GENOMic

By:- Mr. Yogendra Sir

Medical & Nursing Academy, Jaipur

Name:- GAJJU BHAI

Subject:- PHARMA

Batch:- -

Add.- 122, Mohan Nagar, Gopalpura Bypass Road, Near Ridhi Sidhi Circle, Jaipur
Web:- www.genomicacademy.com; Mail:- genomeacademy2021@gmail.com
Contact:- 9829003445, 9829003446, 9829003447, 9829003448, 9829003449

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1. DRUGS AFFECTING BLOOD

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(A) HAEMATINICS –
Blood forming substances indicated in treatment of anemia

1. Iron

Total body iron 2.5 to 5 gram (avg. 3.5 gram)

Ferrous sulphate, Ferrous Gluconet tablet

Iron sucrose injection, Iron Sorbitol injection

USE: - Iron deficiency anemia

Adverse effect- Epigastric Pain, Nausea, Vomiting, Heart Burn, Metallic Taste,
Constipation & Staining of Teeth

Acute iron poisoning- Abdominal Pain, Haematemesis, Diarrhea, Lethargy, Cyanosis,

Dehydration, Acidosis, Convulsion & Shock

Treatment-Desferrioxamine IM/IV

2. Folic acid-(vit.B-9)

Rubifol tab- 5 mg

USE: -magaloblastic anemia

NTD

Mouth ulcer

3. Cynocobalamine (vit.B-12)
Tablet & injection

USE: -Magaloblostic / Pernicious anemia

Neuropathy

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 4. Erythropoietin-
2000-4000 IU/ml SC/IV
promote erythropoiesis
uses-
Anaemia of chronic renal failure
Cancer chemotherapy
To increase blood production pre operative
AIDS patient on Zidovudine

(B) COAGULANT –
Agent that promote blood coagulation

Indicated in hemorrhagic state

Whole blood/plasma provide all factors- best therapy

1. Vit.K(10mg/ml)
Physiological Coagulant

Antidote- oral anticoagulant

USES–

To control bleeding, oral anticoagulant toxicity, dietary deficiency, newborns. Liver

disease, prolonged anti microbial therapy, Obstructive Jaundice

2. Ethamsylate
250-500mg- tab/ inj
Anti hyaluronidase action- improve capillary wall stability

3. Rutin
60 mg tab

4. Anti haemophillic factor

5-10U/kg iv infusion

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5. Fibrinogen
500 mg iv infusion

(C) ANTI COAGULANTS: -

Drugs used to reduce coagulability of blood.

1. In vitro-
Sodium citrate, Sodium oxalate, E.D.T.A.

2. In vivo-
A .Parenteral- Heparin, Enoxaparin sodium

b. Oral Anti Coagulant- Warfarin Sodium, Acenocoumarol, Dicumarol

Phenindione

In vitro-
Sodium citrate- 1.65 g/350 ml blood- Blood transfusion
Sodium edetate- 2mg/ml – Laboratory investigation
Sodium oxalate- 10 mg/ml– Laboratory investigation

In vivo-
A. Parenteral-

Heparin-Natural, HMW, Mucopolysacharide

Mechanism- activate antithrombin-III that bind to active form of factor X, II, IX,
XI, XII, & XIII and inactive them

Onset- Immediate

Duration- 4-6 Hour

1000- 5000 U/ml - IV/SC

Adverse effect- Bleeding, thrombocytopenia, Alopecia, Osteoporosis

Contra indication-bleeding disorder, severe hypertension, chronic alcoholics,

aspirin

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 Anti dote- Protamine sulphate 50 mg/5 ml

Enoxaparin sodium ( LMWH)

(20-40mg)- injection- SC

b. Oral Anti Coagulant-

Warfarin sodium 8-12mg

Acenocoumarol 1-4 mg

Dicumarol 50 mg

Phenindione- 200mg

Onset- Delayed (1-3 Days)

Duration- 3- 6 days

Mechanism- decrease biosynthesis of factor II, VII, IX & X

Adverse effect- Epistaxis, Haematuria, Bleeding in GIT, intra cranial or other

internal

Antidote- Vit. K

USES of anti coagulant-

Deep vein thrombosis & pulmonary Embolism

Myocardial infraction
Unstable angina
Atrial fibrillation
Cerebrovascular disease.
Vascular Surgery & Prosthetic heart valves

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 (D) ANTI PLATELET/ANTI THROMBOTIC –
Drugs that prevent platelets aggregation by interfere platelet function and are useful in
prophylaxix of thromboembolic disorder.

DRUGS-

Aspirin(75 to 150mg),

Clopidogrel(75mg),

Dipyridamole(150- 300mg)

Ticlopidine ( 250 mg)

USES-

Coronary artery disease (Angina &M.I. )

Cerebrovascular disease

Peripheral vascular disease

Venous thromboembolislm

Coronary angioplasty

Stents

Bypass implants

Prosthetic heart valves

(E) TROMBOLYTIC/FIBRINOLYTIC/PLASMINOZEN ACTIVATOR

Drugs that are use to lyse thrombus/ Clot to recanalize occluded blood vessels

Mainly coronary artery

Curative rather than prophylactic

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ACTION-

Convert Plasminogen (inactive) to Plasmin (active) that convert Fibrin (insoluble)/

thrombus to fibrin (soluble)/ dissolution of clot.

DRUGS-

Streptokinase- 7.5-15 lac IU

B-streptococci-C, Antigenic & fever

Urokinase- 2.5- 10 lac IU

Obtain from urine, not antigenic but cause fever

Alteplase (rt-PA) – 50 mg inj

Tenectaplase (rt-PA)

Retaplase (rt-PA)

* rt-PA- Similar to human TPA (tissue plasminogen activator)- prepared from Human
Tissue culture

USES—

Acute M.I – Alternative First line approach to Emergency Percutaneous Coronary

Intervention-thrombolysis favored with in 1-2 hours of onset of MI

Deep vein thrombosis- In leg, Pelvis & Shoulder- up to 60% Treated

Peripheral arterial occlusion-Recanalise 40% limb Artery occlusion ( if uses in 72 hours)

Stroke- Alteplase with in 3 hours

Pulmonary embolism- Indicated for large life threatening pulmonary embolism

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(F) ANTI FIBRINOLYTIC-
Drugs which inhibit plasminogen activation and dissolution of clot

EACA(Epsilon Amino Caproic Acid)

5 gram/20 ml inj

500 mg tab

Tranexaemic Acid

100 mg/ml inj

500 mg tab

Uses-
Overdose of PA

To prevent recurrence of GIT & Subarachnoid haemorrhage

PPH

Abruptio placenta

Menorrhagia

Epistaxis

Peptic ulcer

Occular trauma

Tonsillectomy

Prostate Surgery

(G) HYPOLIDMICS -

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 Drugs that are use to lower down level of lipids &lipoproproteins in blood.

DRUGS-

a. H.M.G. co-a reductase inhibitor-

Atorvastatin(10-40 mg)
Simvastastin(5- 20 mg)
Lovastatin (10- 40 mg)
Rosuvastatin (5- 20 mg)

Decrease cholesterol synthesis

Adverse effect- Headache, Nausea, Bowel upset, Sleep disorder, Myopathy.

b. Fibric acid derivative

fenofibrate(200mg)
Gemfibrozil (300 MG)
Increase activity of lipoprotein lipase- increase destruction of VLDL
Adverse effect- Skin rashes, Body ache, Myopathy

c. Resins-
Cholestyramine (4-16 g)
Decrease cholesterol by decrease bile acid absorption

d. Niacin (B3)-
Nicotinic acid(2-6 g)
Decrease production of VLDL
Adverse effect- cuteneous vasodilation, flushing & itching

e. Other-
Ezetimibe (10 mg)
Decrease cholesterol absorption

USES-

As Antihyperlipidmics (coronary artery disease)

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(H) PLASMA VOLUME EXPANDERS
Drugs that are use to expand plasma volume by retain fluid in vascular
compartment through exerting osmotic pressure.

• Human Plasma
• Human albumin (20% solution 100 ml)
• Degraded gelatin polymer (3.5 % in 500 ml)
• H.E.S (Hydroxy ethyl starch) (6% Solution)
• P.V.P (Poly vinyl pyrrolidone) (3.5% solution) – not prefer
• Dextran- 40 & 70

*Human plasma & Human Albumin- Natural- Best option- But not preferred as PVE due to high
coast

*All other PVE- Also Known as Synthetic colloids

USES-

PVE use in such conditions where plasma Volume deficient or lost like-
Burn, hypovolemic &endtoxin shock, severe trauma, extensive tissue damage.

Temporary use in whole blood loss till blood arrange.

CONTRA INDICATION-

Severe anemia, Cardiac failure, renal insufficiency, pulmonary edema.

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2. GASTROINTESTINAL DRUGS

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(A) EMETICS-
Drugs use to induce vomiting.

DRUGS-

Ipecacunha (Emetine)

Syrup- adult – 15- 30 ml, children- 10 -15 ml

Irritate GIT mucosa & CTZ- Vomiting

Onset- 15 min

Apomorphine –injection

6mg- SC/IM

Stimulate C.T.Z.- Vomiting (Within 5 minutes).

USES-

Induction of vomiting when undesirable ( toxic/overdose ) ingested.

CONTRA INDICATION-

Morphine poisoning, Corrosive material, C.N.S stimulant, Unconscious patient & Kerosene
poisoning

(B) ANTI EMETICS-

Drugs that are use to prevent or suppress vomiting.

DRUGS-

1. Anticholinergics-Hyoscine, Dicyclomine

2. Antihistaminics-Diphenhydramine, Promethazine, Cinnarizine, Cyclizine, Meclozine,

Doxylamine

3.5-HT3 antagonist-Ondensetron, Grainesetron

4. Gastro Kinetic(prokinetic)-Metaclopramide, Domperidone, cisapride, mosapride

5. Neuroleptic-Prochloperazine, chlorpromazine

6. Adjuvant antiemetics- Dexamethasone, Benzodiazepines, Cannabinoids

Anticholinergic-

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Hyoscine

0.2- 0.4 mg- ORAL/IM

DOC- Motion sickness

Antihistaminics- Safer & Prefer For long term use

Promethazine (highly sedative) 25mg tab

Cinnarizine (Anti vertigo) 25- 75 mg

Cyclizine (50 mg) Meclozine (25 mg)- Sea sickness

Doxylamine (10 mg) use along with Pyridoxine in morning sickness

5- HT3 antagonist- Chemotherapy induce vomiting.

Ondensetron- 2mg/ml- inj, 4-8 mg tab

Grainesetron-1mg/ml-inj, 1-2 mg tab

Adverse effect- Headache, Abdominal discomfort

GastroKinetic (prokinetic) - Speeden Gastric emptying.

Metaclopramide(Reglan)

10 mg tab/ inj

Adverse effect-sedation, dizziness, loose stools, Muscle Dystonias

On long term use- Parkinsonism, Galactorrhoea and Gynaecomastia

Domperidone 10-30 mg tab 10 mg/ml drop

Cisapride 10- 20 mg

Mosapride 5 mg tab

Neuroleptic-vertigo associated vomiting

Prochloperazine (stemetil) 5-25 mg tab, 12.5 mg/ml inj

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Adverse effect- Muscle dystonia & EPD

Adjuvant antiemetics-

Dexamethasone 8- 20 mg IV

Benzodiazepines- Diazepam

Cannabinoids- Tetrahydrocannabinol- Dronabinol & Nabilone

(C) DRUGS FOR PEPTIC ULCER-

Peptic ulcer-Occurs in the part of GIT which is exposed to HCl and pepsin
DRUGS-

1. Reduction of gastric acid secretion-

a. H2 –blocker- Ranitidine, Famotidine, Roxatidine

b. Proton pump inhibitor– Omeprazole, Pantaprazole, Rabemeprazole, Esomeprazole,

Lansaprazole

c. Anticholinergic-Propanthaline

2. Neutral Gastric acid (Antaacids)-

Systemic-Sodium bicarbonate

Non systemic- Magnisium hydroxide, Calcium carbonate,Aluminium hydroxidegel

3. .Ulcer protective–

Sucralfate, colloidal bismuth subcitrate

4. Anti H-pylori drugs-

Amoxycillin, Metronidazole,Tinidazole, Clarithromycin, Tetracycline

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1. Reduction of gastric acid secretion-
a. H2 –blocker-

Ranitidine 150- 300 mg

Famotidine 20-40 mg

Roxatidine 75- 150 mg

Advesrse effect- Headache, Diziness

Uses-

Duodenal ulcer – 8 Weeks- 70 to 95%

Gastric ulcer- 8 Weeks – 50 to 75 %

Stress ulcer

Zollinger-Ellinson Syndrome

GERD

Prophylaxis of aspiration Pneumonia

b. Proton pump inhibitor–

Omeprazole 20- 40 mg

Pantaprazole 40 mg

Rabemeprazole 10 -20 mg

Lansaprazole 15-30 mg

Esomeprazole 20- 40 mg

Adverse effects- loose stools, Abdominal pain, Muscle & joint pain &Diziness

Uses-

Duodenal ulcer – 2 to 4 Weeks

Gastric ulcer- 4 to 8 Weeks

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 Stress ulcer

Zollinger-Ellinson Syndrome

GERD

Prophylaxis of aspiration Pneumonia

Neutral Gastric acid (Antaacids)-

Sodium bicarbonate- Systemic action

Magnisium hydroxide- fast action- laxative nature

Aluminium hydroxidegel- Slow action- Constipation nature & decrease phosphate absorption

Calcium carbonate- Potent & Rapidly acting

Megaldrate (hyroxy magnesium aluminate)

3. .Ulcer protective– Sucralfate—

protective coating on ulcer10 ml TDS

Colloidal Bismuth Subcitrate- Increase Mucous, Coating & anti H.pylori action

120 mg tab

4. Anti H-pylori drugs-

H-pylori bacteria( gram- bacilli) produces ulcer&anti H-pylori drugs kill H-pylori bacteria.

Amoxycillin, Metronidazole,Tinidazole, Clarithromycin, Tetracycline

(D) DRUGS FOR CONSTIPATION

(Laxatives/ Purgatives/Cathartics)
Drugs that promote evacuation of bowel

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Laxative or aperients- milder action soft and formed stools
Purgative or cathartics- strong action more fluid evacuation
Constipation- Infrequent production of hard stools requiring straining to pass or sense of
incomplete evacuation.

DRUGS-

1. Bulk luxative-Isapghulla Methyl cellulose, Dietary fibre; Bran

2. Stimulant purgative- Bisacodyl, Senna, Sodium picosulphate, Castor oil, Tegaserod

3. Stool softner- Docusates, Liquid parafin

4. Osomotic purgative- Lactulose

Bulk luxative- Increases stoolswater content & bulk

Isapghulla- Psyllium- Natural colloidal mucilage- Absorb water- Gelatinous mas

3-12 gram

Methyl cellulose 4-6 gram semisynthetic, colloidal, derivative of cellulose

Dietary fibre; Bran- Unabsorbed cell wall & cellulose, pectins, glycoproteins

Stimulant purgative- irritates GIT mucosa- increase intestinal motility- promote evacuation of
bowel

Bisacodyl 5 mg

Senna- Cassia

Sodium picosulphate 5mg/5ml

Castor oil 15-25 ml

Tegaserod 6mg tab
Stool softner-

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 Docusates- emulsify colonic content.
100- 400mg
Liquid parafin- by lubricant action.
15- 30 ml
5. Osomotic purgative-Retains water osmotically in intestine

Lactulose

Uses of Purgative-

a. Functional constipation-

Spastic- Dietary fibre or Bulk laxative

Atonic- Bulk forming, Senna, Bisacodyl

b. Bedridden patient- MI, Stroke, Fracture, post operative

Lactulose, Bisacodyl

c. To avoid straining at stools- Hernia, CVD, Eye surgery

Bulk forming, Lactulose

d. preparation of bowel for surgery-

Saline purgative, Bisacodyl

e. Food/drug poisoning-
Saline purgative

Laxative CI
in undiagnosed abdominal pain, colic or vomiting
Secondary constipation due obstruction in Bowel, hypothyroidism, Hypercalcaemia, malignancies
and drugs like- Opiates, Sedative, Anticholinergics, Antiparkinson, Antidepressant,
Antihistaminic oral Iron and laxative abuse.

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(E) TREATMENT OF DIARROHEA
Passage out of to frequent unformed (poorly formed) watery stools.

Management of diarrhoea-
1. Treatment of fluid depletion, shock & acidosis
2. Drug therapy
3. Maintenance of Nutrition

1. Maintenance of water electrolyte balance (rehydration) - Treatment of fluid depletion, shock

&acidosis

a. O.R.T. (oral rehydration therapy)- Mild (5-7%) to moderate (7.5-10% BW)

b. I.V.R.T. (intra venous rehydration therapy)- Severe (>10 % BW)

2. Drug therapy-

a. Non specific anti diarroheal-

Absorbant- Isapghulla

Anti secretory-

Sulfasalazine 500 mg

Mesalazine 400 mg

Atropine

Racecadotril 100 mg

Antimotility drugs (opoids)-

Loperamide- Opiate analogue

CI below 4 year child

Dipnenoxylate- Synthetic opoid

CI below 6 year child

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b. Specific Antimicrobial drugs-G.I.T. infection associated diarrhoea
Norfloxacin
Ciprofloxacin
Ofloxacin
Metronidazole
Tinidazole
Ornidazole

3. Maintenance of Nutrition- Breast milk, Boiled potato, Banana

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3.RESPIRATORY SYSTEM DRUGS

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(A) DRUGS FOR COUGH
Cough-protective reflux

It is of two types:-

Useful- productive/wet cough

Useless- non productive/dry cough

DRUGS-

(I) Pharyngeal demulcents-

Sooth the throat- symptomatic relief from cough.

Ex-lozenges, glycerine, cough drops.

(II) Expectorants (mucokinetics)-

Expel out cough

By increase bronchial secretion or reduce its viscosity- facilitate its removal by coughing

Useful in productive (wet) cough

a. Bronchial secretion enhancer-

Sodium orPotasium citrate, Potassium iodide,Vasaka,Guainphenesin, Ammonium
chloride
b. Mucolytic-
Bromhexine, Ambroxol, Acetyl Cysteine

(III) Antitussives (cough centre suppressants)-

Useful in non-productive (dry cough) or use to suppress over coughing in wet cough also

a. Opoids-
Codeine, Pholcodeine
b. Nonopoids-
Dextromethorphan, Noscapine

c. Antihistaminics-

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 Promethazine, Chlorpeniramine, Diphenhydramine.

(IV) Adjuvant antitussive (bronchiodilatar) -

Ex- Salbutamol, Terbutaline

(B)DRUGS FOR BRONCHIAL ASTHMA-

BRONCHIAL ASTHMA-

Narrowing of air tube (bronchoconstriction), increase Bronchial secretion & mucosal edema

resulting in congestion of respiratory air way that leads to difficulty in breathing (Dyspnoea),

Wheezing & cough.

Bronchial Asthma- Inflammatory condition

COPD- progressive disease with emphysema and bronchial fibrosis

Approaches to treatment-

Prevention of AG:AB

Neutralization of IgE

Suppression of inflammation & bronchial hyperactivity

Prevention of release of mediators

Antagonism of released mediators

Antagonism of constrictor neurotransmitter

Agonism of dilator neurotransmitter

Directlyacting bronchodilator

1. Bronchodilators-

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 A. Sympathomimetics(B2-agonist)-

Ex- Salbutamol, Terbutalin, Salmeterol, Formeterol

B.Anti cholinergic(m3 antagonist).-

Ex-Atropine methonitrate, Ipratropium bormide

C. Methyl xanthines-

Ex-Theophyline, Aminophyline, Doxophyline

2. Corticosteroid-

Decrease bronchial hyperactivity & inflammation

Ex-Hydrocortisone 100 mg- IV

Fluticasone 50-100 mcg

Budesonide 100-400 mcg

Beclomethasone 50-200 mcg

3. Monoclonal antibody-

Omlizumab- SC/IV

4. Leukotriene antagonist-

Ex- Monteleukast, Zafirleukast

5. Mast cell stabilizer-

Sodium chromoglycate 1mg MDI

Ketotifen 1-2 mg tab

Add. – H1 blocker also

Mild episodic asthma- B2 agonist

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Seasonal Asthma- inhaled steroid and B2 agonist

Mild chronic Asthma- inhaled steroid and B2 agonist

Moderate Asthma- inhaled steroid and B2 agonist

Severe asthma- Inhaled steroid + B2 agonist + Oral LT antagonist/Theophyline

Status Asthmaticus- Hydrocortisone –IV & Salbutamol nebulization

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4.DRUGS ACTING ON C.N.S

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 (A) SEDATIVES & HYPNOTICS

Sedatives- Calm down body but do not induce sleep.

Hypnotics- Induce & maintain sleep.
Both depress C.N.S on Low dose- Sedative & on high dose-hypnotic

DRUGS-
1. Barbitutates-

( a)Long acting - Phenobarbitone

(b) Short acting- Pentobarbitone

(c) Ultra short acting- Thiopentone sodium

2. benzodiazepines-.

Ex- Diazepam Alprazolam, Clonazepam, Lorazepam, Nitrazepam, Clobazam,

Chlordiazepoxide, Flurazepam

3. Newer nonbenzodizepine hypnotics-

Ex- Zopiclone, Zolpidem, Zaleplon

Barbitutates- Having low therapeutic index so higher toxicicity.

( a)Long acting - Phenobarbitone- anti epileptic

(b) Short acting- Pentobarbitone

(c) Ultra short acting- Thiopentone sodium- General anaesthetic

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Benzodiazepines- Having higher therapeutic index lesser toxicity a specific antagonist also develop

(flumazenil) that can be use on over dose so they are more safer than barbiturates.

Ex- Diazepam Alprazolam, Clonazepam, Lorazepam, Nitrazepam, Clobazam,

Chlordiazepoxide, Flurazepam

USES-
Anti Anxiety, Muscle Relaxant, Sedative, Hypnotic, Anti Convulsant, General Anaesthetic.

Newer nonbenzodizepine hypnotics-

Ex- Zopiclone, Zolpidem, Zaleplon

B. ANTI PARKINSONIAN DRUGS

Drugs that have therapeutic effect in Parkinsonism.

Parkinson disease-Extrapyrimidalmotor disorder Characterized by Rigidity, Tremor, Hypokinesia

With secondary manifestation like defective posture & GAIT, Mask like face &Sialorrhoea,

Dementia may accompany.

If untreated- several years- end stage disease- patient rigid unable to move unable to breath properly-

chest infection

PD- progressive degenerative disorder

Cause- Deficiency of dopamine in Striatum (Due to degeneration of neronesin Substantia Nigra

&Nigrostrital Tract)

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Treatment- Increase dopamine & Decrease acetylcholine.

DRUGS-

A. Increase dopaminergic activity

Dopamine precursor-Levodopa (100 mg)

Peripheral Decarboxylase Inhibitor-Carbidopa (10 or 25 mg)

Dopamine Facilitator-Amantidine (100 mg)

Dopamine agonist-Bromocriptine(1.25-2.5 mg)

MAO-B inhibitor-Selegiline (5-10 mg)

COMT Inhibitor-Entacapone(200 mg), Tolcapone(100-200 mg)

B. Decrease cholinergic activity

Ex-

Central anticholinergic-Benzhexol(2-10 mg), Biperiden(2-10 mg)

Antihistaminic- Orphedrine(100-300 mg), Promethazine(25-75 mg)

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 Anticholinergic mainly benefit in tremor

Increase Dopaminergic activity is main therapeutic approach in PD for this purpose levodopa is

First line drug.

Levodopa use along with Carbidopa to increase Levodopa effect

Dopamine precursor-Levodopa (100 mg)

Peripheral Decarboxylase Inhibitor-Carbidopa (10 or 25 mg)

ADEVERSE EFFECT-

Nausea, Vomiting, Postural hypotension, Alteration in taste sensation, Abnormal

Movements, Behavioural effects (Psychosis).

None of the above drug alters the basic pathology of PD

Disease continue to progress

Drugs only provide symptomatic relief and give 3-6 years of productive life.

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 C. DRUGS USED IN MENTAL ILLNESS
(PSYCHOTROPIC DRUGS / PSYCHOPHARMACOLOGICAL
AGENT)

Drugs are those having primary effects on psyche and are used
for the treatment of psychiatric disorders.

PSYCHIATRIC DISORDERS-
Psychosis- severe psychiatric illness with serious distortion of thought&behaviour with delusion &

hallucination (unable to recognise reality and of perception) there is inexplicable misperception

&misevaluation patient unable to meet ordinary demand of life.

a. Cognitive disorder- Delirium & Dementia

b. Functional disorder- Schizophrenia & Paranoids States

Affective disorder- Mania & Depression

Neuroses- anxiety, Phobic states, OCD, Hysterical

PSYCHOTROPIC DRUGS-

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 1. Antipsychotic- Psychosis
2. Antimanic(mood stablizer) – Mania & B.P.D.
3. Anti depressant – Depression, Phobia, OCD & GAD
4. Anti anxiety – anxiety & phobia

5. Psychomimetic/Psychedelic/Psychodysleptic/Hallucinog
en- Produce psychosis like state- cannabis

ANTIPSYCHOTIC-

Having salutary therapeutic effect in psychosis

Psyschosis- Dopaminergic over activity in limbic system

DRUGS-

A. TYPICAL (Dopamine Antagonist)- D2 Blocker action- Decrease dopamine activity of

Psychosis.

Chlorpromazine-(100-800mg/day)-Power full anti emetic also

Haloperidol- (2-20mg/day)- High potency- Also use in treatment of Acute mania

Pimozide- High potency- (2-6 mg)

Flupenazine- High potency- (1-10 mg)

Thioridazine- Low potency-(100- 400 mg)

Flupenthixol- 3-15 mg

Loxapine- 20-200mg

B. Atypical antipsychotic- Minor D2 Blocker& major 5-HT2 antagonist Action.

Clozapine-(50-300mg/day)

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 Olanzepine-(2.5-10mg/day)

Quetipine- (50-400 mg/day)

Ziprasidone-(40-160mg/day)

Risperidone-(2-12mg/day)

PHAMACOLOGICAL ACTIONS -

Reduce irrational behaviour, agitation and aggressiveness and controls psychotic symptomatology.

Disturbed thought & behaviour normalized, anxiety is relieved. Hyperactivity, delusion and

hallucination are suppressed.

USES-

Schizophrenia, Organic brain syndrome, Mania, Anxiety, Antiemetic.

ADVERSE EFFECT-

Drowsiness, Lethargy, Mental confusion, Develop Seizures

Increase Appetite & Weight Gain
Postural Hypotension
Dry Mouth, Blurring of vision & constipation
Galactorrhoea, Gynaecomastia, Amenorrhoea & Infertility

Extra Pyramidal Disturbances-Dose limiting more with high potency Typical

(Haloperidol, Pimozide, Fluphenazine) & less with low potency Typical (Thioridazine) &

Atypical (except Risperidone)

a. Parkinsonism

b. Acute muscular dystonias- Bizarre muscle spasm

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 c. Akhathesia-

d. Malignant neuroleptic syndrome- Rigidity, Tremor, Immobility, Semiconciousness,

Fluctuating BP & HR

e. Tardive dyskinesia

HYPERSENSITIVITY REACTIONS-

Cholestatic jaundice, skin rashes, urticaria, Agranulocytosis, Myocarditis.

ANTI ANXIETY-

Drugs that are used for the treatment of anxiety.

Anxiety- Emotional state, associated with uneasiness, discomfort &concern or fear about future

threat.

Cause- Stress (it is stimulus that can be physical, social, biological etc.)

Two types-

1. Acute stress- Anxiety 2. Chronic Stress- Depression

Treatment- Mild C.N.S. depressant.

DRUGS-

Benzodiazepines-

158
Alprazolam(0.25-1mg), Diazepam (5-30mg), Chlordiazepoxide(20-100mg). Lorazepam 91-6 mg)

ADVERSE EFFECT-

Sedation, psychomotor slowing and cognitive impairment, light headedness, vertigo,

increase appetite.

Azapirones- Buspirone (5-15 mg) – partial agonist of 5-HT1A Receptor

Antihistaminic(sedative)-Hydroxyzine(50-200mg)

B-blocker- Propranolol. (10-40 mg)

ANTI DEPRESSANT

Drugs that are used for the treatment for the depression.

Depression- Characterized by sad mood, loss of interest and pleasure, low energy &guilt.

Cause- Decrease 5-HT &N.Adr. level/activity in brain.

Treatment- Increase 5-HT &N.Adr. level/activity in brain.

DRUGS-

A. Tri Cyclic Anti depressant- Inhibit reuptake of NAdr. & 5-HT

Imipramine(50-200mg/day), Amitriptyline(50-200mg/day), Doxepine(50-150mg/day)

Clomipramine(50-150mg/day)

Desipramine(50-150mg/day), Nortriptyline(50-150mg/day)

Increase N.Adr.& 5-HT Level /Activity in brain-depression retorted

159
 B. Selective Serotonin Reuptake inhibitors(SSRI)-

Fluoxetine(20-50mg/day), Sertraline(50-200mg/day), Escitalopram(10-20mg/day)

Paroxetine (20-50 mg)

Increase 5-HT level/activity in brain-depression retorted.

C. MAO-A Inhibitor- Chlorgyline, Moclobemide (150-300 mg)

Prevent neuronal degradation of Noradrenalin& Serotonin by inhibiting MAO thus

N.Adr. &Serotonin Level /Activity increase in brain-depression retorted.

CHEESE REACTION

D. Atypical Antipsychotic-

Trazadone (50-200 mg)

Mianserine (30-100 mg)

Mitrazepine (15- 45 mg)

Duloxetine (30-80 mg)

Venelaflaxine (75-150 mg)

USES-

Major depression (Endogenous Depression)- Response in 2 to 3 weeks

OCD & Phobia

160
 Neuropathic pain

Enuresis (Bed wetting in children)

Anxiety disorder (GAD)

Panic Disorder

Social Phobia

Migraine- Amitriptyline

Pruritus- Doxepine

ADHD- TCA (Imipramine, Nortriptyline)

ADVERSE EFFECT-

Sedation, Mental confusion- Mainly with TCA specially Amitriptyline (and also with

Trazadone)

Blurring of vision, Dry mouth, Bad taste, Constipation- TCA

Increase appetite & Weight gain- TCA & Trazadone

Postural hypotension, Cardiac arrhythmia- TCA

Sweating & Fine tremor- TCA

Rashes Jaundice- Mianserine

ANTI MANIC/MOOD STABILIZERS-

Drugs that are use for the treatment of mania& BPD

161
DRUGS-
Lithium carbonate (300mg tab) – 600 to 1200 daily in divided dosage

Therapeutic Response -1 to 2 weeks

ADVERSE EFFECTS-

Nausea, vomiting, diarrhea

Thirst, Polyurea

Fine tremors & rarely Seizures

Coarse tremor, Gidiness Ataxia, Motor incoordination, Nystagmus, Mental

confusion, Slurred speech, Drowsiness, Delirium, Coma & Convulsion.

vomiting, Diarrhea, Albuminurea& Arrhythmia.

On long term use- Diabetes Incipidus

If use during pregnancy- foetal goiter.

Lowtherapeutic index, higher toxicity so serum monitoring required on prolonged use.

Serum level maintained in-

Bi Polar Disorder- 0.5- 0.8 meq/L

& In

Mania- 0.8- 1.1/1.2meq/L

Toxicity starts at 1.5 meq/L

162
 and on 2.0 meq/L toxicity symptoms are Coarse tremor, Gidiness Ataxia, Motor

incoordination, Nystagmus, Mental confusion, Slurred speech, Drowsiness,

Delirium, Coma & Convulsion.

Vomiting, Diarrhea, Albuminurea& Arrhythmia.

Treatment- Osmotic diuretics & Sodium bi carbonate

Haemodylysisabve 4 meq/L

Lithium CI during pregnancy

Interaction- high & medium efficacy diuretics- increase plasma lithium level- lithium

toxicity

Tetracycline/A.C.E. inhibitors/ NSAIDS- increase lithium retention- lithium toxicity

Lithium increases sulfonyl urea & insulin action- hypoglycemia.

USES-

Acute Mania

Prophylaxis in BPD

OTHER DRUGS

Carbamazepine- Mania & BPD

Sodium valproate- Acute mania (first line)

Lamotrigine- BPD

Atypical Antipychotic (Olanzapine, Risperidone &Quetipine)- Acute mania

Olanzapine- Maintenance therapy of BPD

Typical Antipsychotic (CPZ/Haloperdo- INJl)- Rapid control of acute mania

D. ANTI CONVULSANT/ANTI EPILEPTIC

163
Epilepsies- Group of C.N.S. disorder characterized by Paroxysmal cerebral dysrhythmia,

manifesting as episodes of loss or disturbance of consciousness, with or without characteristic body

movements (convulsion).

Most of cases idiopathic (primary)

Some may be secondary to Trauma/Surgery on Head, Intracranial Tumour, Tuberculoma,

Cysticercosis & Cerebral Ischemia

Cause- Uncontrolled ectopic discharge of ions.

Seizures- Brief episodes of epilepsies.

Types of Seizures-

A. Generalized seizures- whole body involve

Generalized tonic-clonic(Major epilepsy/grand mal epilepsy)

Absence Seizures(Minor epilepsy/petit mal epilepsy)

Atonic Seizures

Myoclonic Seizures

B. Partial seizures (focal seizures)- Partial body involve.

Simple partial seizures

Complex partial seizures (TPL)

Secondary generalized

164
C. Unclassified Seizure-

Infantille Spasm

Febrile Seizure

Treatment- suppression of uncontrolled ectopic discharge of ions.

MECHANISM OF DRUG ACTION-

A. Drugs acting on Na+ channels (Prolongation of Channel inactivation)-

Phenytoin, Carbamazepine, Valproic acid, Zonisamide Lamotrigine Topiramate,

Lacosamide

B. Calcium channel (Inhibition of t-Type)-

Ethosuximide, Valproic acid, Zonisamide

C. Chloride Channel (Facilitation of GABA mediated opening)-

Barbiturates, Benzodiazepines, Valproic acid,Gabapentine, Vigabatrin, Tigabine

D. Inhibition of GLUTAMATE Synapse-

Phenobarbitone, Phenytoin, Valproic acid, Lamotrigine, Topiramate, Lacosamide,

Lavitiracetam

DRUGS-
1. Barbiturates- Phenobarbitone(60-180mg/day)
Sedation, sudden withdrawal- convulsion
2. Benzodiazepines-Diazepam(0.2-0.3 mg/kg), Clonazepam(0.5-5 mg/kg), Clobazam( 10- 20
mg), Lorazepam(0.1 mg/kg)

3. Carbamazepine (200-400mg)

165
 Sedation, Dizziness, Vertigo, Diplopia, Ataxia, Leucopenia, Water Retention & Aplastic
Anaemia
4.Valproic acid (200-600mg)
Anorexia, Heart Burn, Vomiting, loose Motion, Alopecia, Liver Damage, Agranulocytosis,
Tremor, Epigasric Pain, PCOD, Obesity & Rash
5. Ethosuxumide (250 mg/5ml)
Gastrointestinal intolerance
6. Phenytoin (100 mg Tab/Inj)
Cleft palate, Gum hypertrophy, Hirsutism, Osteomalacia, Magaloblastic Anaemia, Vit, K
Deficiency, Decrease Insulin Release, Lymphadenopathy, Ataxia & Arrhythmia.
6. Gabapentine(300 mg)
Enhance GABA release

7. Zonisamide(25- 100 mg)

Renal stone, Sommolence& Metabolic Acidosis

8. Lamotrigine (25-100 mg)

Sleepiness, Diplopia, Ataxia

9. Vigabatrin (500- 1500mg)

Visual Field Contraction, Alteration of colour vision,Behavioural changes

10. Topiramate (25-100 mg)

Weight Loss, Renal stone

11. Levitiracetam (500-1000 mg)

Irritability, Aggression

12. Lacosamide(50-200 mg)

Ataxia, Vertigo, Diplopia & Tremor

13. Tigabine (4-16 mg)

Sedation, Nervousness, Asthenia & Amnesia

166
USES-

a. Generalized tonic-clonic seizures-

Valproic acid, Lamotrigine,Carbamazepine

b. Partial seizures-

Carbamazepine, Lamotrigine, Valproic acid

c. Absence Seizures-

Valproic acid, Ethosximide

d. Myoclonic-

Valproic acid, Topiramate

e. Atonic-

Valproic acid, Lamotrigine

f. Febrile seizures-

Diazepam

g. Status epilepticus-

Lorazepam, Diazepam

h. Infantile Spasm-

ACTH, Cortticosteroid

i. Eclamptic Seizure-

Magnesium Sulphate

167
** Folic Acid (second & third trimester) Use along with antiepileptic during pregnancy to

minimise Neural Tube Defects.

** Vitamin K (last month) to minimise Risk of Bleeding.

** Valproate- Most Teratogenic

** Lamotrigine- Prefers during Pregnancy

E. ANAESTHETICS-

Drug that are use to induce reversibe loss of sensation.

Two types-

(a) General anesthetics- Effects on Whole body

(b) Local anesthetics- Effects on Particular area

(a) GENERAL ANAESTNETICS –

Drugs that are use to induce General Anaesthesia

GA-

Loss of all sensation specially pain

Immobility & Muscle relaxation

Abolition of Somatic & Autonomic Reflexes

Deep Sleep (Unconscious) & Retrograde Amnesia

Stages of GA-

168
 I- Analgesia- Pain abolish, dream like state

II- Delirium-Loss of consciousness to beginning of normal respiration

Apparent excitement

III- Surgical- onset of regular respiration to cessation of breathing

a. Roving Eyeball
b. Loss of reflexes(corneal & laryngeal)
c. Loss of light reflex & pupil starts dilating
d. Dilated pupil & shallow abdominal Respiration

IV- Medullary Paralysis-Cessation of breathing, failure of circulation & death

DRUGS-

1. Inhalation-

a.Gases-

Nitrous oxide
Given along with O2 (70+30)
Laughing gas
Good analgesic but poor muscle relaxant
Onset quick & smooth and fast recovery

b.Volatile liquid-

Halothane-(0.5-4 %) potent anaesthetic but not good analgesic or muscle relaxant

Ether-not preferred in current

Isoflurane-(1-3%)- Neurosurgery

Desflurane

Sevoflurane

2.Intravenous-

a. Inducible-Fast onset & short duration.

Ex-Thiopentone sodium 3-5 mg/kg (Onset-15 to 20 sec & Duration- 6 to 10 min)

Propofol 2mg/kg (Onset-15 to 45 sec & Duration- 5 to 10 min)

169
 b. Slower-Onsetslow,but duration long.

Ex- Diazepam (0.2-0.5 mg/kg)

Midazolam(1-2.5 mg)

Lorazepam(2-4 mg)

ketamine (dissociative /child anesthesia)-1.5 mg/kg

Fentanyl (2-4 mcg/kg)

Complication of G.A-

Respiratory depression, salivation, laryngospam,nausea,vomiting.

Preanaesthetic medication administered to avoid Complication of G.A(to make

anaesthesia safe and less unpleasant)

Ex- Diazepam, Atropine, Metoclopramide, Ranitidine etc.

** Balance anaesthesia- Inhalation + IV

** Concious sedation-supplemented with LA- Monitored state of altered

consciousness(Diazepam, Midazolam, Fentanyl)

(b) LOCAL ANAESTHETICS-

Act on local area

Consciousness unaltered

Mechanism-block nerve conduction by block Sodium channel

DRUGS-

a.Injectable-

Low potency-Procaine

170
 Intermediate potency-Lignocaine, Prilocaine

High potency- Bupivacaine, Dibucaine, Tetracaine, Ropivacaine

b.surface-

Cocaine, Lignocaine, Tetracaine, Benzocaine, Oxethazaine

USE-

Surface Anaesthesia-Topical application

InfilterationAnaesthesia- Minor surgery

Anti arrhythmic- Xylocard

Conduction block (Nerve Block & Field block)

Epidural anaesthesia-Epidural Space (Thoracic, Lumbar & Caudal)

Spinal anesthesia-Subarachnoid space (below the lower end of spinal cord0

Complication of Spinal Anesthesia-

Respiratory paralysis, Hypotension, Headache, Nausea, Vomiting

F. ANALGESICS-
Drugs that are used to reduce or relieve pain

Two types

1. Narcotic 2. Non narcotic

(i) NARCOTIC/ OPOIDS/ MORPNINE LIKE

Drug that obtain from opiumor it’s semisynthetic and synthetic derivatives.

171
 • Act on C.N.S.

• Produce dependence

• High degree analgesia(relieve visceral pain)

• Induce respiratory depression(on high dose death

DRUGS-

Morphine 10 mg/ml

Codeine

Diacitylemorphine(heroin)

Dextroprophoxyphene

Tramadol

Fentanyl

Pethidine

Pentazocin

USES-

Analgesics

Anaesthetics

Antitussive

Left ventricular failure

CONTRA INDICATION-

172
 Bronchial asthma

Head injury (because it increase I.C.P. &induce vomiting)

Hypotension

Hyporthyroidism.

(ii) NONE NARCOTIC/NSAID’S/NON OPOIDS/ASPIRIN like

• Relieve moderate/weak intensity pain

• Primarily act on peripheral pain mechanism

• Do not produce dependence & C.N.S. depression

MECHANISM-
Act by inhibiting cyclo-oxy-genase (COX) enzyme threw this they inhibit

prostaglandin synthesis which is responsible for pain, fever & inflammation.

DRUGS-

Aspirin

Ibuprofen

Naproxen

flurbiprofen

Aceclofenac

173
 Piroxicam

Ketorolac

Indomethacin

Mephanamic acid

Diclofenac sodium

Nimesulide

Etoricoxib (cox-2 inhibitor)

Paracetamol,

USES-

As analgesic-headache, backache, myalgia, joint pain, toothache, neuralgia,

dysmenorrhoea, post traumatic & post operative.

Anti inflammatory- rheumatoid arthritis, osteoarthritis, acute gout, ankylosing

spondylitis

Antipyretic

Post M.I. & post stroke

174
 Patent ductus arteriosus closure.

ADVERSE EFFECTS-
Epigastric pain, nausea,vomiting,peptic ulcer, headache, dizziness & rashes

(G) C.N.S. STIMULANT

Drug that are use to stimulate C. N. S. (specific area of brain) & having resuscitative value in

coma & fainting.

DRUG-

• Amphetamine, Methylphenidate, Modafinil - ADHD& narcolepsy

• Caffeine, theophylline- As anti asthmatic

• Doxapran – As analeptic (respiratory stimulant)

( H) SKELETAL MUSCLE RELAXANTS-

Drugs that are use to relax skeletal muscles are known as skeletal muscles relaxant (S.M.R.)

Three categories

(A) Neuromuscular blocker (N.M.B.)

(B) Directly acting

(C) Centrally acting

DRUGS-

A.NEURO MUSCULAR BLOCKER – Act on neuron muscular junction

d-Tubocurarine,Pancuronium bromide
Atracurium, Vecuronium

175
 Mivacurium
Succinyl choline, Decamethonium

B.CENTRALLY ACTING – Act on medullary region & medullary centre

Chlorzoxazone, diazepam, Baclofen, Tizanidine, Thicolchiocoside

C.DIRECTLY ACTING –Directly act on muscle end plate

Dantrolene

USES-

(i) N.M.B. –Adjuvant to G.A., Endotracheal intubation, laryngoscopy,Bronchscopy,

ECT, Assisted ventilation, Tetanus, Status epileptic

(ii) Centrally Acting–Acute muscle spasm, Backache, Tetanus, E.C.T., orthopedic

manipulation

(iii) Directly acting-Malignant Hyperthermia & MNS

176
5.AUTOCOIDS & RELATED DRUGD

177
DRUGS FOR TREATMENT OF GOUT
CLASSIFICATION

1. On basis of action-
a. Xanthine oxidase inhibitor-
e.g. allopurinol
Act by inhibiting synthesis of uric acid.
b. Uricosuric –
e.g. Probenecid, Sulfinpyrazone.
Act by increasing excretion of uric acid through uirne
2. On basis of condition of use
a. For acute gout – NSAID, Colchicines, Steroid(prednisolone).
Relieve pain & inflammation
b. For chronic gout – Allopurinol, Probenecid, Sulfinpyrazone
Decrease uric acid

DRUGS FOR TREATMENT OF RHEUMATOID ARTHRITIS

CLASSIFICATION

1. Drugs suppressing (modifying) the disease- disease modifying drugs (DMARDs)-

Immunosuppressant: Methotrexate, Azathioprine, cyclosporine.
Gold
d-penicillamine
HCQS
Sulfasalazine
Leflunomide
2. Biological response modifier-
Ex- Infliximab
Adjuvant drugs- corticosteroids
Ex- Prednisolone
use to relieve pain & inflammation

178
 3. NSAIDs –

Ex- Indomethacin
use to relieve pain & inflammation

ANTIHISTAMINICS
H1 Receptor antagonists (H1 -antihistamines)

CLASSIFICATION-

a. 1st generation – Hydroxyzine(Atarax-25mg), Diphenhydramine, Promethazine

(phenargan), Pheniramine meleate (Avil 4-mg), Meclizine, Chlorpheniramine
Cyclizine,
Higher Sedation & anticholinergic effects.

b. 2nd generation – Fexofenadine (Allegra), Loratidine, Cetrizine

Lesser sedation

ADVERSE EFFECTS:
Dryness of nose, mouth and eyes, sedation and drowsiness.
USES :
To treat and prevent allergic reaction, in blood transfusion, anti emetics, Cough, Cold,
itching, asthma, anti anxiety.

179
6.DRUGS ACTING ON ENDOCRINE
SYSTEM

180
ANTERIOR PITUTARY HORMONES-
Secretion:-contolled by

❖ 5 releasing and 2 inhabiting hormones of hypothalamus

Name of hormone stimulation by inhabitation by

Growth hormone GHRH GHIH(somatostatin)

(GH,somatotropin)
TSH (thyrotropin) TRH GHIH(somatostatin)
FSH GnRH -
LH GnRH -
Prolactin PRH PRIH(Dopamine)
ACTH CRH -
Melanocyte CRH Dopamine
Stimulating hormone

GH deficiency-Dwafism – treatment by GH/analogs

Ex-Somatropin, Somatrem

GH excess- Gigantism &Acromegly- treatment by somatostatin/analogs

Ex-Somatostatin, Octreotide.

Gonadotropins
Anterior pituitary hormones regulating ovarian and testicular fuctions.

Luteinizing hormone (LH)

LH is responsible for the stimulation of the interstitial cells of the testis (leyding cells)
which lead to the production of the testosterone. In the female, is stimulate secretion of
progesterone.

181
Follicular stimulating hormone (FSH)

FSH is responsible for stimulation of follicles secretion of estrogen from follicles in

female & in male support spermetogenesis.

Uses of Gonadotropins-(FSH+LH)

1. Amenorrhoea& infertility
2. Hypogonadotrophic Hypogonadism in male
3. Cryptochism

SyntheticGnRH- Increase release of LH & FSH

EX- Gonadorelin

GnRH agonist- Initially increase Gn but after 1-2 week decrease Gn

Ex-Nafarelin, Triptorelin, Goserelin, Leuprolide

Uterine fibroid, Endometriosis, Assisted reproduction

GnRh Antagonist- Quick GnSupression

Ganirelix, Cetrorelix

Human Chorionic Gonadotropin (HCG)

It is produced in large amount throughout pregnancy.

Prolactin-

Induce milk synthesis

TSH-

Stimulate Thyroid

ACTH-

Promote Steroidogenesis in Adrenal cortex

182
ADRENO CORTICAL STEROIDS (CORTICOSTEROIDS)
Disorders of adrenocortical function:

a. hypofunction of adrenal cortex- addison’s disease.

b. hyperfunction – cushing’s syndrome – deposition of fat on the face and back(moon

face, buffalo hump), hyperglycemia and hypertension.

GLUCOCORTICOIDS
Examples
Natural- hydrocortisone (cortisol), Cortisone and Corticosterone.
Synthetic- Dexamethasone, Prednisolone, Mehylprednisolone, Triamcinolone,
Deflazacort, Fluticasone & Budesonide

PHARMACOLOGICAL ACTIONS

a. Hyperglycemic

b. Osteoporosis

c. Anti-inflammatory-(by inhibiting phospholipase A2& decrease capillary

permeability)

d. Anti – allergic action.

e. suppression of immunity – used as immunosuppressant.

ADVERSE EFFECTS:
a. causing’s syndrome- characterized by moon face, buffalo hump

b. Sodium retention and edema

c. weighty gain due to fluid retention and fat deposition

d. Glycosuria

e. osteoporosis, peptic ulcer, increase susceptibility to infection

f. Muscle wasting (protein catabolism)

183
USES-
Anti inflammatory, anti allergic, organ transplantation, gout, arthritis, asthma, auto

immune disorder.

ANDROGENS
Most important androgen is testosterone.

25 mg IM
ACTION-
Spermatogenesis, growth of prostate, secondary sexual characters in male, epiphysis
closure.Skeletom muscle (anabolic), & Erythropoiesis

ADVERSE EFFECT-

Virilization, Acne, Cholestatic Jaundice, Early closure of epiphysis, Gynaecomastia,

CI- Prostate cancer & Male breast cancer.

USES-

Testicular failure

Hypopituitarism

AIDS related muscle wasting

Ageing

ANABOLIC STEROIDS

184
 Derivatives of testosterone having poor androgenic & more anabolic effects.
Ex- Nandrolone, Oxymethalone, Stanozolol

USE-
Osteoporosis
To enhance physical ability in athletes.

IMPEDED ANDROGENS/ ANTIANDROGEN

Danazol- Decrease Gn secretion
Uses- Endometrisis, Fibrocystic Breast disease
Cyproteron Acetate- Decrease LH
Flutamide- Anti androgenic
Use- Prostate cancer
Bicalutamide- Anti androgenic
Use- Prostate cancer

5- ALPHA REDUCTASE INHIBITOR-

Finasteride, Dutasteride
Use- BHP

ESTROGENS & PROGESTINS-

USES OF ESTROGEN-
To control menopausal symptoms
Senile vaginitis, Dysmenorrhea, Acne
(Estradiol 5 mg IM Dienestrol Cream 0.01%)

Anti Estrogen- Clomiphene citrate

185
 SERM- Tamoxifen Citrate, Raloxifene
Aromatase Inhibitor- decrease Estrogen
Letrozole, Anastrozole- Breast cancer

USES OF PROGESTRON-
Progesterone 10-100 mg IM

As oral contraceptive.
HRT, Treatment of threatened & habitual abortion, Uterine bleeding, Endometriosis.

ANTIPROGESTINE-
Mifepristone

CONTRACEPTIVE
Drugs that are use to prevent conception

MECHANISMS-
Inhibit- spermatogenesis, ovulation, maturation of ovum & implantation, inhibit release
of hormone.
Preparations-

Combined pill= Ethinyl estradiol + Norgestrel( MALA-D)

Phase pill= Ethinyl estradiol + Levonorgestrel(TRIQULAR)

Mini pill= Norgestrel

Post coital Contraception= Levonorgestrel

GOSSYPOL- orally effective male contraceptive(inhibit Spermetogenesis)

186
CENTCRHROMAN (SAHELI)- Nonsteroidal contraceptive.

Mifepristone (progesterone antagonist)- terminates very early pregnancy ( use along with

misoprostol )

THYROIDS & ANTITHYRIODS

THYROIDS-
Thyroixin(T4 )& tri iodo thyronine(T3)- iodine containing derivatives of tyrosine

Deficiency of these hormones leads to-

hypothyroidism that leads to Cretinism, Myxoedema(emergency Hypothyroidism),

Goiter
DRUGS-
Thyroxine Sodium Tablet
USE-
Treatment of Hypothyroidism, Cretinism, Myxoedema, Nontoxic goiter

ANTI THYROIDS
Drugs used for the treatment of hyperthyroidism
DRUGS-

Inhibit Hormone synthesis-

Propylthiouracil, methimazole,Carbimazol

Inhibit Hormone release-

Iodine

Destroy thyroid tissue-

I131

Uses- Hyperthyroidism, preoperative preparation, Thyroid storm, Thyrotoxicosis

DRUGS AFFECTING CALCIUM BALANCE

187
Increase resorption by-corticosteroid,PTH, Thyroxin, Loop diuretic, Alcohlism&
PGE2
Decrease resorption by- Androgen, Estrogen, GH, Calcitonin, Biphosphonate,
Fluoride &Thizide

PARATHYROID HORMONE (PARATHARMONE PTH)

By chief cells of parathyroid gland.
Acton – increase plasma calcium level

On high con.(continuous)-Osteoclast activity dominant-increase bone resorption- increase

plasma calcium level

On intermittent exposure (low con.)- Ostoblast activity dominant- increase bone

formation

Hypoparathyroidism-Lower plasma calcium level, Tetany, Convulsion,

Laryngospasm,Cataract & Psychiatric changes.

Hyperparathyroidism-Hypercalcaemia, Decalcification of bone, Renal Stones

Metastatic calcification, Muscle weakness, Constipation, Deformities & fractures.

** Teriperatide- Recombinant PTH- use in treatment of severe osteoporosis

CALCITONIN-
100 IU/ML

188
 Lowers plasma calcium level by blocking PTH induce bone resorption (decrease

osteoclast activity)

Uses-hypercalcaemic state,Post menopausal women, Paget’s disease

VITAMIN- D
Increase Plasma Calcium Level by increasing absorption of calcium from gut & renal

tubules.

D1 - Mixture of substances found in food

D2 – Calciferol- yeast, fungi, bread & milk
D3 – Cholecalceferol- synthesized in the skin
Caclitriol- Active form of vit D3
Uses- Vit D Deficiency, Rickets, Osteoporosis, Hypoparathyroidism & Fanconi syndrome

Biphosphonates-increase apoptosis of osteoclast

Alendronate 5-10 mg OD
Zoledronic acid 4 mg INJ
Use- Osteoporosis, hypercalcaemia of malignancy, Paget’s disease

ANTI DIABETIC DRUGS

DM- metabolic disorder characterized by hyperglycemia, glycosuria,
hyperlipaemia, negative nitrogen balance and sometimes ketonemia.

189
DM- high blood glucose level- increase glycosylation of tissue protein-
pathological changes- Thickening of capillary basement membrane,
lumen narrowing, atherosclerosis, neuropathy, retinopathy &
nephropathy
Diabetes Mellitus- Two types
1. IDDM- circulating insulin low or very low, more prone to ketosis, less common, low

degree of genetic predisposition & low level of c-peptide

2. NIDDM- insulin in circulation low, normal or even highover 90% cases, high degree

of genetic predisposition

*Abnormality of glucoreceptor

*Insulin restence

* Excess hyperglycemic hormone/obesity

INSULIN
1921- Banting & Best
51 AA- Two chain
A-chain-21 AA & B-chain- 30 AA
Insulin is a polypeptide hormone secreted by beta cells of pancreas in response to arise in blood
glucose level.
o Insulin lowers blood sugar level by glycogenesis, lipogenesis & entrap glucose in
to cell
o Diabetes mellitus occurs due decrease insulin secretion or it’s action.

ACTION OF INSULIN:
hormone of anabolism-storage of fuel/energy.
a. Stimulation of –glycogen synthesis.
b. Lipogensis
c. Uptake of glucose by muscles

190
Route – ineffective orally –given by S.C.injection

ADVERSE EFFECT
a. Hypoglycemia – coma and convulsions
b. Lipodystrophy – at site of injection.
c. Allergy- rashesh

• PREPARATIONS OF INSULIN:
a. Short acting – Human insulin Soluble(0.5-1, 2-4, 6-8 h)
Insulin Zinc suspension(semilente)-Amorphous
b. Intermediate acting – Human insulin Isophane(1-2, 8-10, 20-24 h)
Human insulin Biphasic, Insulin zinc suspension(lente)
c. Long acting –Insulin glargine (2-4, 5-12, 24)
Protamine zinc insulin, Insulin zinc suspension(ultralente)-Crystalline

** Rapid acting insulin- Insulin Lispro, Insulin Aspart (0.2-0.4, 1-2, 3-5)

INSULIN DOSE

Type-I 0.4 – 0.8 U/KG/DAY

Type-II 0.2 – 1.6 U/KG/DAY

ORAL HYPOGLYCEMICS
Drugs lower blood glucose leveland are effective orally.

Insulin sensitizer- Increase action of insulin by improve it’s binding with receptor
1. Biguanides

191
 Ex-Metformine
Long use of biguanides result in development of lactic acidosis and megaloblastic anemia
(due to deficiency of vitamain b12)

2. Thiazolidinediones
Ex- piogitazone

Insulin secretogogues-Increase insulin secretion

a. Sulfonylureas
Ex- Chlorpropamide, Tolbutamide, Glimepiride, Gliclazide, Glipizide

b. Meglitinide analog

Ex-Repaglinide

Alpha glucosidase inhibitor- Inhibit conversion of disaccharide to monosaccharide

Ex- Acarbose, miglitol
DPP-4 Inhibitor- Increase insulin & decrease glucagon
Ex-Sitagliptin, Tenelagliptin

SGLT-2 inhibitor- Decrease glucose reabsorption in renal tubule- Glycosuria

Ex- Dapagliflozin

UTERINE STIMULANTS (OXYTOCICS, ABORTIFACIENTS)

These drugs increase uterine motility, especially at the time of labour.

PP Hormone-Oxytocin (2 IU/ML)

Induction of labour, PPH, Uterine inertia, Breast engorgement

192
 Ergot- Ergometrine, Methylergometrine

PPH

Prostaglandins- PGE2, PGF2α, Misoprostol (PG analog)

Cervix ripening

Others-Ethacridine

UTERINE RELAXANT (TOCOLYTICS)

These drugs use to decrease uterine motility to postpone labour

B2- agonist- Isoxsuprine,Ritodrine

CCB-Nifedipine

Magnesium sulphate (1gram/2ml- inj)- Pre eclampsia &Eclampsia

Loading Dose-

4 gram (20%) –IV over 5 min

Follow by-

10 gram (50%) – IM

If convulsion occurs in 30 min then-2 gram(20%)- IV over 5 min

Maintenance dose-
5 gram (50%) – IM every 4 hour

Focus on- RR(16/min), Patellar Reflux & Urine output (30 ml/hour)

If RR drop Use antidote –Calcium Gluconate

Normal plasma level- 1.5- 2 mEq/L or 1.8- 2.4 mg/dl

193
Therepeutic- 4-8mEq/Lor 4.8- 9.6mg/dl

ECG changes- 5-10mEq/Lor 6-12mg/dl

Decrease deep tendon reflex & Respiratory depression – 10mEq/Lor 12mg/dl

Respiratory Arrest- 15mEq/Lor18mg/dl

Cardiac arrest-above 20mEq/Lor 24mg/dl

194
7.ANTI MICROBIAL DRUGS

195
ANTI MICROBIAL DRUGS

Drugs that are designated to inhibit/kill the infecting organism

CHEMOTHERAPY- Treatment of any systemic infection or neoplasm by the help of chemical

agent is known chemotherapy.

CHEMOTHERAPY- Treatment by chemotherapeutics agents.

Two types-

1. Anti microbial drugs (only systemic) 2. Anti neoplastic agent

(1) Anti microbial drugs/Anti infective (use in infection)

(i) Topical (ii) Systemic

It includes use of-

a. Antibiotics

Ex- Penecillin, cephalosporines

b. Others

Ex- sulfonamides

Anti microbial can be-

Antibacterial – Amoxycillin

Antifungal- Griseofulvin

Antiviral – Acyclovir

Antiprotozoal - Metronidazole

Antihelminthic - Albendazole

(2) Anti neoplastic/Anti cancer- use in cancer

196
It includes

a. Antibiotics b. others

Ex- doxorubicin Ex- methotrexate

ANTIBIOTICS-

Chemical agents that are obtained from microorganism and are use to kill or inhibit the
microorganism / host defective cell.

Classification of antimicrobial-

A. according to spectrum of activity-

(a) Broad spectrum

Ex- Chloramphenicol
(b)Narrow spectrum
Ex- Streptomycin

B. mechanism of action-

(a) Inhibit cell wall synthesis-

Ex- Penicillins, Cephalosporines

(b) Inhibit protein synthsis-

Ex-Tetracyclines, Chloramphenicol

(c) Inhibit DNA gyrase-

Ex- Ciprofloxacin

(d) Cause misreading of m-RNA codone-

Ex- Streptomycin

E. Type of action-

197
 (a) Primary bacteriostatic-

Ex- Tetracycline, Chloramphenicol

(b) Primary bacteriocidal-

Ex- Penicillins, Cephalosporines

ANTI MICROBIAL

(A) SULFONAMIDES
SULFONAMIDES- First antimicrobial agent effective against pyogenic bacteria.

DRUGS

Sulfadiazine, sufamethoxazole, sulfadoxime, silver sulfadiazine, sulfacetamide etc.

ACTIVITY-

Primary bacteriostatic on high dose bactericidal,effective against gram positive & gram
negative bacteria.

Mechanism – Sulphonamide compete with PABA for bacterial folate synthetase by

inhibit folate synthase inhibit folic acid synthesis

ADVERSE EFFECT-

Allergic reactions, thrombocytopenia, hypothyroidism, goitre, kernecterus(neonatal

jaundice), S J reaction, Crystalurea

USES-

Ulcerative colitis,U.T.I., Meningococcal meningitis, Conjunctivitis,Malaria etc.

198
COTRIMOXAZOLE
It is fixed dose combination of ofTrimethprim + Sulfamehoxazole in 1:5 ratio.

cotrimoxazole(Trimethprim 80mg+ Sulfamehoxazole 400mg) Mar. Prep. Septran

it is bacteriocidal

uses & adverse effect similar to sulfonamides.

(B) QUINOLONES
Synthetic antimicrobial having quinolone structure

1. Nalidixic acid 0.5 gram

Effective against gram (-) bacteria

Use- urinary antiseptic

2. FLURO QUINALONES-
Synthetic antimicrobial agent

DRUGS-

FIRST GENERATION-

Norfloxacin 400mg

Ciprofloxacin 500mg

Ofloxacin 200-400mg

SECOND GENERATION-

Levofloxacin 250-500mg

Gatifloxacin 200-400mg

Sparfloxacin 200-400mg

Moxifloxacin 400 mg (0.5% e/d)

199
ACTIVITY-

Mainly effective against gram negative aerobic bacteria.

Mechanism- act by inhibiting bacterial D.N.A. gyrase enzyme which is required for
DNA replication thus by inhibiting this inhibitDNA replication.

USES-

U.T.I., Typhoid,Bacterial gastroenteritis, Tuberculosis, Meningitis, Respiratory infection

Conjunctivitis (Eye drop- Ciplox)

ADVERSE EFFECTS-

Nausea, vomiting,dizziness,headache,photosensitivity, cartilage damage, prolong QT

interval.

C./I.- In children (Ciprofloxacin) &during pregnancy(all FQ).

(C) BETA LACTAME ANTIBIOTICS

Antibiotics that contain B-lactame ring

Four categories

1.PENICILLINS 2. CEPHALOSPORINES
3. MONOBACTAMS 4. CARBAPENEMS

1. PENICILLIN
It is the first natural antibiotic that was discovered in 1928
byAlexenderfleming& used clinically first in 1941.

200
DRUGS-

• Natural –Ineffective orally&narrow spectrum of activity

Benzyl penicillin (penicillin-G)- 0.5-5 mu – I.M.
Benzathine penicillin (penidureinj 12 mu) –I.M.
• Semi Synthetic-Effective orally & broad spectrum of activity
Amoxycillin(500mg), Cloxacillin(500mg), Ampicillin(500mg), Piperacillin(1-4 gram),
Ticarcillin, Nafcillin, Methicillin
Clavulanic acid(125mg), Sulbatum (250-500mg), Tazobactum (250-500mg)
I- betalactamase inhibitor

ACTIVITY-
NATURAL-

Mainly effective against gram (+) cocci & bacilli & gram (-) cocci bacteria.
SEMISYNTHETICeffective against gram (+) cocci & bacilli & gram (-) cocci & bacilli
(also) bacteria.

Mechanism- Act by inhibiting bacterial call wall synthesis

USES-

Pharyngitis, Otitis media (streptococcal infection), Pnemonia,

Meniningitis(meningococal)

Gonorrhoea,Diphtheria, Syphilis, RTI,UTI

Amoxycillin combined with clavulanic acid to increase activity.

ADVERSE EFFECTS-

Local irritancy, hypersensitivity, superinfection

201
 2. CEPHALOSPORINES-
DRUGS-
First generation-more- gram (+) weak gram(-)
Cephalexin 250-500mg

• DOC – UTI during pregnancy

Second generation- more gram(-) & anaerobes
Cefuroxime 200mg

• Not effective against pseudomonas

Third generation-more effective against gram negative enterobacteriaceae&
pseudomonas but less effective against gram positive cocci & anaerobes
Cefixime(200mg oral), Cefotaxime (250- 1000 mg), Ceftriaxone (250-
1000 mg), Ceftazidime (250- 1000 mg), Cefoperazone (250- 1000 mg)
Cefpodoxime (200 mg oral)
Fourth generation- similar to third but high resistant to beta lactamase
Cefpirome 1000mg IM/IV
cefepime 1000mg IV

• Indicated in serious hospital acquired infection

MECHANISM-Bactericidal, act by inhibiting cell wall synthesis.

USES-

AS alternative to penicillin, R.T.I., U.T.I., Meningitis, Syphilis, Septicemia, Typhoid,

Gonorrhea, Surgical prophylaxis

ADVERSE EFFECT-

I.M. injection painful, diarrhea, hypersensitivity, nephrotoxicity.

3. MONOBACTAMS
Aztreonam 0.5-2 gram IM/IV
Effective against gram negative enteric bacilli, H. influenza & pseudomonas

202
4. CARBAPENEMS
Imipenem (with cilastin) 500 mg IV ( degrade by dehydropeptidase-I)- Renal tubule

• Can cause seizure

Meropenem 0.5–2 gram slow IV

• effective against gram positive and gram negative bacteria (both aerobes and anaerobes)
• More gram negative aerobes less gram positive cocci
• Reserve drug for nosocomial infection like septicaemia & febrile neutropenia
Faropenem 200 mg tablet

• Indicated in respiratory, ENT & genitourinary infection

(D) AMINOGLYCOSIDES-
DRUGS-

Sterptomycin(first line drug T.B.),Amikacin(250-500mg), Tobramycin(eye

drop),Gentamycin(injection & Cream), Neomycin(Cream),Kanamycin(second line drug
TB), Sisomicin, Netilmicin,Spectinomycin, Framycetin

ACTIVITY-

Mainly effective against most aerobicgram negative bacilli.

Mechanism-Inhibit protein synthesis by bind several sites of 30 & 50s ribosome cause
misreading of m-RNA codone.

• Netimicin- For serious infection only& least ototoxic

• Spectinomycin -Gonorrhoea in penicillin allergic patient
• Amikacin, Gentamycin & Tobramycin- Gram negative with pseudomonas
• Neomycin- oral- Gut sterlization

ADVERSE EFFECT-

Nephrotoxicity,Damage to VIII Cranial nerve(Auditory nerve), Neuromuscular Blockage.

USES-

U.T.I., Gastroenteritis, Conjunctivitis, Skin infection,etc.

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(E) MACROLIDE ANTIBIOTICS
DRUGS-

Erythromycin,Azithromycin(250-500mg), Clarithromycin, Roxithromycin(150-300mg),

Spiramycin.

ACTIVITY-

Effective mainly against Gram Positive bacteria& few gram negative bacteria.

Mechanism- Inhibiting protein synthesis by acting on 50’S ribosomes.

*Clarithromycin- Rx of Mycobacterium avium complex & also for h. pylori induced

peptic ulcer.

* Spiramycin- DOC for Rx of Toxoplasmosis in pregnancy.

* Erythromycin- in infant- Risk of hypertrophic pyloric stenosis.

ADVERSE EFECT-

Epigastric pain, hypersensitivity,hepatitis

USES-

As an alternative to penicillin, U.R.T.I., Whooping Cough, Chancroid, Skin infection etc.

(F) BROAD SPECTRUM ANTIBIOTICS–

1. TETRACYCLINES
2. CHLORAMPHENICOL
1. TETRACYCLINES
DRUGS -

204
 Tetracycline(250-500mg), Oxytetracycline(250-500mg), Doxicycline(100mg),
Demeclocycline(150-300 mg), Mincocycline(100 mg),.

It is broad spectrum antibiotic

EFFECTIVE AGAINST:

All Gram(+)ve and gram(-)ve cocci

most gram (+)ve bacilli and

Some gram (-)ve bacilli and

Also effective against- Spirochedes, Rickettsia, Mycoplasma, Entamoeba histolytica

&Plasmodia..

Mechanism of action:-

Bacteriostatic, Inhibit protein synthesis by acting on 30s ribosome.

ADVERSE EFFECT-

Liver damage, Kidney damage, Photo toxicity, In children’s discoloration (yellowish) of

bones &teeth, if pregnant women then– Suppression of bone growth in foetus, increase
intra cranial pressure, Antianabolic effect, Diabetes incipidus, hypersensitivity,
suprinfection.

USES-

Mixed Injection, Cholera, Chlamydial Infection, Atypical Pneumonia, Cholera, Plague,

Brucellosis, Rickettsial fever, Acne, Malaria

2. CHLORAMPHENICOL
It is broad spectrum antibiotic

EFFECTIVE AGAINST:

Gram(+)ve and gram(-)ve cocci

most gram (+)ve bacilli and

205
 Some gram (-)ve bacilli and

Also effective against- Spirochedes, Rickettsia, Mycoplasma.

Mechanism of action-

Bacteriostatic, inhibit protein synthesis by acting on 50 s ribosomes.

DOSE- 250-500mg.
ADVERSE EFFECT-
Bone Marrow Depression,Hyper Sensitivity,Gray Baby Syndrome(Due to Deficiency of
Glucuronide Enzyme).

USES-

Entericfever(typhoid),Anaerobic infection, Halicobactorinfluenza(Pyogenic Meningitis),

UTI, Intraocular infection, Conjunctivitis & External ear infection.

(G) OTHER ANTIBIOTICS-

1. Lincosamide-Antibiotic
Inhibit protein synthesis by acting on 50 s ribosomes

Similar to macrolide

Additional-Anaerobes &aerobic gram negative bacilli

Ex-Clindamycin, Lincomycin

2. Glycopeptide- Antibiotic
Inhibit cell wall synthesis

MRSA & gram positive cocci

Ex-Vancomycin, Teicoplanin

3. Oxazolidinone- Synthetic
Inhibit Protien synthesis

206
 VRSA
Linezolid
4. Mupirocin- Antibiotic
Gram positive
5. Fusidic acid- Steroidal Antibiotic
Gram positive.
6. Pleuromutilns-
Inhibit Protein synthesis
Retapamulin- topical treatment of impetigo
7. Glycylcyclines-
Tigecycline- Broad spectrum
8. Streptogramins-Bacteriocidal
Quinpristine-Dalfopristin
9. Polypeptide antibiotic- Bactericidalbut high toxicity
Polymyxin B and Colistin
Detergent like action, effective against gram negative bacteria
Bacitracin
Inhibit cell wall synthesis, effective against gram positive bacreria

** Neosporin powder-

Neomycin + Bacitracin + Polymyxin-B

ANTI TUBERCULAR DRUGS

Drug that are used in the treatment of tuberculosis.

Tuberculosis- very slowly progressive infection

Caused by- mycobacterium tuberculosis/ bovis (gram positive bacilli).

Mainly effects to lungs (pulmonary tuberculosis)

Combination of more than one drug is given in the treatment of T.B. to prevent emergence of
resistance

207
Classification

a. First line- More effective lesser toxic

Ex-Isoniazid, Rifampicin,Pyrazinamide, Ethambutol, Streptomycin.

b. Second line- lesser effective more toxic

Ex-kanamcyin, Amikacin, PAS,Thaiacetazone,Ethionamide,Cycloserine, Ofloxacin,
Levofloxacin etc.

• Isoniazide- Peripheral neuritis, Enzyme inhibitor

• Rifampacin- Orange red colour urine
• Ethambutol- Potical neuritis
• Streptomycin- Aminoglyocoside

• All first line cidal except Ethambutol

• H, Z, E – inhibit mycolic acid synthesis

• R- inhibit DNA dependent RNA synthesis

• H, R, Z –Hepatitis

• H- Rapidly growing

• Z- Slow growing

• R- Spurters

• H, R, E- Both intra & extracellular

• Z- intracellular

• S- Extracellular

• Maximam sterilizing action- Z

• Maximum CSF penetration- Isoniazise

• Minimum CSF penetration- Streptomycin

208
 • S- CI during pregnancy
• Pregnancy-HRE (india)
• Children- HZR
• To prevent latent infection- children- 9 month –H (if HIV then 12 month)
• Mono drug resistance TB- Single First line drug resistance except rifampacin
• Poly drug resistance TB- two or more first line drug resistance both H & R

• MDR TB- Both H & R resistance

ANTI LEPROTIC DRUG

- Drugs that are use in the treatment of leprosy.
Causative agent – mycobacterium laprae
- It is very slowly progressive bacilli gram(+) ve.
- It mainly affects to – skin,nerves.

DRUGS

I. Sulfones:
Ex.dapsone- LAPROSTSTIC
Dose- 25-100 mg.
Similary action with sulfonamide (Inbition of PABA)
HaemolyticAnaemia
CI- G6PD deficiency

II. PHENAZANINE devivative:-

Ex.clofazimine- Reddish black colur of skin
Dose -50-100 mg
III. Antitubercular drugs:
Ex- Rifampin, Ethionamide

IV. Antibiotics-
Ex-Claritromycin, Ofloxacin, Mincocycline

• Multi bacillary leprosy- 12 month- RCD

• Paucibacillary leprosy- 6month- RCD

209
ANFTIUNGAL DRUGS
Classification
Topical antifungal- Clotrimazole, Miconazole
Systemic antifungal- Fluconazole
According to mechanism of action-
a. Drugs acting on cell membrance -.ketoconazole, Amphotericin B,
Terbinafine,fluconazole, Itraconazole
b. Drugs affecting cell division(microtubules)- Griseofulvin
c. Drugs affecting nucleic acid synthesis - 5-FC(flucytocine)

ANTI MALARIAL
CLASSIFICATION-
1. Drugs effective against Pre &Exoerythrocytic phase (Tissue schizontocide)-

Primaquine

2. Drugs effective against Eythrocytic phase ( Erythrocytic schizontocide) -Chloroquine,

Artemisinin, Quinine, Mefloquine, Pyrimethamine

3. Gamatocide- Primaquine

4. Antibiotics e.g. tetracycline

➢ chloquine acts by inhibiting polymerization of hemoglobin to form hemozoin

➢ primaquine causes hemolythicanemia patients of G6– PD
➢ Casual prophylaxis- target preerythocytic phase- Primaquine
➢ Suppressive prophylaxis- Erythrocytic phase- CQ, MQ & Doxycycline
➢ Clinical cure-Erythrocytic schizontocide-Q, CQ, Sulfonamide, Doxycycline
➢ Radical cure- Exoerythrocytic phase(Vivax)- Primaquine
➢ Gametocide- Primaquine
➢ Vivax- CQ + PQ
➢ Vivax –CQ resistance- Q + D + PQ
➢ Falciparum-CQ + PQ or Sulp + Pyre + PQ
➢ Falciparum CQ resistance- Q + D or Arte +Sulp + Pyre or Arte + Lume

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ANTI AMOEBIC
CLASSIFICATION-

1. Luminal
Ex- Diloxanide furoate, Tetracycline
2. Tissue Amoebicide-
a. Extraintestinal- Choloquine
b. both intestinal and extra intestinal- Metronidazole, Tinidazole, Secnidazole,
Emetine

➢ Metronidazole shows disulfiram like action with alcohol

➢ Metronidazole- Cacinogenic
➢ Metronidazole- Also effective in anaerobic bacterial infection
➢ Soidiumstilbogluconate- Kalaazar
➢ Pentamidine- Kalaazar

ANTIVIRAL DRUGS
Classification

Anti-HerpesDrugs
Ex- Idoxuridine, Acyclovir, Famiciclovir, Ganiciclovir, Foscarnet

• Anti-herpes Drugs- Inhibit viral DNA

• Acyclovir- Effective against Herpes simplex-I & II & Varicella zoster

• Ganciclovir- DOC -CMV

Anti Influenza Drugs

211
 Ex- Amantadine, Rimantadine, Oseltamavir, Zanamavir

• Amantidine&Rimantidine- Prevent uncoating of Influenza-A virus

(Decreaseduration of symptoms of influenza)

• Oseltamavir&Zanamavir- Prevent virion release- Effective against both

Influenza-A & Influenza-B

Anti-HepatitsDrugs

Ex- Ribavirin, Lamivudine, Entecavir, INF α

• Anti-Hepatits Drugs- Effective against- Hepatitis-B & Hepatitis-C virus

• INF α- Use in Rx of chronic Hepatitis-B virus infection

• INF α + Ribavirin- Acute & chronic Hepatitis-C virus infection
• Entecavir- DOC- Chronic Hepatitis-C virus infection

Anti-retroviral Drugs

a. NRTI- Zidovudine (AZT),Stavudine, Lamivudine,Abacavir, Tinofovir

b. NNRTI- Nevirapine, Efavirenz, delavirdine,
c. PI- Ritonavir, Saquinavir, Lopinavir, Indinavir
d. ENTRY Inhibitor-Ibalizumab
e. INTEGRASE Inhibitor- Raltegravir, Dolutegravir

• Reverse transcriptase inhibitor-Competitive inhibitor (NRTI), Non-

competitive inhibitor (NNRTI)
• PI- Inhibit maturation of infectious virion
• ENTRY Inhibitor- Prevent entry/ Fusion
• INTEGRASE Inhibitor- prevent viral DNA integration in nuclear genome

• ART- 2NRTI + 1NNRTI/II or 2NRTI + 1PI

• Infant prophylaxis- Z + N for 6 weeks

• PEP- T + L + PI for 28 days (start within 72 hours)

• Nevirapine- Use to prevent vertical transmission better option Zidovudine

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ANTI HELMINTHIC DRUG
Drugs that either kill (vermicide) or expel (vermifuge) infesting helminths.

Ex- Albendazole, Mebendazole, Thiabendazole, Praziquental, Ivermectine, Niclosemide,

Piperazine, Pyrental pamoate, Levimisole, Diethyl carbemazine.

Effective against various worms belonging to Nematodes,Cestodes& Trematodes.

Nematodes-

Round worm (Ascaris)-Albenda, Mebenda

Hook worm (Ancylostoma)- Pyrantel,Albenda, Mebenda

Thread worm (Enterobious)-Pyrantel,Albenda, Mebenda

Whip worm (Trichuris)-Albenda, Mebenda

Filaria (Wucheria- DEC) (Burgia- Ivermectin)

Cestodes-

Tape worm (Taenia- Praziquental) (Neurocysticercosis-Albendazole)

Trematodes-

Flukes (Scistosoma)-Praziquental

DEC- Use in Rx of Eosinophilia

Ivermectin (6 mg)- Orally effective drug in scabies

213
8. ANTI CANCER DRUGS

214
 ANTI CANCER DRUGS

1. Cytotoxic drugs:
a. Alkylating agent-Drugs that kill fast dividing cells by alkylation (DNA)
Ex-Cyclophosphamide, Chlorambucil, thio-TEPA, Ifosfamide, Melphalan,
Busulfan, Procabazine
b. Antimetabolites- Affect nucleic acid synthesis
Ex-Methotrexate, 6-MP, 5-FU, 6-TG, Azathioprine
c. Plant derivatives- Interfere in cell cycle
Ex- vincristine, vinblastine, paclitaxel, docetaxel, Etoposide.
d. Antibiotics-Interfere with DNA template function
Ex- Doxorubicin, Bleomycin, Mitomycin-C, Actinomycin-D,
Daunorubicin
e. Others-
Ex- Cisplatin, carboplatin (Cross linking of DNA) Imatinib (tyrosine kinase
inhibitor)

• Acute leukaemia- Vincristine, 6-MP, Cyclophosphamide

• Chronic lymphatic leukaemia- Chlorambucil, Cyclophosphamide
• Chronic Myeloid leukaemia- Busulfan, Imatinib
• Hodgkin’s disease- Vinblastine, Dacarbazine
• Multiple Myeloma- Melphalan, Prednisolone, Cyclophosphamide
• Wilms Tumour- Actinomycin-D, Vincristine
• Cancer lung- Cyclophosphamide, Vincristine, Doxorubicin
• Carcinoma Cervix- Mitomycin, Cisplatin
• Osteogenic Sarcoma- MTX, Doxorubicin
• Haemorrhagic Cystitis- Cyclophosphamide, Ifosfamide Rx- Mesna
• Cyclophosphamide-Alopecia & SIADH
• Busulfan- Pulmonary fibrosis, adrenal insufficiency & hyperpigmentation
• Cisplatin- Emesis, nephrotoxicity & Ototoxicity
• Procarbazine- Most leukemiogenic
• 5-FU- Hand & foot syndrome
• Bleomycin-Pulmonary fibrosis
• Doxorubicin&Daunorubicin- Cardiotoxic

2. Drugs affecting hormonal balance:

215
 Prednisolone- Acute childhood leukaemia & breast cancer
Ethinylestradiol- Prostate carcinoma
Tamoxifen- Breast carcinoma
Letrozole-Breast carcinoma
Anastrtazole-Breast carcinoma
Flutamide- Prostate Carcinoma
Bicalutamide- Prostate Carcinoma
Finasteride- Prostate Carcinoma
Nafarelin- Prostate/Breast carcinoma
Hydroxyprogesterone- Endometrial carcinoma

❖ All cancerous drugs are highly toxic – effect on all rapidly dividing and normal cells

ADVERSE EFFECT

a. Bone marrow toxicity – Anaemia& Granulocytopenia

b. Alopecia – baldness
c. Live, kidney, skin toxicity etc.
d.
A. TABLE OF CHOICE OF DRUGS
Disease Drug of choice
Chloramphenicol resistant typhoid Ciprofloxacin
Whooping cough,diphtheria Erythromycin
Mycoplasma infection Erythromycin
Cholera prophylaxis Doxycycline
Plague Streptomycin
Genital prophylaxis Acyclovir
Kala-azar Pentamidine
Syphills Penicillin G
Cellulities Nafcillin (or) oxacillin
Actinomycosis Penicillin G
Leprosy Dapsone
Ascariasis Albendazole
Hook worm infection Mebendazole
Giardiasis, vaginitis Metronidazole
Cutaneous candidiasis Nystatin powder (or) cream
Systemic fungal infection Amphotericin B
Malaria Quinine + doxycycline
Plamodiumfelciperum Artesunate

B. TABLE OF IMPORTANT SIDE EFFECT

Drugs Important side effect

216
 Sulfonamides Crystalluria
Ciprofloxacin Affects bone and cartilage
Pencillins Anaphylaxis
Erythromycin Cholestatic jaundice
Clindamycin Pseudomembroanous colitis
Streptomycin Ototoxicity, neuromuscular blockade
Tetracyclins Fanconi like syndrome, photo sensitivity,
dental and bone effect
Chloramphenicol Gray baby syndrome, bone marrow
depression
Ketoconazole Heptotoxicity
INH Peripheral neuritis
Rifampicin Hepatotoxicity, orange red coloured
secretions
Ethmbutol Optic and peripheral neuritis
Metronidazole Metallic taste, nausea
Anti cancer drugs Bone marrow depression, GIT ulceration,
perforation
Phenytoin Gum hypertrophy, hirsutism
Morphine Respiratory depression, addiction
Aspirin Salicylism, GIT ulceration
Paracetamol Hepatotoxicity
Phenylbutazone Bone marrow depression
Halothane Malignant hyperthermia
N2o Diffusion hypoxia
Barbiturates Respiratory depression, dependence
Atropine Dry mouth
Alpha blockers Reflex tachycardia
Minoxidil Hirsutism

C. DRUGS INTERACTION WITH ANTIBIOTIC

Antibiotic Interacting drug Drug reactions
Metronidazole Warfarin Potentiation of anti
coagulation
Griseofulvin Alcohol Dilsulfiram reaction
Metronidazole Alcohol Dilsulfiram reaction
Rifampicin Warfarin Diminished effects of
warfarin
Tetracycline Penicillin Inhibits of action of
penicillin
Tetracycline lithium Increase lithium retention
Chloramphenicol Warfarin Potentiation of anti
coagulation

217
 D. MECHANISM OF ACTION OF IMPORTANT ANTIBIOTICS
Drugs Mechanism of action
Poly mixins, bacitracin,amphotericim B Alter cell wall permeability
Pencillin, cephalosporins, vancomycin Inhibit cell wall synthesis
Tetracycline, chloramphenicol Inhibit protein synthesis
erythromycin
Rifampicin,metronodazole Interface with DNA function
Aminoglycosides, streptomycin Misleading of m-RNA
Anti viral drugs Interfere with DNA synthesis
Fluroquinolones-ciproflaxacin Inhibit DNA gyrase

E. ANTI DOTE OF SOME RUGS

Poison Antidote
Paracetamol N-acetyl cysteine
Mercury/arsenic BAL (british anti lewisite)
CO Oxygen
Cynide Amylnitrate
Opioids Naloxone
Atropine Physostigmine
Oraganophosphates Antropine, pralidoxime
Benzodiazepines Flumazenil
Fluorides Milk
Iron Desferroxime
Methtrexare Leucovorine
Heparin Protamin sulphate
Lead BAL, Dimercaprol
Benzodiazepines Flumazenil
Opoids (morphine) Naloxone
Vit. K Oral anti coagulant
Methnol Ethenol, fomepizole
Organophosphate Atropine, pralidoxime
LSD Phenothiazine
Histamine Adrenaline
Atropine Physostigmine

EMERGENCY DRUGS

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Salbutamol
Treatment of an acute asthma attack
Diphenhydramine
Treatment of allergic reaction
Epinephrine
Treatment of cardiac arrest, anaphylaxis, or acute asthma attack
Glucose, oral (usually in a
tube) Treatment of hypoglycemia
Nitroglycerin
Treatment of an acute anginal attack

Oxygen Treatment of emergency situations in which pt. is having difficulty

breathing
Atropine
Increase in cardiac rate

B-Blockers Reduction in blood pressure

Dextrose 50% IV solution for hypoglycemia; when pt. can't swallow

Diazepam/alprazolam
Initial treatment of status epilepticus
Glucagon
Management of severe hypoglycemic reactions
Hydrocortisone
Treatment of allergic reactions, anaphylaxis, or adrenal crisis
Morphine
Opioid analgesic used to treat the pain associated with MI
Spirits of ammonia
Treatment of syncope
Bretylium
Treatment of arrhythmias

Procainamide
Treatment of arrhythmias

Treatment of arrhythmias
Verapamil
Treatment of arrhythmias
Lidocaine
Treatment of benzodiazepine overdose
Flumazenil
Treatment of opioid overdose
Naloxone

1. AMINOPHYLLINE- Antiasthmatic& COPD Preparations

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 Loading dose: 5 mg/kg (ideal body wt). Maintenance: 0.5 mg/kg/hr.

2. AMIODARONE HYDROCHLORIDE-Ventricular and supraventricular arrhythmias.

Dosage: 200 mg 3 times/day

3. ATROPINE SULFATE- Bradycardia 500 mcg every 3-5 mins, Organophosphorus poisoning
pre anesthetic medication

4. CALCIUM GLUCONATE- Hypocalcaemia 10-50 mmol/day. IV Hypocalcaemic tetany

2.25 IV infusion. Antidote in severe hypermagnesaemia; Severe hyperkalaemia 10 mL of
10%

5. CAPTOPRIL-ACE Inhibitors-HTN, Heart failure, MI. . HTN in diabetic nephropathy.

6. CLONIDINE- Antihypertensives- HTN, Migraine prophylaxis.

7. DIAZEPAM- relief of anxiety, agitation & tension due to psychoneurotic states & transient
situational disturbances
Dosage: 10mg/2ml

8. DIGOXIN-Inotropics-Cardiac failure accompanied by atrial fibrillation; management of

chronic cardiac failure where systolic dysfunction or ventricular dilatation is dominant;
management of certain supraventricular arrhythmias, particularly chronic atrial flutter &
fibrillation.
Dosage: 5mg/2ml

9. DIPENHYDRAMINE- antihistamine-Hay fever, urticaria, vasomotor rhinitis, angioneurotic

edema, drug sensitization, serum & penicillin reaction, contact dermatitis, atopic eczema,
other allergic dermatoses, pruritus, food sensitivity, parkinsonism, motion sickness.Dosage:
50mg/ml

10. EPINEPHRINE- Acute asthmatic attacks, Advanced cardiac life support

Dosage: 1mg/ml

11. FUROSEMIDE- loop diuretics- edema, hypertension

Dosage: 20mg/2ml

12. HYDRALAZINE HYDROCHLORIDE- antihypertension- For hypertensive patient

Dosage: 20mg/ml

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13. HYDROCORTISONE SODIUM SUCCINATE- endocrine, hematologic, rheumatic &
collagen disorders, dermatologic, ophth, GI, resp & neoplastic diseases, edematous states,
control of severe incapacitating allergic conditions, TB meningitis w/ subarachnoid block or
impending block when used concurrently with appropriate anti-TB chemotherapy, shock
secondary to adrenocortical insufficiency or shock unresponsive to conventional therapy
when adrenocortical insufficiency may be present
100 mg/ 2 mL, 250 mg/ 2 mL

14. ISOSORBIDE-5- MONONITRATE- prophylactic treatment of angina pectoris.

Dose-30 mg, 60 mg

15. ISOSORBIDE DINITRATE- unresponsive left ventricular failure secondary to acute MI,
severe or unstable angina pectoris
Dose: 10 mg/10mL

16. MAGNESIUM SULFATE- anticonvulsant- prevention & control of convulsions in patients

w/ preeclampsia or eclampsia, control of HTN,
Dosage: 250 mg/10 mL

17. MEPERIDINE HYDROCHLORIDE -relief of moderate to severe pain, pre-op medication,

support of anesth&obstet analgesia
Dosage: 100 mg/ 2mL

18. METOCLOPRAMIDE- antiemetic & anti-spasmodic

Dosage: 10 mg/ 2mL

19. MIDAZOLAM HYDROCHLORIDE-hypnotics & sedatives- Dosage: 5mg/5mL

20. MORPHINE SULFATE- Relief of moderate to severe pain not responsive to non-narcotic
analgesics. Premed. Analgesic adjunct in general anesthesp in pain associated w/ cancer, MI
& surgery. Alleviates anxiety associated w/ severe pain. Hypnotic for pain-related
sleeplessness.
Dosage: Adult 5-20 mg IM/SC 4 hrly.

21. NICARDIPINE HYDROCHLORIDE- IV infusion Dilute to 10-20 mg/100 mL (conc of

1.01-0.02%). Indication: Hypertensive emergencies or urgencies, peri-op & post-op HTN,

22. NTG PATCH-Prevention of angina pectoris due to coronary artery disease

Dosage: Starting dose: 0.2-0.4 mg/hr. Dosing schedule: Daily patch-on period of 12-14 hr&

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 daily patch-off period of 10-12 hr.

23. PARACETAMOL-Analgesics (Non-Opioid) & Antipyretics

Dosage: Adult &childn ≥10 yr 2-3 mL, ≤10 yr 1-2 mL. Depending on severity of case, dose
may be repeated 4 hrly. In severe cases, dose may be administered by IV very slowly

24. PHENYTOIN- Dosage: Adult Initially 100 mg tid. Maintenance: 300-400 mg daily.
indication: Tonic-clonic& complex partial (psychomotor, temporal lobe), prevention &
treatment of seizures occurring during or following neurosurgery

25. TERBUTALINE- Indication: For reversible airways obstruction, in asthma, COPD.

Decreases uterine contractility & may be used to arrest premature labor

26. VERAPAMIL HYDROCHLORIDE-, chronic coronary insufficiency, angina pectoris,

paroxysmal supraventricular tachycardia, tachyarrhythmias, long-term treatment after MI.

27. IPRATROPIUM INHALATION- Bronchodilator for treatment of bronchospasm associated

w/ COPD, including chronic bronchitis, emphysema and asthma- 0.5 mg/2 mL

28. FENOTEROL/IPRATROPIUM BROMIDE-prevention and treatment of symptoms in

chronic obstructive airway disorders with reversible bronchospasm

29. BUDESONIDE-regular treatment of asthma where use of a combination (inhaled

corticosteroid and long acting beta 2 agonist) is appropriate

30. TERBUTALINE SULFATE- Indication: relief of bronchospasm in obstructive airway

diseases-Dose: Adult 5-10 mg, Children 2-5mg

31. HEPARIN SODIUM-Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)

Dosage: 5000 iu/1 mL; 25000 iu/1 mL
treatment and prophylaxis of thromboembolic disorders
Have on hand protamine sulfate, specific heparin antagonist

32. ESMOLOL HYDROCHLORIDE-Beta blockers- supraventricular tachycardia; post-

operative tachycardia or hypertension; non-compensatory sinus tachycardias; intra-operative
tachycardia or hypertension; unstable angina, non ST segment elevation MI
Dosage: 100mg/10ml

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33. D- 50%
Indication: for hypoglycemia

34. POTASSIUM CHLORIDE

Dosage: 40 meqs/20 ml
Indication: for hypokalemia, acute MI

35. SODIUM BICARBONATE- metabolic acidosis, systemic or urinary alkalinization, antacid,

cardiac arrest
Dosage: 10mEq/10ml; 50mEq/50ml

36. DOPAMINE- shock and hemodynamic imbalances, hypotension

Dosage: 40 mg/Ml; 80 mg/mL; 160 mg/mL

37. DOBUTAMINE- increased cardiac output in short term treatment of cardiac decompensation
caused by depressed contractility
Dosage: 12.5 mg/mL

38. LIDOCAINE -Local anesthetic, ventricular arrhythmias caused by MI, cardiac manipulation
or cardiac glycosides
Dosage: 2% - 5%
39. MANNITOL- test dose for marked oliguria or suspected inadequate renal function, oliguria,
to reduce intraocular or intracranial pressure, diuresis in drug intoxication
Dosage: 5% , 10%, 15%, 20%, 25% in 500cc/1,000cc

40. DEXTROSE 5% IN WATER (D5W) SOLUTION- fluid replacement and caloric

supplementation in patients who can’t maintain adequate oral intake or are restricted from
doing so- Dosage: 250ml bottles (5g dextrose/100ml water)

USE OF DRUGS DURING PREGNANCY

The safety of approximately 50 % of medications for the mother and fetus remains unknown

FIVE CATEGORIES

Class A

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 No risk in controlled human studies
Examples
Acetaminophen
Pyridoxine (Vitamin B6)
Class B
No risk in controlled animal studies

Examples
Amoxicillin
Cephalosporin antibiotics

Class C
Small risk in controlled animal studies
Examples
1. Codeine
2. Dicloxacillin

Class D
Strong evidence of risk to the human fetus
Examples
Rifampicin
Fluoroquinolones
Aminoglycosides

Class X
Never to be used in Pregnancy
Very high risk to the human fetus
Examples
Thalidomide
Oral contraceptive pills
Misoprostol

LIST OF COMMONLY USED DRUGS IN PREGNANCY AND

THEIR CATEGORIES
Drugs Category
Analgesics and Antipyretics B and C
Acetaminophen B
Phenacetin B
Aspirin C

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Drugs Category
Antiemetics B and C
Doxylamine B
Meclizine B
Cyclizine B
Dimenhydrinate B
Antibiotics B, C and D
Penicillin, Ampicillin, Amoxycillin, B
Cloxacillin Cephalosporins B
Erythromycin B
Gentamicin C
Amikacin C/D
Streptomycin D
Sulphonamides B/D
Tetracyclines D
Amoebicides B
Metronidazole
Anthelmentics B
Piperazine
Mebendazole
Antimalarials C
Antifungals C
Anti TB Drugs B and C
Ethambutol B
INH C
Rifampicin C
Pyrazinamide C
PAS C
Vitamins
B,C,D,E,folic acid A
Hormones
Thyroxin A
Androgens X
Estrogens X
Progestogens-
Hydroxyprogestrone D
Medroxyprogestrone D
Norethindrone X
Norgestrel X

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Drugs Category
Bronchodilators C

MEDICATIONS CONTRAINDICATED IN PREGNANCY

Drug Comments
Vitamin A and its derivatives
Significant risk of spontaneous abortion and risk of many
including isotretinein,
significant anomalies
accutane and etretinate.
May cause kidney damage in the fetus when used in II and III
ACE inhibitors trimester, decrease in the amount of amniotic fluid and
deformities of face, limbs and lungs
Use during I trimester produces defects like nasal hypoplasia and
a depressed nasal bridge; termed as Fetal warfarin Syndrome.
Anticoagulants- warfarin
Use during II and III trimesters is associated with increased risk
of fetal malformations
Safe but if taken for long time osteoporosis and decrease in
- Heparin
number of platelets in pregnant women occurs
Estrogen and Androgens Genital tract malformations
Thyroid preparations-
Methimazole Overactive and enlarged Thyroid gland
Carbimazole Overactive and enlarged Thyroid gland
Radioactive iodine Underactive Thyroid gland in fetus
Propylthiouracil Safe
Anticonvulsants-
Carbamazepine Risk of birth defects
Bleeding problem in the newborn which can be prevented if
pregnant woman takes Vit. K by mouth every day for a month
Phenytoin, Phenobarbitone
before delivery or if the newborn baby is given an injection of
Vit. K soon after birth
Risk of birth defects.
Trimethadione Increased risk of miscarriage in the women
Increased risk of birth defects in fetus; including a cleft palate
Sodium valproate and abnormalities of the heart, face, skull, hands or abdominal
organs
Birth defects (mainly of the heart), lethargy, decreased muscle
tone, underactivity of Thyroid gland and nephrogenic diabetes
Antidepressants- Lithium insipidus in the new born. Ebstein's anomaly (tricuspid valve
malformation) has been reported in a number of foetuses exposed
to this drug

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Drug Comments
NSAIDs
Delay in start of labor, premature closing of ductus arteriosus,
Aspirin and other Salicylates jaundice, brain damage in the fetus and bleeding problems in the
woman during and after delivery and in the newborn
Slowed bone growth, permanent yellowing of the teeth and
Antibiotics- Tetracycline
increased susceptibility to cavities in the body
Chloramphenicol Gray Baby Syndrome
Ciprofloxacin Possibility of joint abnormalities (seen in animals)
Kanamycin and Streptomycin Damage to fetus's ear resulting in deafness (risk of ototoxicity)
Sulfonamides Jaundice and brain damage in newborn

Antineoplastic agents-

Birth defects such as less than expected growth before birth,

Busulfan underdevelopment of lower jaw, cleft palate, abnormal
development of skull bones, spinal defects, ear defects and club
foot.
Chlorambucil
Cyclophosphamide
Methotrexate
A very low level of sugar in the blood of newborn. Inadequate
Oral Hypoglycemic drugs
control of diabetes in the pregnant woman
Chlorpropamide
Tolbutamide

List of some of the drugs whose use is contraindicated during pregnancy along with the harmful
damaging effects they may produce on the fetus

USE OF DRUGS DURING BREAST FEEDING

Drugs safe to take in usual doses
NAME OF DRUG USE
Acetaminophen Used for pain relief
Acyclovir and valacyclovir Antiviral for herpes infections

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Antacids Used to treat upset stomachs
Bupivacaine A local anesthetic
Caffeine A stimulant
Antibiotics for lung, ear, skin, urinary tract,
Cephalosporins
throat, and bone infections
Clotrimazole Used to treat yeast and fungal infections
Contraceptives (progestin-only) Used for birth control
Used to treat inflammation of joints and other
Corticosteroids
conditions
Decongestant nasal sprays Used to treat stuffy noses
Digoxin Used to treat heart problems
Erythromycin Used for skin and respiratory infections
Fexofenadine Antihistamine for allergies and hay fever
Fluconazole Used to treat yeast infections
Heparin and LMW heparins Used to keep blood from clotting
Ibuprofen Used for pain relief
Inhalers, bronchodilators, and corticosteroids Used for asthma
For diabetes; dosage required may drop up to
Insulin
25 percent during lactation
Laxatives, bulk-forming and stool softening Used to treat constipation
Lidocaine A local anesthetic
Loratadine Antihistamine for allergies and hay fever
Low molecular weight heparins (enoxaparin,
Anticoagulants
dalteparin, tinzaparin)
Magnesium sulfate Used to treat preeclampsia and eclampsia
Methyldopa Used to treat high blood pressure
Used to prevent or control bleeding after
Methylergonovine (short courses)
childbirth
Metoprolol A beta-blocker used to treat high blood pressure
Miconazole Used to treat yeast infections
Used for high blood pressure and Raynaud's
Nifedipine
syndrome of the nipple
Penicillins Used to treat bacterial infections
A beta blocker used to treat heart problems, and
Propranolol
high blood pressure
Theophylline Used to treat asthma and bronchitis
Tretinoin Cream used for acne
Thyroid replacement Used to treat thyroid problems
Vaccines (except smallpox and yellow fever)
Vancomycin An antibiotic

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Verapamil Used for high blood pressure
Warfarin Used to treat or prevent blood clots

Drugs probably safe in usual doses

Little is known about the effects of these drugs on a breastfeeding infant, but if there is an effect,
it will probably be mild. In rare cases, a child has an allergic reaction.

NAME OF DRUG USE

ACE inhibitors Used to treat high blood pressure
Used to treat intestinal and gall bladder spasms; may reduce
Anticholinergic agents
milk supply
Anticonvulsants Used for seizures and mood disorders
May reduce milk supply and cause infant drowsiness or
Antihistamines
fussiness
Antituberculars Used to treat tuberculosis
Used to suppress the immune system following organ
Azathioprine
transplants
Barbiturates (except
For sedation and tension headaches
phenobarbital)
Bupropion For depression
Clindamycin Used to treat abdominal and vaginal infections
Used to treat congestion associated with colds or allergies;
Oral decongestants
often reduces milk supply
Ergonovine (short course) Used to treat uterine bleeding. May reduce milk supply.
Fluconazole Antifungal
Gadolinium Contrast agent for MRI studies
Haloperidol Used to treat psychosis
Histamine H2 blockers Used to treat stomach problems
Labetalol Used for high blood pressure; caution with preterm babies
Hydrochlorothiazide (low doses) Diuretic for high blood pressure
Lorazepam Used to treat anxiety
Used for hyperthyroidism; less than 20 mg/day is probably
Methimazole
safe
Used for gastrointestinal problems and to increase milk
Metoclopramide
supply
Midazolam Sedative used in anesthesia
Naproxen Used for pain relief; okay if baby is at least 1 month old
Oxazepam Used to treat anxiety

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 Paroxetine Used to treat depression
Phenothiazines
Propofol Sedative used in anesthesia
Propylthiouracil (PTU) Used to treat hyperthyroidism
Quinidine Used to treat heartbeat irregularities
Quinolone antibacterials Treatment of urinary tract infections
Salicylates (occasional use) Used for pain relief
Sertraline Used to treat depression
Spironolactone Used to treat high blood pressure
Sumatriptan Used to treat migraines
Tetracyclines < 14 days Used to treat acne and urinary tract infections
Trazodone Used for depression and sleep
Tricyclic antidepressants (avoid
Used to treat depression; nortriptyline preferred
doxepin)
Verapamil Used for high blood pressure

CONTRAINDICATED DRUGS IN LACTATION

1. Medications that decrease milk production
1. Bromocriptine
2. Diuretics
2. Chemotherapeutic Medications
1. Cyclophosphamide
2. Cyclosporine
3. Doxorubicin
4. Methotrexate
5. Gold salts
6. Propylthiouracil
7. Methimazole

3. Radioactive Chemicals used in Nuclear Medicine

1. Gallium-67 (in Breast Milk up to 14 days)
2. Indium-111 (in Breast Milk up to 20 hours)
3. Iodine 131 (in Breast Milk up to 14 days)
4. Radioactive Sodium (in Breast Milk up to 96 hours)
5. Technetium-99m (in Breast Milk up to 3 days)
4. Cardiovascular medications to avoid in Lactation
1. Avoid Atenolol and use other Beta Blockers only with caution
2. Avoid Acebutolol
3. Avoid Amiodarone

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5. Miscellaneous Medications
1. Dextroamphetamine
2. Ergotamine
3. Lithium
4. Metronidazole
5. Chloramphenicol
6. Potassium iodide
7. Phenindione (Anticoagulant)
6. Drugs of Abuse
1. Amphetamine
2. Cocaine
3. Heroin
4. Marijuana
5. Nicotine
6. Phencyclidine

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