Contents

General Pharmacology : Part 1  1

General Pharmacology : Part 2  7

Drugs Acting on Autonomic Nervous System  14

Drugs acting on Cardiovascular System : Part 1  20

Drugs acting on Cardiovascular System : Part 2  24

Drugs Acting on Kidney  30

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Drugs Acting on Central Nervous System  32

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Antibiotics : Part 1  42

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Antibiotics : Part 2  7@ 48
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Drugs Acting on Endocrine System  54

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Autacoids  61
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Drugs Acting on Respiratory System, GIT and Blood  66

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Anti Neoplastic agents and Immunomodulators  73

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 General Pharmacology : Part 1 1

GENERAL PHARMACOLOGY : PART 1 ----- Active space -----

Types of Drugs 00:07:58

Orphan drugs :
Used for rare diseases ↓Profitability (↓Development of drug).
Note : Orphan receptor Receptor with unknown ligand.
Essential drugs :
Meets healthcare needs of the majority of a population :
• Inexpensive. • Safe.

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• Non-toxic. • Single molecule (Not fixed dose

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• Easily available.

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combination).

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• Efficacious. 7@
Prescription/legend drugs : Require prescription (Under Schedule H).
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Spurious drugs : Does not produce expected effect as drug component is falsified.
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Misbranded drugs : Incorrect or missing information on drug label.

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Adulterated drug : Unwanted additive in drug.

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Rational Drug Use :

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Use of right drug for right disease & patient; at right dose, duration & route with
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right dispensation & monitoring (“Right price” not included).

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Movement of Drug Through the Body (ADME) 00:08:00

Absorption Distribution Metabolism Excretion

Note : Pharmacodynamics Drug induced change in body via receptor binding (Drug receptor effect).

Drug Absorption 00:10:10

• M/c mechanism : Passive diffusion along concentration gradient.

(Lipid soluble; Unionised drugs pH of drug = pH of medium).
• Maximum absorption of drug in GIT : Small intestine (D/t large surface area).
• Poor oral absorption : Drugs with large size (Eg : Proteins Drugs with -tide/-ase/-mab).

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 2 Pharmacology

----- Active space ----- Types of Tablets/Capsules :

Plasma concentration
Controlled release : Drug covered with a
membrane.
Sustained release : Over a period of time; drug
embedded within layers.
Conventional release : Peak present.

Time
Uses of controlled/sustained release :
• ↑Duration of effect ↓no. of doses. (Useful if t1/2/< 4h).
• ↓Risk of acute toxicity : D/t lower/absent peak concentration.
Enteric coated drugs :

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• HCl-resistant membrane coating used.

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• Prevents drug breakdown in acidic pH of stomach.

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Extent of Absorption : Rate of Absorption :
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• Amount of drug absorbed. • Amount of drug absorbed per

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• AKA bioavailability. unit of time.

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• Formula : • Determined by Tmax.

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AUCoral
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Bioavailability =
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AUCI/V
Plasma Concentration

Cmax (Maximum PC)

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(AUC = Area under curve)

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Plasma Concentration

AUCI/V
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AUCoral Tmax Time

(Time to achieve Cmax)

Time Note R A T E : Rate Tmax

AUC Extent
ATP-binding Cassette (ABC) :
AKA : p-glycoprotein/Multi-drug resistance (MDR)-1 pumps.

Physiological functions :
1. Intestine/liver : Drug efflux (Eg : Digoxin).
↓Drug concentration in systemic circulation due to removal.
2. Blood brain barrier : Limit drug exposure to central nervous system.
Removes drugs that cross the BBB No central effects (Eg : Loperamide).
3. In liver : Excretion of bile acids.
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 General Pharmacology : Part 1 3

----- Active space -----

Pathological function :
Cancer cells/bacteria : Use the pump to remove drug. (Confers resistance AKA MDR-1 pump).
p-GP/MDR-1 substrates p-GP/MDR-1 inducers
• Loperamide • Digoxin Enzyme inducers like :
• Methadone • Erythromycin, Clarithromycin • Rifampicin
• Nelfinavir • Quinidine • Phenytoin
• Cyclosporine • Ranolazine • Carbamazepine
• CCB (Verapamil) • Sotagliflozin
Significance :
1. pGP substrates competitively inhibit each other ↑Toxicity of either drug.
Eg :
- Clarithromycin + Digoxin Digoxin toxicity.

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- Quinidine Loperamide induced CNS toxicity (Crosses BBB).

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2. pGP inducers cause drug failure.

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Eg : Rifampicin + Digoxin ↑Digoxin efflux Rx failure.
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3. pGP substrates can cause cholestatic jaundice :
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D/t competitive inhibition of bile acid excretion. Eg : Cyclosporine.

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4. pGP inhibitors can be used to reverse drug resistance.

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M/c used : Verapamil.

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Drug Distribution
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Volume of Distribution (Vd) :

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High volume of distribution Low volume of distribution

↑Extravascular concentration. ↑Intravascular concentration.
Systemic circulation Systemic circulation

Tissues Tissues

Formulae :
Apparent Vd (aVd) (Liters) = D = Dose via IV route
C0 Initial PC
Loading dose = aVd x CT (Target PC)

Note : Loading dose ∝ aVd.

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 4 Pharmacology

----- Active space ----- Significance :

Dialysis : Not effective for high Vd drugs.
Drugs with ↑Vd (BAD DOC) Antidote
Benzodiazepine Flumazenil
b-blocker Glucagon
Amphetamines Ammonium chloride
Digoxin Digibind
Opioids Naloxone
Organophosphates Atropine
Calcium channel blockers Calcium gluconate
Plasma Protein Binding :
Proteins :

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Albumin (M/c) Alpha-1-acid glycoprotein

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Binds to acidic drugs Binds to basic drugs

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• Aspirin • Opioids
• Anti-coagulant (Warfarin) 7@ • Tricyclic anti-depressants
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• Anti-epileptics/Anti-psychotics/ • b-blockers
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Anti-depressants • Anti-arrhythmics
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• Antibiotics (Sulfonamides) (Amiodarone/Lidocaine)

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Significance :
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1. Liver cirrhosis :
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↓Albumin production ↓Drug binding ↑Free drug ↑Toxicity.

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2. Nephrotic syndrome/Chronic kidney disease :

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↑Albumin excretion ↑Drug excretion Drug failure.

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3. ↑Alpha-1-acid glycoprotein :
Seen in RA, IBD, MI ↓Free drug Drug failure.
Drug Metabolism 00:45:12

Phase I vs. Phase II Reactions :

Phase I reactions Phase II reactions
Purpose Drug inactivation Make drug water soluble
M/c reaction Oxidation Glucuronidation
M/c enzyme CYP3A4 Glucuronyl transferase (GT)
Note :
• Nomenclature of enzymes :
C Y P 3 A 4
Cytochrome P450 enzymes Gene isoform number
(Heme protein with pigment Family
that absorbs 450 nm light) Sub-family
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 General Pharmacology : Part 1 5

• Crigler-Najjar syndrome : ↓GT ↑Toxicity of Irinotecan (Anti-cancer). ----- Active space -----
Atazanavir (Anti-HIV).
Drug - Enzyme Interaction :

Enzyme inducers Enzyme inhibitors

Effect Cause drug failure Cause drug toxicity
Mnemonic : GRAB PC Mnemonic : QuICK VEG, Disk
• Griseofulvin • Quinidine
• Rifampicin • Isoniazid, Protease inhibitors
• Alcohol (Chronic consumption) • Cimetidine, Chloramphenicol, Ciprofloxacin
Examples
• Benzopyrene • Ketoconazole, Itraconazole, Fluconazole
• Phenytoin, Phenobarbital, • Valproate Erythromycin, Clarithromycin
Primidone • Grapefruit juice
• Carbamazepine, Cigarettes • DEC, Delavirdine, Disulfiram
Important Rifampicin :

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• Erythromycin Theophylline toxicity
drug • OCP failure

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• Clarithromycin Statin toxicity

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interactions • C/I in HIV with TB

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Drugs Metabolised by Plasma Esterase : 7@
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Quick action of plasma esterase Short t1/2 of drugs.

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Examples : Plasma Esterase Can Readily Metabolise Short Acting drugs.

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• Procaine, cocaine. • Mivacurium.

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• Esmolol. • Succinylcholine.
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• Clevidipine. • Acetylcholine.
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• Remifentanil, Remimazolam.
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Drug Excretion 00:54:52

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M/c organ : Kidney (Drug needs to be ionized & water soluble).

(Acidic drug Basic media and vice versa).
Significance :
Drug toxicity :
They promote
• Acidic drugs (Aspirin, Phenobarbital) Alkalinisation of urine with bicarbonate. ionisation of these
drugs:so become
• Basic drugs (Amphetamines) Acidification of urine with ammonium chloride. less absorbable

Mechanisms :
• Filtration : Only free drug excreted.
• Tubular secretion : Free + plasma protein bound drug excreted.

Calculations :
Rate of drug elimination : Amount of drug excreted per unit of time.
Rate = P.C. x clearance (In mg/hr)

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 6 Pharmacology

----- Active space ----- Infusion rate (IR) : Amount of drug to be administered per unit of time.
IR : Rate of drug elimination = P.C. x clearance
Maintenance dose : Dose required to maintain steady state of drug P.C.
MD = P.C. x clearance x time
Half-life :
t1/2 = 0.693 x Vd = 0.693
Clearance Kelimination

Note : Infusion rate & maintenance dose ∝ Clearance.

Order of Kinetics :
Zero order kinetics First order kinetics
Constant amount Constant proportion

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Definition
eliminated per hour eliminated per hour

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• T1/2↑ • T1/2 constant

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Effect of
• Clearance↓ 7@ • Clearance constant
↑sing dose
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• P.C. : Disproportionate↑ • P.C. : Proportionate↑

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Risk of toxicity
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Higher Lower
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on overdosing
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Zero ATP Has Made Weak :

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• Alcohol
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• Theophylline, Tolbutamide
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Examples • Phenytoin Most drugs

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• Heparin
• Methanol
• Warfarin

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 General Pharmacology : Part 2 7

GENERAL PHARMACOLOGY : PART 2 ----- Active space -----

Drug Binds to Receptor Causes Effect.

Factors Affecting Pharmacodynamics :
Affinity :
• Tendency of a drug to bind to its receptor.
• Marker of dose Affinity α 1 .
Dose
Efficacy :

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• Maximum clinical effect produced by a drug (Most important factor).

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• Marker of effect of drug.

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Potency :
• Relative dose of a drug required to produce particular effect. 7@
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• Potency α 1 .
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Dose
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Dose-Response Curve (DRC) 00:05:45

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Graded Curve :
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Response is graded. • Efficacy : Height of curve.

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C C > A > B.
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A HELP
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• Potency : Left shift.

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Response

A > B > C.
B
• Affinity :
Compared only if acting on the same receptor.
- Parallel graphs = Same receptor.
Log (Time)
- A > B.
Individual responses noted.

Quantal Curve :
Effect Toxicity Lethality • Response : Binary (Yes/No) Eg : Sedation.
100% • Population response noted.
population (%)
Response of

• In 50% population, dose required to cause :

50%
- Effect : ED50 (Marker of potency).
- Toxicity : TD50
Marker of toxicity.
ED50 TD50 LD50 - Lethality : LD50
Note : Lethality checked only in animals.
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 8 Pharmacology
LD: Dose at which 50%
of animals die
TD : Dose at which 50 %
----- Active space ----- Therapeutic Index (TI) : mein adverse effects hote h
• Marker of drug safety. ED: dose at which 50% show
effective effects
1. In humans : TI = TD50 / ED50.
TI : Denotes safety and efficacy in
2. In animals : TI = LD50 / ED50. a “POPULATION’
• Significance : Small change in dose Toxicity (Eg : Lithium has ↓TI).
Therapeutic Window/Range : Drugs needing monitoring

More important indicator of toxicity than TI.

Minimum toxic concentration

Plasma conc.

Therapeutic window
Minimum effective concentration

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Time

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Drug Receptor Interaction

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00:20:23

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Intrinsic efficacy graphs :
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Antagonist Full agonist

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-1 Inverse agonist 0 Partial agonist +1

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(Min. effect)
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(Max. effect)
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Full agonist (Maximal effect)

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Partial agonist (Submaximal effect)

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Antagonist (M/c) (No effect)

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Inverse agonist/antagonist (Opposite effect)

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Type of Antagonism :
1. Physical/Pharmacokinetic antagonism :
• Affected by physical binding of antagonist.
• Eg : Charcoal in alcohol toxicity (Adsorbs alcohol Preventing absorption by
intestine).
2. Chemical antagonism :
• Chemical reaction causes antagonism.
• Eg :
- Heparin (Negative charge) - Protamine sulphate (Positive charge).
- Iron - Desferrioxamine (Chelation).
3. Physiological antagonism : 
• Opposite effect caused by binding on different receptors.
• Eg :
- Histamine via H1 Bronchoconstriction.
- Adrenaline via β2 Bronchodilatation.
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 General Pharmacology : Part 2 9

4. Competitive and Non-competitive antagonism : ----- Active space -----

Competitive inhibition Non-competitive inhibition

Response
P P

Graph

Log dose Log dose Log dose

Change in graph Right shift in DRC ↓Height of DRC
• Vmax : Constant • ↓Vmax
• Efficacy : Constant • ↓Efficacy
Change in reaction
• ↑Km • Km : Constant
• • Potency : Constant

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↓Potency

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RECEPTORS

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Type of receptor Sub-types 7@ Examples
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• GABAA
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Ligand gated ion • Glutamate (NMDA, AMPA, Kainate)

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-
channel • Nicotinic
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• 5HT3
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• EGFR • VEGFR
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Tyrosine kinase receptors • Insulin, IGF-1 • Her-2

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• Toll-like receptors
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Serine/threonine kinase receptors TGFR

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Enzymatic
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• Cytokine receptors (Eg : Leptin)

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Janus kinase receptors (JAK) • Prolactin receptor

• Growth hormone receptor
Guanylyl cyclase linked receptor ANP & BNP (Vasodilatation)
• Thyroid • Estrogen
Located in nucleus (TREP) • Retinoic acid • Progesterone
Nuclear • Retinoid X • PPAR
• Mineralocorticoid • Androgen
Located in cytoplasm
• Glucocorticoid • Vitamin D
Note : Insulin & IGF-1 are present in areas of ↑rate of growth.

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 10 Pharmacology

----- Active space ----- G-Protein Coupled Receptors (GPCRs) :

GPCR MOA Examples Drugs
↑αS-GTP
• Salbutamol
+ Adenylate cyclase β2-receptor • Ritodrine

↑cAMP
Gs
Cardiac & Smooth
skeletal muscles muscles β1-receptor • Dobutamine

Contraction Relaxation
↑αq-GTP

+ Phospholipase C

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• Oxytocin

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Gq ↑IP3(2o messenger) α1, M1, M3

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• Angiotensin

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↑Ca2+ production 7@
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Smooth muscle contraction.

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• ↓cAMP
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Gi/o • ↓Ca2+ Relaxation M (Heart)

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2 -
(Inhibitory) • Open K+ channels
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Rho-kinase - :
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• Fasudil Angina
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+ Rho-kinase
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(Vasodilator)
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G12/13 • Netarsudil Glaucoma

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Smooth muscle • Belumosudil Immunosuppression

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contraction (Targets B-cells)

Drug Safety 00:41:50

Pre-clinical trials : Only on animals.

Clinical Trials :
Investigational New Drug (IND) : Drug under trial.
Phases of a clinical trial :
Phase Features studied Target population
• Toxicity • 20 to 100 healthy volunteers
I • Maximum tolerable dose • 1 to 2 years
• Pharmacokinetics, Pharmacodynamics • Open label trial
• Therapeutic exploratory trial/Efficacy trial • 100 to 500 patients
II • Efficacy determined • 2 to 3 years
• Dose range/Dose safety • Randomized Control Trial (RCT)

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 General Pharmacology : Part 2 11

Phase Features studied Target population ----- Active space -----

• 500 to 3000 patients
• Therapeutic confirmatory trial • 3 to 5 years
• Efficacy & safety confirmed • Drug approved by :
III
- CDSCO - India
Drug marketed. - FDA - USA
• RCT/RUCT

• Many thousands of pt.

Post marketing surveillance
IV • No specific duration
(If ADR is rare/long term)
• Open label trial.

Note :
• Phase I & phase II done together for toxic drugs like anti-cancer/anti-HIV.
- Patients are taken up directly.

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- 20 to 100 patients involved.

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• Non-mandatory phase :

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- Phase 0 (Microdosing) : 100 mcg of drug given. 7@
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- Phase V (Pharmacoepidemiology) : Case control study, cohort study etc.

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Adverse Drug Reactions (ADR)

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Types of ADR :
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Mnemonic : ABCDE.
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Type Features Examples

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• Enhanced effect of drug

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A : Attenuated Antihypertensive causing hypotension

• Dose dependent
• Dose independent Drug causing hypersensitivity
B : Bizarre
• Immune mediated (Eg : Penicillin causing rash)
C : Chronic Dose & duration dependent ↑Steroids ↑HPA suppression
Delay in time from exposure Drugs causing teratogenicity
D : Delayed
to ADR (Eg : NTDs d/t valproate)
E : End-of-use/ Opioid withdrawal
D/t stoppage of dose
withdrawal (HTN d/t clonidine withdrawal)

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 12 Pharmacology

----- Active space ----- Pharmacovigilance :

Flow of ADR information
Patient with ADR presents to hospital

ADR treated
Reported to software ‘VIGIFLOW’

National coordinating centre (IPC Ghaziabad)

forms conclusive ADR report

CDSCO (New Delhi) Bans the drug

(To maintain drug safety)
Reports to International Pharmacovigilance Centre
(Sweden-Uppsala)
Vigibase : Largest database of pharmacovigilance (In Sweden).

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Therapeutic Drug Monitoring (TDM) 00:55:00

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Principle : Plasma concentration (PC) correlates to effect/side-effect.
Indications : 7@
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1. Clinical effect not easily quantified.

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2. Drugs having low therapeutic index :

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• Aminoglycosides. • Digoxin.
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• Antiepileptics. • Cyclosporine.
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• Lithium. • Tacrolimus, Tricyclic

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• Theophylline. antidepressants.
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3. Drugs with variable metabolism.

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Eg : Metabolised by acetylation.
Dosage examples :
1. Digoxin :
• 0.5 to 0.9 ng/mL : Therapeutic range.
• >0.9 ng/mL : Effect constant, ↑risk of toxicity.
• >2 ng/mL : Toxicity.
• >1.2 ng/mL : Increased mortality in atrial fibrillation.
2. Lithium :
• 0.6 to 1.0 mEq/L : Mania prophylaxis
Therapeutic range.
• 1.0 to 1.5 mEq/L : Mania treatment
• >1.5 mEq/L : Toxicity.
• >4 mEq/L : Dialysis needed.
3. Theophylline :
• 5 to 15 mg/L : Therapeutic range.
• >15 mg/L : Toxicity.
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 General Pharmacology : Part 2 13

Miscellaneous 00:59:10 ----- Active space -----

Pharmacogenetic Conditions :
ADR caused in certain individuals d/t genetic difference.
1. Acetyl transferase polymorphism Drugs metabolized by acetylation
• NAT 1 gene : Fast acetylators. Mnemonic : HIPS Dance
• NAT 2 gene : Slow acetylators. • Hydralazine. • Sulfonamides.
• Isoniazid. • Dapsone.
2. Malignant hyperthermia : • Procainamide.
D/t lignocaine, halothane, succinylcholine. All can cause drug induced SLE
3. G-6-PD deficiency associated hemolysis : Dr. MANISh
• Dapsone. • Antimalarial : Primaquine >
• Nitrofurantoin. Chloroquine > Quinine.

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• Methylene blue. • Sulfonamides.

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• Isoniazid. • Nalidixic acid.
7@
4. Glucuronyl transferase polymorphism : Causing irinotecan toxicity.
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5. CYP450 enzyme polymorphism :

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• CYP2C19 : Activates clopidogrel.

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• CYP2C9 : Metabolizes warfarin.

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Polymorphism Variable drug effects.

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Antidepressants.
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• CYP2D6 : Metabolizes
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Opioids.
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6. VKORC 1 gene (For Vitamin K oxidoreductase) : Variable metabolism of warfarin.

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7. Succinylcholine associated prolonged apnea (D/t atypical pseudocholinesterase).

8. Thiopurine methyl transferase polymorphism :
Causing toxicity of Azathioprine, 6-mercaptopurine & 6-thioguanine.

Pregnancy Drug Categories :

Drug categories

Safe + Used in pregnancy Teratogenic risk + Teratogenic +

Used in pregnancy Avoided in pregnancy
A > B > C (Benefit > Risk) (Risk > Benefit)

D X
Eg : Valproate Eg : Thalidomide

Note : Schedule X drugs.

• High abuse potential.
• Narcotropics (Amphetamine, ketamine etc).
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 14

----- Active space -----

DRUGS ACTING ON
AUTONOMIC NERVOUS SYSTEM

Regulation of ANS :
Parasympathetic NS Sympathetic NS
Muscarinic (M/c : M3)
Receptor α or β
or nicotinic
Norepinephrine (NE)
Exceptions :
D
Neurotransmitter Acetylcholine (ACh) • Dopamine 1 Renal blood
vessels : Vasodilation (Diuresis)
• ACh in adrenals & sweat glands

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Sweating :

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• Regulated by sympathetic NS.
7@
• Mediated via ACh to muscarinic receptors.
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• Atropine/Datura poisoning blocks M3 ↓ Sweating Hyperthermia.

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Drugs Acting On ACh 00:03:40

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-
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1. Aminoglycosides Presynaptic voltage gated Ca2+ channels ↓ ACh.

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- -
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2. Botulinum toxin ACh release Muscle contraction Respiratory

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paralysis.
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Drugs Acting On NE/Dopamine 00:05:18

VMAT2 inhibitor ↓Dopamine (Used in movement disorders).

• Tetrabenazine : DOC for Tics a/w Tourette syndrome.
Huntington’s chorea.
• Deutetrabenazine, Valbenazine : DOC for Tardive dyskinesia.
(Longer acting)
Parasympathomimetic Parasympatholytic Sympathomimetic Sympatholytic
• ↑Cognition • ↓Cognition β-blocker s/e :
• Donepezil (DOC) • Scopolamine : For • Depression
CNS -
in Alzheimer’s narcoanalysis • Insomnia
disease/dementia (DOC : Thiopentone ) • Nightmares
Pupil Active miosis Passive mydriasis Active mydriasis Passive miosis

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 Drugs Acting on Autonomic Nervous System 15

----- Active space -----

Parasympathomimetic Parasympatholytic Sympathomimetic Sympatholytic

Drugs :
• Tropicamide Drugs :
• Atropine • Phenylephrine
• Homatropine • Ephedrine
• Cyclopentolate
Pilocarpine (DOC) : • Ocular fundus exam. Drugs :
Pupil Closed angle • In uveitis/corneal ulcers
Prevent synechiae • Phenoxybenzamine
glaucoma Ppt • Prazosin
• C/I : Closed angle glaucoma Acute congestive
glaucoma
Cycloplegic function :
• ↓Iridocyclitis pain No cycloplegic function
• Refractive error testing

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↑ ↓ - -

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Glycopyrrolate (Does not

gm
Oro-
pharyngeal Pilocarpine, Cevimeline cross BBB) > Atropine :
7@
For xerostomia As pre-anaesthetic - -
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secretions
(Sjogren syndrome) medication
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(Prevent aspiration)
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Bronchoconstriction Bronchodilatation ( M3 - ) Bronchodilatation ( β2 + ) Bronchocnstriction

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β2 - agonists
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(S/e : Hyperglycemia)
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• SABA
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- Salbutamol
For COPD :
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- Terbutaline
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• Tiotropium - Pirbuterol BA/COPD

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(DOC)
Bronchi LAMA (OD) • LABA
C/I : Bronchial asthma • Umeclidinum - Formeterol -
(BA) & COPD • Revefenacin - Salmeterol
• Aclinidium IAMA (BD) • vLABA
• Ipratropium SAMA - Olodaterol
(QID). COPD
- Vilanterol
only
- Carmoterol
SABA & formoterol are
relievers (Fast acting)
• ↑ HR • ↓ HR
• ↓ HR • ↑ HR
• ↑ AV conduction • ↓ AV conduction
• ↓ AV conduction • ↑ AV conduction
• ↑ Contraction • ↓ Contraction
Heart Atropine (DOC) : Epinephrine : β-blockers (DOC) :
• AV Block • Bradycardia • Atrial fibrillation/
- • Bradycardia (Max 3 mg) (In children) flutter
1 mg 3-5 1 mg 3-5 1 mg • Cardiac arrest • HOCM
min min • Aortic dissection

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 16 Pharmacology

----- Active space -----

Parasympathomimetic Parasympatholytic Sympathomimetic Sympatholytic

↑ HCl secretion ↓HCl secretion Vasoconstriction
Vasodilation (α-blocker)
↑ Contraction ↓Contraction (α-agonist)
Pre-op HTN in
Spinal anaesthesia
Phaeochromoytoma :
induced hypotension :
Pirenzepine, Telenzepine : Phenoxybenzamine
• ↓ HR : Ephedrine
Peptic ulcer disease (DOC)
• Normal HR :
(F/b β-blocker :
Phenylephrine
Prevents arrhythmia)
Phentolamine (1V) : DOC
• Cheese reaction
(MAO - +
Postural hypotension : Cheese/wine)

om
Blood Midodrine (DOC) • Clonidine withdrawal
vessels HTN.

l.c
Bethanecol, Neostigmine :

ai
& GIT • Gastroparesis • Intra-op HTN in

gm
• Post-operative ileus pheochromocytoma
Anti-spasmodics : 7@
54
• Dicyclomine (M/c) HTN with BPH :
t2

Cardiogenic, septic,
• Glycopyrrolate Terazosin, Doxazocin,
ha

neurogenic shock :
ks

• Scopolamine Prazosin
Norepinephrine (DOC)
aa

(DOC : Scorpion bite)

m
ar
sh

Anaphylactic shock :
|

Epinephrine (DOC)
w

• IM route : 0.3 to 0.5 mg β-blockers : HTN in

ro
ar

(1 : 1000 dilution) young age

M

• IV route :
©

↑ Risk for V-fib

Relaxation ( β3 + )
Contraction (M3 + ) Relaxation ( M3 - ) Bladder sphincter : -
Contracts (α1)
Overactive bladder
(Urge incontinence) :
• Fesoterodine
Bladder Bethanechol, Neostigmine : • Darifenacin • Overactive bladder
detrusor • Post-op urinary (Urge incontinence) :
• Oxybutinin M3 Mirabegron (DOC)
retention • Solifenacin selective -
(β3 agonist)
• Bladder atony/ • Tolterodine,
• Stress incontinence :
overflow incontinence. • Trospium ( x BBB)
Duloxetine (SNRI)
S/E : Dementia (Via M1);
• Least in : Darifenaci,
Solifenacin, Trospium
Skeletal
Contraction Relaxation Contraction Relaxation
muscles

Pharmacology revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Autonomic Nervous System 17

----- Active space -----

Parasympathomimetic Parasympatholytic Sympathomimetic Sympatholytic

Edrophonium (DOC) :
• Tensilon test : For Dx of myasthenia
gravis (MG)
• Myasthenic vs. cholinergic crisis (Dx) β2 agonists :
Neostigmine : Dx & Rx of MG NDMR • Tremor : S/e
Skeletal - Cobra bite (NM receptor • Clenbuterol : β-blockers :
muscles - NDMR reversal blocker) : Performance ↓ Exercise tolerance
Pyridostigmine (DOC) : Muscle relaxants enhancer
Mx of MG (Banned)
Pre-medication atropine before
edrophonium/neostigmine :
Prevent muscarinic s/e

om
Side Effects Of Drugs 00:30:30

l.c
ai
gm
Drugs Symptoms Treatment
• Miosis : Pin-point pupil 7@
• Atropine + Pralidoxime :
54

• Salivation, Sweating ↑ OP poisoning

t2

Cholinergic poisoning
• Involuntary urination/defecation • Atropine only :
ha
ks

• Bradycardia Carbamate poisoning

aa

• Mydriasıs
m
ar

• Dry mouth
sh

Anticholinergic poisoning
• Urine retention/constipation Physostigmine
|

(Atropine, Datura)
• Tachycardia
w
ro

• Hyperthermia, dry skin

ar
M

• Bronchospasm
©

• Bradycardia Glucagon
β-blockers • Insomnia, nightmares (Source of cAMP for the
• Blocks hypoglycemia symptoms heart)
• Exercise intolerance
• Postural hypotension
α-blockers • Ejaculation abnormality -
• Floppy iris

Miscellaneous 00:32:33

Cardioselective β-blockers : Mr. BEAN Cardiologist.

• Metaprolol.
• Betaxolol, Bisoprolol.
• Esmolol (Shortest acting).
• Atenolol, Acebutolol.
• Nebivolol Most cardioselective, Antioxidant action + .
• Celiprolol.
Pharmacology revision • v4.0 • Marrow 8.0 • 2024
 18 Pharmacology

----- Active space ----- β-blockers With :

1. α-blockers (vasodilatation) : Carvedilol, Labetalol (M/c).
2. No release : Nebivolol.
3. Calcium channel blocker : Carvedilol.
4. Longest action : Nadolol.

Effect Of Catecholamines On HR :

Isoprenaline (↑↑)
Epinephrine (↑)
HR Dobutamine (Normal)

Norepinephrine (Reflex bradycardia via vagus)

om
l.c
ai
Note : NE with atropine/transplanted heart = ↑↑HR.

gm
7@ Epinephrine Dilution :
Dopamine :
54
t2

Use similar to NE Dilution Route of administration

ha

Dose dependant action :

ks

S/c, IM;
aa

1 : 1000
Continuous IV infusion. Endotracheal
m
ar

1V; Intraosseous,
sh

Dose (mcg/kg/min) Effect (Receptor) 1 : 10,000

Intracardiac (Not used)
|

0-2 Diuresis (D1)

w

1 : 100,000 Local; vasoconstriction

ro

2-10 ↑Contraction of heart (β1)

ar

1 : 100,000 or
M

>10 Vasoconstriction (α1) Local (With lignocaine)

1 : 200,000
©

Blood Pressure Effects 00:38:44

Dale’s phenomenon :
Threshold concentration of epinephrine for α1 > β2.

α1
BP

β2

Biphasic response :
Initial high conc : Drug metabolism Later, low conc :
↑BP (α1 mediated) and excretion ↓ BP (β2 mediated)

Pharmacology revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Autonomic Nervous System 19

Vasomotor reversal of Dale : ----- Active space -----

• Epinephrine + α blocker in living system.
• Only ↓ in BP d/t unopposed β2 action

BP

β2

Vasomotor re-reversal of Dale :

• Epinephrine + β-blocker in living system.

om
• Steep ↑ in BP d/t unopposed α1 action.

l.c
ai
gm
α1
7@
54

BP
t2
ha
ks
aa
m
ar
sh
|
w
ro
ar
M
©

Pharmacology revision • v4.0 • Marrow 8.0 • 2024

 20

----- Active space ----- DRUGS ACTING ON CARDIOVASCULAR SYSTEM :

PART 1

Anti-arrhythmic Drugs 00:00:14

SVT & PSVT

• Arising from atrium.
• Aim : Block AV node (Prevent conduction into ventricles).

Drugs : ABCD
IV drugs : • A : Adenosine

om
Order of

l.c
• Acute attack • B : Beta blocker

ai
preference

gm
• ↓BP • C : CCB (Diltiazem/Verapamil) Oral
• D : Digoxin 7@ (Chronic Mx)
54
t2

Mx :
ha
ks

a. SVT/PSVT :
aa
m
ar
sh

↓BP Normal BP
|
w

(Unstable) (Stable)
ro
ar
M

Cardioversion Carotid massage (↑Vagal )

©

H/o asthma/COPD

Absent Diltiazem/Verapamil

Adenosine (DOC)
• IV rapid push.
• Adults : 6 mg.
• Children : 0.1 mg/kg

Note :
• Adenosine, β blocker : S/e Bronchoconstriction (C/I : Asthma).
• Adenosine : S/e A. fibrillation.
• Digoxin indication : SVT/PSVT + Chronic CHF.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Cardiovascular System : Part 1 21

b. Atrial fibrillation : ----- Active space -----

Acute attack Chronic mx

Cardioversion ± Rate Rhythm

Ibutilide (IV) (Ventricular <100/m) Aim : Block myocardial cells generating AP
Aim : Block AV node
• Na+ channel - : - AP
• β blocker (DOC) • K+ channel - : - repolarization
• CCB (In COPD, asthma) - Amiodarone (DOC)

VENTRICULAR FIBRILLATION & TACHYCARDIA

V. tachycardia : Block myocardial cells.

om
• Na+ channel -

l.c
ai
• K+ channel -

gm
- Amiodarone (DOC) 7@
54
Exception
t2

Digoxin/Ischemia-induced V. tach/V. fib : DOC Lidocaine

ha
ks
aa

V. fibrillation : Defibrillation (TOC).

m
ar
sh

LONG QT SYNDROME
|
w

Can cause Torsades de pointes (Fatal).

ro
ar
M
©

Acute attack Mx Long term mx

(Congenital & acquired)
Congenital Acquired
DOC : MgSO4
• Doc : β blocker Avoid QT prolonging drugs.
• TOC : Pacing (ICD)
WPW SYNDROME
Cause : Anatomical accessory pathway.
• Acute Mx : IV Procainamide.
• Long term Mx :
- DOC : Flecainide (S/E Most arrhythmogenic) .
- TOC : Radiofrequency ablation of accessory pathway.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 22 Pharmacology

----- Active space ----- Drugs in Heart Failure 00:27:30

ACUTE
M/c cause : MI (M/c of LV).

Mx : BNP analogue :
• Nesiritide (IV).
↓LV contraction Pulmonary edema • Metabolized by : N eprilysin (Neutral
endopeptidase).
DOC : IV Dobutamine DOC : Iv Furosemide Neprilysin - : (↑BNP)
(Maintains N HR, • Sacubitril
No ↑O2 demand) Alternative : • Formulation : Sacubitril + Valsartan
No response • Nitroglycerine. • Rx : Chronic CHF
• S/E : Angioedema C/I : ACEI.

om
PDE 3 - : • BNP analogues.

l.c
Milrinone (Inodilator) Omapatrilat :

ai
gm
• NEP - + ACE -
7@ • Not used (Banned).
54
t2

CHRONIC
ha
ks

Drugs : Mx of new case orally :

aa

• For symptomatic Rx: 1st : Furosemide (symptomatic)

m
ar

- Furosemide
sh

x 1 week
|

- Digoxin 2 : ACEI/ARB
nd
w
ro

• To ↓mortality : SHIVA Beta OR

ar
M

- Sacubitril . - Ivabradine. Sacubitril + Valsartan (Preferred)

©

- Spironolactone. - Vericiguat ( ↑cGMP).

- SGLT 2 - (-gliflozines). - ACEI/ARB. 3rd : β blocker (BCMN)
- Hydralazine. - β blocker.
• Bisoprolol • Metoprolol
• Carvedilol • Nebivolol

Hypertension 00:41:50

Mild to Moderate HTN :

<55 yr (Young) ≥55 yr (Old)
• Normal vessel • Calcified, atherosclerotic (Stiff)
Pathology
• ↑Renin • ↓Renin
• DOC : CCB (Amlodipine)
• DOC : ACEI/ARB
Drugs • Diuretics (Thiazides) :
• Beta blocker
Chlorthalidone

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Cardiovascular System : Part 1 23

Mx : ----- Active space -----

<55 y ≥55 y

ACEI/ARB CCB

No response
ACEI/ARB + CCB
No response
Add Diuretics
No response
Resistant hypertension : Resistant to at least 3 classes of drugs with
one being a diuretic.
(Pathology : ↑Aldosterone)

om
Add Spironolactone (DOC)

l.c
ai
Drugs for HTN with co-morbidities (Irrespective of age) :

gm
• DM. 7@
• Migraine.
54

• CKD.
t2

ACEI/ARB • Hyperthyroidism.
ha

• Nephrotic syndrome.
ks

• Stable angina. Beta

• Scleroderma.
aa

• Anxiety disorder. blocker

m

• Osteoporosis Thiazides
ar

• Essential tremor.
sh

• Renal stones/colic ( ↑Ca2+ absorption

|
w

from tubules)
ro

• Raynaud’s disease.
ar
M

• Cyclosporin induced CCBs

©

HTN.
• BPH α - : Prazosin

Severe Hypertension :
Hypertensive emergency Hypertensive urgency
BP ↑ ≥220/125 mmHg
End organ damage + -

IV drugs : HELEN Dance

• Hydralazin • NTG
Oral drugs
• Esmolol • Nitroprusside
• DOC : Clonidine
Drugs • Lasix • DHP
• ACEI/ARB
• Labetalol : - Clevidipine
• CCB
(DOC pregnancy) - Nicardipine (DOC)
• Enalapril

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 24

----- Active space ----- DRUGS ACTING ON CARDIOVASCULAR SYSTEM :

PART 2

Drugs Used in Angina 00:00:06

STABLE & PRINZMETAL ANGINA

Acute angina Rx : S/L NTG (DOC).
Long term Mx :

Stable Prinzmetal
(↓Preload) (Coronary vasospasm)

om
• DOC : CCB

l.c
ai
• Long acting nitrates :

gm
↓Acute attack ↓Mortality S/E Postural hypotension
• CCB 7@
• Statins
54
• Long acting nitrates • Aspirin
t2

• Beta blockers (Best) • ACEi/ARB

ha

• Ivabradine
ks
aa

• Ranolazine
m

• Nicorandil
ar
sh

• Trimetazidine
|
w

Ivabradine : Trimetazidine : (Antimetabolite)

ro
ar

• MOA : - Funny channel/IF current MOA : - Partial FA oxidase (P-Fox)

M
©

- SA node - TG metabolism

↓HR, normal contraction. ↑Glycolysis (Less ATP)

(Bradycardiac drug)
• S/E : ↓Oxygen demand.
- Luminous phenomenon.
Nicorandil :
(Colored halos)
K+ channel opener
- ↑A-fib. Vasodilator
Ranolazine : Fasudil :
• MOA : - Late inward Na+ channel. - Rho-kinase
• S/E :
- ↓Resistance to insulin (↑HbA1c).
- ↓Risk of A-fib.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Cardiovascular System : Part 2 25

Side Effects of Anti-anginal Drugs 00:08:24 ----- Active space -----

Amiodarone :
Mnemonic : Potassium channel blocker makes liver, nerve and skin toxic.
• Pulmonary fibrosis : C/I in ILD; baseline CXR done.
• Corneal microdeposits : Whorl-like, asymptomatic.
• Blue colored skin (Ceruloderma) : Sunscreen.
• Myocarditis.
• Liver toxicity : Baseline LFT done.
• Neuropathy.
• Alpha receptor - causes hypotension.
• Photosensitivity (Brown skin) : Sunscreen.
• Thyroid (Hypo > hyper) : Baseline TFT done.

om
l.c
Note : Anti-arrhythmics

ai
gm
• Longest acting : Amiodarone.
• Shortest acting : Adenosine. 7@
54
t2

Anti-Arrhythmics Causing QT Prolongation/Torsades :

ha
ks

Class Ia :
aa

• Na+ & K+ channel - .

• Quinidine.
m

• Delay in repolarisation
ar

• Procainamide.
sh

& depolarisation.
|

• Disopyramide.
w
ro
ar

Class III :
M
©

• Sotalol.
• Amiodarone.
• Only K+ channel - .
• Dronedarone.
• Delay in repolarisation.
• Dofetilide.
• Ibutilide.
• Vernakalant.

Note : Drugs causing ↑QT.

• Quinidine.
• Quetiapine.
• Methadone.
• Moxifloxacin (Max. QT prolongation among FQs).
• Macrolides.
• Mycobacterial drugs : Bedaquiline, Delamanid.
• Muscarinic (H1 ) receptor - : Aztemizole, Terfenadine.
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 26 Pharmacology

----- Active space ----- DIGOXIN

S/E : C/I :
Mnemonic : DIGOXIN. • Increased risk of toxicity.
• Dialysis, defibrillation C/I. Mnemonic : KMC in Manipal Rocks
• Increases K+. - ↓K+.
• Gynaecomastia. - ↓Mg2+.
• Ocular S/E : Green halos. - ↑Ca2+ (Increase).
• Xanthopsia : Yellow vision. - MI.
• Increases risk of arrhythmia - Renal failure.
(M/c : V. bigeminy). • WPW syndrome :
• Nausea/vomiting AV node - ↑WPW pathway.
• HOCM :
Antidote : Digibind
↑Contraction worsens LV outflow

om
MOA : Blocks Na+/K+/ATPase. tract obstruction.

l.c
ai
gm
RAAS INHIBITORS 7@
ACEi : ARB :
54
t2

• Angioedema Losartan :
ha
ks

(Laryngeal edema Tracheostomy). Mnemonic : PUT

aa

• Dry cough. • PPARr + : ↓insulin resistance.

m
ar

• ↑Uric acid excretion :

sh

DRI :
|

HTN with gout DOC.

w

• Aliskiren.
ro

• Thromboxane A2 - : Antiaggregant.
ar

• Direct renin - .
M

Telmisartan :
©

Max insulin resistance : HTN with DM

DOC
C/I of RAAS - :
• Pregnancy.
• B/L renal artery stenosis.
• Renal failure.

CALCIUM CHANNEL -
• Headache. • Constipation : Verapamil.
• Ankle edema d/t amlodipine. • AV block : Diltiazem/verapamil.

Prevention : + ACEi/ARB C/I with beta blockers

(Causes total conduction block Asystole)

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Cardiovascular System : Part 2 27

Hypolipidemic Drugs 00:26:31 ----- Active space -----

Aims :
1. ↓LDL (In atherosclerotic CVD). 2. ↓TG (To avoid pancreatitis)
• Statins DOC • Fibrates.
Inadequate response • Icosapent.
• Bempedoic acid. • Omega 3 fatty acid.
• Ezetimibe. 3. ↑HDL
• Inclisiran. Niacin : Max ↑HDL
• PCSK-9 - . (Last drug to ↓LDL, VLDL).
• Bile acid binding resins.
• Lomitapide.
STATINS

om
l.c
• Most potent : Pitavastatin > Rosuvastatin

ai
gm
Ceiling effect DOC (Max ↓LDL). 7@
54

• Longest acting : Rosuvastatin > Atorvastatin.

t2
ha

• All metabolized by CYP450 except : Pravastatin .

ks
aa
m

DOC : Protease inhibitors causing dyslipidemia

ar
sh

(Enzyme - Statin toxicity)

|
w
ro

MOA :
ar
M

• Hypolipidemic effect : • Pleiotropic effects : (All except ↓LDL)

©

( - HMG CoA reductase). - Antiaggregant, anticoagulant.

- ↓LDL, VLDL, TG. - Anti-inflammatory, antioxidant.
- ↑HDL, Lipoprotein-A. - ↑NO.
- Plaque stabilization.
Uses : S/E :
• DOC : • Myopathy.
- Type II hyperlipoproteinemia. • Hepatotoxicity.
(Familial hypercholesterolemia). • Insulin resistance.
• Primary & secondary prophylaxis
C/I :
of MI and stroke (ASCVD).
• Pregnancy.
• Night time dosing, except :
• Children :
- Rosuvastatin. Very long
- <10 yrs.
- Atorvastatin. acting.
- <8 yrs (Pravastatin).
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 28 Pharmacology

----- Active space -----

Drugs MOA (Imp) Uses S/E

- ATP citrate lyase :
Bempedoic acid • ↓Cholesterol synthesis. Add on to statins -
• ↓LDL.
Bile acid binding • Hypertriglyceridemia.
• Add on
salts : • Hyperchloremic acidosis.
• Cholestyramine.
- Enterohepatic circulation • Preferred :
• GI upset.
of bile acid : ↓LDL - Pregnancy.
• Colestipol. • ↓Absorption of other drugs.
- Children.
• Colesevelam. • Least with Colesevelam.
PCSK-9 - : Prevent LDLr degradation :
• Evolocumab. • ↓LDL (Max).
• Alirocumab. • ↓Lipoprotein-a. Add on -
↓PCSK-9 synthesis : Is a small interfering RNA

om
Inclisiran. Breaks PCSK-9 mRNA : ↓LDL

l.c
ai
Blocks angiopoietin like

gm
Evinacumab
protein 3 & LPL : ↓LDL, TG.
7@
Familial hypercholesterolemia -
Block MTP (Microsomal
54
Lomitapide
triglyceride transport protein).
t2
ha

Fibrates :
ks

DOC :
• Clofibrate. + PPAR-α, ↑LPL synthesis :
aa

• Hypertriglyceridemia. • Cholelithiasis.
m

• Fenofibrate. • ↓TG, chylomicrons.

• Chylomicronemia • Myopathy.
ar

• Bezafibrate. • ↓VLDL.
sh

syndrome.
• Gemfibrozil.
|
w

• ↓TG rich VLDL synthesis

ro
ar

by liver. • Hypertriglyceridemia.
M

Icosapent -
• - Platelet aggregation • Add on to statins.
©

↓CVS mortality.
Toxicity :
• Hepatotoxicity.
↓Hormone sensitive lipase
Niacin Dyslipidemia with ↓HDL. • Insulin resistance.
synthesis.
• Flushing.
DOC : Aspirin
• - NPC1 L1 receptor
Ezetimibe (Small intestine). Add on to statins. -
• - Cholesterol absorption.

Note : Lipoprotein-A
• ↑ : Statins.
• ↓ : Niacin, PCSK 9 - .

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Cardiovascular System : Part 2 29

Mx : ----- Active space -----

High LDL :

Without clinical ASCVD and LDL <190 With clinical ASCVD or LDL >190

Moderate intensity High intensity

• Rosuvastatin : 5-10 mg • Rosuvastatin : 20-40 mg

• Atorvastatin : 10-20 mg • Atorvastatin : 40-80 mg

Familial hypercholesterolemia :
High dose statins

om
No response

l.c
Add Ezetimibe and/or PCSK-9 -

ai
gm
No response
Add Lomitapide or Evinacumab 7@
54
t2
ha

Hypertriglyceridemia :
ks
aa
m

Risk of ASCVD
ar
sh
|

Absent Present
w
ro
ar
M

Moderate Moderate-severe Statins

©

TG : 150-499 TG : 500-999
Add Icasopent
Lifestyle Fibrates. (↓ses TG & LDL)
TG >500
modification.
Fibrates.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 30

----- Active space ----- DRUGS ACTING ON KIDNEY

Diuretics 00:00:05

MOA & site Uses Side effects

↓K . • +

•
Metabolic acidosis.
• Acetazolamide (DOC) :
Renal stones + .
•
Carbonic Acute mountain sickness.
Blocks carbonic •
Hypersensitivity : Rash,
anhydrase • Acetazolamide/Dichlorphenamide :
anhydrase in PCT. BM suppression.
inhibitors Familial hypokalemic periodic
• NH3↑ : C/I in liver cirrhosis
paralysis.
(D/t ↑ risk of hepatic
encephalopathy).

om
l.c
• Furosemide : DOC for

ai
Loop • Blocks Na -K -2Cl
+ + -
pulmonary edema,

gm
• ↓Ca2+ : Rx of
diuretics pump in thick renal insufficiency.
7@ hypercalcemia
(C/I with ascending limb. • Torsemide : Longest acting.
54
• Ototoxic : C/I with
amino- • Indirect vasodilators : • Bumetanide : Most potent.
t2

aminoglycoside.
ha

glycosides) ↑Prostaglandins. • Ethacrynic acid : Most ototoxic. • ↓K+.

ks

• Most useful drugs when GFR <40. • Metabolic

aa
m

• DOC for : alkalosis.

ar

- HTN with edema. • ↑Uric acid.

sh

• ↑Glucose. • ↑Ca : Rx HTN

2+
- Nephrogenic DI.
|

• Blocks Na -Cl
+ -
with osteoporosis/
w

- Other edema (As add on). • ↓Mg2+.

ro

cotransporter in DCT. renal stones.

• Chlorthalidone
ar

Thiazides : Long acting,

• Direct vasodilators • C/I in HTN with
M

preferred in HTN.
• Open K+ channels. DM/gout (↑Uric
©

• Indapamide : Hepatic excretion.

acid & glucose)
• Metolazone : Effective if GFR <40,
add-on to furosemide
Spironolactone/Eplerenone :
• Spironolactone/
• DOC in resistant HTN & cirrhotic
Potassium Eplerenone : Blocks • ↑K+.
edema (+ Furosemide).
sparing aldosterone. • Metabolic acidosis.
Amiloride (DOC) :
diuretic • Amiloride : Blocks ENaC • Spironolactone : Gynecomastia.
• Lithium induced DI.
in collecting duct.
• Liddle syndrome.
Mannitol (Mnemonic : ABCDE)
• Acute congestive glaucoma. • ↑/↓K+.
Osmotic Solute free water loss : • Braking of diuretics. • ↑/↓Na+.
diuretics PCT & loop. • Cerebral edema. • Pulmonary edema.
• Dialysis dysequilibrium. • C/I in existing renal failure.
• Expected renal failure (Impending).

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Kidney 31

Vasopressin Related Drugs 00:15:00 ----- Active space -----

Drug Uses Side effects

Vasopressin antagonist :
SIADH :
3rd line Vasopressin
• Conivaptan (IV).
antagonists. • Hypokalemia.
• Tolvaptan
Oral. Rx : • Hepatotoxicity (Tolvaptan).
• Mozavaptan
• Free H2O restriction : 1st line.
• Saline infusion : 2nd line.
Vasopressin analogs :
• Vasopressin Not preferred due to ↑toxicity -
• Terlipressin DOC in acute variceal bleed -
• Central DI.
• Nocturnal enuresis.

om
• Desmopressin -
• vW disease ↑vWF.

l.c
ai
• Hemophilia A ↑Factor VIII.

gm
7@
54
t2
ha
ks
aa
m
ar
sh
|
w
ro
ar
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 32

----- Active space ----- DRUGS ACTING ON CENTRAL NERVOUS SYSTEM

Anti-Epileptic Drugs 00:00:10

Epilepsy DOC Valproate

• GTCS MOA :
Valproate
• Myoclonic seizure (JME) • - Ca2+ channel.
Ethosuximide • - Na+ channel.
Absence seizure • - GABA transaminase
(Alternative Valproate)
(↑GABA).
• Partial seizure
Carbamazepine
• Rolandic epilepsy Cannabidiol

om
Mixed seizure syndrome : • Uses : LGS, DS, TS.

l.c
• Lennox Gastaut Syndrome (LGS) Valproate • S/E : Hepatotoxic.

ai
gm
• Dravet Syndrome (DS) • C/I : Children <2 yr.
Seizure in neonates 7@
Phenobarbital
54

Alcohol withdrawal
t2

Lorazepam
ha

Status epilepticus
ks

Infantile spasm with Tuberous

aa

Vigabatrin
m

Sclerosis (TS)
ar
sh

Infantile spasm without TS or

ACTH
|

Salaam spasm (West syndrome)

w
ro
ar

In Pregnancy :
M

Teratogenicity
©

• Min : Levetiracetam (DOC) < Lamotrigine.

• Max : Valproate (A/w neural tube defects).

Mx :
Eg : Female on Valproate

Pregnant Planning pregnancy

Continue valproate Drug free interval

(Changing Withdrawal seizures)
No seizure Seizure
+
Therapeutic drug monitoring
Levetiracetam
+
Folic acid
4000 mcg 400 mcg
H/o NTD in previous pregnancy No h/o NTD

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Central Nervous System 33

Psychiatric Drugs 00:07:52 ----- Active space -----

MANIA
Mania DOC
• Acute mania
Atypical antipsychotic : Aripiprazole
• Mania in pregnancy
• Mania prophylaxis
Lithium
• Bipolar disorder
(Also used to Rx leucopenia)
• Hypnic headache
Rapid cycler
Valproate
(BPD pt. with >4 episodes of mania/depression in 1 yr)
Most teratogenic in BPD Valproate
Least teratogenic in BPD Lamotrigine
Acute mania mx : Aripiprazole + lithium.

om
DEPRESSION

l.c
ai
Withdrawal :

gm
Depression DOC
Depression 1st line : SSRI/SNRI 7@ • Seen with :
54

With insomnia or Mirtazapine - Venlafaxine (SNRI).

t2

erectile dysfunction (NASSA)

ha

- Paroxetine (SSRI).
ks

Mnemonic : Life can end • Not seen with :

aa

• Lithium
m

With suicidal tendency - Fluoxetine (SSRI)

ar

• Clozapine
sh

• ECT (Longest acting : 10d)

|
w

• Vilazodone
ro
ar

• Vortioxetine (MSAA)
M
©

Post partum depression :

Novel antidepressant • Brexanolone :
(Continuous IV 60 hrs)
• Zuranolone : Oral
• Ketamine : Intranasal

Degenerative Disorders  00:15:00

PARKINSONS DISEASE
Mx : Effect of disease on life style

Minimal Significant

1. MAO-B - : 2. - NMDA : 3. No drug <65 yrs ≥65 yrs

Selegeline Amantadine
(DOC) • S/E : D2 agonist Levodopa
- Ankle edema DOC DOC
- Livedo reticularis
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 34 Pharmacology

----- Active space ----- D2 Agonists :

• Oral drugs : • S/E :
- Pramipexole. - Fatigue.
- Ropinirole. - Compulsive sexual activity.
- Rotigotine (Transcranial patch). - Compulsive gambling.
Levodopa :
• With Carbidopa ( - peripheral DOPA decarboxylase).
• C/I : P sychosis (Absolute). • S/E : Mnemonic DOPA
Angle closure glaucoma - Dyskinesis DOC : Amantadine.
(Relative). - Orthostatic hypotension.
• On-off phenomenon : - Psychosis DOC : Pimavanserin.
DOC Entacapone (COMT - ). - Angle closure glaucoma

om
(D/t mydriasis).

l.c
ALS

ai
gm
Management :
7@
• Muscle spasticity.
54
t2

• Drugs (Mnemonic : REST Bed).

ha

- Riluzole (DOC).
ks
aa

- Edaravone.
m

- neurodegeneration.
ar

- Sodium phenylbutyrate taurursodiol (SP-T).

sh

- Tofersen (Only in SOD-1 gene mutation).

|
w

Symptomatic relief.
ro

- Baclofen (GABA B + ).
ar
M

ALZHEIMERS
©

• DOC : Donepezil • New : - β amyloid proteins (Mild disease)

No response - Aducanumab.
Add Memantine (NMDA - ). - Lecanemab.
Never used as monotherapy. - Donanemab.
MISCELLANEOUS
Disorder DOC
Trigeminal neuralgia Carbamazepine
• Post herpetic neuralgia
Pregabalin/gabapentin
• Spinal cord injury
(Use : Peripheral neuropathy)
• Restless leg syndrome
Atypical antipsychotic (Except Clozapine, olanzapine)

Psychosis Another atypical antipsychotic

Typical antipsychotics (Suffix : -zine/-peridol)

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Central Nervous System 35

Disorder DOC ----- Active space -----

ADHD Methylphenidate
ADHD with Tourette syndrome Clonidine
ADHD with family h/o drug abuse Selective NE reuptake - : Atomoxetine, Reboxetine
Tics a/w Tourette syndrome
Tetrabenazine
Huntington’s chorea

Migraine & Sleep Disorders 00:31:30

MIGRAINE
Prophylaxis :
• Propranolol (DOC) .
• Topiramate.

om
l.c
Treatment :

ai
gm
1. 5HT 1B/1D +
7@
Oral : Sumatriptan, Rizatriptan (Fastest oral drug).
54
- (DOC)
t2

S/c : Sumatriptan (Overall fastest).

ha
ks

- C/I : Angina (D/t vasoconstriction).

aa
m

2. Ergotamines :
ar
sh

- Very potent vasoconstrictor Gangrene of organs with end

|

arterial disease.
w
ro

3. New drugs :
ar
M

- 5HT 1F + : Lasmiditan.
©

- CGRP - :
• Eptinezumab.
• Fremanezumab.
• Galcanezumab. S/c for prophylaxis.
- CGRP receptor - :
• Erenumab.
• Olcegepant .
• Rimegepant. Oral for either Rx/prophylaxis.
• Ubrogepant.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 36 Pharmacology

----- Active space ----- SLEEP DISORDERS

Narcolepsy : Modafinil DOC.
Insomnia : DOC

H/o drug abuse/elderly Others

DORA : - wakefulness Z compounds : Ramelteon : Melatonin +

• Suvorexant • Zolpidem
• Daridorexant • Zaleplon Only sleep induction

Sleep induction & maintenance

Opioids 00:40:56

om
l.c
ai
Condition Drug

gm
7@
↓withdrawal symptom : Prevent relapse :
• Methadone • Naltrexone
54
Opioid dependence
t2

• Buprenorphine
ha

• Morphine (DOC) C/I : Head trauma (↑ICP)

ks

Labour analgesia
aa

• Pethidine
m
ar

Opioid induced constipation Methyl naltrexone : DOC

sh

Post-op ileus Alvimopan : DOC

|
w

α2 + :
ro
ar

Post anesthetic chills • Pethidine/meperidine (DOC)

M

• Tramadol
©

Opioid contraindicated in MI Pentazocin

Opioid toxicity Naloxone
Opioid with :
Partial agonist (PA) at μ Buprenorphine
& antagonist at kappa
PA at μ & full agonist at kappa Pentazocine
5-HT & NE reuptake - Tramadol
MAO - Pethidine
Rett syndrome Trofinetide
Fredrich's ataxia Omaveloxolone

Note :
• Constipation.
• Convulsion. No tolerance for these side effects.
• Constriction of pupil (Miosis).
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 Drugs Acting on Central Nervous System 37

Mx of Dependencies 00:45:06 ----- Active space -----

ALCOHOL DEPENDENCE
FDA approved Rx :
a). Anti-craving drugs : b). Aversive Rx :
LFT 3. Disulfiram :
- Aldehyde dehydrogenase
<3 times↑ ≥3 times↑

1. Naltrexone : Doc 2. Acamprosate ↑Acetaldehyde (Toxic)

(Hepatotoxic) (Aversion to alcohol)

Non-FDA approved :
• Anti-craving drugs. • Topiramate.
• Benzodiazepines. • Baclofen.

om
l.c
• Clonidine. • Ondansetron.

ai
gm
SMOKING 7@
First Line :
54
t2

Drugs : Nicotine replacement :

ha
ks

• Bupropion : Anti-depressant. • Nasal spray :

aa

• Varenicline : - Needs prescription (Schedule 4).

m
ar

- Partial agonist at - Most effective.

sh
|

NE receptor (α4β7) • Patch.

w
ro

- Most effective. • Gums. Need alkaline saliva

ar
M

• Lozenge. for absorption

©

Do not drink anything

15 min before usage.
Mx :

Maintainence : ↓break through cravings :

• Varenicline. • Nicotine spray.
• Bupropion. • Gum.
• Nicotine patch. • Lozenge.

Second Line :
• TCA.
• Clonidine.
• Cystine.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 38 Pharmacology

----- Active space ----- Side Effects of CNS Drugs 00:51:56

ANTI - EPILEPTICS
Valproate : (Mnemonic VALPROIC). Carbamezapine : (Mnemonic HEADS).
• Vomiting & nausea. • Hyponatremia :
• Alopecia. - Delayed S/E.
• Liver toxicity. - M/c in elderly.
• Pancreatitis. • Hypersensitivity :
• Rash. - Eosinophilia.
• Obesity : PCOS. - Aplastic anemia.
• Increase ammonia. - Agranulocytosis.
• Carnitine : Antidote for • Ataxia.
hepatotoxicity & hyperammonemia. • Diplopia.

om
• Tab : Tremor, teratogenic max. • SJS : HLA B1502 gene.

l.c
ai
Phenytoin : (Mnemonic HYDANTOIN). Oxcarbazepine/Eslicarbazepine :

gm
• Hirsutism. 7@ • ↓Hypersensitivity.
54
• Hyperplasia of gum. • ↑Hyponatremia.
t2

• Lymphadenopathy.
ha

Lamotrigine :
ks

• Diplopia.
aa

SJS (Rash) : Started at low dose.

m

• ↓Vit D (Hypocalcemia).
ar

Topiramate : (Mnemonic RAM eat less).

sh

• Ataxia Therapeutic drug

• Renal stones.
|

monitoring & adjust dosage.

w
ro

• Nystagmus. • Angle closure glaucoma : Eye

ar
M

• Teratogenic : Facial clefts. examination before starting.

©

• Osteomalacia. • Metabolic acidosis.

• Increased bleeding in Newborn • Weight loss.
(↓Vit K). Use : Obesity.

ANTI - DEPRESSANTS
Drugs S/E
SSRI/SNRI :
• Anxiety • Erectile dysfunction
• Transient anxiety & insomnia Rx :
5-HT2 + • Insomnia • Delayed ejaculation Benzodiazepines (1 month).
SSRI/SNRI • Vivid dreams • Anorgasmia • Secondary use :
5-HT3 + Nausea, vomiting Premature ejaculation.
5-HT4 + Loose stools TCA :
Muscarinic • Constipation, dry mouth • C/I :
TCA - • Urine retention, mydriasis - BPH.
“Pramine”
H1 - Obesity, sedation - Glaucoma.
“Triptaline”
α1 - Postural hypotension • Toxicity : Bicarbonate.
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 Drugs Acting on Central Nervous System 39

Drugs S/E ----- Active space -----

SNRI -
Mirtazapine H1 - Sedation, obesity
Bupropion Seizure, max anxiety
• Cheese reaction
MAO -
• Serotonin syndrome
Trazodone Priapism

MAO - :
• Cheese reaction Rx : IV Phentolamine.
• Serotonin syndrome Rx : Lorazepam Cyproheptadine.

ANTI-PSYCHOTICS
D2 Receptor Block :

om
• EPS. • Min : Clozapine.

l.c
ai
• Hyperprolactinemia. • Zero : Pimavanserin - 5HT2

gm
• Max : Risperidone . 7@
(Only drug not acting on D2).
54
t2

Other Receptors :
ha
ks

Muscarinic :
aa

• Constipation, urine retention. • Mydriasis.

m
ar

• Dry mouth. • Max : Clozapine > Olanzapine.

sh
|
w
ro

H1 : Sedation. Zero S/E (Wt : Neutral)

ar
M

H1 & 5HT : Obesity. Mnemonic “ABCZ”

©

α1 : • Aripiprazole.
• Postural hypotension. • Brexpiprazole.
Partial agonist :
• Metabolic (Dyslipidemia & • Cariprazine.
5HT2 & D2
hyperglycemia). • Ziprasidone.

Clozapine :
• DOC : Resistant schizophrenia.
• S/E : Mnemonic SAMOSA.
- Sialorrhea (Wet pillow). - Obesity.
- Agranulocytosis. - Sedation.
- Myocarditis. - Angle closure glaucoma.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 40 Pharmacology

----- Active space ----- EPS

EPS Symptom Cause DOC

• Beta blockers : DOC
Akathesia: M/C Restlessness Unknown
• Benzodiazepines
Acute dystonia • Abnormal posturing Anticholinergics : DOC
(Earliest) • Facial grimacing • Trihexyphenidyl (Benzhexol)
• D2 -
• Benztropine
• Tremor • Metoclopramide inj.
Parkinsonism • Biperiden
• Bradykinesia Antihistaminics : Promethazine
• Facial dyskinesia :
- Tongue protrusion
Tardive dyskinesia - Lip smacking VMAT-2 - :
D2 upregulation • Valbenazine
(Most late) • Limb dyskinesia :
- Piano finger movement • Deutetrabenazine

om
- Foot tapping

l.c
Neuroleptic • Muscle rigidity • Dantrolene DOC - Ryr

ai
gm
malignant syndrome • Hyperthermia D2 - • Bromocriptine + D2
(Most lethal) • ANS instability 7@ (Most specific drug)
54
t2

Lithium
ha

01:10:50
ks
aa

Side effects : (Mnemonic HOTHEAD)

m
ar

• Hypothyroidism. • Hypercalcemia (↑PTH).

sh

• Obesity. • Ebstein anomaly :

|
w

• Tremor : C/I pregnancy (1st trimester).

ro
ar

- Fine : Normal plasma conc. • Acne.

M
©

- Coarse : Toxicity. • Diabetes insipidus (Thirst).

Interaction :
• Thiazide > K+ sparing diuretic.
• Vomiting, diarrhea. ↓S. Na ↑Li tubular reabsorption.
• Fasting.

Therapeutic drug monitoring:

• Sample taken 12 hrs after last dose + 6th day of Rx.
• Doses (mEq/L) :
- Prophylaxis of mania : 0.6 - 1.
- Acute mania : 1 - 1.5.
- Toxicity : >1.5.
- Dialysis : >4.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Central Nervous System 41

Side Effects of Opioids 01:14:40 ----- Active space -----

μ receptor effects (Mnemonic : MUSCARINE).

• Miosis.
• Urine retention.
• Sedation.
• Constipation, convulsion. Opposite Withdrawal symptoms.
• Analgesia.
• Respiratory depression.
• Increase muscle rigidity.
• No bile flow : Contraction of sphincter of Oddi.
• Euphoria.

om
l.c
ai
gm
7@
54
t2
ha
ks
aa
m
ar
sh
|
w
ro
ar
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 42

----- Active space ----- ANTIBIOTICS : PART 1

Cell wall synthesis - : (Bactericidal) Protein synthesis - : (Bacteriostatic)

• Beta lactams : • Vancomycin • Tetracyclins • Linezolid
- Penicillins (Glycopeptide) • Macrolides • Streptogramin
- Cephalosporin • Bacitracin • Clindamycin • Aminoglycosides (Cidal)
- Carbapenems • Cycloserine
- Monobactams • Fosfomycin

Antibiotics

Acting on cell membrane : (Bactericidal) Fluoroquinolones :

om
• Colistin Ciprofloxacin (Bactericidal)

l.c
• Daptomycin (Lipopeptide)
Antifolate :

ai
gm
• Sulfonamides (Static)
7@
• Cotrimoxazole (Cidal)
54
t2

Severe
Preference : Beta lactams Resistance Vancomycin
ha

Add on :
ks

Infection Aminoglycoside.
aa
m
ar

Cell Wall Synthesis Inhibitors

sh

00:04:32
|
w

1. Fosfomycin :
ro
ar

UDP-G UDP-M.
M

2. Cycloserine :
©

L-alanine D-alanine.
3. Bacitracin :
- bactoprenol phosphorylation.
4. Vancomycin :
- polymerization.
5. Beta-lactams :
- crosslinking.

Cell wall synthesis

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 1 43

BETA - LACTAMS ----- Active space -----

Penicillins :
Drug Use Penicillin resistance :
DOC : Mnemonic SLY GRAM +ve • Mediated by β - lactamases (Penicillinase)
• Streptococcus Penicillinase resistant penicillin (PRPs) :
Benzathine • Syphilis Cloxacillin, Methicillin
penicillin G : • Leptospirosis ( - β-lactamase/penicillinase)
• I/M • Yaws Counteracted by : Altered PBP
• Longest acting • Gas gangrene (Mec-A gene)
(28 days) • Rat bite fever
MRSA
• Actinomycosis
• Meningococcus
Vancomycin DOC
• Respiratory infection ( - d-alanine)
Amoxicillin
• UTI d-alanine d-lactate
Ampicillin Listeria meningitis (DOC) VRSA

om
Piperacillin Pseudomonas

l.c
ai
Daptomycin DOC.

gm
Note : Rationale for regimes in severe infections. 7@
54

Eg : Endocarditis Ampicillin/Vancomycin + Gentamicin (Aminoglycoside).

t2
ha

(Cell wall synthesis - )

ks

CEPHALOSPORINS
aa
m
ar

Drugs Uses
sh

1 gen :
st
|
w

Cefazolin DOC : Surgical prophylaxis

ro
ar

3 gen :
rd
M
©

DOC :
Ceftriaxone • Typhoid
(Paraenteral) • Meningitis (Empirical)
• Gonorrhea
Cefixime Typhoid (Oral DOC)
Ceftazidine Pseudomonas (DOC)
Cefoperazone Pseudomonas
4th gen : Note :
• Pseudomonas • Typhoid • 2nd gen cephalosporins not
• Cefepime • Enterobacter • Meningitis used.
• Cefpirone • ESBL • Gonorrhea
(Extended Spectrum β - lactamase) • Severe pseudomonas Rx :
5th gen Ceftazidine + Gentamicin
• Ceftobiprole • MRSA • Meningitis
• Ceftaroline • Typhoid • Gonorrhea

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 44 Pharmacology

----- Active space ----- CARBAPENEMS

Imipenem :
• Combined with Cilastatin - renal dihydropeptidase (↓imipenem metabolism).
• DOC :
- ESBL. - Acinetobacter.
- Serratia. - Enterobacter.

MISCELLANEOUS
Drug Use
Bacitracin (Ointment) Staph. nasal carriers
Cycloserine Second line TB
Fosfomycin UTI
Note : Last line drugs (Resistance)

om
• Linezolid : VRE.

l.c
ai
• Streptogramin : Reserved for last. Gram positive.

gm
• Daptomycin : VRSA. 7@
54

• Colistin : MDR gram -ve organisms.

t2
ha
ks

Protein Synthesis Inhibitors 00:24:24

aa
m
ar

Drugs Uses Note :

sh
|

Tetracycline Scrub typhus Rx

w
ro

Mnemonic : My Pink RBC.

ar

• Mycoplasma (STD).
M

Doxycycline : Mild-moderate Severe

©

• Plague prophylaxis.
• Least nephrotoxic.
• Rickettsia : Scrub typhus.
• C/I pregnancy & children. Doxycyclin Doxycyclin +
• Borrelia, Brucella.
• Chlamydia, Cholera. Azithromycin
Macrolides
Anaerobic infections
DOC :
Erythromycin • Pertussis.
• Diphtheria. Supra Infra
DOC : diaphragmatic diaphragmatic
• Chlamydia.
• Legionella. Atypical
Clindamycin Metronidazole
Azithromycin • Mycoplasma. pneumonia. +
• Campylobacter.
• Chlamydia, cholera in pregnancy. Gentamicin
• Cholera in children. (If severe)

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 1 45

Drugs Uses ----- Active space -----

• Toxic shock syndrome DOC :

Clindamycin (Cidal drugs ↑toxin release).
• Anaerobes.
• Monotherapy : Gram negative.
Aminoglycoside • Add on for :
As monotherapy, not active against : - Gram positive/negative.
• Anaerobes. - Aerobe/anaerobe.
• Typhoid. • DOC :
• Gram positive organisms. - Tularemia Gentamycin or
- Plague streptomycin

Antifolate drugs 00:35:42

Well concentrated in urine : UTI.

om
l.c
Used against protozoa.

ai
gm
SULFONAMIDE 54
7@
Drugs Uses
t2
ha

Sulfadiazine +
DOC : Toxoplasmosis
ks

Pyrimethamine (Teratogenic)
aa
m

DOC :
ar

Sulfadiazine (Topical) • Burn prophylaxis

sh

• Fungal keratomycosis
|
w
ro

DOC :
ar

Mnemonic : (Cautery PINS)

M

Cotrimoxazole :
• Cystitis • Isospora
©

Trimethoprim +
• Cyclospora • Nocardia
Sulphamethoxazole (1:5 ratio)
• Cepacia burkholderia • Sarcocyst
• Pneumocystis • Stenotrophomonas
Note:
• Toxoplasmosis in pregnancy : Spiramycin.
• Stenotrophomonas Rx : Cotrimoxazole + ticarcillin.
• Cepacia burkholderia Rx :
- Cotrimoxazole.
- Ceftriaxone.
- Carbapenems.
- C/I : Colistin.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 46 Pharmacology

----- Active space ----- Fluoroquinolones 00:39:54

- DNA gyrase.
Well concentrated in urine & stool.
Ciprofloxacin : Respiratory fluoroquinolones :
• DOC : • Gemifloxacin.
- Pyelonephritis (Urine). • Levofloxacin : Max oral bioavailability.
- Traveler’s diarrhea. • Moxifloxacin
- Typhoid carrier. (Stool). - Max t1/2.
- Shigella. - Max mycobacterial activity.
• Contact of meningococcal - Max QT prolongation, seizure.
meningitis. - Max hepatic excretion
(Safe in renal failure; not used in UTI).

om
Note : Regimen for CAP

l.c
Amoxicillin + Azithromycin If penicilin Respiratory Lefamulin.

ai
gm
(G+ & G-) (Atypical org) resistance fluoroquinolones (Last line)
7@
54
t2
ha

Side Effects 00:46:20

ks
aa
m
ar

Drugs S/E & C/I

sh

• S/E : Mnemonic Tetra PACKET

|
w

- Photosensitivity - Kidney : ↑Urine

ro

- Acute renal failure

ar

Tetracyclines Diabetes insipidus

M

- Calcium binding - Esophagitis

©

(↓bone growth) - Teeth : Yellow

• C/I : Pregnancy, children, antacids
• S/E :
- Nephrotoxicity
- Neuromuscular toxicity
- Ototoxicity (Outer hair cell : Irreversible)
Aminoglycosides
Auditory : Vestibular :
Amikacin Streptomycin (+Minocycline)
• C/I : Pregnancy
• S/E : Mnemonic Macro SD Card
- Motilin receptor + : Hypertrophic pyloric stenosis
Erythromycin - Skeletal muscle weakness
(Can be used in pregnancy) - Diarrhea
- Cardiac : QT prolongation
- Cholestatic jaundice

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 1 47

Drugs S/E & C/I ----- Active space -----

• S/E : Mnemonic PQRST

- Photosensitivity
- QT prolongation
Fluoroquinolones
- Rash
- Seizure
- Tendonitis, tendon rupture
• S/E : Mnemonic Bone Marrow
- Bone marrow suppression (Monitor platelets)
Linezolid - MAO -
- Mitochondrial toxicity : Optic neuritis, lactic acidosis
• C/I : Along with Anti-Ca drugs
• S/E :
Beta lactams : - Pseudomembranous colitis
3 gen cephalosporin >
rd
- Hypersensitivity

om
Amoxicillin a. Type 1 : Rash, anaphylaxis

l.c
b. Type 2 : Hemolysis

ai
gm
Beta lactams
Mnemonic : PMT
• S/E :
7@
54
• Cefoperazone
- Disulfiram like reaction
t2

• Cefamandole
ha

- Hypoprothrombinemia (Bleeding)
• Moxalactam
ks
aa

• Cefotetan
m

Imipenam • S/E : Seizures

ar
sh

• S/E : Mnemonic Folic Acid makes RBC

|

- Fetal kernicterus
w
ro

- Acute intermittent porphyria

ar
M

Sulfonamides - Methemoglobinemia (Cyanosis non responsive to O2)

©

- Rash
- Bone marrow suppression
- Crystalluria
• S/E :
- Red man syndrome (Histamine release Flushing)
Vancomycin - Ototoxicity
- Nephrotoxicity : Use Matzke nomogram for dosing, based on
creatinine clearance
Note :
• Staphylococcal nasal carrier : Mupirocin.
• Pseudomembranous colitis : Fidaxomicin.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 48

----- Active space ----- ANTIBIOTICS : PART 2

Non-Retroviral Drugs  00:00:14

Drugs Uses Side effects

Oral Valacyclovir > Acyclovir DOC : HSV/VZV -
Topical Acyclovir Local infections -
IV Acyclovir DOC : HSV encephalitis Crystalluria Renal failure
Oral Valganciclovir > Ganciclovir DOC : CMV retinitis Bone marrow suppression
IV Ganciclovir DOC : CMV pneumonia -

om
Resistant herpes
Foscarnet Electrolyte imbalance

l.c
(Non-responsive to VZV/HSV)

ai
gm
DOC : Recurrent laryngeal
Intralesional Cidofovir -
papillomatosis
7@
54
t2
ha
ks
aa

Disease DOC Other drugs

m
ar

Oseltamivir (Oral)
sh

New drug : Baloxavir :

|

- Neuraminidase
w

Anti-influenza : • - RNA polymerase

ro

A/B/Bird flu Resistance/No response (Endonuclease)

ar

• Inhalational Zanamivir
M

• Only Rx : One dose

• Rx : 5 days; Prophylaxis : 7 days
©

Tenofovir : IFN-α :
• No limited duration • Only 48 weeks (Toxic)
Anti-hepatitis B :
• Avoided in hepatic • Used in hepatic
decompensation decompensation
Direct acting agents (Oral) :
• Sofosbuvir : NS 5B -
Anti-hepatitis C : -
• Velpatasvir : NS 5A -
• Paritaprevir : Protease -
Prophylaxis :
RSV Ribavarin (DOC) • Palivizumab
• Nirsevimab

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 2 49

Antiretroviral Drugs 00:08:06 ----- Active space -----

NRTI NNRTIs
1. Lamivudine Derivatives E mtricitabine (Hence not
used together) :
S/e : Pigmentation of palms
and soles.
2. Tenofovir :
• S/e : Nephrotoxic Nevirapine
• C/I : DOC : Prevent Perinatal HIV
-Renal failure transmission in neonates
-Safety unknown in <10 yrs, <30 kg

Abacavir used
(S/E : SJS a/w HLAB5701)

om
Entry Inhibitors Integrase inhibitors

l.c
ai
gm
• Ibalizumab (IV) : CD4 - (HIV 1)
• Dolutegravir
• Maraviroc : CCR5 - (HIV 1 & 2) 7@ • Elvitegravir
54
• Fostemsavir : Gp 120 - (HIV 1)
• Raltegravir
t2

• Enfuvirtide (S/c) : Gp 41 - (Fusion - )

ha
ks

Protease inhibitor
aa
m
ar

• Used <6 yrs • Atazanavir : No dyslipidemia

sh

• Lopinavir : • Indinavir
|

Used as LPV/r = 90% LPV + 10% Ritonavir S/e : Renal stones

w
ro

• Ritonavir : • Tipranavir
ar

- Most potent enzyme - S/e : Intracranial bleed

M
©

- Used as booster : - Metabolism

- Do not boost : Nelfinavir

Note :
Cobicistat : Used as a booster with Atazanavir, Darunavir, Elvitegravir.
Regimen (Rx & post exposure prophylaxis) :
2 NRTI + Miscellaneous

Tenofovir + Lamivudine + Dolutegravir (TLD Regimen)

If <10yrs/<30kg/Renal failure + <6 yrs

Abacavir LPV/r

Pre-exposure : Tenofovir + Lamivudine.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 50 Pharmacology

----- Active space ----- Antifungal Drugs 00:19:44

Amphotericin-B S/e :
• Hypokalemia : KCl for prevention.
• Nephrotoxic :
- Load pt. with 1-2L NaCl. Drug DOC
- Combined with liposome. • Kala-azar
Amphotericin B
• Mucormycosis
Candidiasis Rx : (IV with 5% dextrose)
• Cryptococcal meningitis
• Oral candidiasis : Clotrimazole. Candida :
• Systemic Echinocandins • Mucocutaneous
• Non-albicans (Caspofungin). Fluconazole infection
(Except oral)
• Recurrent vaginal candidiasis : Azoles
• Albicans
- Oteseconazole (Azole).

om
• Taenia cruris
Itraconazole

l.c
- Ibrexafungerp (- β • Taenia corporis

ai
gm
glucan synthase). Voriconazole Aspergillosis
7@ T. capitis
Mucormycosis :
54
Griseofulvin
(Oral with fatty food)
t2

• Posaconazole.
ha

Natamycin Fungal corneal ulcer

ks

• Isavuconazole.
aa

Terbinafine Onychomycosis
• Amphotericin B.
m
ar
sh
|
w

Antihelminthic Drugs
ro

00:27:06
ar
M
©

DOC : Albendazole Other drugs DOC

• Roundworm • Strongyloides
Ivermectin
• Whipworm Soil transmitted • O. volvulus
Nematodes • Hookworm • Loa loa : DEC
• Enterobius vermicularis • Filariasis : IDA (Ivermectin, DEC, Albendazole)
• Trichinella spiralis • Dracunculus : Metronidazole
• Neurocysticercosis • Intestinal T. solium
• T. saginata
Cestodes 1st drug : Prednisolone (↓edema) Praziquantel
• H. nana
• Echinococcus • D. latum
• Others flukes and schistosoma : Praziquantel
Trematodes -
• Fasciola hepatica : Triclabendazole

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 2 51

Antiprotozoal Drugs 00:30:52 ----- Active space -----

Disease MX

Intestinal Extraintestinal

Amoebiasis Asymptomatic Symptomatic

Paromomycin f/b Metronidazole

(Luminal amoebicide)
Visceral (Kala azar) :
• IV : Liposomal amphotericin B
Leishmaniasis • Oral : Miltefosine DOC : PKADL
Cutaneous :

om
• Na+ Stibogluconate

l.c
African (IV drugs) :

ai
gm
• West African : Oral Fexinidazole (DOC)
Trypanosomiasis 7@
American (Chagas Disease) :
54

• Benznidazole
t2
ha

Cryptosporidiosis Nitazoxanide : - PfoR

ks

Babesiosis Atovaquone + Azithromycin

aa
m

Toxoplasmosis Sulfadiazine + Pyrimethamine

ar
sh

• Giardiasis
|

• Amoebiasis
w

DOC : Metronidazole
ro

• Trichomoniasis
ar

•
M

Bacterial vaginosis
©

MALARIA
Severe Falciparum malaria :
Doc : IV Artesunate (48 hrs)
P. vivax P. falciparum/Resistant P. vivax (ACT)
DOC : Chloroquine x 3 days
+ • Artesunate + Sulfadoxine + pyrimethamine
Uncomplicated malaria Primaquine x 14 days • Artemether + Lumefantrine : North east India
OR • Quinine + Tetra/Doxy/Clindamycin
Tafenoquine x once
Uncomplicated malaria • 1st trimester : Quinine + Clindamycin
Chloroquine
in pregnancy • 2nd trimester : ACT

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 52 Pharmacology

----- Active space ----- Prophylaxis :

Duration of travel

<6 wks ≥6 wks

Doxycyline 100 mg/day Mefloquine 250 mg/week

Start 2 days before Start 2 weeks before

Travel ends
Continue for 4 weeks.
Antitubercular Drugs 00:41:20

FIRST LINE

om
l.c
ai
Isoniazid Rifampicin Pyrazinamide Ethambutol

gm
• Activated by catalase peroxidase
MOA
• - Mycolic acid synthesis
- RNA polymerase 7@ - -
54

Action Cidal Cidal (max) Cidal Static

t2
ha

Target type Replicating Non-replicating/Persisters Replicating

ks
aa

bacteria Intra + Extracellular Intracellular Extracellular

m
ar

Liver (max) Kidney

Excretion Liver Liver
sh

(Safest in RF) (C/I in RF)

|
w
ro

Side effects :
ar
M

Isoniazid (↓Vit B6) Rifampicin Pyrazinamide Ethambutol

©

• ↓GABA : • Red orange secretions/urine • Most hepatotoxic • Optic neuritis

Euphoria, hallucination, (Avoid contact lens) • Hyperuricemia • Red - green
psychosis, neuropathy • Respiratory symptoms • Hip joint pain color blindness
• ↓Haeme : Anemia (Flu-like) with continuous dosing (Arthralgia) (green > red)
• Rx : Vit B6 • Permanently stop :
• Toxicity : Seizure - Purpura (↓ Platelet)
- Pulmonary syndrome
- Rx : IV pyridoxine
- 1 g for 1 g Isoniazid
- Max 5 gm

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Antibiotics : Part 2 53

SECOND LINE DRUGS ----- Active space -----

Bedaquiline Delamanid Pretomanid

MOA - ATP synthase Free-radical production
About Bactericidal, taken with food (↑Absorption)
Side effects QT prolongation (C/I : Arrhythmia) -
• Sequestered in
tissues • 99% Plasma protein bound
Pharmacokinetics • T1/2 : 165 days • Metabolised by albumin -
• Dosing is intermittent : • C/I : Albumin <2.8
3d/week
Note : Ethionamide (S/e : Hypothyroidism).

Antileprosy Drugs 00:54:38

om
1st line :

l.c
ai
• Rifampicin : Most cidal.

gm
• Dapsone : M/c side effect Haemolysis in G6PD deficiency.
7@
54
• Clofazamine side effect Skin pigmentation, ichthyosis.
t2
ha

2nd line :
ks
aa

• Minocycline.
m
ar

• Clarithromycin.
sh

• Fluoroquinolones (Cidal).
|
w
ro

- Moxifloxacin.
ar

- Ofloxacin.
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 54

----- Active space ----- DRUGS ACTING ON ENDOCRINE SYSTEM

Antidiabetic Drugs  00:00:10

BASED ON MOA
↑ Insulin Release :
Can cause hypoglycemia (S/e).
1. Sulfonylureas : Glyburide, Gliclazide.
2. Meglitinides : Repaglinide, Nateglinide.
3. GLP-1 agonists :
Liraglutide (S/c); Semaglutide → DOC for obesity (S/c or oral).

om
4. DPP-4 inhibitors :

l.c
ai
Sitagliptin, Saxagliptin, Linagliptin (Hepatic excretion → Safe in renal failure).

gm
↓ Insulin Resistance : 7@
54
t2

MoA : Stimulation of PPAR-γ (Nuclear receptor)

ha
ks

Drugs : Pioglitazone, Rosiglitazone.

aa
m

Side effects :
ar

• Bladder cancer.
sh

• Retention of Na+ & H2O → Edema, CHF.

|

• Bone : Fractures in females. • Hepatotoxic.

w
ro

↓ Hepatic Glucose Production :

ar
M

Drug : Metformin (Anchor drug for Type 2 DM). Side effects :

©

MoA : Activates AMPK - Gluconeogenesis. • Loose stools (Diarrhea).

Other uses : • Low B12.
• PCOS : for anovulation (But, Doc : Letrozole). • Lactic acidosis.
• Non-alcoholic steatohepatitis (NASH).
↑ Urinary Glucose Excretion :
1. SGLT-2 inhibitors : Canagliflozin, Dapagliflozin, Empagliflozin.
2. SGLT-1 & 2 dual blocker : Sotagliflozin.
Side effects of SGLT-2 blockers :
• ↓ BP • Rare :
(D/t loss of glucose,
• Dehydration Na+ & water in urine) - Diabetic ketoacidosis (DKA).
• Diuretic effect - Bone fractures (No sex
(Can be used in CHF) predeliction).
• ↑Risk of UTI/vaginal candidiasis(D/t glycosuria).

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Endocrine System 55

↓ Glucose Absorption : ----- Active space -----

MOA : α-Glucosidase inhibitor (↓ Starch & disaccharide breakdown).

Drugs : Acarbose, Voglibose, Miglitol.
Side effects : Flatulence (M/c), diarrhoea (D/t undigested starch & disaccharide).

Insulin :
Duration of action Insulin & features Side effect
Shortest & Cough, ↑Risk of lung cancer
Afrezza (Inhalational)
fastest acting (C/I in asthma, COPD)
• Route : S/c
• Use : Post-prandial hyperglycemia
• Regular : Slow acting (60 min before food)
Short acting
• Glulisine

om
• Aspart Fast acting (15 min before food)

l.c
• Lispro

ai
gm
• Route : S/c
7@ • Hypoglycemia
• Use : Maintenance
(↑Risk with short acting)
54

Intermediate acting • NPH (Cloudy white)

t2

• Hypokalemia
• Lente (30% short acting semilente/powder +
ha

• Lipodystrophy
ks

70% long acting ultralente/crystal)

aa

• Route : S/c
m
ar

• Use : Maintenance
sh

• Glargine : W
 hite crystals on combining with other
|

Long acting
w

insulin
ro

• Detemir
ar
M

• Degludec : Longest acting (OD/BD)

©

Insulin Regimen :
1 fast acting (Postprandial ↑glycemia) + 1 long acting (Maintenance).

Amylin Analog :
Drug : Pramlintide
Use : Type I DM and Type II DM (For postprandial hyperglycemia).

Miscellaneous :
Drugs :
• Colesevelam
In Type II DM.
• Bromocriptine

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 56 Pharmacology

----- Active space ----- GnRH Related Drugs 00:18:28

GnRH agonists (M/c) : Goserelin, Buserelin, Nafarelin & Leuprolide.

GnRH antagonists : Ganirelix, Abarelix, Cetrorelix & Elagolix.

Dosing, Uses and Side Effects :

GnRH agonists produce different effects when dosed intermittently vs.
continuously.
GnRH agonists (intermittent) GnRH agonists (Continuous)/GnRH antagonists
MoA ↑ LH/FSH ↓ LH/FSH (↓ Estrogen/Testosterone)
↓ Estrogen ↓ Testosterone
• Infertility (Anovulation/
Uses Oligospermia) • ER +ve breast Ca
• Prostate cancer (DOC)
• Endometrial fibrosis

om
• Delayed puberty • Precocious puberty
• Endometriosis

l.c
ai
gm
• Multiple gestation • Osteoporosis • Osteoporosis
Side 7@
• Ovarian cyst • Vaginal atrophy • Impotence
effects
54

• Ovarian cancer • Hot flashes • Gynecomastia

t2
ha
ks
aa
m
ar

Drugs for Contraception 00:21:52

sh
|
w
ro
ar

Regular contraception Emergency contraception

M
©

Mini pills/POP : Mifepristone : Ulipristal :

• ↑ Cervical mucus viscosity. • Blastocyst detachment. Dose : 30mg x 1 tablet
• ↓ Sperm penetration. • Dose for emergency : within 5 days.
• - Blastocyst implantation. 600mg 1 tab within 3d.
(Not used commonly)

Combined OCP : Levonorgestrel :

Inhibition of ovulation. Dose :
• 0.75 mg x 2 tabs.
(12 h apart within 3 d)
• 1.5 mg x 1 tab (Within 3d).

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Endocrine System 57

Growth Hormone Related Drugs 00:23:30 ----- Active space -----

Classification & drugs Uses Side effects

Mnemonic : CHILDReN
• Carpal tunnel syndrome
• Hyperglycemia
• DOC in dwarfism d/t GH • ICT is raised.
GH analogs :
deficiency • Leukemia
Somatrem/Somatotropin
• ↑Proliferation & growth. • Diabetes
• C/I :
- Retinopathy in DM
- Neoplasia.
GH releasing hormone

om
l.c
(GHRH analog) : • Diagnosis of dwarfism.

ai
gm
• Sermorelin • ↓Abdominal fat of lipodystrophy -
• Macimorelin 7@
in HIV patients (Tesamorelin).
54

• Tesamorelin
t2
ha

• Route : S/c
ks
aa

• DOC for :
m
ar

Somatostatin analogs : - Acromegaly.

sh

• Octreotide - Secretory diarrhea.

|

• Hypothyroidism
w

• Lanreotide - Glucagonoma/VIPoma/
ro

• Gall stones
ar

(long acting) Somatostatinoma.

M
©

• Pasireotide • Other uses :

- Thyrotrope adenoma.
- Acute variceal bleeding.
Drug resistant acromegaly
GH receptor antagonist : ↑Size of pituitary adenoma
Pegvisomant (Monitor : MRI; visual field exam)
(Octreotide/Lanreotide resistant)
Note : Gall stones also caused by fibrates.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 58 Pharmacology

----- Active space ----- Drugs Used in Osteoporosis 00:28:23

Drugs MoA & uses Side effects

↓Bone resorption
Bisphosphonates : • MoA :
• Oral : - - Faresyl pyrophosphate synthase
• Esophagitis (Oral drugs) :
- Alendronate
Prevention : Full glass of water
- Risedronate Induce apoptosis of osteoclasts.
+ empty stomach + avoid lying
• IV - Block ruffled border synthesis.
down (↓Reflux).
- Zolendronate • Uses (DOC) :
• Osteonecrosis of jaw.
(Most potent, - Osteoporosis (Oral preferred)
• Femoral chalk stick fracture
longest acting) Duration : 3y (IV) to 5y (Oral).
(D/t brittleness of bone).
- Panidronate - Paget’s disease/hypercalcemia of

om
l.c
malignancy (IV preferred).

ai
gm
• Osteonecrosis of jaw
Denosumab Blocks RANK Ligand 7@
• Femoral fractures
54
t2

• MOA : Selective Estrogen Receptor

ha
ks

Modulator (SERM). • Hot flashes

aa

Raloxifene
• Indication : Post menopausal osteoporosis • Thrombosis
m
ar

with ↑risk of breast cancer.

sh
|

Calcitonin • MoA : Inhibits resorption. • Liver cancer.

w
ro

(Not preferred) • Use : Paget’s; Prophylaxis of osteoporosis. • Breast cancer.

ar
M

↑Bone formation
©

• MoA : Stimulate osteoblast mediated

• Hypertension.
Teriparatide formation.
• Osteosarcoma ;
(PTH analogue) • Use : Bisphosphonate induced fracture.
C/I in Paget’s disease.
• Duration : Max. 2 yr.
Romosozumab Blocks sclerostin -

Note : Strontium ranelate

• MoA : ↓Bone resorption + ↑Bone formation (Only drug).
• Use : Osteoporosis.
• Not FDA approved.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting on Endocrine System 59

Steroid Hormone Related Drugs 00:35:10 ----- Active space -----

Potency Half-life Uses

DOC for replacement :
Hydrocortisone Glucocorticoids(GC)↑ x 1 8 - 12
• Addison’s disease.
(Similar to cortisol) Mineralocorticoid (MC)↑x 1 hours
• Congenital adrenal hyperplasia (CAH).

Prednisone/ GC↑ x 4
Prednisolone MC↑ x 0.8

GC↑ x 5 12 - 36
Methylprednisolone -
MC↑ x 0.8 hours
• ↓Inflammation

om
• ↓Immunity

l.c
ai
GC↑ x 5

gm
Triamcinolone
MC = 0 7@
54
t2

• Surfactant
ha

Dexamethasone/ GC↑ x 30 36 - 72
ks

Maturation
aa

Betamethasone MC = 0 hours
m

• CAH pregnancy.
ar
sh
|
w

Note : Triamcinolone, Dexamethasone & Betamethasone : Pure glucocorticoids.

ro
ar
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 60 Pharmacology

----- Active space ----- Thyroid Related Drugs 00:41:47

Hyperthyroidism :
MoA Uses Side effects
DOC for :
• Hyperthyroidism in 1st trimester.
Propylthiouracil • Thyroid storm
Hepatotoxic
(Multiple doses) (β-blocker used to prevent A.
Fib).
Inhibits thyroid peroxidase.
Teratogenic :
Carbimazole DOC for Hyperthyroidism : • Choanal/Esophageal
Methimazole (OD) Overall & 2nd & 3rd Trimester. atresia.
• Cutis aplasia.

om
• - Thiol endopeptidase

l.c
ai
Potassium iodide Pre-operative preparation of thy-

gm
Lugol’s iodide - T3, T4 release. roid gland for surgery.
-
• ↓Thyroid size. 7@
54
• ↓Vasculogenesis/Bleeding.
t2
ha

Propranolol
First line in thyroid storm
ks

Propylthiouracil Inhibit peripheral conversion of

aa

Amiodarone T4 to T3.
Propranolol > CCB -
m

(Treatment of A. Fib).
ar

Steroids
sh

• Thyroid cancer. • Secondary cancer.

|

Radioactive iodide
w

Destroy follicular cells (Thyroid • Recurrent Grave’s disease. • Permanent

ro

(I131)
• Hyperthyroidism in elderly.
ar

ablation) by β & γ rays. Hypothyroidism.

(I123 : Used in Imaging)
M

• C/I : In pregnancy
©

Hypothyroidism :
MoA Uses Side effects
• Oral route (On empty stomach,
• Osteoporosis.
30m before food) :
• Atrial fibrillation
- DOC : Replacement.
Levothyroxine T4 salt (Long acting) (↓ Dose used if pre-
- Thyroid cancer (d/t ↓TSH).
existing arrhythmia + ).
• IV route :
• Thyrotoxicosis Symptoms.
- Myxedema coma.
• Oral route :
T3 given and stopped before
radioactive iodine treatment
Liothyronine T3 salt -
TSH ↑I131 uptake.
• IV route : Myxedema coma.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Autacoids 61

AUTACOIDS ----- Active space -----

Anti-Histaminics 00:00:10

H 1 blockers.
First generation Second generation
Crosses (Sedating) : M 1 - effect.
Cross blood- C/I in Children.
Elderly. Does not cross BBB (Non-sedating).
brain barrier
Drivers/pilots.
1. Antihistamine with muscarinic - • Cetirizine

om
effect : Most sedative 2nd gen drugs.
• Levocetirizine

l.c
ai
- Promethazine, diphenhydramine,

gm
and dimenhydrinate. • Astemizole Cause QT prolongation.
- Used in : Acute dystonia, 7@
• Terfenadine
54
Meniere’s disease and motion
• Fexofenadine : Least sedative overall.
t2

sickness.
ha

• Loratadine.
ks

2. Doxylamine : For morning sickness.

aa

Formulated with Vit. B6 • Desloratadine : Most potent.

m
ar

Drugs and ↑GABA (Calming effect). • Rupatadine : Inhibits Platelet Activating

sh

their uses Factor (PAF)

3. Chlorpheniramine : Least sedative.
|

↓inflammation.
w
ro

4. Doxepin : Currently under TCA.

•
ar

Olopatadine
M

5. Cyproheptadine : Currently under • Levocabastine

©

5HT2 - . • Ketotifen Topical anti-histaminics.

6. Hydroxyzine : • Azelastine
- For pruritis. • Astemizole
- Used in non-allergic rhinitis • Azelastine (Nasal spray) : Allergic rhinitis.
(D/t antimuscarinic effect).
• Oral drugs : DOC for urticaria.

Motion Sickness :
1. Scopolamine : Transdermal patch.
• DOC.
• Apply patch night before travel.
• Reapplication : After 2 to 3 days.
2. Promethazine :
• Oral tablet.
• 1 hour before travel.
• Highly sedative.

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 62 Pharmacology

----- Active space ----- Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) 00:07:58

NON-SELECTIVE NSAIDS
Acetaminophen (Paracetamol) :
Use : Analgesic & antipyretic effect.
Side effect :
Hepatotoxic (M/c cause of poisoning worldwide).
• ↑risk in chronic alcoholics/fasting.
• HPE : Centrilobular necrosis + periportal sparing.
• Cause : Metabolite NAPQI Depletes Glutathione.
• Toxic dose :
- 150 - 250 mg/kg or 10 g total : Hepatotoxic.
- >20 g : Fatal.

om
- Treatment of toxicity :

l.c
• DOC : N-acetyl cysteine Blocks NAPQI.

ai
gm
Replenishes glutathione.
7@
• If no response : Fulminant liver failure Emergency liver
54

transplantation.
t2
ha

Aspirin :
ks
aa

Dose dependent effects :

m
ar

• 50 - 325 mg OD : Anti-aggregate.
sh

• 325 - 650 mg SOS : Pain/fever Rx.

|
w
ro

• 3 - 4 g/day (Divided dose) : Anti-inflammatory (Eg. RA).

ar
M

Side effects :
©

• Reye’s syndrome : Hepatic encephalopathy.

- C/I in viral fever in children.
• ↑Uric acid : C/I in gout.
Management of toxicity :
• Bicarbonates (Alkalinize urine ↑excretion).
• If pulmonary edema developed : Dialysis.
Indomethacin :
MOA :
• Inhibits COX.
• Blocks leukocyte migration.
Use :
• DOC for acute gout.
• Closure of patent ductus arteriosus(PDA).
Ibuprofen :
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 Autacoids 63

DOC for closure of PDA in India. ----- Active space -----

Piroxicam :
Long-acting : D/t enterohepatic circulation Used for Chronic pain.
Nimesulide : Ketorolac :
Hepatotoxic : C/I in Children <12 y. Uses Post-operative pain (↑Potency).
Adults : Use > 10 days Eye pain.
SELECTIVE COX-2 INHIBITORS
Features :
• ↓risk of gastric ulcer.
• ↑risk of myocardial infarction (MI) : Not preferred.
Celecoxib, Etoricoxib : Last line for pain & inflammation.

om
Lumiracoxib : Hepatotoxic (Banned).

l.c
Parecoxib : Post-operative pain.

ai
gm
Valdecoxib, Rofecoxib :↑Risk of MI (Banned).
7@
54

Prostaglandin Analogs 00:18:20

t2
ha
ks
aa

Prostaglandin Analog Uses

m
ar

• Abortion (+ Mifepristone)
sh

Misoprostol • NSAID induced gastric ulcer

|

• Maintain patency of DA
w

Prostaglandin E1
ro

• Maintain patency of DA
ar

Alprostadil
M

• Erectile dysfunction
©

• Cervical ripening (DOC)

Prostaglandin E2 Dinoprostone
• PPH
Carboprost PPH
Prostaglandin F2 alpha
Latanoprost/Bimatoprost Open angle glaucoma
• Epoprostenol (Synthetic)
• Iloprost
Prostaglandin I2 • Beraprost Analogs Pulmonary HTN
• Treprostinil
• Selexipag : Receptor agonist
Pulmonary HTN : Rx
Stage II/III :
• Endothelin - : Bosentan, Ambrisentan.
• Alternative : PG I 2 analogues ; PDE 5 - (Sildenafil) ; inhalational NO.
• CCBs may be used only if vasoreactive test + .
Stage IV : Epoprostenol.
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 64 Pharmacology

----- Active space ----- PPH

DOC : Oxytocin.

Disease Modifying Anti-Rheumatoid Drugs (DMARDs) 00:21:40

Conventional DMARDs Biological DMARDs Targeted DMARDs

1. Methotrexate (DOC) : Route : Parenteral Last line drugs :
Anchor drug (D/t universal use) 1. Anakinra : IL 1 - JAK inhibitors
2. Hydroxychloroquine 2. Rituximab: CD 20 - Route : Oral
3. Sulfasalazine 3. TNF - α blockers : Block 1. Baricitinib
4. Cyclophosphamide lymphocyte activity (CAGE) 2. Upadacitinib
5. Immunomodulators - Certolizumab 3. Tofacitinib
- Azathioprine - Adalimumab
- Cyclosporine - Golimumab
- Mycophenolate mofetil - Etanercept

om
- Leflunomide : - Infliximab

l.c
Block pyrimidine synthesis 4. IL-6 - :

ai
( - Dihydroorotate dehydrogenase) • Sarilumab • Tocilizumab

gm
5. CD80/86 - : Abatacept
7@
54
t2

↓Immunity Not given together

ha
ks

Management of RA :
aa

New case of RA
m
ar
sh

Methotrexate (DOC) : ↑adenosine

|
w
ro

Inadequate response (Add)

ar
M

+ MTX :
©

Sulfasalazine or Leflunomide or Biological DMARDs

Triple therapy +
Hydroxychloroquine (HCQ)
Note :
S/e of HCQ :
Corneal deposits (Whorled) & bull’s eye retinopathy Routine eye exam.

Anti-gout Drugs 00:29:34

Acute Gout :
• Aim : ↓Inflammation.
• DOC : Indomethacin.
• Alternative : Colchicine - microtubules - chemotaxis.
Chronic Gout :
• Aim : ↓Uric acid (UA).

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Autacoids 65

Xanthine Oxidase Inhibitors : ----- Active space -----

• MOA : - UA synthesis. • Side effects :
• Drugs : - Xanthine stones.
1. Allopurinol (DOC). - Steven Johnson syndrome (SJS).
2. Oxypurinol (If SJS with Allopurinol). - Acute gout.
3. Febuxostat (Most effective).

Uricosuric drugs :
• MOA : ↑UA excretion.
• Drugs :
1. Sulfinpyrazone
2. Probenecid Monotherapy + add on drugs.
3. Benzbromarone
Effective in renal failure.

om
4. Lesinurad : Only as add-on

l.c
ai
• S/e : Urate stones, acute gout Add indomethacin/colchicine.

gm
Uricase analogs : 7@
54
Pegloticase:
• MOA : Metabolize UA.
t2

UA to Allopurinol
ha

• Drug : Pegloticase (Last line).

ks
aa

• Rasburicase is used to prevent tumor lysis syndrome.

m
ar

Note : Tumor lysis syndrome.

sh

• ↑UA d/t chemotherapy induced cell death.

|
w
ro

• Risk : Solid tumor < leukemia.

ar
M

• DOC : Allopurinol. Rasburicase.

©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 66

----- Active space -----

DRUGS ACTING ON RESPIRATORY SYSTEM, GIT,
BLOOD

Asthma 00:00:10

Histamine : Bronchoconstriction & inflammation.

Drugs Action/Use S/E
• Bronchodilation :
- Adenosine A1 - • Adenosine A1 - :
Methylxanthines : - PDE 3 > 4 - Seizure, arrhythmia,
• Theophylline • Anti-inflammatory : diuresis

om
• Aminophylline - PDE 4 - , ↑IL-10 • PDE 3 - :

l.c
- Histone deacetylase + GIT upset, headache

ai
gm
(Similar to steroids)
ICS : 7@
54
• Fluticasone : Most potent
• Hoarseness of voice
t2

• Ciclesonide • DOC : Persistent BA

ha

Soft steroids (M/c)

• Beclomethasone • TOC : Acute attack (ICS + formoterol)
ks

• Oral candidiasis
aa

- Inactive orally ; activated in the lungs.

m

- ↓risk of oropharyngeal candidiasis

ar
sh

Acute exacerbation of BA :
|

Systemic steroids (Oral/IV) ↑b2 receptor density ↑agonist -

w
ro

in bronchi effect
ar
M

LOX - : Zileuton - -
©

LTC4/D4 - : Montelukast Persistent asthma (Add-on) Hepatotoxic

Mast cell stabilizers :
• Cromolyn sodium - Safest
• Nedocromil
Not effective in atopic
Anti IgE : Omalizumab Severe persistant BA
dermatitis
• Anti IL-5 :
- Reslizumab
- Mepolizumab Severe eosinophilic BA -
• Anti IL-5 R : Benralizumab
• Anti IL-4 R : Dupilumab
Mx of acute asthma attack : New drugs COPD :
• ICS + formoterol. • Roflumilast : PDE4 - .
• Salbutamol 5 min ICS (when taken separately). • Ensifentrine : PDE3 - .
• Salbutamol 1 min Repeat (If >1 puff required).

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting and Respiratory System, GIT and Blood 67

Antitussives 00:06:54 ----- Active space -----

1. Dry Cough :
Centrally acting agents ( - medullary centre) :

Opioids : Non-opioids :
• Dextromethorphan (M/c)
Mild-moderate : Severe (Eg : Bronchial Ca) NMDA - S/E : Hallucinations (↑r/o abuse)
• Codeine • Methadone • Diphenhydramine
• Pholcodine • Morphine • Noscapine
• Hydrocodone • Levopropoxyphene

2. Productive Cough :
1. Expectorant : Guaifenesin.
2. Mucolytics : Liquifies mucous.

om
a. N-acetyl cysteine : Break disulfide bond.

l.c
b. Ambroxol/bromhexine : Depolymerize mucopolysaccharide.

ai
gm
Mx : Syrup Guaifenesin + ambroxol/bromhexine + salbutamol.
 7@
54
t2

Peptic Ulcer Disease 00:10:32

ha
ks

Aim : Ulcer healing ↓HCl secretion.

aa
m
ar

Drugs Uses S/E

sh

DOC :
|

PPI : • GIT upset

w

• PUD
ro

• Omeprazole Esomeprazole • Pneumonia

ar

• GERD • Pseudomembranous colitis

(Isomer; long acting)
M

• ZES • Iron, B12, Ca2+ deficiency

©

• Pantoprazole
• H. pylori
• Lansoprazole Osteoporosis (Hip #)
• Barrett’s esophagus
• Rabeprazole • Hypergastrinemia
(Life long)
Vonoprazan :
• K competitive acid blocker
+

(PCAB) H. pylori -
• Blocks basal + food induced
acid secretion
Cimetidine :
H2 - : DOC : • Females : Galactorrhea (↑prolactin)
• Cimetidine Prophylaxis of aspiration • Males : ( - androgen)
• Ranitidine pneumonia (Post op patients) - Impotence
• Famotidine - Gynaecomastia
NSAID induced gastric ulcer • Diarrhoea
Misoprostol (PGE1 analogue)
(Most specific) • Abdominal cramps
• PUD • Constipation
Sucralfate
• Rectal ulcer • Gastric bezoars

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 68 Pharmacology

----- Active space ----- Drugs Uses S/E

Bismuth subsalicylate/ • H. pylori • Constipation
subcitrate • Traveller’s diarrhea • Black colour stool & tongue
Antacids : Salts of • PUD
• Al (Constipation) • Dyspnea ↓absorption of other drugs
• Mg (Diarrhea) • GERD
Note : With sucralfate.
• Antacid : 30 min after.
• Food : 1 hr before.
• Other drugs : 2 hrs before.
Prokinetics 00:17:50

Use : Gastroparesis.

om
l.c
a. D2 Antagonists :

ai
gm
Also used as anti-emetics.
1. Metoclopramide : 7@
54

- Also 5HT3 - ; 5HT4 + .

t2
ha

- S/E : Acute dystonia (Crosses BBB); hyperprolactinemia.

ks
aa

2. Domperidone : No EPS.
m
ar

b. Other Drugs :
sh
|

• 5HT4 agonists : Mosapride, itopride, prucalopride.

w
ro

• Motilin receptor agonists : Erythromycin, mitemcinal.

ar
M

• CCK 1/A receptor antagonist : Dexloxiglumide.

©

Anti-emetics 00:19:20

Drugs for chemotherapy induced nausea/vomiting :

Group Drugs Other uses :
• Ondansetron (Shortest) • Morning sickness.
5HT3 antagonists (DOC)
• Palonosetron (Longest, most potent) • Post-op vomiting.
• Aprepitant • Radiation induced vomiting.
NK1R antagonists • Rolapitant
• Netupitant
CBR1 agonists • Dronabinol S/E : Hypotension,
(2nd line) • Nabilone blood shot eyes
• Dexamethasone
Other • Metoclopramide
• Olanzapine

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting and Respiratory System, GIT and Blood 69

Laxatives 00:20:47 ----- Active space -----

↑stool softening
↑water in intestine ↑intestinal contraction ↑stool bulk
(Least effective)
1. Bisacodyl, senna, cascara :
- ↑low grade inflammation of 1. Probiotics :
1. Osmotic laxatives :
large intestine ↑contraction Beneficial
- Mannitol
- Effect : After 6-8 hrs (Night microbes 1. Docusate
- 2nd line for constipation
dose) sodium
- Hepatic encephalopathy
- Max 10 days (Short term Rx) - Lactobacillus (Surfactant)
• Polyethylene glycol (PEG)
- Senna : - Saccharomyces
DOC : IBS + constipation
a. Melanosis coli - B. clausii
b. Pink/Yellow brown urine
2. Chloride secretory agents :
- Lubiprostone :
2. Prebiotics :

om
( + Type II chloride
Dietary fibers

l.c
channels) 2. 5HT-4 agonists :

ai
- Linaclotide : 2. Docusate

gm
- Mosapride
( + Guanylate cyclase) - Methylcellulose calcium
- Prucalopride 7@ - Psyllium husk
↑cGMP + CFTR
54

- Bran
t2

3. Tenapanor :
ha

- Na+- proton exchanger

ks
aa
m

Anti-Diarrheal Agents
ar

00:23:48
sh
|
w
ro

Secretory : Non-secretory (For IBS) : Biliary :

ar
M

Octreotide : DOC. • DOC : Loperamide (Opioid) Bile acid binding resins :

©

• 5HT3 antagonist : Alosetron. • Colesevelam.

- In females. • Colestipol.
- S/E : Ischemic colitis. • Cholestyramine.

Blood 00:24:46

ANTI-AGGREGANTS
Drugs Uses S/E
COX-1 inhibitor : Primary prophylaxis :
Bleeding
Aspirin (↓TXA2) MI & stroke
PAR-1 blocker : Primary prophylaxis : Intracranial bleed
Vorapaxar MI (C/I : Stroke/TIA)
GP IIb/IIIa blocker :
• Abciximab • PCI in MI • Bleeding
• Tirofiban • Unstable angina • Thrombocytopenia
• Eptifibatide

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 70 Pharmacology

----- Active space ----- AD/P2Y12 Blockers :

Irreversible : Reversible :
1. Clopidogrel : 1. Cangrelor :
Primary prophylaxis : MI and stroke. - Adenosine analog.
2. Ticlopidine (Toxic) : - IV, short acting.
S/E : Agranulocytosis, TTP-HUS, - Use : PCI in MI.
Thrombocytopenia. 2. Ticagrelor :
3. Prasugrel (Most potent) : - Oral.
- Causes : Intracranial bleed C/I : Stroke/TIA. - Use : Acute coronary syndrome,
- Use : PCI in MI. MI, stroke prophylaxis.

Anti-Coagulants 00:27:21

Drugs Uses Extra

om
Direct Oral AC (DOAC) :
• DVT Rx
• Oral DTI : Dabigatran 1. No monitoring required

l.c
• DOC : DVT prophylaxis

ai
• Oral Xa - : 2. Antidotes :

gm
• DOC : Prophylaxis of thrombosis
- Apixaban • Dabigatran : Idarucizumab
- Edoxaban 7@
in non-valvular atrial fibrilliation
• Oral Xa - : Andexanet alfa
54
(Native valve)
- Rivaroxaban
t2
ha

1. S/E :
ks
aa

• Skin necrosis : Protein C & S↓

m

• Purple toe
ar
sh

Warfarin : - VKOR • DVT Rx & prophylaxis • Teratogenic :

|

• ↓factors 2, 7, 9, 10 • DOC prophylaxis of thrombosis in - Mid facial hypoplasia

w

(First)
ro

(Last) valvular atrial fibrillation - Stippled epiphyseal calcification

ar

• ↓Protein C & S (2nd) (Mechanical valve) - CNS defects

M

2. Antidote :
©

• 4 factor prothrombin complex > FFP

• Vit K
Parenteral DTI (PEDTI) :
• Argatroban : DOC
• Desirudin Heparin induced thrombocytopenia Monitor aPTT
• Bivalirudin
• Lepirudin
Note :

Prophylaxis in A-fib Coagulation monitoring :

Mechanical valve Native valve Not required : Required :

• DOAC UFH, Parenteral DTIs, Warfarin
Warfarin DOAC • LMWH
aPTT PT/INR
Exception • Fondaparinux
Severe mitral stenosis (SA < 1.5 cm2)

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Drugs Acting and Respiratory System, GIT and Blood 71

ANTICOAGULANTS : INDIRECT THROMBIN INHIBITORS ----- Active space -----

UFH LMWH Fondaparinux

• Large size • Smaller • Smallest
• - Xa = IIa • - Xa > IIa • - Xa only
• S/c : Prophylaxis (Low bioavailability)
S/c : Prophylaxis & Rx
• IV : Rx
Single dose
Short acting : Multiple doses
(Removed by macrophages) DOC : Thrombosis, MI, DVT,
pulmonary embolism
Avoid in renal failure
Safe in renal failure
(Excreted unchanged by kidney)
S/E : Mnemonic HOT
• Hyperkalemia, hair loss.

om
• Osteoporosis.

l.c
• Thrombocytopenia (HIT) Risk Max : UFH > LMWH.

ai
gm
Zero : Fondaparinux.
7@
Fibrinolytics 00:37:45
54
t2
ha

t-PA analogues : S/E : Bleeding.

ks

• Alteplase.
aa
m

• Reteplase. Antidotes :
ar
sh

• Tenecteplase (Most specific). • Tranexamic acid (DOC).

|

• e-Aminocaproic acid (EACA).

w

Uses :
ro

• MI (Only STEMI).
ar
M

• Pulmonary embolism.
©

Hematopoetic Agents 00:40:28

Group Drug Uses S/E

• Pure red cell aplasia
• Anemia of CRF
Erythropoiesis : (Most dangerous)
• Epoetin alpha • Anemia by chemotherapy
Erythropoietin • Hypertension
• Darbepoetin (Long acting) • Zidovudine anemia
analogues. • Thrombosis
• Anemia of dialysis
• Iron deficiency
Granulopoiesis : • Lenograstim
1. G-CSF analog • Filgrastim • Neutropenia
• Lipegfilgrastim (DOC : Lipegfilgrastim)
- Long acting Bone pain
• HIV
- Given once during a CT cycle • Chemotherapy
2. GM-CSF analogue Sargramostim

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 72 Pharmacology

----- Active space ----- Group Drug Uses S/E

Thrombopoiesis :
• Oprelvekin Thrombocytopenia by CT
1. IL-11 analog
ITP
• Eltrombopag
2. Thrombopoietin agonist (New drug : Spleen tyrosine
• Romiplostim
kinase - ) Fostamatinib)
-
↓bleeding in liver cirrhosis
• Lusutrombopag
3. Other patients planned for procedures
• Avatrombopag
(Eg : Dental extraction)

om
l.c
ai
gm
7@
54
t2
ha
ks
aa
m
ar
sh
|
w
ro
ar
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 Anti Neoplastic agents and Immunomodulators 73

ANTI NEOPLASTIC DRUGS & ----- Active space -----

IMMUNOMODULATORS

Anti Cancer Drugs  00:00:30

DOC of cancers :
Brain tumor : Temozolomide
Lung Ca : Cisplatin Head & Neck Ca : Cisplatin
Alt : Cetuximab (EGFR - /HER-1 - )
Hepatocellular Ca : Sorafenib Regimen :

om
+ 5-FU
Esophageal Ca Upper GI Ca :

l.c
ai
Gastric Ca Cisplatin

gm
Pancreatic Ca : Gemcitabine 7@
Colorectal Ca (Lower GI) :
54
t2

Folinic acid +
ha

5-Fluorouracil (5-FU) + (FOLFOX/FOLFIRI)

ks

Renal cell Ca : Pembrolizumab

aa

Oxaliplatin/Irinotecan
m
ar
sh

Anal Ca : 5-FU + Mitomycin-C

|
w
ro
ar
M
©

Urogenital Ca (DOC : Cisplatin)

Cancer Add on Rx (for regimen)
Uterine/Ovary Ca Paclitaxel
If relapse Pembrolizumab.
Bladder Ca Gemcitabine
Cervix Ca (Only Cisplatin)
Testicular Ca BEP (Bleomycin + Etoposide + Cisplatin)
Note : Mitomycin-C Prevents laryngo-tracheal stenosis.

Ca Breast :

ER + HER-2 +
Trastuzumab (DOC)
Premenopausal Post-menopausal No response
Neratinib
Tamoxifen Letrozole
Pertuzumab
(Aromatase - )
Lapatinib

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 74 Pharmacology

----- Active space ----- Leukemia :

Acute Chronic

ALL : VPAD regimen AML : CML : CLL :

• Vincristine Cytarabine BCR-ABL Tyrosine kinase - FCR regimen
• Prednisolone + 1st gen : Imatinib (DOC) • Fludarabine
• Asparaginase Daunorubicin/ No response • Cyclophosphamide
• Daunorubicin Idarubicin 2 gen :
nd
• Rituximab
• Dasatinib
Note : • Nilotinib
• Hairy cell leukemia : Cladribine (DOC). • Bosutinib
No response
• Sickle cell disease : Hydroxyurea (DOC). 3 gen : Ponatinib
rd

If T-315 I mutation in enzymatic site

Asciminib : - Allosteric site

om
Omacetaxine : - BCR-ABL protein

l.c
ai
Lymphoma :

gm
7@
54
Hodgkin lymphoma : ABVD regimen Non-Hodgkin lymphoma
t2

• Adriamycin
ha

• Bleomycin Low grade : High grade : R-CHOP regimen

ks

• Vinblastine
aa

FCR regimen • Rituximab

m

• Dacarbazine • Cyclophosphamide
ar

If relapsed • Hydroxydaunorubicin
sh

• Oncovin (Vincristine)
|

Nivolumab
w

• Prednisolone
ro

(Immune checkpoint - )
ar
M

Side Effects of Anti-Cancer Drugs 00:17:25

©

Side-effect Causative drug

SIADH Vincristine
Cerebellar Toxicity (Ataxia, dysarthria) Cytarabine
• Doxorubicin D/t iron-induced free radicals
Cardiotoxicity • Daunorubicin Prevention : Dexrazoxane
• Trastuzumab (Iron-chelation)
Pulmonary fibrosis Bleomycin > Busulfan
Hepatotoxicity Methotrexate
Hemorrhagic cystitis Ifosfamide > Cyclophosphamide (Prevention : MESNA)
Hand & foot syndrome : Bright red discoloration Capecitabine > 5-FU (Prevention : Vitamin B6)
Peripheral neuropathy Vincristine, Cisplatin, Paclitaxel
Diarrhea Irinotecan (Rx : Loperamide)
Flagellate dermatitis (On back) :
Bleomycin
Longitudinal hypopigmented strips
Pharmacology Revision • v4.0 • Marrow 8.0 • 2024
 Anti Neoplastic agents and Immunomodulators 75

MISCELLANEOUS ANTI-CANCER DRUGS ----- Active space -----

Kinase Inhibitors :
1. Imatinib : BCR-ABL TK - (CML). Olaparib : 
2. Gliteritinib : FLT-3 kinase - (AML). • Poly-ADP ribose polymerase (PARP) -
3. Dabrafenib : BRAF - . • For Ca breast.
Melanoma
4. Cobimetinib : MEK 1/2. Bortezomib : 
5. Idelalisib : PI-3 K - . • Proteasome -
6. Ibrutinib : Bruton’s TK - (B-cell Lymphomas). • For multiple myeloma.
Asparaginase : • ↑Risk of herpes infection/reactivation
• For leukemia. (Prevent : Acyclovir).
• S/E : Sonidegib : Hedgehog pathway -
- Hyperglycemia. Retinoic acid (DOC) : Pro-myelocytic leukemia.

om
- Hyperlipidemia.

l.c
Nomenclature of monoclonal antibodies
- Hypercoagulation.

ai
gm
- Hemorrhage. Suffix -mab : Monoclonal antibodies.
7@ Source :
- Hypersensitivity.
54

• -u/-zu-mab : Human.
t2
ha

• -xi-mab : Chimeric.
ks

Immune Check-point Inhibitors :

aa
m
ar
sh

PD-1 - PDL-1 - CTLA4 -

|

• Retifanlimab • Duravalumab Ipilimumab

w
ro

• Nivolumab • Avelumab
ar

• Dostarlimab • Atezolizumab
M

• Cemiplimab
©

• Pembrolizumab

Drugs for Lung Cancer 00:29:40

Non-small cell lung cancer

Based on driver mutation

Absent Present
PDL-1 expression

>50% <50% EGFR mutation ALK mutation

(L858R) (Anaplastic lymphoma kinase)
Immunotherapy Immunotherapy
(Atezolizumab/ + 1st gen : 1st gen : Crizotinib
Pembrolizumab) Chemotherapy Gefitinib/Erlotinib L1196 mutation
Resistance : 2 gen :
nd

T790M mutation Alectinib, Brigatinib, Ceritinib

Non-squamous : Squamous : 3 gen : Osimertinib
rd
G1202R mutations
Cisplatin + Pemetrexed Cisplatin + Paclitaxel
3 gen : Lorlatinib
rd

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 76 Pharmacology

----- Active space ----- Small cell lung cancer :

Cisplatin + Etoposide + Immunotherapy (Atezolizumab/Durvalumab).

Note :
Named trials in NSC Lung Ca :
• Keynote 189 : Chemotherapy + Pembrolizumab.
• Uncheckmate 227 : Ipilimumab + Nivolumab.

Immunomodulators 00:32:40

Immunomodulator MOA & Uses Side Effects

• Common to both (Tacrolimus > Cyclosporine) :
- Nephrotoxicity - HTN
• Calcineurin inhibitors : - Neurotoxicity - Hepatotoxicity
• Cyclosporine

om
↓Transcription of IL-2 in CD4 cells - Hyperkalemia - Hyperglycemia
• Tacrolimus
• 1st line drugs • Cyclosporine only :

l.c
GVHD

ai
- Hirsutism - Hyperplasia of gums

gm
- Hyperlipidemia - Hyperuricemia
7@
• Everolimus
54
m-tor inhibitors Hypokalemia
t2

• Sirolimus
ha

Hepatotoxic, bone marrow suppression

ks

Azathioprine Prodrug of 6-mercaptopurine

aa

(Rarely used)
m

Belatacept CD80/86 inhibitor -

ar
sh

Alemtuzumab CD52 inhibitor -

|
w

Belumosudil Rho kinase - -

ro
ar

• Anti-inflammatory Phocomelia : - Cereblon & tubulin

M
©

• Anti-angiogenic
Thalidomide - Vasculogenesis;↑free radicals
• Anti-neoplastic
• Immunosuppressant - Fetal development (Short limbs)
Block IL-2 receptors/CD25
Basiliximab -
(Prophylaxis of acute graft rejection)
Blocks CD3
Muromonab Cytokine release syndrome
(Rx of acute graft rejection)
Mycophenolate
Block IMP dehydrogenase GIT upset
Mofetil
Blocks dihydro-oratase
Leflunomide BM suppression, hepatotxic
dehydrogenase

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

 om
l.c
ai
gm
7@
54
t2
ha
ks
aa
m
ar
sh
|
w
ro
ar
M
©

Pharmacology Revision • v4.0 • Marrow 8.0 • 2024

©
M
ar
ro
w
|
sh
ar
m
aa
ks
ha
t2
54
7@
gm
ai
l.c
om