosinophilia, acute cholestatic treatment for C. difficile possibly
ii. Fidaxomicin oral bioavailability hepatitis, enzyme inhibitor with lower relapse rate
Ketolide, structurally related to macrolide, same MOA and For CAP including multi-drug
spectrum as erythromycin but macrolide-resistant QT prolongation, enzyme inhibitor, hepatic resistant organisms, A ketolide not
iii. Telithromycin organisms are susceptible to telithromycin ; For CAP dysfunction a macrolide in chemical structure
Cross-resistance between
clindamycin and macrolides is
Binds 30s ribosomal subunit, inhibit transpeptidation, common ; Resistance is due to
bacteriostatic ; For anaerobic infections (Bacteroides), methylation of binding sites and
alternative against gram + cocci (MRSA), endocarditis GI disturbance, skin rash, neutropenia, hepatic enzymatic inactivation ; G- aerobes
prophylaxis esp in those allergic to Pens, PCP pneumonia, dysfunction, possible superinfection are resistant because of poor
D. Lincosamides: Clindamycin, toxoplasmosis (+ Pyrimethamine), skin and soft tissue (Pseudomembranous colitis - C. difficile penetration through th eouter
lincomycin infection overgrowth) membrane

22
 Binds 50s ribosomal subunit, constricting the channel
where polypeptides are extruded thus tRNA synthetase is
also inhibited --> decreased free tRNA ; For infections Inhibits CYP450 enzymes causing
E. Streptogramin: Quinupristin- caused by drug-resistant gram + cocci (MRSA, VRSA, PRSP, Injection site reaction, anthralgia-myalgia multiple drug interactions ;
Dalfopristin resistant E. faecium) syndrome BACTERICIDAL
Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation Inhibits CYP450 enzymes causing
by blockin formation of the tRNA-ribosome-mRNA ternary multiple drug interactions ;
complex, bacteriostatic ; Reserved for infections caused by Resistance is due to
drug-resistant gram + cocci (MRSA, VRE, PRSP), Listeria, Thrombocytopenia, neutropenia, serotonin decreasedaffinity of drug to binding
F. Oxazolidinone: Linezolid Corynebacteria syndrome, neuropathy, optic neuritis site
Aminoglycosides & Spectinomycin AG are given IM or IV only, have
concentration dependent killing, is
not capabale of penetrating the
blood brain barrier, low tissue
penetration, SYNERGISTIC effect
with cell wall synthesis inhibitors
due to enhancement of transport to
the inside of the bacterial cell ;
mechanism of resistance of AG:
plasmid-mediated formation of
General MOA of all aminoglycosides (AG) is by inhibiting nephrotoxicity (reversible - Acute Tubular inactivating enzymes "group
protein synthesis by binding to 30s subunit: (1) block Necrosis esp in elderly, if given with transferase" --> catalyze the
formation of the initiation complex (2) cause misreading of Amphotericin B, Cephalosporin and acetylation of amine functions and
the code on the mRNA template (3) inhibit translocation, Vancomycin)), ototoxicity (irreversible), the transfer of phosphoryl or
bactericidal ; For serious infections caused by aerobic gram neuromuscular blockade (Curare-like block --> adenylyl groups to the oxygen
– bacteria (E.coli, Enterobacter, Klebsiella, Proteus, respiratory paralysis. Remedy: Calcium, atoms of the hydroxyl groups of AG,
Providencia, Pseudomonas, Serratia, Haemophilus, Neostigmine and Mechanical Ventilator) ; S. For Streptomycin, resistance is due
Moraxella, Shigella), endocarditis, ocular infections ; If pneumoniae is resistant to Gentamicin, to changes in the ribosomal binding
given together with Pens, may be used for Listeria, Enterococci is resistant to amikacin, gentamicin, site ; Gentamicin and tobramycin
A. Gentamycin, tobramycin Enterococcus and G+ cocci tobramycin but NOT streptomycin are the most vestibulotoxic and
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For serious infections caused by aerobic gram
– bacteria (E.coli, Enterobacter, Klebsiella, Proteus,
Providencia, Pseudomonas, Serratia, Haemophilus,
Moraxella, Shigella), endocarditis, ocular infections, Least resistance and narrowest
multidrug resistant TB (2nd line) ; If given together with nephrotoxicity (reversible), ototoxicity therapeutic window ; used for
B. Amikacin Pens, may be used for Listeria, Enterococcus and G+ cocci (irreversible), neuromuscular blockade streptomycin-resistant TB
hypersensitivity, nephrotoxicity (reversible), Administered intramuscularly ; if
Inhibits protein synthesis by binding to 30s subunit, ototoxicity (irreversible), neuromuscular given together with Pens can be
bactericidal ; For TB, tularaemia, bubonic plague, blockade, teratogen (congenital deafness), used for enterococcal endocarditis,
C. Streptomycin brucellosis injection site reactions TB plague and tularemia
Limited to topical and oral use due
Inhibits protein synthesis by binding to 30s subunit, to nephrotoxicity, kanamycin is
bactericidal ; For skin infections, bowel preparations for hypersensitivity, nephrotoxicity (reversible), most ototoxic ; Neomycin has the
D. Neomycin, kanamycin, elective surgeries, hepatic encephalopathy, visceral ototoxicity (irreversible), neuromuscular most skin reactions (allergic
paromomycin leishmaniasis (paromomycin) blockade reactions, contact dermatitis)
Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For drug-resistant gonorrhoea, gonorrhoea in nephrotoxicity (reversible), ototoxicity Ototoxcity of AG's can be increased
E. Spectinomycin penicillin allergic patients (irreversible), neuromuscular blockade by loop diuretics
Inhibits protein synthesis by binding to 30s subunit, hypersensitivity, nephrotoxicity (reversible), For Treatment of serious infections
bactericidal ; For serious infections caused by aerobic gram ototoxicity (irreversible), neuromuscular caused by organisms resistant to
F. Netilmicin – bacteria blockade other aminoglycosides
Sulfonamides, Trimethoprim & Quinolones
low solubility in acidic urine causing
A. Sulfonamides: Silver
formation of stones ; Resistance is
sulfadiazine, mafenide acetate
GI upset, mild hepatic dysfunction, acute due to plasmin-mediated
i. Short acting: Sulfisoxazole hemolysis in G6PD deficiency, nephrotoxicity (decreased intracellular
ii. Intermediate acting: (precipitate in the urine at acidic pH --> accumulation of the drug, increased
Sulfamethoxazole crystalluria, hematuria), hypersensitivity (cross- production of PABA by bacteria,
Inhibits dihydropteroate synthase, bacteriostatic ; For burn allergenicity with other related drugs such OHAs decreased sensitivity of
infections, for G=, G-, Chlamydia and Nocardia, Simple oral and diurectics), exfoliative dermatitis, dihydropteroate synthetase to
sulfas (UTI), Sulfacetamide (ocular infection, topical), polyarteritis nodosa, SJS, hematotoxicity sulfas and production of
Mafenide and Silver sulfadiazine (burn infection, topical), (granulocytopenia, thrombocytopenia, aplactis dihydrofolate reductase that has
Sulfasalazine (Ulcerative colitis and RA, oral), Sulfadizaine + anemia), kernicterus ; Drug Interactions: decreased affnity for the drug ;
iii. Long acting: Sulfadoxine Pyrimethamine + Folinic acid (Toxoplasmosis, oral) warfarin, methotrexate, bilirubin sulfonamides are formulated in a
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; For UTI, respiratory, ear and GI upset, acute hemolysis in G6PD deficiency,
sinus infections (Hemophilus, Moraxella, Aeromonas), DOC nephrotoxicity, hypersensitivity, hematotoxicity, Sulfonamides are weakly acidic
B. Combination: Co-trimoxazole for P. jiroveci pneumonia and Nocardiosis, toxoplasmosis, kernicterus ; trimethoprim toxicity: antifolate while Trimethroprim is a weak base
(Sulfamethoxazole + Back-up for cholera typhoid fever shigellosis, G- sepsis, effects (megaloblastic anemia, leukopenia, ; remedy for antifolate effects:
Trimethoprim) MRSA, Listeria granulocytopenia) Folinic acid supplement
C. Fluoroquinolones Avoid in pregnancy due to absence of safety data
General SE: GI distress, skin rashes, HA, dizziness,
Inhibits DNA replication by binding to DNA gyrase and insomnia, increased LFT, phototoxicity, CNS
topoisomerase IV (G+) and Topoisomerase II (G-), effects (dizziness, headache), tendinitis and
bactericidal, inhibition of Topoisomerase II results in tendon rupture, opportunistic infection by
blockade of relaxation of supercoiled DNA that is catalyzed Candida and Streptococci ; CI in pregnancy and in General properties of quinolones:
by DNA gyrase while inhibition of Topoisomerase IV children (damage growing cartilage --> good oral bioavailability, high Vd,
interferes with the separation of replicated chromosomal arthropathy), enhance toxicity of t1/2 3-8hrs, absorption is impeded
DNA during cell division ; General use of FQs: For infections methylxanthines (theophylline) ; Mechanism of by antacids, elimination is via
of the urogenital and GI tract by G- (gonococci, E. coli, resistance for Quinolones: decreased intracellular kidneys by tubular secretion (may
Klebsiela, Campylobacter, Enterobacter, Pseudomonas, accumulation via efflux pumps, change in porin compete with probenecid for
Salmonella, Shigella), respiratory tract, skin and soft tissue structure, chnages in sensitivity of target enzyme excretion) EXCEPT for
i. First Generation infection ; may be used against meningococcal carrier svia point mutations in the antibiotic binding MOXIFLOXACIN ; Norfloxacin does
Fluoroquinolones: Norfloxacin, state, for treatment of TB and prophylaxis in neutropenic region, mutations in the quinolone resistance not achieve adequte plasma levels
Nalidixic acid patients determining region of the gyrA gene that for use in systemic infections

23
 high resistance esp for C. jejuni,
Inhibits DNA replication by binding to DNA gyrase and GI distress, skin rashes, HA, dizziness, insomnia, gonococci, G+ cocci like MRSA,
topoisomerase IV (G+) and Topoisomerase II (G-), increased LFT, phototoxicity, CNS effects Pseudomonas and Serratia ; are
bactericidal, bactericidal ; For UTI and GIT infections (gram (dizziness, headache), tendinitis and tendon used as alternative to Ceftriaxone
ii. Second Generation – rods, gonococci, gram + cocci), atypical pneumonia rupture, opportunistic infection by Candida and and Cefixime in gonorrhea ;
Fluoroquinolones: Ciprofloxacin, (Mycoplasma, Chlamydophila), Mycobacteria ; increased Streptococci ; CI in pregnancy and in children Ofloxacin can be used against C.
ofloxacin, Enoxacin Norfloxacin activity against G- (damage growing cartilage --> arthropathy) trachomatis

"Respiratory Quinolones" ;
Moxifloxacin and Gemifloxacin are
the newest members of this family
and are condisered to have the
broadest spectrum of activity with
increased activity aginst anaerobes
ang atypical agents ; FQ elimination
is via kidneys by tubular secretion
(may compete with probenecid for
excretion) EXCEPT Moxifloxacin ;
NEVER use moxifloxacin in UTI ;
Levofloxacin is used in CAP caused
by Chlamydia, Mycoplasma and
Legionella ; Gemifloxacin,
Levofloxacin and Moxifloxacin can
prolong QT ; Levofloxacin has
superior activity against G(+)
bacteria including S. pneumoniae ;
All have relatively long t1/2
permitting once daily dosing ; Oral
Inhibits DNA replication by binding to DNA gyrase and GI distress, skin rashes, HA, dizziness, insomnia, absorption is impaired by cations ;
topoisomerase IV (G+) and Topoisomerase II (G-), increased LFT, phototoxicity, CNS effects Gatifloxacin can cause
iii. Third Generation bactericidal, bactericidal ; For lung infections caused by
(dizziness, headache), tendinitis and tendon hyperglycemia in DM Px and
Fluoroquinolones: Levofloxacin, gram + cocci, atypical pneumonia (Chlamydia, rupture, opportunistic infection by Candida and hypoglycemia in patients also
Gemifloxacin, Moxifloxacin, mycoplasma) ; less G- activity compared to 2nd gen but Streptococci ; CI in pregnancy and in children receiving OHA and was withdrawn
Sparfloxacin increased activity against G+ cocci, enterococci, MRSA (damage growing cartilage --> arthropathy) from the market in 2006 (USA)
GI distress, skin rashes, HA, dizziness, insomnia,
increased LFT, phototoxicity, CNS effects
(dizziness, headache), tendinitis and tendon
Inhibits DNA replication by binding to DNA gyrase and rupture, opportunistic infection by Candida and
iv. Fourth Generation topoisomerase IV (G+) and Topoisomerase II (G-), Streptococci ; CI in pregnancy and in children additional SE: diabetes
Fluoroquinolones: Trovafloxacin, bactericidal, bactericidal ; has broad spectrum activity (damage growing cartilage --> arthropathy) QT (gatifloxacin), hepatotoxicity
Alatrofloxacin (gram – and gram +), enhanced activity against anaerobes prolongation (trovafloxacin)
D. Miscellaneous agents
Reactive reduction by ferredoxin forming free radicals that
disrupt electron transport chain, bactericidal ; For
anaerobic or mixed intra-abdominal infections, vaginitis GI irritation, metallic taste, headache, dark urine,
(trichomonas, gardnerella), pseudomembranous colitis, leukopenia, dizziness, ataxia, neuropathy, DOC for amoebiasis, giardiasis and
i. Metronidazole, tinidazole brain abscess, protozoal infections seizures and disulfiram reaction Pseudomembranous colitis
single OD dose can prevent
Forms multiple reactive intermediates when acted upon by GI irritation, skin rashes, pulmonary infiltrates, recurrent UTI ; acidification of urine
bacterial nitrofuran reductase, bactericidal ; For UTI phototoxicity, neuropathies, hemolysis in enhances activity ; adjust dose in
ii. Nitrofurantoin (except Proteus and Pseudomonas) patients with G6PD deficiency renal patients
Antimycobacterial Drugs Most impt drug in TB, prevent
neurotoxicity by giving pyridoxine
(vit B6) ; structural congener of
pyridoxine ; high level resistance
due to deletion of KatG gene
whichh codes for catalase-
peroxidase enzyme involved in
bioactivation of INH, low level
hepatotoxicity, neurotoxicity (seizures, peripheral resistance due to deletion og inhA
Inhibits mycolic acid synthesis, bactericidal ; For TB, for neuritis, insomnia, restlessness, muscle gene which encodes the target
A. Isoniazid (nicotinic acid latent infection, given as a sole drug for prophylaxis of twitching), acute hemolysis in G6PD deficiency, enzyme which is an acyl protein
derivative) close contacts and skin test converters drug-induced lupus reductase ; Potent CYP450 inhibitor
Potent CYP450 inducer ; rapid
development of resistance if used
alone ; resistance is due to changes
of drug sensitivity of the
polymerase enzyme; undergoes
enterohepatic recirculation ; orange-
colored metabolites ; delay
Inhibits DNA-dependent RNA polymerase, bactericidal ; For emergence of resistance to
TB, leprosy, prophylaxis for meningococcal and dapsone ; Rifabutin is equally
staphylococcal carrier states, drug-resistant infections effective as anti-mycobacterial
(MRSA, PRSP) when given together with Vancomycin, can red-orange urine, light chain proteinuria, skin agent with less drug interaction and
B. Rifamycin derivatives: be used as sole drug in the treatment of latent TB in INH- rash, thrombocytopenia, nephritis, it is the preferred anti-TB for AIDS
Rifampicin, rifabutin, rifapentine, intolerant patient or in close contact of patients with INH- hepatotoxicity, flulike syndrome, anemia, impair patients ; Rifamixin is not absorbed
rifamixin resistant strains of the organism antibody response in the GIT and is used for traveler's
dose-dependent visual disturbances (decreased Resistance is due to mutation in
visual acuity, red green color blindness, emb gene ; dose adjustment id
Inhibits arabinosyl transferases involved in the synthesis of retrobulbar neuritis, retinal damage, optic needed in renal patients ; always
arabinogalactan in mycobacterial cell wall, bacteriostatic ; neuritis), headache, confusion, hyperuricemia, used in combination with other
C. Ethambutol (butanol derivative) For TB peripheral neuritis drugs for TB

24
 Most hepatotoxic anti-TB drug, also
known as sterilizing agent ; require
metabolic conversion via
pyrazinamidases in MTb ; resistance
Unknow MOA, bacteriostatic but can be bactericidal on hepatotoxicity, nongouty polyarhtralgia, is via mutation in pncA gene which
actively dividing mycobacteria, is metabolozed to asymptomatic hyperuricemia, myalgia, GIT codes for pyrazinamidases and
D. Pyrazinamide (pyrazine pyrazinoic acid, t 1/2 is increased in liver and kidney irritation, maculopapular rash, porphyria, increased efflux systems ; decrease
derivative) disease ; For TB photosensitivity ; CI in pregnancy dose in hepatic and renal patients
E. Streptomycin (aminoglycoside) for MDRTB (TB meningitis, miliary TB, severe organ TB) see entry see entry
Drugs for Leprosy
Most active drug against M. leprae ;
used in combination with rifampicin
and clofazimine ; Acedapsone is a
GI irritation, fever, skin rashes, repository form of dapsone which
Inhibition of folic acid synthesis, bacteriostatic ; For methemoglobinemia, acute hemolysis in G6PD has drug action that can last for
A. Sulfones: Dapsone, acedapsone leprosy, alternative for PCP pneumonia deficiency patients several months
Binds to guanine bases in bacterial DNA, bactericidal ; For
B. Clofazimine leprosy GI irritation, skin discoloration a phenazine dye
Antifungal Agents
Control infusion reactions by
slowing the rate of infusion and
premedication with antihistamines,
additive nephrotoxicity with other
nephrotoxic drugs
(aminoglycosides) ; highly lipid
Binds to ergosterol in fungal cell membranes, forming infusion reactions (chills, fever, muscle spasms, soluble, poorly absorbed in the GIT ;
artificial pores, fungicidal, WIDEST antifungal spectrum ; vomiting, hypotension), dose limiting high Vd except in the CNS with a
For systemic fungal infections (aspergillus, blastomyces, nephrotoxicity (decreased GFR, ATN with t1/2 of 2weeks ; resistance is due to
candida, Cryptococcus, histoplasma, mucor), for initial magnesium and potassium wasting, decreased decreased level of ergosterol or
A. Polyene antifungal: induction before followup treatment with azoles, can be erythropoietin), neurotoxicity (seizure, neuronal change in membrane structure ; has
Amphotericin B used topically in mycotic corneal ulcers and keratitis damage) the WIDEST antifungal spectrum
Accumulated in fungal cells by the action of permease and decrease dose in renal patients ;
converted by cytosine deaminase to 5-FU, which inhibits resistance is due to decreased
thimidylate synthase, pyrimidine antimetabolite, activity of fungal permease and
fungistatic ; given together with ampho B and Triazoles - deaminase ; has synergistic effect
For cryptococcal infection, systemic candidal infections, reversible myelosuppresion, alopecia, when given with ampho B and
B. Flucytosine chromoblastomycosis hepatotoxicity Triazoles.
C. Azole Antifungals
Limited to topical use because of
systemic toxicity ; narrow antifungal
spectrum ; resistance is due to
Inhibit 14α-demethylase --> decreased ergosterol chnages in the sensitivity of target
production --> increased permeability of cell membrane, enzyme ; Potent CYP450 inhibitor ;
Inhibits fungal P450-dependent enzymes blocking GI disturbances (vomiting, diarrhea), rash, Ketoconazole is rarely used due to
ergosterol synthesis, fungistatic ; For chronic hepatotoxicity, drug interaction, gynecomastia, drug interactions and narrow
i. Ketoconazole (Imidazole) mucocutaneous candidiasis, dermatophytosis menstrual irregularities and infertility spectrum
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; DOC for candidiasis
(esophageal, oropharyngeal, vulvovaginitis), alternative to Ampho B in the
coccidioidomycosis, cryptococcal meningitis (treatment GI disturbances (vomiting, diarrhea), rash, treatment of C. neoformans, as
ii. Fluconazole (Triazole) and prophylaxis) hepatotoxicity effective as Ampho B in candidemia
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; DOC for blastomycosis,
sporotrichosis, dermatophytosis esp onchomycosis,
chromoblastomycosis ; alternative for infections due to
Aspergillus, Coccidioides, Cryptococcus and Histoplasma , GI disturbances (vomiting, diarrhea), rash, may also be used for subcutaneous
iii. Itraconazole (Triazole) for esophageal candidiasis resistant to fluconazole hepatotoxicity chromoblastomycosis
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; co-DOC for invasive
aspergillosis, alternative in candidemia, for fluconazole- GI disturbances (vomiting, diarrhea), rash,
resistant organisms, for candidal esophagitis and hepatotoxicity, blurring of vision in 30% of
iv. Voriconazole (Triazole) stomatitis in AIDS patients patients, CI in pregnancy wider specturm azole
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; For Candida and BROADEST spectrum triazole ; the
Aspergillus, as prophylaxis of fungal infection during only azole with activity against
cancer chemotherapy, salvage therapy in invasive GI disturbances (vomiting, diarrhea), rash, Rhizopus sp. (mucormycosis) ;
v. Posaconazole (Triazole) aspergillosis hepatotoxicity Potent CYP450 inhibitor
Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell membrane,
Inhibits fungal P450-dependent enzymes blocking
ergosterol synthesis, fungistatic ; For mucocutaneous
vi. Clotrimazole, miconazole, candidiasis, dermatophytosis, seborrheic dermatitis, Limited to topical use because of
ketoconazole pityriasis versicolor None when administered topically systemic toxicity
Inhibit beta-glucan synthase which produces β(1-->2)
glycan which is a cellwall component, thus decreasing
fungal cell wall synthesis, fungostatic ; For disseminated
and mucocutaneous candidiasis who fail to respond to all are given IV ; micafungin can
D: Echinocandins: Caspofungin, amphoB, for mucormycosis, salvage therapy for invasive headache, GI distress, rash, fever, flushing increase levels of cyclosporine and
anidulafungin, micafungin aspergillosis (histamine release), elevated liver enzymes tacrolimus

25
 given PO ; Accumulates in keratin ;
headache, mental confusion, GI irritation, potent CYP450 inducer ; absorption
photosensitivity, hepatotoxicity, disulfiram is increased by intake of fatty meal ;
Interferes with microtubule function in dermatophytes, reaction, drug interactions (decreases resistance is due to decreased
inhibits synthesis and polymerization of nucleic acids, bioavialability of warfarin) ; contraindicated in transport of drug into the fungal
E. Griseofulvin fungistatic ; For dermatophytosis porphyria cell wall
Inhibits withg ergosterol synthesis by inhibiting fungal given PO and topical, also
squalene oxidase leading to increased squalene which accumulates in keratin, more
interferes with ergosterol synthesis, fungicidal ; For effective than griseofulvin in
F. Terbinafine dermatophytosis, onchomycosis GI upset, rash, headache, taste disturbances onchomycosis
Binds to ergosterol in fungal cell membranes, forming
artificial pores, fungicidal ; For candidiasis ((oropharyngeal, Minimal mucocutaneous
esophageal and vaginal), for GI fungal infections in absorption, available as swish and
G. Nystatin (polyene) patients with impaired defense mechanisms nephrotoxicity (severe) swallow preparation
Antiviral Agents
A. Anti-Herpes given PO, topical and IV ; dose
adjustment in renal patients ; No
activity against strains of HSV with
absent thymidine kinase activity ;
resistance is due to changes in viral
Activated by viral thymidine kinase (TK) to forms that DNA polymerase ; Valacyclovir is a
inhibit viral DNA polymerase, guanosine analog, prodrug that is converted to
competitive substrate for DNA polymerase, causes chain Acyclovir and reached plams levels
termination after its incorporation into the viral DNA ; For 3-5x (longer t1/2) more than
infections due to HSV1, HSV2, VZV (mucocutaneous and acyclovir ; Penciclovir does not
genital herpes, prophylaxis in AIDS and in other cause chain termination ;
i. Acyclovir, valacyclovir, Immunocompromised states such as organ transplant nausea, diarrhea, headache, delirium, tremor, Famciclovir is a prodrug which is
penciclovir, famciclovir, docosanol patients, herpes
Inhibits fusion encephalitis,
between the HSVneonatal HSVand
envelope infection
plasmaetc. seizures, hypotension, nephrotoxicity converted to Penciclovir in vivo
membrane, prevents viral entry and subsequent nausea, diarrhea, headache, delirium, tremor, topical preparation shortens
ii. Docosanol replication seizures, hypotension, nephrotoxicity healing
given astime
IV or intraocular implant
(for CMV retinitis) ; No activity
against strains of HSV with absent
thymidine kinase activity ; CMV
resistance is due to mutation in
viral DNA polymerase and in the
Inhibits viral DNA polymerase causing chain termination, genes that code for the activating
guanosine derivative ; For infections due to CMV, HSV1, viral phosphotransferase ;
HSV2, VZV ; For prohylaxis and treatment of CMV retinitis Valganciclovir is a prodrug of
iii. Ganciclovir, valganciclovir and other CMV infections in the immunocompromised leukopenia, thrombocytopenia, mucositis, ganciclovir with increased oral
(anti-CMV) patients hepatotoxicity, seizures, neutropenia bioavialability
Active against strains of HSV with
Inhibits viral DNA polymerase causing chain termination ; absent thymidine kinase activity ;
For CMV retinitis, mucocutaneous HSV infections, acyclovir- resistance is due to mutation in
resistance, ganciclovir-resistance, genital warts and DNA polymerase ; dose adjustment
iv. Cifodovir (anti-CMV) molluscum contangiosum nephrotoxicity in renal patients
Active against strains of HSV with
Inhibits viral RNA polymerase, DNA polymerase, and HIV absent thymidine kinase activity ;
reverse transcriptase, binds to pyrophosphate binding site does not require phosphorylation
; as alternative for prophylaxis and treatment of CMV for antiviral activity ; resistance is
retinitis, gancyclovir-resistant strains of CMV, HSV nephrotoxicity, electrolyte abnormalities due to mutations in DNA
infection in patients with AIDS, also used in organ (hypocalcemia), GU ulcerations, CNS effects polymerase gene ; dose adjusment
v. Foscarnet (anti-CMV) transplantation (headache, hallucination, seizures) in renal patients
used topically only because it is
rapidly metabolized into the
GI irritation, paresthesia, tremor, convulsion, inactive form and because it has a
vi. Vidarabine adenine analog ; For HSV, VZV, CMV hepatic dysfunction, CI in pregnancy toxic potential
topical only because it is too toxic
vii. Idoxuridine, trifluridine pyrimidine analogs ; For herpes keratitis (HSV-1) irritation, blurred vision, photophobia fo systemic use
injected intravitreally ; concurrent
systemic use of anti-CMV in threapy
antisense oligonucleotide that binds to mRNA of CMV is recommended to protect against
causing inhibition of early protein synthesis ; For CMV extraocular and contralateral retinal
viii. Fomivirsen retinitis iritis, vitritis, increased IOP, changes in vision CMV disease
B. Drugs for HIV
these are prodrugs converted by
host cell kinases tp triphosphates
causing competitive binding of
Inhibit HIV reverse transcriptase after phosphorylation by natural nulecotides to the dNTP-
cellular enzymes, acts as chain terminators via insertion binding site of Reverse
into the growing DNA chain ; For HIV infection, prevention Transcriptase ; resistance is due to
i. NRTI: of maternal-fetal HIV transmission see specific drugs below mutation in pol gene
good oral bioavailability, T1/2 is 12-
a. Abacavir guanosine analog hypersensitivity reaction 24hrs, resistance is slow
acute pancreatitis, peripheral neuropathy, oral bioavailability is decreased by
diarrhea, hepatic dysfunction, hyperuricemia, food and chelating agents ; dose
b. Didanosine (ddI) NRTI CNS effects adjustment in renal patients
aesthenia, GI upset, headache,
hyperpigmentation of palms of soles, CI in
pregnancy, children, renal and hepatic and per orem once a day treatment,
c. Emtricitabine NRTI patients dose adjustment in renal patients
80% oral bioavailability ;may also
be used for Hepa B infection ;
HAART, dose adjustment in renal
d. Lamivudine (3TC) NRTI GI upset, headache, fatigue, insomnia patients
peripheral neuropathy esp if given together with good oral bioavailability, dose
e. Stavudine (d4T) NRTI Zalcitabine, lactic acidosis with hepatic steatosis adjustment in renal patients

26
 oral bioavailabilty is 25-40% ;
a nucleotide but acts as NRTI, competitively inhibits RT, GI upset, asthenia, headache, Fanconi syndrome, halflife is 60hours ; also used
f. Tenofovir cause chain termination after incorporation into DNA AKI against HBV
peripheral neuropathy, pancreatitis, esophageal increased oral bioavailability, dose
g. Zalcitabine (ddC) NRTI ulceration, stomatitis, arthralgias adjustment in renal patients
BM suppression (anemia, neutropenia, dose adjustment in uremic patients
thrombocytopenia), acute cholestatic hepatitis, and cirrhosis ; affected by enzymes
h. Zidovudine (ZDV) Azidothymidine or AZT agitation, insomnia, myalgia, headache, GI upset inducers and inhibitors
Inhibits HIV reverse transcriptase, no phosphorylation Delavirdine and Nevirapine (rash, increased binds to a different binding site ;
ii. NNRTI: Delavirdine, efavirenz, required, do not compete with nucleoside triphosphate ; AST/ALT, Efavirenz (teratogenicity), Etravirine resistance is due to mutations in pol
etravirine, nevirapine For HIV infection (increased cholesterol and triglycerides) gene
metabolized by CYP3A4 and
CYP2D6, affected by enzyme
a. Delavirdine NNRTI rashes, teratogenic inducer and inhibitor
enhanced absorption by fatty
CNS dysfunction, skin rash, increased plasma meals, drug interactions are
b. Efavirenz NNRTI cholesterol, teratogenic common
nausea, vomiting, diarrhea, increased
c. Etravirine NNRTI, for drug-resistant HIV cholesterol, triglycerides and LFTs NEWEST NNRTI
used as a singledose to prevent HIV vertical transmission at good oral bioavailability,t1/2 is
d. Nevirapine the onset of labor and also given to the neonate rash, SJS, TEN >24hours
General SE: hyperglycemia, insulin resistance,
hyperlipidemia, altered body fat distribution
iii. Protease Inhibitor: (buffalo hump, gynecomastia, truncal obesity,
Atrazanavir, Darunavir, facial and peripheral lipodystrophy) due to the
Fosamprenavir, Indinavir, cleaves precursor polyprotein to form the final structural inhibition of lipid-regulating proteins which have Resistance is due to mutation in pol
Nelfinavir, Lopinavir-Ritonavir, protein of the mature virion core, inhibits viral protein active sites with structural homology to that of gene ; are potent CYP3A4 inhibitor
Saquinavir, Tipranavir processing ; For HIV infection HIV protease esp Ritonavir
per orem absorption requires acidic
environment ; can penetrate CSF
and seminal fluid ; is not associated
with dyslipidemia, fat deposition or
peripheral neuropathy, skin rash, metabolic syndrome ; CYP3A4 and
a. Atazanavir Protease Inhibitor hyperbilirubinemia, QT prolongation 2C9 inhibitor
rash, hepatotoxicity, hypersensitivity ; CI in Given together with Ritonavir in
b. Darunavir Protease Inhibitor patients with sulfa allergy patients resistant to other PIs
GI upset, paresthesia, rash, CI in pregnant
patients and children if drug uses propylene a prodrug that is converted to the
glycol as solvent ; does not have risk for active drug Amprenavir ; absorption
hyperlipidemia, fat maldistribution, is impaired by fatty food ; used with
c. Fosamprenavir Protease Inhibitor hyperglycaemia and insulin resistance lowdose Ritonavir
nausea, vomiting, diarrhea, thrombocytopenia, decreased bioavailability in the
hyperbilirubinemia, nephrolithiasis, insulin presence of food ; affected by
d. Indinavir Protease Inhibitor resistance enzyme inhibitors and inducers
there is increased compliance with
used as a combination drug: uses subtherapeutic dose of this drug ; Ritonavir has “boosting
ritonavir which inhibits CYP3A4 mediated metabolism of effect” on other PI due to enzyme
e. Lopinavir-Ritonavir lopinavir GI upset (well-tolerated side effects) inhibitory effect
absorption is increased by food,
short half-life ; has the most
favorable safety profile for
f. Nelfinavir Protease Inhibitor Diarrhea pregnancy
Protease Inhibitor ; subtherapeutic doses inhibit CYP3A4- good oral bioavailability esp when
mediated metabolism of other Pis (Indnavir, Lopinavir, taken with meals ; affected by
g. Ritonavir Saquinavir) which permits lower dose of the other PI GI upset, bitter taste, paresthesia, increased LFT's enzyme inducer and inhibitors
Protease Inhibitor ; given together with low dose Ritonavir affected by enzyme inducers and
h. Saquinavir to improve compliance and decrease GI upset nausea, vomiting, diarrhea, dyspepsia, rhinitis inhibitors
newer drug ; induces P-glycoprotein
transporters which leads to
alteration of GI absorption of other
i. Tipranavir Protease Inhibitor ; given with Ritonavir for PI-resistant HIV GI upset, rash, hepatotoxicity drugs
iv. Entry inhibitors:
Binds to gp41 subunit of viral envelope glycoprotein,
preventing fusion of viral and cellular membranes ; For
a. Fusion Inhibitor: Enfuvirtide, previously drug-treated patients with persistent HIV injection site reaction, hypersensitivity reaction, subcutaneous and usually given
Docosanol replication despite ongoing therapy increased incidence of bacterial pneumonia together with other HIV agents
Blocks viral attachment by blocking CCR5, a
b. CCR5 receptor antagonist: transmembrane protein involved in the attachment of HIV cough, diarrhea, muscle and joint pains, good tissue penetration ; affected
Maraviroc to host cell ; For HIV infection increased LFTs by enzyme inhibitors and inducers
C. Drugs for Influenza
Amantadine is also used in treating
parkinsonism ; should be given
within 48hrs of exposure ;
Rimantadine has longer halflife and
doe snot need dose-adjustment for
Inhibit early step replication and prevent uncoating by renally-impaired Px ; there is
i. Uncoating inhibitors: binding to M2 proton channels ; For influenza A and GI irritation, dizziness, cerebellar dysfunction increased resistance observed with
Amantadine, rimantadine rubella (ataxia, dysarthria), livedo reticularis amantadine
Inhibits neuraminidase which cleaves sialic acid residues DOC for influenza (including H1N1) ;
from viral proteins and surface proteins of infected cells , GI effects (Oseltamivir), bronchospasm in Oseltamivir is PO while Zanamivir is
ii. Neuraminidase inhibitors: decrease release of progeny virus ; For influenza A and B, asthmatics and cough with throat discomfort intranasal ; Peramivir has been
Oseltamivir, Zanamivir, Peramivir shortens duration of symptoms (Zanamivir ) given temporary emergency use
D. Drug for HBV and HCV

27
 cytokine, increased activity of JAKS leading to
phosphorylation of signal transducers and activation of
transcription (STATS) which causes increased formation of
antiviral proteins , also increases NK cells that destroy
infected liver cells, Degrades viral RNA via activation of alopecia, myalgia, severe depression, flu-like
host cell RNAse (ribonuclease) ; For chronic HBV, HCV syndrome, thyroid dysfunction, reversible slow absorption, given IM or SC
infection, Kaposi sarcoma, genital warts, prevents hearing loss, neutropenia ; Contraindications once a day 3x week but the PEG-
dissemination of HZV in cancer patients and decreased include autoimmune disease, history of cardiac form is only given once a week,
i. Interferon-α CMV shedding after renal transplantation arrhythmia and pregnancy given topically for genital warts
Dipiroxil is a prodrug of Adefovir ;
Telbivudine is a newer drug
(nucleoside analog) but
develpoment of resistance is rapid,
it is as effective as lamivudine ;
Inhibits HBV DNA polymerase causing chain termination Tenofovir is an anti-RT drug that is
after incorporation into the viral DNA ; For lamivudine- also effective in chronic HBV, it is
ii. Adefovir, Dipivoxil, resistant Hepatitis B infection, suppresses HBV replication Lactic acidosis, renal toxicity, severe active against lamivudine and
Telbivudine, Tenofovir and improves liver histology and fibrosis hepatomegaly with steatosis entecavir-resistant strains
is as effective as lamivudine, longer
iii. Entecavir guanosine nucleoside, inhibits DNA polymerase headache, dizziness, fatigue, nausea t1/2 of 12hrs
Coinfection between HBV and HIV
may increase the risk of pancreatitis
with lamivudine use ; longer t1/2 in
HBV infected cells than in HIV
see entry, also active for HBV, rapidly suppresses HBV (lower dose required in HBV than in
iii. Lamivudine (3TC) replication see entry HIV)
Inhibits guanosine triphosphate formation, prevents
capping of viral mRNA, blocks RNA-dependent RNA given PO, IV or aerosol, avoid
polymerase, inhibit replication of many DNA and RNA concomitant administration of
viruses like Influenza A and B, parainfluenza, paramyxo anatcids ; Early IV administration of
viruses, HCV and HIV ; For HCV infection (with IFN-α) and ribavirin decreases mortality in viral
RSV infection, decreases mortality in viral hemorrhagic haemolytic anemia, conjunctival and bronchial hemorrhagic fevers ; monotherapy
iii. Ribavirin fevers irritation, teratogen is NOT effective
Antiprotozoal Drugs
A. Antimalarial drugs
accumulates in the food vacuole of plasmodia —> Prevents May precipitate porphyria ;
polymerization of heme into hemozoin —> inc heme Chloroquine is 4-aminoquinoline
concentration which is toxic to the parasite, Blood derivative, can be given PO and has
schizonticide ; For malaria (non-falciparum, chloroquine- high Vd, absorption is decrease by
sensitive), DOC for acute attacks of non-Falciparum and antacids ; resistance is due to dec.
sensitive Falciparum malaria, used as chemoprophylaxis GI irritation, skin rash, headache, severe skin intracellular accumulation via inc
except in regions where P. falciparum is resistant, for lesions, peripheral neuropathies, myocardial activation of membrane pumps, dec
i. Chloroquine, autoimmune diseases such as rheumatoid arthritis, depression, retinal damage, auditory impairment, intravacuolar accumulation via
hydroxychloroquine amoebic liver abscess psychosis transporter encoded by pfcrt gene
Complexes with double stranded DNA to prevent strand
separation —> blocks DNA replication and transcription to Quinine is commonly used with
RNA, blood schizonticide ; For malaria (chloroquine- cinchonism (headache, tinnitus, vertigo), doxycycline or clindamycin to limit
resistant) and severe falciparum malaria (quinidine), given hemolysis in G6PD deficiency, blackwater fever, toxicities, PO and IV (in severe
together with Doxycycline and or Clindamycin to shorten blurring of vision, GI upset, disturbance n cardiac infection) ; NEVER use as
ii. Quinine, Quinidine gluconate duration of disease conduction ; CI in pregnancy prophylaxis
Unknown MOA, blood schizonticide ; For
chemoprophylaxis (chloroquine-resistant areas) ; 1st line
drug (weekly administration) for prophylaxis in all areas
with Chloroquine resistance), alternative to quinine in GI distress, skin rash, headache, dizziness, cardiac
acute attacks and uncomplicated infections from conduction defects, psychiatric disorders
iii. Mefloquine falciparum malaria (psychosis), neurologic symptoms, seziures is a 4-quinoline derivatives, PO
8-aminoquinoline, Forms quinoline-quinone metabolites
which are electron-transferring redox compounds that act
as cellular oxidants, tissue schizonticides, gametocides ; Eradicates hypnozoites in the liver,
For malaria, eradicates liver stages of P. vivax and P. ovale preventing malarial relapse, PO ,
(radical cure of P. vivax and P. ovale), alternative as GI distress, pruritus, headaches, should be used with a blood
primary prevention, terminal prophylaxis (vivax, ovale), methemoglobinemia, hemolysis in G6PD schizonticide, 14-day course of Tx
iv. Primaquine PCP pneumonia deficient patients ; CI in pregnancy after Tx with choloroquine
Atovaquone disrupts mitochondrial electron transport, also effective against Mefloquine-
blood and tissue schizonticide, proguanil inhibits folate resistant Falciparum infection ;
synthesis, sporonticide ; For treatment and Proguanil has a t1/2 12-16h ;
chemoprophylaxis of chloroquine-resistant falciparum, abdominal pain, nausea, vomiting, diarrhea, Atovaquone is an alternative for P.
v. Atovaquone-proguanil protective vs. Mefloquine-resistant falciparum headache, rash, increased liver enzymes jiroveci infection
Sequential blockade of folic acid synthesis (sulfadoxine
blocks Dihyrodpteroate synthetase, Pyrimethamine blocks GI disturbances, teratogen (enamel dysplasia and t1/2 is usually >100h, PO, highly
vi. Sulfadoxine-pyrimethamine Dihydrofolate reductase, blood schizonticide and discoloration), hepatotoxicity, nephrotoxicity, protein bound ; pyrimethamine is a
(Fansidar) sporonticide ; For malaria (for Chloroquine-resistant) photosensitivity, vestibulotoxicity, hemolysis sporonticide
Impairs progeny of malarial apicoplast genes, resulting in GI disturbances, teratogen (enamel dysplasia and
abnormal cell division, blood schizonticide ; For discoloration), hepatotoxicity, nephrotoxicity,
Do not drink with milk (decreased
vii. Doxycycline chemoprophylaxis in multi-drug resistant strains photosensitivity, vestibulotoxicity absorption), PO
Lumefantrine used in combination
with artemether (Co-arthem) for
uncomplicated falciparum infection
; Halofantrine is never used for
Unknown MOA, active vs the erythrocytic stage of all 4 prophylaxis because of
strains including Chloroquine-resistant, blood schizonticide abdominal pain, diarrhea, vomiting, cough, rash, cardiotoxicity and embryogenecity,
; For chloroquine-resistant malaria and severe falciparum headache, pruritus, elevated liver enzymes, Lumefantrine has minimal
viii. Halofantrine , lumefantrine malaria cardiotoxicity, teratogen cardiotoxicity

28
 Co-artem is the DOC for
uncomplicated falciparum malaria
in the Philippines ; Combination
therapy of artemesinins with one or
two long-acting antimalarial drugs
(amodiaquine, mefloquine,
sulfadoxine/pyrimethamine or
lumefantrine) is favored to retard
the development and progression
of drug resistance in P. falciparum ;
is metabolized in the food vacuole of protozoa —> Forms not given as Prophylaxis due to
ix. Artemsinin, artesunate, toxic free radicals in malarial food vacuole, blood short t1/2 (1-3h) ; the only reliably
artemether, dihydroartemsinin schizonticide ; For malaria (falciparum and MDR strains) nausea, vomiting, diarrhea ; SAFE in pregnancy effective meds vs Quinine-resistant
MOA same as chloroquine (inhibits the digestion of low-cost, given as combination with
x. Amiodaquine hemoglobin) ; For chloroquine-resistant falciparum agranulocytosis, aplastic anemia Artesunate
B. Anti-amoebiasis
Unknown MOA, converted to Diloxanide freebase (active
amobecide), luminal amebicide ; DOC for asymptomatic converted in vivo into Diloxanide
i. Diloxanide Furoate cyst carrier of E. histolytica flatulence, nausea, abdominal cramps freebase which is the amoebicide
Reserved only for situations where
Inhibits protein synthesis by blocking ribosomal movement metronidazole can’t be used , given
along messenger RNA, tissue amebicide ; back up drug for GI distress, muscle weakness, CV dysfunction SC or IM , usually given together
ii. Emetine, dehydroemetine severe intestinal, hepatic and extraintestinal amebiasis (arrhythmias and CHF) with luminal amebicides
halogenated hydroxyquinoline, Unknown MOA, luminal GI distress, thyroid enlargement, skin reactions
amebicide ; Alternative to Diloxanide for mild to severe due to iodine toxicity, neurotoxicity (peripheral Usually used in combination with
ii. Iodoquinol intestinal amebiasis neuropathy, visual dysfunction) metronidazole, PO
given PO, IV or topical,
Metronidazole t1/2 is 6-8h,
Tinidazole t1/2 is 12-14h; dose
adjustment in renal patients, well
Reactive reduction by ferredoxin forming free radicals that distributed even in CSF ; active
disrupt electron transport chain, tissue amebicide ; DOC against protozoan and bacteria
for severe intestinal wall disease and in hepatic abscess GI irritation, metallic taste, headache, dark urine, (Bacteroides and Clostridium, DOC
and other extra intestinal amebic disease, DOC for leukopenia, dizziness, ataxia, neuropathy, for Pseudomembranous colitis) ;
iii. Metronidazole, Tinidazole, trichomoniasis, also used for giardiasis, bacterial vaginosis seizures, disulfiram reaction, opportunistic causes potentiation of warfarin
Secnidazole (Gardnerella vaginalis), anaerobic infections, H. pylori PUD infections, parestheisa, CI in pregnancy action ; bets taken with meals
may be given together with
tetracycline in mild intestinal
An aminoglycoside, Inhibits protein synthesis, binds to 16S disease ; superior to Diloxanide in
ribosomal subunit, luminal amebicide ; For intestinal asymptomatic carries but SE limits
iv. Paromomycin amebiasis, cryptosporidiosis headaches, dizziness, rashes, arthralgia its use
Reactive reductions by ferredoxin forming free radicals
that disrupt electron transport chain, tissue amebicide ;
For metronidazole-resistant amebiasis, giardiasis, may also be used in helminthic
v. Nitazoxanide cryptosporidiosis (DOC) GI distress infections
C.Drugs for Pneumocystis and Toxoplasmosis
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; DOC for prophylaxis and GI upset, acute hemolysis in G6PD deficiency,
treatment of Pneumocystosis, prophylaxis (T. gondii, I. nephrotoxicity, hypersensitivity, hematotoxicity, Recommended at CD4 count < 200,
i. Co-trimoxazole belli) kernicterus given daily, PO or IV
Unknown MOA but may involve inhibition of glycolysis or respiratory stimulation followed by depression, Administered by nasal
interference with NA metabolism of Protozoans and Fungi hypotension, hypoglycaemia, anemia, spray/aerosol, given once a month
; For prophylaxis and treatment of pneumocystosis and neutropenia, hepatitis, pancreatitis, inhalant if used for prophylaxis, IV or IM for
ii. Pentamidine trypanosomiasis route has minimal SE 21 days if for Tx of active disease
an alternative drug for
gastric irritation, glossitis, neurologic symptoms Toxoplasmosis is Clindamycin ,give
Sequential blockade of dihydropteroate synthase (headache, insomnia, tremors, seizures), daily for 3-4 weeks if for Tx of active
(sulfadiazine) and dihydrofolate reductase hematotoxicity (megaloblastic anemia, toxoplasmosis , if for Toxoplasma
(pyrimethamine) ; DOC for prophylaxis and treatment of thrombocytopenia), pseudomembranous colitis encephalitis, give for at least 6
iii. Pyrimethamine-sulfadiazine toxoplasmosis (clindamycin) weeks
Atovaquone disrupts mitochondrial electron transport ;
For mild to moderate PCP, as chemoprophylaxis for abdominal pain, nausea, vomiting, diarrhea, has increased absorption in the
iv. Atovaquone Chloroquine resistant malaria (with Proguanil) fever, increased liver enzymes presence of food, PO
D. Drugs for Trypanosomiasis
Unknown MOA but may involve inhibition of glycolysis or
interference with NA metabolism of Protozoans and Fungi respiratory stimulation followed by depression,
; For hemolymphatic stage of T. gambiense and T. hypotension, hypoglycaemia, anemia, do not use for latter stages because
rhodiense, For prophylaxis and treatment of neutropenia, hepatitis, pancreatitis, inhalant it does not cross the BBB, also used
i. Pentamidine pneumocystosis route has minimal SE for Kala-azar and PCP
fatigue, nausea, vomiting, seizures, shock fever,
Polyanionic compound, Unknown MOA ; DOC for early rash, headache, paresthesia, neuropathies, renal Do not cross blood brain barrier ,
hemolymphatic stages of African sleeping sickness, abnormalities (proteinuria), chronic diarrhea, Used in combination with
ii. Suramin Alternative to Ivermectin in onchocerciasis haemolytic anemia and agranulocytosis melarsoprol
Suicide inhibitor of ornithine decarboxylase ; DOC for diarrhea, vomiting, anemia, thrombocytopenia,
iii. Eflornithine advanced west African sleeping sickness leukopenia, seizures Crosses blood brain barrier, PO, IV
Crosses BBB, administered
Organic arsenical, inhibits enzyme sulfhydryl (-SH) groups parenterally because it causes GI
iv. Melarsoprol in trypanosomes ; DOC for African sleeping sickness GI irritation, reactive encephalopathy upset
Nitrofurazone derivative, Inhibits trypanothione reductase
which is unique to the parasite ; DOC for Chagas disease /
American Sleeping sickness (Trypanosoma cruzi),
alternative for African sleeping sickness, also for nausea, vomiting, fever, rash, restlessness,
v. Nifurtimox mucocutaneous leishmaniasis insomnia, neuropathies, seizures Does not cross BBB
Drugs for Leishmaniasis

29
 IV ; alternative for leishmaniasis are
as follows: Pentamidine or
Miltefosine (for visceral
leishmaniasis), Fluconazole or
Metronidazole (for cutaneous
Pentavalent antimony, Inhibits glycolysis or effects on NA GI symptoms, fever, rash, arthralgia, healdache, leishmaniasis) and Amphotericin B
vi. Sodium Stibogluconate metabolism ; DOC for Leishmaniasis myalgia, sterile abscesses, cardiotoxicity (for mucocutaneous leishmaniasis)
Anthelmintics
Selectively inhibits microtubule synthesis and glucose Greatly affected by enzyme
uptake in nematodes, ovicidal ; Whipworm infections inducers and inhibitors ;
(drug of choice), Also a primary drug (together with GI irritation, agranulocytosis, alopecia, Elevated Contraindicated in pregnancy, Use
A. Mebendazole albendazole) for ascariasis, pinworm, Trichinosis, Visceral liver enzymes cautiously in patients with Cirrhosis

primary drug for ascariasis,

ancylostomiasis, trichuriasis ; safety
in pregnant and children is not yet
established ; Improved penetration
Inhibits microtubule assembly, larvicidal and ovicidal ; DOC (> Praziquantel) of the
for Ascariasis, Hookworm, Pinworm, Hydatid disease ; Also subarachnoid space in
used for Whipworm infections, Cutaneous & Visceral Larva Neurocysticersosis
migrans, Cysticercosis (larval stages of T. solium), reversible leukopenia, alopecia, elevation of liver Should not be given to patients with
B. Albendazole Angiostrongylus cantonensis, Capillaria philippinensis function tests, bone marrow suppression Cirrhosis
Immobilizes microfilariae by an unknown mechanism —> headache, malaise, weakness, anorexia, filarial
inc susceptibility to host defense mechanism ; DOC for fever (fever, rashes, ocular damage, joint and May cause mazzotti reaction when
C. Diethylcarbamazine filariasis and eye worm disease (Loa-Loa) muscle pain, lymphangitis) used for onchocerciasis

Antidote for Mazzoti reaction:

Intensifies GABA-mediated neurotransmission in antihistamine and NSAIDs ; CI in
nematodes —> immobilizes parasites —> removal by Mazzotti reaction (fever, headache, dizziness, pregnancy, children 5 y.o. and
reticuloendothelial system ; Used for Strongyloidiasis (drug rashes, pruritus, tachycardia, hypotension, pain Avoid concomitant use with other
of choice), Onchocerciasis, Cutaneous larva migrans, in muscles and joints and lymph glands), corneal drugs that enhance GABA activity
D. Ivermectin Filariasis (back up) opacities (Barbituraates, BZDs etc)

Stimulates nicotinic receptors at NMJ of nematodes —>

depolarization-induced paralysis, Causes release of ACh Contraindicated in patients with
and inhibition of Cholinesterase, Kills adult worms not eggs hepatic dysfunction (may cause an
; DOC for pinworm, may be used also for Hookworm, GI distress headache, weakness, dizziness, increase in LFT) ; No study on
E. Pyrantel pamoate Trichostrongylus and Ascaris infections insomia, rash, fever, pregnant and children <2y.o.

Structural congener of Mebendazole, same MOA as

Mebendazole, Selectively inhibits microtubule synthesis Gastrointestinal irritation, Headache, Dizziness,
and glucose uptake in nematodes, Inhibits fumarate Drowsiness, Leukopenia, Hematuria,
reductase. Ovicidal, has anti-inflammatory and Hypersensitivity reactions (SJS), Hepatotoxicity
immunosuppressive action in the host ; Used for (intrahepatic cholestasis, liver failure), Reactions CI in renal and liver disease and in
F. Thiabendazole Trichinosis (drug of choice), Strongyloidiasis (backup) caused by dying parasites pregnancy

Increases membrane permeability to calcium —>

contraction of trematode and cestode muscle —> muscle Used with steroid when treating
paralysis, vacualization and death ; DOC for trematodes neurocysticercosis to dec swelling ,
(schistosoma, paragonimus, clonorchis, opistorchis, contraindicated in ocular
Fasciolopsis, Heterophyes) and cestodes (taenia, cysticercosis (may cause irreparable
diphyllobothrium, Hymenopelsis) together with eye damage) ; May be used as an
Niclosamide ; for infection by small and large intestinal headache, dizziness, nausea, malaise, Inc ICP, adjunct to Albendazole in Hydatid
G. Praziquantel flukes ; alternative to Albendazole in Cysticerci seizure (neurocystecercosis) ; CI in pregnancy disease
Uncouples oxidative phosphorylation or by activating
ATPases, scoleces and segments are killed but NOT Ova ;
alternative drug to Praziquantel for cestode infection
(Taenia, Diphyllobotrium), not effective in cystecercosis Avoid ethanol consumption for 48
(use Albendazole or Praziquantel instead) or Hydatid hours upon drug consumption ;
disease (use Albendazole), effective in the Tx of infections Safety in children <2y.o. and
H. Niclosamide from small and large intestinal flukes GI distress, headache, rash, fever pregnanct not yet established

GABA agonist —> paralyze ascaris —> expelled by normal Contraindicated in pregnancy,
peristalsis , block ACh at the myoneural junction --> impaired renal or hepatic function
expulsion via normal peristalsis ; As alternative for or with a history of epilepsy or
I. Piperazine ascariasis GI upset chronic neurologic disease
Unknown MOA ; co-DOC (with Triclabendazole) for Tx of
Fascioliasis (sheep liver fluke), as alternative for Nausea,vomiting, diarrhea, abdominal cramps,
J. Bithionol paragonimiasis phototoxicity, rash do not use in Px <8y.o.
an organophosphate prodrug —> Dichlorvos (AchE
inhibitor) -> muscle contraction —> paralysis ; Active vs
K. Metrifonate Schistosoma haemoatobium Excess cholinergic stimulation (DUMBBELSS) CI in pregnancy
GI upset, pruritus, eosinophilia, urticaria,
pulmonary infiltrates, fever, orange-red
effective solely in Schistosoma mansion (intestinal discoloration of urine ; CI in pregnancy and
bilharziasis) - on male immature forms and adult seizure disorder, proteinuria, microscopic Px is not allowed to drive within
L. Oxamniquine schistosomal forms ; MOA is unknown hematuria, 24hrs after intake of Oxamniquine
Cancer Chemotherapy
all are Cell-cycle non-specific ; Universal MOA: form
reactive molecular species that alkylate nucleophilic Resistance is due to increased DNA
groups on DNA bases, particularly the N-7 of guanine repair, decreased drug permeability
leading to cross-linking of bases, abnormal base pairing and production of trapping agents
A. Alkylating agents and DNA strand breakage such as thiols

30
 Forms DNA cross-links, resulting in inhibition of DNA bone marrow suppression, hemorrhagic cystitis, Rescue therapy is MESNA and
synthesis and function, Cell-cycle nonspecific, hepatotoxicity, alopecia, SIADH, pulmonary hydration; metabolite is acrolein
i. Nitrogen Mustards: Mechlorethamine has additional MOA: converts to a toxicity, cardiac dysfunction ; Mechorethamine which is important for
Cyclophosphamide, Chlorambucil, reactive cytotoxic product ; For non-hodgkin’s lymphoma, SE include marked vesicant action, sterility, Cyclophosphamide’s anti-cancer
Mechlorethamine breast cancer, ovarian cancer, neuroblastoma, CLL myelosuppresion, alopecia effect and also its toxicity
Forms DNA cross-links, resulting in inhibition of DNA IV, Rescue therapy is Amifostine,
synthesis and function, Cell-cycle nonspecific ; component decreased nephrotoxicity by giving
of regimen For testicular cancer, ovarian cancer, bladder nausea, vomiting, nephrotoxicity, neurotoxicity mannitol with forced hydration ;
ii. Platinum Analogs: Cisplatin, cancer and lung cancer ; Oxaliplatin is used also for (peripheral neuritis), ototoxicity (acoustic nerve Carboplatin is less nephrotoxic but
Carboplatin, oxaliplatin advanced colon CA damage), hematotoxicity has more myelosuppression
Forms DNA cross-links, resulting in inhibition of DNA pulmonary fibrosis, adrenal insufficiency, skin
iii. Alkyl sulfonate: Busulfan synthesis and function, Cell-cycle nonspecific ; For CML pigmentation Spares the bone marrow
Forms DNA cross-links, resulting in inhibition of DNA
iv. Nirtosoureas: Carmustine, synthesis and function, Cell-cycle nonspecific ; For brain CNS toxicity (dizziness, ataxia), nausea and Highly lipophilic allowing ease of
lomustine tumors, melanoma, skin cancer vomiting, bone marrow suppression, skin flushing passage through BBB into the CNS
a reactive agent which forms hydrogen peroxide, which
generates free radicals that cause DNA strand scission, cell bone marrow suppression, pulmonary toxicity, PO, can pemetrate the CSF,
v. Others: Procarbazine, cycle non-specific ; component of reigned For Hodgkin’s hemolysis, disulfiram reaction,skin reactions, LEUKEMOGENIC, CPY450 inhibitor,
Dacarbazine lymphoma, non-hodgkin’s lymphoma, brain tumors peripheral neuropathy, CNS dysfunction Dacarbazine is phototoxic
all are cell-cycle specific , they also have
B. Antimetabolites immunosuppressant action PO, IV, Rescue therapy is
Leucovorin (Folinic acid) ; cytotoxic
due to formation of polyglutamate
derivatives ; resistance is due to
decreased drug accumulation,
changes in drug sensitivity or
Inhibits dihydrofolate reductase, decreases synthesis of activity of DHF reductase and
thymidylate, amino acids, purine nucleotides —> interfere decreased formation of
with NA and CHON metabolism ; cell cycle specific ; For polyglutamates ; clearance is
choriocarcinoma, acute leukemia, non-hodgkin, primary dependent on renal function
CNS lymphoma, breast cancer, head and neck cancer, therefore adequate hydration is
i. Folate antagonist: bladder cancer ; also for psoriasis, rheumatoid arthritis, bone marrow suppression, pulmonary infiltrates important to prevent crystallization
Methotrexate ectopic pregnancy and fibrosis, mucositis, crystalluria, hepatotoxic into stones
6-MP metabolism inhibited by
allopurinol and febuxostat ,
Resistance is due to decreased
are activated by hypoxanthie-guanine activity of HGPRT, increased
phosphoribosyltransferase (HGPRT) to toxic nucleotides alkaline phosphatase activity (which
ii. Purine antagonist: 6- which inhibit enzymes in purine metabolism —> Inhibits inactivates the toxic nucleotide) ,
Mercaptopurine, 6-thioguanine, de novo purine nucleotide synthesis , cell cycle specific ; bone marrow suppression, hepatic dysfunction undergo significant FPE (by
fludarabine, cladribine For acute leukemia (AML, ALL), CML (necrosis, jaundice, cholestasis) xanthine
IV, oxidase)to CSF, causes
can distribute
“thymineless” death of cells,
Resistance is due to decreased
activation of 5-FU, increase
converted to 5-fluoro-2’-deoxyuridine-5’-monophosphate thymidylate synthase activity and
(5-FdUMP) which Inhibits thymidylate synthase, decreased sensitivity of this enzyme
incorporation inhibits DNA synthesis and function, cell ; another metabolite is 5-
cycle specific ; For bladder cancer, breast cancer, colorectal florouridine-5’triphosphate (FUTP)
cancer, anal cancer, head and neck cancer, liver cancer and which incorporates into RNA —>
iii. Pyrimidine antagonist: 5- ovarian cancer, topically for keratoses and superficial basal interfere with RNA processing and
Fluorouracil cell skin cancer bone marrow suppression, GI irritation, alopecia function
a cytosine arabinoside, activated by kinases to Ara- Most specific for the S-phase of the
Cytidine Triphosphate (AraCTP) which Inhibits DNA cell cycle, Resistance is due to
polymerase —> inhibition of DNA synthesis and repair, decreased uptake and decreased
iv. Pyrimidine antagonist: inhibits ribonucleotide reductase with reduced formation GI irritation, bone marrow suppression, conversion to AraCTP, a cytosine
Cytarabine (ARA-C) of dNTPs, cell cycle specific ; For AML, ALL, CML neurotoxicity arabinoside
a deoxycytidine analog, converted to Gemcitabine
diphosphate which inhibits ribonucleotide reductase with
reduced formation of deoxyribonucleotide triphosphate
required for DNA synthesis, Gemcitabine triphosphate is
incorporated into DNA causing chain termination, cell cycle
v. Pyrimidine antagonist: specific ; For pancreatic cancer, bladder cancer, non-small bone marrow suppression, neutropenia,
Gemcitabine cell lung cancer, non-Hodgkins lymphoma pulmonary toxicity a deoxycytidine analog
C. Natural Anticancer Drugs all are cell-cycle specific
Prevents assembly of tubulin dimers into microtubule
assembly blocking the formation of mitotic spindles,
causes cell arrest at metaphase, cell cycle specific ; For
acute leukemias, lymphomas, wilms tumor and IV, highly distributed except in CSF,
neuroblastoma ; Vinblastine For lymphomas, Acts primarily in M phase of cancer
neuroblastomas, testicular carcinoma and Kaposi sarcoma cell cycle, Resistance is due to
i. Vinca alkaloid: Vincristine, ; Vinorelbine For non-small cell lung cancer and breast Neurotixicity (areflexia, peripheral neuritis, increased efflux of drugs via
Vinblastine, Vinorelbine cancer paralytic ileus) membrane drug transporter
Induces DNA breakage by inhibiting DNA topoisomerase II,
inhibits mitochondrial electron transport, cell cycle specific
; Combination regimen For lung cancer, prostate cancer, PO, high Vd ; dose adjustment in
ii. Podophyllotoxin: Etoposide, testicular cancer, non-hodgkin’s lymphoma, germ cell and renal patients ; Act on the Late S
Teniposide gastric cancer bone marrow suppression, alopecia, GI distress and early G2 phase
Inhibits DNA topoisomerase I which cute and relegates
single DNA strands during normal DNA repair, cell cycle
iii. Camptothecins: Topotecan, specific; For advanced ovarian cancer (2nd line), small cell Irinotecan can be used for
Irinotecan lung cancer, Irinotecan For metastatic colorectal cancer bone marrow suppression, diarrhea metastatic colorectal cancer
Interferes with mitotic spindle synthesis by preventing
microtubule disassembly into tubulin monomers, cell cycle Paclitaxel (neutropenia, thrombocytopenia,
specific ; For solid tumors - advanced breast and ovarian peripheral neuropathy, hypersensitivity),
cancer, lung cancer, gastroesophageal cancer, prostate Docetaxel (neurotoxicity, bone marrow
iv. Taxanes: Paclitaxel, Docetaxel cancer, bladder cancer, head and neck cancer suppression) Act on M phase
D. Antitumor antibiotics

31
 Intercalates between base pairs, inhibits topoisomerase II,
generates free radicals, blocks synthesis of RNA and DNA
causing DNA strand scission, causes membrane disruption,
cell cycle non-specific ; Doxorubicin For Hodgkins and Non-
Hodgkins lumphoma, myelomas, sarcomas, breast cancer,
endometrial cancer, lung cancer, ovarian cancer and
thyroid cancer ; Daunorubicin For acute leukemias
Idarubicin For AML, Epirubicin For breast cancer and
i. Anthracycline: Doxorubicin, gastroesophageal ; Mitoxantrine For acute myeloid
Daunorubicin, Idarubicin, leukemias, Non-Hodgkins lymphoma, breast and alopecia, nausea, vomiting, Cardiotoxicity Rescue therapy is Dexrazoxane and
Epirubicin, Mitoxantrone gastroesophageal cancer (dilated cardiomyopathy, CHF) liposomal formulation of the drug
Generated free radicals which bind to DNA and causes
DNA strand breaks leading to inhibition of DNA synthesis,
intercalates with DNA, cell cycle specific ; Component of IV, inactivated by tissue
regimens in Hodgkins lymphoma and testicular cancer, pneumonitis, pulmonary fibrosis, alopecia, aminopeptidases, Most specific for
lymphomas and squamous cell cancer, head and neck mucocutaneous reactions, hypersensitivity the G2 phase of cell cycle, a
ii. Bleomycin cancer, skin cancer reactions glycopeptide
Binds to double stranded DNA, inhibits DNA-dependent
RNA synthesis, cell cycle non-specific ; For melanoma, bone marrow suppression, skin reactions, GI
iii. Actinomycin D wilm’s tumor, choriocarcinoma, Kaposi sarcoma irritation None
Metabolized into an alkylating agent that cross-links DNA ;
In combination regimens for adenocarcinoma of the cervix, severe myelosuppression, toxic the heart, liver,
iv. Mitomycin C stomach, pancreas and lungs lungs and kidneys IV, used for hypoxic tumor cells
E. Miscellaneous Anticancer Drugs
i. TK inhibitor: Imatinib, Tyrosine kinase inhibitor of the protein product of bcr-abl Resistance is due to mutation is bcr-
Dasatinib, Nilotinib oncogene in CML ; For CML, GIST diarrhea, myalgia, fluid retention, CHF abl gene
ii. Growth Factor Receptor Inhibitor
recognizes a surface protein in breast CA cells that
a. Her-2-neu inhibitor: overexpress Her-2-neu receptors for epidermal growth nausea, vomiting, chills, fever, headache,
Trastuzumab factor cardiotoxicity (CHF) None
EGFR (Epidermal Growth Factor Receptor) regulate
signaling involved in cellular proliferation, invasion and
metastasis and angiogenesis, it also inhibits cytotoxic
activity of some anti-cancer and radiation treatment,
Gefitinib and Erlotinib are capable of inhibiting EGFR’s
Tyrosine Kinase domain ; Cetuximab (+ Irinotecan and
Oxalipatin) For metastatic colon cancer and Head and Neck
cancer ; Panitumumab For refractory colorectal cancer ;
b. EGFR inhibitor: Cetuximab, Gefitinib and Erlotinib as second-line agents for non-small Erlotinib can also be used for
Panitumumab, Gefitinib, Erlotinib cell lung cancer folliculitis, diffuse hair loss, dry skin, paronychia advanced pancreatic cancer
VEGF (Vascular Endothelial Growth Factor) has a role in
angiogenesis required for metastasis, Inhibits binding of
VEGF to VEGFR leading to inhibition of VEGF signalling,
inhibits tumor vascular permeability but enhances tumor
blood flow and drug delivery ; Sorefenib Sunitinib and
Pazopanib inhibits multiple receptor Tyrosine Kinase
c. VEGF Inhibitor: Bevacizumab, including those associated to VEGF ; For metastatic hypertension, arterial thrombosis, impaired may also be used in non-small cell
Sorafenib, Sunitinib, Pazopanib colorectal cancer, breast cancer, diabetic retinopathy wound healing, proteinuria, GI perforation lung CA and renal CA
Binds to a surface protein in NHL cells, induces
complement-mediated lysis, direct cytotoxicity and
induction of apoptosis ; For Non-Hodgkin’s lymphoma and hypersensitivity reaction, bone marrow
iv. Rituximab other lymphomas suppression None
Endogenous glycoproteins with antineoplastic, alopecia, myalgia, depression, thyroid
immunosuppressive and antiviral actions ; For hairy cell dysfunction, hearing loss, bone marrow
v. Interferon alpha leukemia, early CML, T-cell lymphoma suppression None
Depletes serum asparagine ; For ALL, T-cell auxotrophic CA
(leukemia and lymphomas) that require asparagine for acute pancreatitis, bleeding, severe
vi. Asparaginase growth hypersensitivity reaction None
Allows DNA transcription and differentiation of immature Only vitamin that can cure cancer,
leukemic promyelocytes into mature granulocytes ; For retinoic acid syndrome (dyspnea, fever, weight treat retinoic acid syndrome with
vii. All-Trans retinoic acid acute promyelocytic leukemia gain, peripheral edema) dexamethasone
viii. Protease Inhibitor: a reversible inhibitor of 26s proteasome in mammalian cell
Bortezomib ; For multiple myeloma peripheral neuropathy, thrombocytoppenia
F. Hormonal Anticancer Agents
Suppresses inflammation and immune response, may
trigger apoptosis and work on nondividing cancer cells ; adrenal suppression, growth inhibition, muscle
i. Prednisone For CLL, Hodgkin’s lymphoma, leukemia, lymphoma wasting, osteoporosis, salt retention see entry
Estrogen antagonist actions in breasts tissue and CNS,
estrogen agonist effects in uterus, liver and bone ; For
hormone-responsive breast cancer, Toremifene For hot flushes, thromboembolism, endometrial Prevents osteoporosis and decrease
ii. SERM: Tamoxifen, Toremifene advanced breast cancer hyperplasia, endometrial cancer risk of atherosclerosis
GnRH analogs (leuprolide) must be
iii. Androgen antagonist: co-administered to prevent acute
Flutamide Androgen antagonist ; For prostate cancer gynecomastia, hot flushes, impotence flare-up of prostate cancer
Increased LH, FSH secretion with intermittent hot flushes, sweats, headache, osteoporosis,
iv. GnRH analog: Leuprolide, administration, reduced LH and FSH secretion with gynecomastia, gynecomastia, testicular atrophy,
Goserelin Nafarelin prolonged continuous administration ; For prostate cancer impotence, bone pain see entry

v. Aromatase inhibitor: Reduces estrogen synthesis by inhibiting aromatase; For nausea, diarrhea, hot flushes, bone and back Effective againsts breast cancer that
Anastrazole, Letrozole advanced breast cancer pain, dyspnea, peripheral edema have become resistant to tamoxifen

Drugs Used in the Treatment of Gastrointestinal Diseases [Divided into 2 classes: agents that reduce intragastric acidity and agents that promote mucosal defense

32
 Impairs absorption of tetracyclines,
flouroquinolones,itraconazole and
iron --> should not be given within 2
hours with these drugs ; When used
regularly in large doses needed to
significantly raise the stomach pH,
antacids, decrease recurrence rate
Sodium bicarbonate: Belching, metabolic of peptic ulcers ; Aluminum and
alkalosis. Calcium carbonate: hypercalcemia, Magnesium are always given
A. Antacids: Magnesium- renal insufficiency, metabolic alkalosis (milk- together to cancel out each other's
Aluminum Hydroxide, Calcium Neutralize stomach acid by reacting with protons in the alkali syndrome) exc for Aluminum Magnesium adverse effects ; Avoid in renally
carbonate, Sodium bicarbonate lumen ; For peptic ulcer disease, Gastroesophagal reflux Hydroxide impaired patients ; DOA: 1-2 hours

Cimetidine is a potent inhibitor of

CYP450. Highly effective in
suppressing nocturnal acid
secretion but only modest effect on
meal- stimulated secretion ; avoid
in renally and hepatically (severe)
impaired patients ; are highly
Gynecomastia (cimetidine only), Diarrhea, selective and does not affect H1
B. H2 receptor antagonist: Competitive pharmacologic block of H2 receptors ; For headache, fatigue, Myalgias, constipation, and H3 receptors, may also reduce
Cimetidine, Ranitidine, peptic ulcer disease, Zollinger-Ellison syndrome, Nosocomial pneumonia, Mental status changes, seceretion of pepsin ; DOA: 6-10hrs
Famotidine, Nizatidine Gastroesophagal reflux, dyspepsia Bradycardia, Hypotension, Blood dyscrasias ; Reduces acid secretion by 60-70%

usually enetric coated, t1/2 is 1-

2hrs but DOA of is around 24hrs,
needs 3-4 days treatment to
achieve full effectiveness ;
decreases bioavailability drugs that
require acidity for GI absorption ;
when used for PUD together with 2
Irreversible blockade of H/K ATPase in active gastric antibiotics, achieve 90% cure ;
C. Proton Pump Inhibitor: parietal cells, Long lasting reduction of meal stimulated Diarrhea, headache, abdominal pain, Reduces acid secretion by 90-98% ;
Omeprazole, Lansopraole, and nocturnal acid secretion ; For Peptic ulcer Malabsorption syndrome (Vit B12, Ca, Fe, Zn, should be taken on an empty
Rabeprazole, Pantoprazole, disease(DOC), Zollinger-Ellison syndrome, Digoxin, Ketoconazole), Infections (respiratory, stomach since food decreases its
Esomeprazole Gastroesophageal reflux, dyspepsia enteric), Hypergastrinemia, Atrophic gastritis bioavailability by 50%
D. Mucosal Protective Agent:
polymerizes in acidic environmet —> polymers bind to
injured tissue and forms a protective covering over ulcer Highly insoluble, requiring frequent
bed, Accelerates healing of peptic ulcers and reduces dosing (QID) ; chemically:
i. Sucralfate recurrence rate ; For Peptic ulcer disease constipation, dizziness, flatulence, dry mouth Aluminum Sucrose Sulfate
forms a protective coating on ulcerated tissue, stimulates
mucosal protective mechanisms, direct antimicrobial Black stools, darkening of tongue,
effects and sequestration of enterotoxins ; For Peptic ulcer Encephalopathy (Atraxia, headaches, confusion, Reduces stool frequency and
ii. Bismuth Salicylate disease, Dyspepsia, Infectious diarrhea seizures) liquidity in infectious diarrhea
PGE1 analog, Activates EP receptors, causes increased
HCO3 and mucus secretion and inhibits acid secretion in
the stomach, causes uterine contraction ; For Peptic ulcer
disease, Prevention of NSAID-induced gastric mucosal Abdominal pain, Diarrhea, Uterine cramping, see entry, decreases ulcer in NSAIDs
iii. Misoprostol injury, Abortifacient Miscarriage induced ulceration
E. Prokinetics
Metoclopramide and domperidone block D2 receptors,
Erythromycin stimulates motilin receptor, Increases gastric
emptying and intestinal motility ; As Antiemetic for post
i. Metoclopramide, operative/chemotherapy vomiting, Diabetic gastroparesis Domperidone does not cross the
Domperidone, Erythromycin, (drug of choice), Neostigmine for acute large bowel Parkinsonism, Extrapyramidal effects, BBB (less toxic) ; Increases LES
Neostigmine distention Hyperprolactinemia pressure (helpful in GERD)
F. Laxatives
Indigestible, hydrophilic colloids that absorb water,
i. Bulk-forming: Psyllium, forming a bulky emollient gel that distends the colon and
Methylcellulose, Polycarbophil promotes peristasis ; For constipation Diarrhea None

ii. Stool-softener: Docusate, Soften stool material, Permitting water and lipids to Diarrhea, Aspiration,(Lipid pneumonitis),
Glycerine, Mineral oil penetrate the stool ; For constipation Malaabsorption of fat-soluble vitamins (A, D, E, K) None
iii. Osmotic: Lactulose, Soluble but nonabsorbable compound that result in
Magnesium oxide, Magnesium increased stool liquidity due to an obligate increase in Diarrhea, Flatus, Abominal cramps, Electrolyte
hydroxide, Sorbitol, Magnesium fecal fluid ; For Constipation, Hepatic encephalopathy abnormalities (hyperphosphatemia,
citrate, Sodium phosphate, (lactulose), Preparation for endoscopy (polyethylene hypocalcemia, hypernatremia, hypokalemia,
Polyethylene Glycol glycol) hypermagnesemia) None
iv. Stimulant: Bisacodyl, Aloe, Unknown. Directly stimulate enteric nervous system and
Senna, Cascara, Castor oil colonic electrolyte and fluid secretion Diarrhea can cause melanosis coli
Lubiprostone is a Chloride channel activator which
stimulates Cl secretion into the intestines leading to
increased fecal fluid content, Methylnaltrexone and
v. Miscellaneous: Lubiprostone, Alvimopan are Opioid receptor antagonist that block mild nausea, stomach pain, mild diarrhoea,
Methylnaltrexone, Alvimopan intestinal mu receptors, but not the CNS bloating, headache NONE

33
 Do not use in children less than 4
years of age (increased chance of
Activates opioid receptors in enteric nervous system. Slows causing paralytic ileus), Reverse
G. Anti-diarrheals: Diphenoxylate, motility with negligible CNS effects, Kaolin (+pectin) ileus by administering Betanechol.
Loperamide, Kaolin+Pectin, absorbs bacterial toxin and fluid leading to decreased stool Drowsiness, Nausea, Paralytic ileus, interfere Direct m-agonist, Kaolin is hydrated
Colloidal Bismuth liquidity ; for Diarrhea (nonspecific, noninfectious) with absorption of other drugs Magnesium Aluminum Silicate
H. Drugs for IBS
i. laxatives, antidiarrheals and
low-dose TCA see entry see entry see entry
ii. Anticholinergics: Dicylomine, see entry ; antispasmodic for abdominal pain, for IBS with
Hyoscyamine prominent diarrhoea see entry see entry
iii. 5HT3 antagonist: Alosteron see entry ; For IBS with severe diarrhoea severe constipation, ischemic colitis see entry
see entry ; activate type2 chloride channels in small
iv. Lubiprostone intestines ; For IBS with predominant constipation see entry see entry
I. Anti-emetics
Blocks chemoreceptor trigger zone and enteric nervous
i. Ondansetron, Granisetron, system 5-HT3 receptors ; For Vomiting (Post Headache, Dizziness, Constipation, QRS and QT
Dolasetron, Palonosetron chemothereaphy, postoperative) prolongation (Dolasetron only) see entry
antagonist of the Neurokinin-1 receptor in the areas
postrema that is activated by substance P and other
ii. Aprepitant tackykinins ; For post-chemotherapy nausea and vomiting fatigue, dizziness, diarrhea an enzyme inhibitor
iii. Scopoloamine see entry ; For motion sickness emesis see entry see entry
J. Drugs for IBD
Unknown. Probably inhibits production of eicosanoid
i. Aminosalicylates: Mesalamine, inflammatory mediators (PG and LT) and interfering with Gastrointestinal upset,Headaches, Arthralgias,
Balsalazine, Olsalazine, cytokines ; For Inflammatory bowel disease (mild to Myalgias, Bone marrow suppression, Malaise, Not useful for treating active flare
Sulfasalazine moderate) Hypersensitivity reactions ( severe) ups of disease
ii. Other agents: Antibiotics,
Immunosuppressibe
antimetabolites (Azathioprine, 6- see entry ; Natalizumab is a Mab that blocks intergrins in
MP, Methotrexate), anti-TNF circulating leukocytes, restricted to severe refractory
(Infliximab), Natalizumab Crohn’s disease multifocal leukoencephalopathy see entry
K. Miscellaneous Agents
For pancreatic enzyme replacement, improve digestion of
fats proteins and carbohydrates ; For pancreatic
i. Pancreatic lipase: Pancreatin or insufficiency due to Cystic Fibrosis, pancreatitis and
Pancrealipase pancreatectomy hyperuricemia Taken with every meal
a bile acid derivative that decreases cholesterol content of
bile by decreasing hepatic cholesterol secretion and other
ii. Drugs that inhibit formation of effects on hepatocyte canalicular membrane ; For headache, dizziness, mild stomach pain,
Gallstones: Ursodiol gallstone in patients refusing or not eligible for surgery rhinorrhea, sore throat, rash hair loss None

Drugs Used For Cough

decrease sputum activity ; Usually derivatives of cysteine;

reduce disulfide bridges that bind glycoproteins to other Chest tightness, Disagreeable odor, Drowsiness,
proteins such as albumin ; Also act as antioxidants & may Fever, Hemoptysis, Increased volume of
reduce airway inflammation ; Orally available drugs are bronchial secretions, Irritation of tracheal or
A. Mucolytics : N-acetylcysteine, well-tolerated; but of little benefit in acute respiratory bronchial tract, Nausea, Rhinorrhea, Stomatitis, available as IV, PO, IM and
Carbocysteine, Ambroxol condition Vomiting inhalational forms

Drowsiness, Incomplete or Infrequent Bowel

may act as an irritant to gastric vagal receptors, and Movements, Inducing of a Relaxed Easy State,
recruit efferent parasympathetic reflexes that cause Stomach Cramps, dizziness or headache, a rash,
B. Expectorants: Guiafenesin glandular exocytosis of a less viscous mucus mixture. or. nausea, vomiting, or stomach upset Are often emetics (ipecac, guaifenesin)

DO NOT suppress in bacterial lung

infections, asthma, bronchiectasis
(suppurating bronchial
inflammation) or chronic bronchitis
Used for dry painful cough of neoplasia or pleural disease ; where antitussives can cause
Irritative cough in inflammation of the respiratory tract harmful sputum thickening &
C. Antitussives (epiglottitis); in hemoptysis retention

Morphine may be effective but

indicated only in intractable cough
from bronchial carcinoma ;
Dextromethorphan has no addictive
i. Centrally-acting: Opioid Decreases secretions in the bronchioles, thickens potential, no analgesic effect,
antitussives (codeine, decreased sensitivity of the medullary/ CNS cough centers sputum & inhibits ciliary activity, reducing produces less constipation and
dextromethorphan) to peripheral stimuli and decreased mucosal secretion clearance of thickened sputum, Constipation inhibition of mucociliary clearance
Centrally acting antitussive but is
neither chemically or
ii. Centrally-acting: Non-opioid Somnolence, nausea, vomiting, diarrhea, pharmacologically related to
(butamirate citrate) act through receptors in the brainstem to inhibit cough dizziness and hypotension opioids

does not cause side effects such as

Non-opoid drug with a peripheral action by inhibiting the Nausea, vomiting, heartburn, diarrhea, fatigue, constipation or respiratory
iii. Peripherally-acting: afferent pathways that generate the cough reflex weakness, drowsiness, dizziness, headache, depression which can be produced
Levodropropizine (modulates C-fibre activity) palpitations by opioid antitussives

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ifenesin)

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