Pharmacological Classification Of Drugs PDF

 Pharmacological CLASSIFICATION OF DRUGS with Doses and Preparations  Pharmacological CLASSIFICATION OF DRUGS with Doses and Preparations FOURTH EDITION KD Tripathi MD Ex-Dire...

 Pharmacological CLASSIFICATION OF DRUGS with Doses and Preparations  Pharmacological CLASSIFICATION OF DRUGS with Doses and Preparations FOURTH EDITION KD Tripathi MD Ex-Director-Professor and Head of Pharmacology Maulana Azad Medical College and associated LN and GB Pant Hospitals New Delhi ® JAYPEE BROTHERS MEDICAL PUBLISHERS (P) LTD New Delhi St Louis (USA) Panama City (Panama) London (UK) Ahmedabad Bengaluru Chennai Hyderabad Kochi Kolkata Lucknow Mumbai Nagpur Published by Jitendar P Vij Jaypee Brothers Medical Publishers (P) Ltd Corporate Office 4838/24 Ansari Road, Daryaganj, New Delhi - 110002, India Phone: +91-11-43574357, Fax: +91-11-43574314 Registered Office B-3 EMCA House, 23/23B Ansari Road, Daryaganj, New Delhi - 110 002, India Phones: +91-11-23272143, +91-11-23272703, +91-11-23282021, +91-11-23245672 Rel: +91-11-32558559, Fax: +91-11-23276490, +91-11-23245683 e-mail: [email protected], Website: www.jaypeebrothers.com Offices in India Ahmedabad, Phone: Rel: +91-79-32988717, e-mail: [email protected] Bengaluru, Phone: Rel: +91-80-32714073, e-mail: [email protected] Chennai, Phone: Rel: +91-44-32972089, e-mail: [email protected] Hyderabad, Phone: Rel:+91-40-32940929, e-mail: [email protected] Kochi, Phone: +91-484-2395740, e-mail: [email protected] Kolkata, Phone: +91-33-22276415, e-mail: [email protected] Lucknow, Phone: +91-522-3040554, e-mail: [email protected] Mumbai, Phone: Rel: +91-22-32926896, e-mail: [email protected] Nagpur, Phone: Rel: +91-712-3245220, e-mail: [email protected] Overseas Offices North America Office, USA, Ph: 001-636-6279734 e-mail: [email protected], [email protected] Central America Office, Panama City, Panama Ph: 001-507-317-0160, e-mail: [email protected] Website: www.jphmedical.com Europe Office, UK, Ph: +44 (0) 2031708910, e-mail: [email protected] Pharmacological Classification of Drugs with Doses and Preparations © 2010, KD Tripathi All rights reserved. No part of this publication should be reproduced, stored in a retrieval system, or transmitted in any form or by any means: electronic, mechanical, photocopying, recording, or otherwise, without the prior written permission of the author and the publisher. This book has been published in good faith that the material provided by author is original. Every effort is made to ensure accuracy of material, but the publisher, printer and author will not be held responsible for any inadvertent error(s). In case of any dispute, all legal matters are to be settled under Delhi jurisdiction only. First Edition : 1986 Second Edition : 1990 Third Edition : 2006 Fourth Edition : 2010 ISBN 978-93-5025-078-5 Typeset at JPBMP typesetting unit Printed at Ajanta Offset  Preface A systematized listing of drugs according to their primary actions, mechanisms, chemical nature, clinical uses and/ or other characterstics is the first step to learn about them. The mental exercise to prescribe a drug for a patient starts with identifying the class of drugs to be prescribed and then selecting the specific member most appropriate for that patient according to its subclass/group/individual characteristic. For example, the first thing one decides is whether an analgesic or an antihypertensive or an anti- biotic is to be prescribed; then proceeds to consider which type of analgesic (opioid/nonopioid), or antihypertensive (β blocker/ACE inhibitor, etc.), or antibiotic (β-lactam/ fluoroquinolone, etc.) is required and then which specific member is most suitable. On the other hand, every drug is known by its class and subclass, e.g. furosemide is a high-ceiling diuretic, glibenclamide is a sulfonylurea antidiabetic. Thus, the importance of grouping and compartmentalizing drugs cannot be over-emphasized. The phenomenal increase in the number of drugs in recent years has further underscored the need for drug classifications. However, drug classifications have been criticised for being arbitrary and imperfect because of nonuniform criteria often adopted and frequent lack of watertight distinctions among drugs of different subgroups. Nevertheless, basing on pharmacological differences and applying practical criteria, meaningful drug classifications vi Preface can be devised. Though, any drug has multiple actions/ properties, it can be designated by the most outstanding one. For example, labelling atenolol as a cardioselective β blocker summarises its actions, uses, etc. This booklet has adopted such a pragmatic approach and presented classifications of drugs which have been accepted by a wide section of professionals/students dealing with drugs. The present edition has been thoroghly revised and updated to include drugs marketed till Dec. 2009. To be useful to medical/pharmacy students as well as to practitioners, the doses (including pediatric doses wherever relevant), frequency and route(s) of administra- tion along with leading brand names of drugs and different types of dosage forms (oral, parenteral, topical, etc.) are listed distinctively after each class of drugs. Thus, essential prescribing information has been incorporated. Single drug formulations are mainly mentioned. Combined drug formulations find a place wherever important or relevant. The listing of brand names is restricted to only 1–4 per drug, and is not exhaustive. Synonyms and alternative names of drugs and classes of drugs are also mentioned. Two separate indices, one of nonproprietary (generic) names and the other of proprietary (brand) names of drugs have been provided for ready reference. It is hoped that the booklet will coutinue to serve as an aid to remembering drug names, knowing about them, and prescribing them correctly. The credit for meticulous production of this booklet goes to the staff of M/s Jaypee Brothers. New Delhi K.D. Tripathi 6th April 2010  Explanatory Notes 1. The proprietary (brand) names appear in capital letters. The information on dosage form(s) is printed in maroon colour. 2. The doses and regimens are given in smaller type, while nonproprietary (generic) names appear in bigger type. 3. If no brand name of a drug is listed, it is not currently marketed in India, or is marketed only in combina- tions. This can be found out from the composition of the combined formulations given. 4. If the route of administration is not specified, the drug is administered only orally, and the dose mentioned is the oral dose. 5. Drug doses mentioned without specifying frequency of administration indicate the quantity for a single dose.  Abbreviations amp Ampoule AP Action potential BD Twice daily BHP Benign hypertrophy of prostate BSA Body surface area cap Capsule Ch Child dose cm Centimeter CR Continuous release Distab Dispersible tablet DS Double strength DTPA Diethylene triamine pentaacetic acid e.c. Enteric coated ER Extended release ERP Effective refractory period ext Extract g Gram GITS Gastrointestinal therapeutic system hr hour i.d. Intradermal i.m. Intramuscular inj Injection IU International unit i.v. intravenous kg Kilogram L Litre LES Lower esophageal sphincter x Abbreviations liq Liquid m Meter max Maximum mEq Milliequivalent mg Milligram min Minute ml Millilitre MR Modified release MU Mega (million) unit MW Molecular weight μg Microgram OD Once daily oint Ointment Pot. Potassium QID Four times a day rDNA Recombinant deoxyribonucleic acid s.c. Subcutaneous s.l. Sublingual Sod Sodium SR Sustained release susp Suspension syr Syrup tab Tablet TCID50 Tissue culture infective dose 50% TDS Three times a day THFA Tetrahydrofolic acid TTS Transdermal therapeutic system U Unit UV Ultra violet yr Year (age) ZE Zollinger-Ellison  Contents 1. Drugs Acting on Autonomic Nervous System...... 1 Cholinergic Drugs, Anticholinergic Drugs, Drugs Acting on Autonomic Ganglia, Adrenergic Drugs, α-Adrenergic Blocking Agents, β-Adrenergic Blocking Agents, Drugs used for Glaucoma 2. Autacoids and Related Drugs................................. 13 Histaminergic Agonists, H1-Antagonists, 5-Hydroxytryptamine (5-HT) Antagonists, Drugs for Migraine, Prostaglandins (PGs) and their Analogues, Antipyretic-Analgesics and Nonsteroidal Antiinflammatory Drugs (NSAIDs), Antirheumatoid Arthritis Drugs, Antigout Drugs 3. Drugs for Respiratory Disorders............................ 23 Drugs for Cough, Drugs for Bronchial Asthma 4. Hormones and Related Drugs................................. 30 Anterior Pituitary Hormones and Related Drugs, Thyroid Hormone, Thyroid Inhibitors, Antidiabetic Drugs, Corticosteroids, Androgens and Related Drugs, Drugs for Erectile Dysfunction, Estrogens and Related Drugs, Progestins, Oral Contraceptives, Uterine Stimulants, Uterine Relaxants 5. Drugs Acting on Peripheral (somatic) Nervous System.......................................................... 47 Skeletal Muscle Relaxants, Local Anaesthetics 6. Drugs Acting on Central Nervous System........... 51 General Anaesthetics, Preanaesthetic Medication, Sedative- Hypnotics, Antiepileptic Drugs, Antiparkinsonian Drugs, Antipsychotic Drugs, Drugs for Mania and Manic-Depressive (Bipolar) Disorder, Antidepressants, Antianxiety Drugs, Opioid Analgesics, Complex Action Opioids and Opioid Antagonists, Central Nervous System Stimulants, Cognition Enhancers xii Contents 7. Cardiovascular Drugs................................................ 66 Antihypertensive Drugs, Antianginal Drugs, Drugs for Peripheral Vascular Diseases, Drugs for Congestive Heart Failure, Antiarrhythmic Drugs 8. Drugs Acting on Kidney.......................................... 75 Diuretics, Antidiuretics 9. Drugs Affecting Blood.............................................. 78 Haematinics, Coagulants, Anticoagulants, Fibrinolytics, Antifibrinolytics, Antiplatelet Drugs, Hypolipidaemic Drugs, Plasma Expanders 10. Gastrointestinal Drugs.............................................. 88 Drugs for Peptic Ulcer, Antiemetics, Drugs for Gastroesophageal Reflux Disease, Laxatives, Nonspecific Antidiarrhoeal Drugs 11. Antibacterial Drugs................................................... 97 Sulfonamides, Cotrimoxazole, Quinolones, Beta-Lactam Antibiotics (Penicillins, Cephalosporins, Monobactams, Carbapenems), Aminoglycoside Antibiotics, Tetracyclines, Chloramphenicol, Macrolide Antibiotics, Lincosamide Antibiotics, Aminocyclitol Antibiotic, Glycopeptide Antibiotics, Oxazolidinone, Polypeptide Antibiotics, Urinary Antiseptics, Antitubercular Drugs, Antileprotic Drugs 12. Antifungal, Antiviral, Antiprotozoal and Anthelmintic Drugs................................................. 115 Antifungal Drugs, Antiviral Drugs, Antimalarial Drugs, Antiamoebic Drugs, Drugs for Giardiasis, Drugs for Trichomoniasis, Drugs for Leishmaniasis, Anthelmintics 13. Anticancer Drugs..................................................... 129 Antineoplastic Drugs 14. Miscellaneous Drugs............................................... 133 Immunosuppressants, Chelating Agents, Locally Acting Drugs on Skin and Mucous Membranes, Antiseptics and Disinfectants, Ectoparasiticides, Vaccines, Antisera and Immuneglobulins Index of Nonproprietary Names of Drugs.................. 149 Index of Proprietary (Brand) Names of Drugs.......... 167  Drugs Acting on 1 Autonomic Nervous System Cholinergic Drugs (Cholinomimetic, Parasympathomimetic) CHOLINERGIC AGONISTS 1. Choline esters: Acetylcholine, Methacholine, Carbachol, Bethanechol 2. Alkaloids: Muscarine, Pilocarpine, Arecoline ANTICHOLINESTERASES 1. Reversible a. Carbamates: Physostigmine (Eserine), Neostigmine, Pyridostigmine, Edrophonium, Rivastigmine*, Donepezil*, Galantamine* b. Acridine: Tacrine* 2. Irreversible a. Organophosphates: Dyflos (DFP), Echothiophate, Malathione£, Diazinon£, Tabun$, Sarin$, Soman$ b. Carbamates: Carbaryl£, Propoxur£ * Cerebroselective; used for Alzheimer’s disease £ Insecticides $ Nerve gases for chemical warfare Preparations 1. Bethanechol: 10–40 mg oral, 2.5–5 mg s.c. UROTONIN 25 mg tab. 2. Pilocarpine: 0.5–4% topically in eye. PILOCAR 1%, 2%, 4% eye drops; CARPINE 0.5% eye drops; PILODROPS 2% eye drops. 2 Drugs Acting on Autonomic Nervous System 3. Physostigmine: 0.5–1.0 mg oral/i.m., 0.25–0.5% topically in eye. BI-MIOTIC 0.25% eye drops with 2% pilocarpine nitrate. 4. Neostigmine: 15–30 mg oral, 0.5–2.5 mg s.c./i.m. PROSTIGMIN, MYOSTIGMIN, TILSTIGMIN 15 mg tab, 0.5 mg/ml in 1 ml and 5 ml inj. 5. Pyridostigmine: 60–180 mg oral. DISTINON, MYESTIN 60 mg tab. 6. Rivastigmine: Initially 1.5 mg BD, increase every 2 weeks by 1.5 mg/day upto 6 mg/day. EXELON, RIVAMER 1.5, 3, 4.5, 6.0 mg caps. 7. Donepezil: 5 mg at bed time once daily (max 10 mg/day). DONECEPT, DOPEZIL 5, 10 mg tabs. 8. Galantamine: 4 mg BD (max 12 mg BD). GALAMER 4, 8, 12 mg tabs. Anticholinergic Drugs (Muscarinic receptor antagonists, Parasympatholytic, Atropinic) 1. Natural alkaloids Atropine, Hyoscine (Scopolamine). 2. Semisynthetic derivatives Homatropine, Atropine methonitrate, Hyoscine butyl bromide, Ipratropium bromide, Tiotropium bromide. 3. Synthetic compounds (a) Mydriatics: Cyclopentolate, Tropicamide (b) Antisecretory-antispasmodics: (i) Quaternary compounds: Propantheline, Oxyphe- nonium, Clidinium, Pipenzolate methylbro- mide, Isopropamide, Glycopyrrolate. (ii) Tertiary amines: Dicyclomine, Valethamate, Pirenzepine. (c) Vasicoselective: Oxybutynin, Flavoxate, Tolterodine. (d) Antiparkinsonian: Trihexyphenidyl (Benzhexol), Procyclidine, Biperiden.  Anticholinergic Drugs 3 Preparations 1. Atropine: 0.6–2.0 mg i.m./i.v. (Ch. 10 μg/kg), 1–2% topically in eye. ATROPINE SULPHATE 0.6 mg/ml inj, 1% eye drop/oint. 2. Hyoscine hydrobromide: 0.3–0.5 mg oral/i.m. (Ch. 10 μg/ kg). 3. Hyoscine butyl bromide: 20–40 mg oral/i.m./s.c./i.v. BUSCOPAN 10 mg tab, 20 mg/ml amp. 4. Atropine methonitrate: 2.5–10 mg oral/i.m. MYDRINDON 1 mg (adult), 0.1 mg (child) tab; in SPASMOLYSIN 0.32 mg tab. 5. Propantheline: 15–30 mg oral. PROBANTHINE 15 mg tab. 6. Oxyphenonium: 5–10 mg (Ch. 3–5 mg) oral. ANTRENYL 5, 10 mg tab. 7. Clidinium: 2.5–5 mg oral. In SPASRIL, EQUIREX 2.5 mg tab with chlordiazepoxide 5 mg. NORMAXIN 2.5 mg with dicyclomine 10 mg and chlordiazepoxide 5 mg tab. 8. Pipenzolate methyl bromide: 5–10 mg (Ch. 2–3 mg) oral. In PIPTAL 5 mg tab. 4 mg/ml drops with dimethyl polysiloxane, also PIPEN drops. 9. Isopropamide: 5 mg oral. In STELABID, GASTABID 5 mg tab. with trifluoperazine. 10. Dicyclomine: 20 mg oral. CYCLOMINOL 20 mg tab, 10 mg/ml liquid; DIOSPAS 10 mg, 20 mg tabs, CYCLOPAM INJ. 10 mg/ml in 2 ml, 10 ml, 30 ml amp/vial, also 20 mg tab with paracetamol 500 mg; in COLIMEX 20 mg with paracetamol 500 mg tab, 10 mg/ml drops with dimethicone. 11. Valethamate: 8 mg i.m., 10 mg oral, repeated as required. VALAMATE 8 mg in 1 ml inj, EPIDOSIN 10 mg tab, 8 mg inj. 12. Glycopyrrolate: 0.1–0.3 mg i.m./i.v., 1–2 mg oral. GLYCO-P 0.2 mg/ml amp., 1 mg in 5 ml vial, PYROLATE 0.2 mg/ml, 1 ml amp, 10 ml vial. 13. Ipratropium bromide: 40–80 μg by inhalation/nasal spray. IPRAVENT 20 μg/puff metered dose inhaler, 2 puffs 3–4 times daily; 250 μg/ml respirator soln., 0.4–2 ml nebulized in conjunction with a β2 agonist 2–4 times daily. 4 Drugs Acting on Autonomic Nervous System Also used to control rhinorrhoea in perennial rhinitis and common cold; IPRANASE–AQ 0.084% nasal spray (42 μg per actuation), 1–2 sprays in each nostril 3–4 times a day. 14. Tiotropium bromide: 18 μg by inhalation. TIOVA 18 μg rotacaps, 1 rotacap by inhalation OD. 15. Oxybutynin: 5 mg BD/TDS oral; children above 5 yr 2.5 mg BD. OXYBUTIN, CYSTRAN, OXYSPAS 2.5 mg and 5 mg tabs. 16. Flavoxate: 200 mg TDS. URISPAS, FLAVATE 200 mg tab. 17. Tolterodine: 2 mg BD. TORQ, ROLITEN 1, 2 mg tabs. 18. Homatropine: 1–2% topically in eye. HOMATROPINE EYE, HOMIDE 1%, 2% eye drops. 19. Cyclopentotate: 0.5–1.0% topically in eye. CYCLOMID EYE, 0.5%, 1.0%, CYCLOGYL 1% eye drops. 20. Tropicamide: 0.5–1.0% topically in eye. OPTIMIDE, TROPICAMET, TROMIDE 1% eye drops; TROPAC- P, TROPICAMET PLUS 0.8% + phenylephrine 5% eye drops. 21. Trihexyphenidyl (benzhexol): 2–10 mg/day; PACITANE, PARBENZ 2 mg tab. 22. Procyclidine: 5–20 mg/day; KEMADRIN 2.5, 5 mg tab. 23. Biperiden: 2–10 mg/day oral, i.m. or i.v.: DYSKINON 2 mg tab., 5 mg/ml inj. Drugs Acting on Autonomic Ganglia GANGLIONIC STIMULANTS Selective nicotinic Nonselective/muscarinic agonists agonists Nicotine (small dose) Acetylcholine Lobeline Carbachol Dimethylphenyl Pilocarpine piperazinium iodide Anticholinesterases (DMPP) MCN 343-A Tetramethyl ammonium (TMA) Varenicline  Adrenergic Drugs 5 Preparations 1. Nicotine transdermal: NICOTINELL-TTS 10, 20, 30 cm 2 patches releasing 7, 14, 21 mg nicotine per 24 hr respectively. In those smoking > 20 cigarettes every day—start with 30 cm2 patch, shift to smaller patches every 3–5 days, treat for 3–4 weeks. 2. Nicotine chewing gum: NULIFE 1, 2, 4 mg chewing gum; In those smoking > 20 cigarettes/day—start with 4 mg gum chewed slowly for 30 min when urge to smoke occurs—gradually reduce to 2 mg gum and then 1 mg gum. In less heavy smokers—start at lower doses. GANGLION BLOCKING AGENTS A. Competitive blockers Quaternary ammonium compounds Hexamethonium, Pentolinium Amines (secondary/tertiary) Mecamylamine, Pempidine Monosulfonium compound Trimethaphan camforsulfonate B. Persistent depolarising blockers Nicotine (large dose) Anticholinesterases (large dose) Adrenergic Drugs (Sympathomimetics) 1. Directly acting Adrenaline, Noradrenaline, Isoprenaline, Dopamine, Phenylephrine, Methoxamine, Xylometazoline, Salbutamol 2. Indirectly acting Tyramine 3. Mixed action Ephedrine, Amphetamine, Mephentermine 6 Drugs Acting on Autonomic Nervous System THERAPEUTIC CLASSIFICATION 1. Pressor agents Noradrenaline Phenylephrine Ephedrine Methoxamine Dopamine Mephentermine 2. Cardiac stimulants Adrenaline Dobutamine Isoprenaline 3. Bronchodilators Isoprenaline Bambuterol Salbutamol (Albuterol) Salmeterol Terbutaline Formoterol 4. Nasal decongestants Phenylephrine Naphazoline Xylometazoline Pseudoephedrine Oxymetazoline Phenyl propanolamine 5. CNS stimulants Amphetamine Methamphetamine Dexamphetamine 6. Anorectics Fenfluramine Sibutramine Dexfenfluramine 7. Uterine relaxant and vasodilators Ritodrine Salbutamol Isoxsuprine Terbutaline Preparations 1. Adrenaline (Epinephrine): 0.2–0.5 mg s.c./i.m.; ADRENALINE 1 mg/ml inj. 2. Noradrenaline (Norepinephrine, Levarterenol): 2–4 μg/min i.v. infusion; ADRENOR, NORAD, NOR-DRIN 2 mg (base)/2 ml amp.  Adrenergic Drugs 7 3. Isoprenaline (Isoproterenol): 20 mg s.l., 1–2 mg i.m., 5–10 μg/min i.v. infusion; NEOEPININE 20 mg sublingual tab, ISOPRIN 4 mg/2 ml inj. 4. Dopamine: 0.2–1.0 mg/min i.v. infusion; DOPAMINE, INTROPIN, DOPACARD 200 mg/5 ml amp. 5. Dobutamine: 2.5–10 μg/kg/min i.v. infusion; CARDIJECT 50 mg/4 ml and 250 mg/20 ml inj, DOBUTREX, DOBUSTAT 250 mg inj. 6. Ephedrine: 15–60 mg oral, 15–30 mg i.m./i.v.; 0.5–0.75% topically in nose. EPHEDRINE HCL 15, 30 mg tabs, SUFIDRIN 50 mg in 1 ml inj, ENDRINE 0.75% nasal drops. 7. Phenylephrine: 5–10 mg oral, 2–5 mg i.m., 0.1–0.5 mg slow i.v. inj, 30–60 μg/min i.v. infusion, 0.25% topically in nose, 5–10% topically in eye; in DECOLD PLUS 5 mg with paracetamol 400 mg + chlorpheniramine 2 mg + caffeine 15 mg tab; FRENIN 10 mg in 1 ml inj, in FENOX 0.25% with naphazoline 0.025% nasal drops, DROSYN 10% eye drops, in DROSYN-T, TROPAC-P 5% with tropicamide 0.8% eye drops. 8. Methoxamine: 10–20 mg i.m., 3–5 mg slow i.v. inj; VASOXINE 20 mg/ml inj. 9. Mephentermine: 10–20 mg oral/i.m., also by i.v. infusion. MEPHENTINE 10 mg tab, 15 mg in 1 ml amp, 3 mg/ml in 10 ml vial. 10. Amphetamine: 5–15 mg oral; BENZEDRINE 5 mg. tab. 11. Dexamphetamine: 5–10 mg (children 2.5–5 mg) oral; DEXEDRINE 5 mg. tab. 12. Methamphetamine: 5–10 mg oral: METHEDRINE 5 mg. tab. 13. Sibutramine: Start with 10 mg OD, increase to 15 mg OD if needed; OBESTAT, SIBUTREX, SIBUTRIM 5 mg, 10 mg caps. 14. Xylometazoline: 0.05%–0.1% topically in nose; OTRIVIN 0.05% (pediatric), 0.1% (adult) nasal drops. 15. Oxymetazoline: 0.025–0.05% topically in nose; NASIVION, SINAREST 0.025% (pediatric), 0.05% (adult) nasal drops. 16. Naphazoline: 0.1% topically in nose; PRIVINE 0.1% nasal drops. 17. Pseudoephedrine: 30–60 mg oral TDS; SUDAFED 60 mg tab, 30 mg/5 ml syrup; in SINAREST 60 mg with chlorpheniramine 2 mg + caffeine 30 mg + paracetamol 8 Drugs Acting on Autonomic Nervous System 500 mg tab; in CHESTON 30 mg with chlorpheniramine 2 mg + bromhexine 4 mg per tab and per 5 ml syr; in ACTICOLD 60 mg with chlorpheniramine 4 mg + paracetamol 500 mg tab; in CODYLEX 60 mg with chlorpheniramine 4 mg + ibuprofen 400 mg tab. 18. Phenylpropanolamine: 25–50 mg TDS; In ACTIFED 25 mg with triprolidine 2.5 mg tab; in ESKOLD 50 mg with diphenylpyraline 5 mg spansule; in FLUCOLD 25 mg with chlorpheniramine 2 mg + paracetamol 500 mg tab. 19. Ritodrine: 50–200 μg/min i.v. infusion, 10 mg i.m./oral 4–6 hourly; YUTOPAR, RITROD 10 mg/ml inj (5 ml amp), 10 mg tab. RITODINE 10 mg tab, 10 mg in 1 ml inj. 20. Isoxsuprine: 5–10 mg oral, i.m. 4–6 hourly, DUVADILAN 10 mg tab, 40 mg SR cap, 10 mg/2 ml inj. Note: For doses and preparations of β2 agonist broncho- dilators (salbutamol, etc.) See p. 26. α -Adrenergic Blocking Agents I. Nonequilibrium type (i) β-Haloalkylamines: Phenoxybenzamine II. Equilibrium type (competitive) A. Nonselective (i) Ergot alkaloids: Ergotamine, Ergotoxine (ii) Hydrogenated ergot alkaloids: Dihydroergotamine (DHE), Dihydroergotoxine (iii) Imidazolines: Tolazoline, Phentolamine (iv) Miscellaneous: Chlorpromazine, Ketanserin B. α1 selective: Prazosin, Terazosin, Doxazosin, Alfuzosin, Tamsulosin C. α2 selective: Yohimbine  α-Adrenergic Blocking Agents 9 Preparations 1. Phenoxybenzamine: 20–60 mg/day oral, 1 mg/kg slow i.v. infusion over 1 hour; FENOXENE 10 mg cap, 50 mg/ml inj, BIOPHENOX 50 mg/ml inj. 2. Ergotamine: For migraine 1–3 mg oral/sublingual, repeat as required (max 6 mg in a day); rarely 0.25–0.5 mg i.m. or s.c.; ERGOTAMINE, GYNERGEN, INGAGEN 1 mg tab, 0.5 mg/ml and 1 mg/ml inj. 3. Dihydroergotamine: For migraine 2–6 mg oral (max 10 mg/ day), 0.5–1 mg i.m., s.c. repeat hourly (max 3 mg); DIHYDERGOT, DHE 1 mg tab, MIGRANIL 1 mg/ml inj. 4. Dihydroergotoxine (codergocrine): For dementia 1–1.5 mg oral or sublingual, 0.15–0.6 mg i.m., HYDERGINE 1.5 mg tab, CERELOID 1 mg tab. 5. Phentolamine: 5 mg i.v. repeated as required; REGITINE, FENTANOR 10 mg/ml inj. 6. Prazosin: Start with 0.5–1 mg at bedtime; usual dose 1–4 mg BD or TDS; PRAZOPRES 0.5, 1.0 and 2.0 mg tabs. MINIPRESS XL: PRAZOSIN GITS 2.5 mg and 5 mg tablets; 1 tab OD. 7. Terazosin: Usual maintenance dose 2–10 mg OD; HYTRIN, TERALFA, OLYSTER 1, 2, 5 mg tab. 8. Doxazosin: 1 mg OD initially, increase upto 8 mg BD; DOXACARD, DURACARD, DOXAPRESS 1, 2, 4 mg tabs. 9. Alfuzosin: 2.5 BD-QID or 10 mg OD as modified release tab. ALFUSIN, ALFOO 10 mg ER tab. 10. Tamsulosin: URIMAX, DYNAPRES 0.2, 0.4 mg MR cap; CONTIFLO-OD 0.4 mg cap; 1 cap (max 2) in the morning with meals. 11. Yohimbine: 2 mg oral; YOHIMBINE 2 mg tab. 10 Drugs Acting on Autonomic Nervous System β -Adrenergic Blocking Agents Nonselective (ββ 1 and β 2) a. Without intrinsic sympathomimetic activity Propranolol, Sotalol, Timolol b. With intrinsic sympathomimetic activity Pindolol c. With additional α blocking property Labetalol, Carvedilol β 1) Cardioselective (β Metoprolol, Atenolol, Acebutolol, Bisoprolol, Esmolol, Betaxolol, Celiprolol, Nebivolol GENERATIONWISE CLASSIFICATION 1. First Generation (older, nonselective) Propranolol, Timolol, Sotalol, Pindolol 2. Second Generation (β β 2 selective) Metoprolol, Atenolol, Acebutolol, Bisoprolol, Esmolol 3. Third Generation (with additional α blocking and/ or vasodilator property) Labetalol, Carvedilol, Celiprolol, Nabivolol Preparations 1. Propranolol: Oral—10 mg BD to 160 mg QID (average 40–160 mg/day). Start with a low dose and gradually increase according to need; i.v.—2 to 5 mg injected over 10 min with constant monitoring. It is not injected s.c. or i.m. because of irritant property. INDERAL, CIPLAR 10, 40, 80 mg tab, 1 mg/ml inj., BETABLOC 10, 40 mg tab. 2. Sotalol: 80 mg BD–160 mg TDS oral; SOTAGARD 40, 80 mg tabs. 3. Pindolol: 5–15 mg BD; PINADOL 5 mg tab, VISKEN 10, 15 mg tab. 4. Metoprolol: 25 mg BD–100 mg QID oral, 5–15 mg slow i.v. inj; BETALOC 25, 50, 100 mg tab, 5 mg/ml inj., LOPRESOR, METOLAR 50, 100 mg tab.  Drugs for Glaucoma 11 5. S(–) Metoprolol: 12.5 mg BD–50 mg QID; METPURE–XL 12.5, 25, 50 mg ER tabs. 6. Atenolol: 25 mg OD–50 mg BD; BETACARD, ATEN, TENORMIN 25, 50, 100 mg tabs. 7. S(–) Atenolol: 12.5–50 mg OD; ATPURE 12.5, 25, 50 mg tabs. 8. Acebutolol: 200 mg BD–400 mg TDS oral; 20–40 mg slow i.v. injection; SECTRAL 200, 400 mg tabs, 10 mg/2 ml amp. 9. Bisoprolol: 2.5–10 mg OD; CONCOR, CORBIS 5 mg tab. 10. Esmolol: 0.5 mg/kg i.v. injection followed by 0.05–0.2 mg/kg/ min i.v. infusion; MINIBLOCK 100 mg/10 ml, 250 mg/10 ml inj. 11. Celiprolol: 100 mg OD–300 mg BD; CELIPRES 100, 200 mg tab. 12. Nebivolol: 5 mg OD (start with 2.5 mg OD in elderly; NODON 5 mg tab, NEBICARD 2.5, 5 mg tabs. 13. Labetalol: Start with 50 mg BD, increase to 100–200 mg TDS oral. In hypertensive emergencies 20–40 mg slow i.v. injection every 10 min till desired response is obtained. NORMADATE 50, 100, 200 mg tab; LABESOL, LABETA 20 mg/ 4 ml inj. 14. Carvedilol: CHF: Start with 3.125 mg BD for 2 weeks, if well tolerated, gradually increase to max. of 25 mg BD. Hypertension/angina: 6.25 mg BD initially, titrate to max. of 25 mg BD. CARVIL, CARLOC, CARVAS 3.125, 6.25, 12.5, 25 mg tabs; ORICAR 12.5, 25 mg tabs. Drugs Used for Glaucoma 1. β -adrenergic blockers: Timolol, Betaxolol, Levobunolol, Cartiolol, Metipranolol. 2. α -adrenergic agonists: Adrenaline, Dipivefrine, Apraclonidine, Brimonidine. 3. Prostaglandin analogues: Latanoprost, Isopropyl unoprostone, Travoprost, Bimatoprost. 4. Miotics: Pilocarpine, Physostigmine. 5. Carbonic anhydrase inhibitors: Acetazolamide, Dorzolamide. 6. Osmotic diuretics: Mannitol, Glycerol (Glycerine). 12 Drugs Acting on Autonomic Nervous System Preparations 1. Timolol: Start with 0.25% eye drops BD, change to 0.5% drops in case of inadequate response. 0.5% OD as gel forming solution. GLUCOMOL, OCUPRES, IOTIM, LOPRES 0.25% and 0.5% eye drops. TIMOLAST 0.5% gel forming eye drops (long acting). Timolol 0.5% + Latanoprost 0.005%: LAPROST PLUS, LATOCHEK-T eye drops. 2. Betaxolol: 0.5% topically in eye BD; OPTIPRES, IOBET 0.5% eye drops. 3. Levobunolol: 0.5% topically in eye OD; BETAGAN 0.5% ophthalmic solution. 4. Dipivefrine: 0.1% topically in eye BD; PROPINE 0.1% eye drops. 5. Apraclonidine: 0.5–1.0% topically in eye; ALFADROPS-DS 1% eye drops. 6. Brimonidine: 0.2% topically in eye TDS; ALPHAGAN, BRIMODIN, IOBRIM 0.2% eye drops. 7. Latanoprost: 0.005% topically in eye OD in evening; LACOMA, XALATAN, IOPROST, 9 PM 50 μg/ml eye drops (store in cold place). 8. Travoprost: 0.004% topically in eye OD in evening; TRAVATAN 0.004% eye drops (store at 4-8° C). 9. Bimatoprost: 0.03% as eye drops OD in evening; LUMIGAN, CAREPROST 0.03% eye drops (store at 4-8° C). 10. Pilocarpine: 0.5%–4% topically in eye; CARPINE, PILOCAR 0.5%, 1%, 2%, 4% eye drops. 11. Acetazolamide: 250 mg OD–BD; DIAMOX, SYNOMAX 250 mg tab. 12. Dorzolamide: 2% topically in eye BD–TDS; DORTAS, DORZOX 2% eye drops. 13. Mannitol hypertonic: 20% 100–350 ml infused i.v.; MANNITOL 20% i.v. infusion vac 100, 350 ml. 14. Glycerine: 50% 100–200 ml as retention enema.  Autacoids and 2 Related Drugs Histaminergic Agonists 1. Nonselective (H1+H2+H3) agonists Histamine Betahistine: 4–8 mg 6 hourly; VERTIN 8 mg tab. 2. Selective H1 agonists 2-Methylhistamine, 2-Pyridyl ethylamine, 2-Thiazolyl ethylamine. 3. Selective H2 agonists 4-Methylhistamine, Dimaprit, Impromidine. 4. Selective H3 agonists (R) α-Methylhistamine, Imetit. H1-Antagonists (Conventional Antihistaminics) 1. Highly sedative Diphenhydramine, Dimenhydrinate, Promethazine, Hydroxyzine 2. Moderately sedative Pheniramine, Cyproheptadine, Meclozine (Meclizine), Buclizine, Cinnarizine 3. Mildly sedative Chlorpheniramine, Dexchlorpheniramine, Dimethin- dine, Triprolidine, Mebhydroline, Cyclizine, Clemastine 4. Second generation (Nonsedating) Terfenadine, Fexofenadine, Astemizole, Loratadine, Desloratadine, Cetirizine, Levocetirizine, Azelastine, Mizolastine, Ebastine, Rupatadine. 14 Autacoids and Related Drugs Preparations 1. Diphenhydramine: 25–50 mg oral; BENADRYL 25 mg cap, 12.5 mg/5 ml syr. 2. Dimenhydrinate: 25–50 mg oral, i.m.; DRAMAMINE 16 mg/ 5 ml syr, 50 mg tab, GRAVOL 50 mg tab. 3. Promethazine: 25–50 mg oral, i.m. (1 mg/kg); PHENERGAN 10, 25 mg tab., 5 mg/ml elixer, 25 mg/ml inj. 4. Hydroxyzine: 25–50 mg oral, i.m.; ATARAX 10, 25 mg tab., 10 mg/5 ml syr, 6 mg/ml drops, 25 mg/ml inj. 5. Pheniramine: 20–50 mg oral, i.m.; AVIL 25 mg, 50 mg tab, 15 mg/5 ml syr, 22.5 mg/ml inj. 6. Cyproheptadine: 4 mg oral; PRACTIN, CIPLACTIN 4 mg tab., 2 mg/5 ml syrup. 7. Meclozine (Meclizine): 25–50 mg oral; In DILIGAN 12.5 mg + niacin 50 mg tab., In PREGNIDOXIN 25 mg + Caffeine 20 mg tab. 8. Buclizine: 25–50 mg oral; LONGIFENE 25 mg tab, 6 mg/5 ml syrup. 9. Cinnarizine: 25–50 mg oral; STUGERON, VERTIGON 25 and 75 mg tab. 10. Chlorpheniramine: 2–4 mg (0.1 mg/kg) oral, i.m.; PIRITON, CADISTIN 4 mg tab. 11. Dexchlorpheniramine: 2 mg oral; POLARAMINE 2 mg tab., 0.5 mg/5 ml syrup. 12. Dimethindene: 1 mg oral; FORISTAL 1 mg tab., 2.5 mg SR tab. 13. Triprolidine: 2.5–5 mg oral; ACTIDIL 2.5 mg tab. 14. Mebhydroline: 100–300 mg oral; INCIDAL 50 mg (base) tab. 15. Cyclizine: 50 mg oral; MAREZINE 50 mg tab. 16. Clemastine: 1–2 mg oral; TAVEGYL 1 mg tab., 0.5 mg/5 ml syr. 17. Fexofenadine: 120–180 mg oral; ALLEGRA, ALTIVA, FEXO 120, 180 mg tab. 18. Astemizole: 10 mg oral; STEMIZOLE, HISTALONG, STEMIZ, 5 mg, 10 mg tab., 1 mg/ml susp.  5-Hydroxytryptamine Antagonists 15 19. Loratadine: 10 mg oral; LORFAST, LORIDIN, LORMEG, 10 mg tab, 1 mg/ml susp. 20. Desloratadine: 5 mg oral; DESLOR, LORDAY 5 mg tab. 21. Cetirizine: 10 mg oral; ALERID, CETZINE, ZIRTIN, SIZON 10 mg tab, 5 mg/5 ml syr. 22. Levocetirizine: 5 mg oral; LEVORID, LEVOSIZ, TECZINE 5 mg tab. 23. Azelastine: 4 mg oral, 0.28 mg intranasal; AZEP NASAL SPRAY 0.14 mg per puff nasal spray. 24. Mizolastine: 10 mg oral; ELINA 10 mg tab. 25. Ebastine: 10 mg oral; EBAST 10 mg tab. 26. Rupatadine: 10 mg oral; RUPAHIST 10 mg tab. Note: For H2-Antagonists (H2-Antihistaminics) See p. 88, 89. 5-Hydroxytryptamine (5-HT) Antagonists 1. Nonselective 5-HT antagonists/partial agonist- antagonists Ergotamine, Lysergic acid diethyl amide (LSD), 2- Bromo-LSD, Methysergide, Cyproheptadine, Cinnarizine. 2. 5-HT2 antagonists Ketanserin, Ritanserin, Clozapine, Risperidone, Olanzapine. 3. 5-HT3 antagonists Ondansetron, Granisetron, Tropisetron. Drugs for Migraine A. During attack 1. Simple analgesics: Paracetamol, Aspirin (low dose), Metamizol, Codeine. 2. Nonsteroidal antiinflammatory drugs (NSAIDs): Ibuprofen, Naproxen, Diclofenac, Mephenamic acid. 16 Autacoids and Related Drugs 3. Antiemetics: Metoclopramide, Domperidone, Prochlorperazine, Promethazine. 4. Ergot alkaloids: Ergotamine, Dihydroergotamine (DHE). 5. Selective 5-HT IB/ID receptor agonists: Sumatriptan, Rizatriptan, Zolmitriptan, Naratriptan, Frovatriptan. B. For prophylaxis of attacks 1. Propranolol (also other β blockers) 2. Amitriptyline (also other tricyclic antidepressants) 3. Flunarizine (also verapamil) 4. Methysergide, Cyproheptadine Preparations 1. Ergotamine: 1 mg oral/sublingual half hourly till relief obtained (max. 6 mg), 0.25–0.5 mg s.c./i.m.; ERGOTAMINE, INGAGEN, GYNERGEN 1 mg tab, 0.5 mg/ml inj. MIGRANIL: Erogotamine 1 mg, caffeine 100 mg, belladonna dry ext 10 mg, paracetamol 250 mg tab. MIGRIL: Ergotamine 2 mg, caffeine 100 mg, cyclizine 50 mg tab. VASOGRAIN: Ergotamine 1 mg, caffeine 100 mg, paracetamol 250 mg, prochlorperazine 2.5 mg tab. ERGOPHEN: Ergotamine 0.3 mg, belladonna dry ext. 10 mg, phenobarbitone 20 mg tab. 2. Dihydroergotamine (DHE): 1–2 mg half hourly (max 10 mg), 0.5–1.0 mg i.m.; DHE 1 mg tab, MIGRANIL 1 mg/ml inj. 3. Sumatriptan: 6 mg s.c., 50–100 mg oral at the onset of migraine attack, may be repeated once within 24 hours if required. Those not responding to the first dose should not be given the second dose; SUMINAT, SUMITREX 25, 50, 100 mg tabs, MIGRATAN 50, 100 mg tabs, SUMITREX-INJ KIT 6 mg in 0.5 ml inj.; also SUMINAT 25 mg per actuation nasal spray. 4. Rizatriptan: 10 mg at the onset of migraine attack, may be repeated after 2 hours if required. Those not responding to the first dose should not be given the second dose; RIZACT, RIZATAN 5 mg, 10 mg tabs.  Prostaglandins and their Analogues 17 5. Flunarizine: 10–20 mg OD, children 5 mg OD; NOMIGRAIN, FLUNARIN 5 mg, 10 mg caps/tab. Note: For preparations of other drugs See Index. Prostaglandins (PGs) and their Analogues 1. PGE 2 (Dinoprostone): PROSTIN-E 2 for induction/ augmentation of labour, midterm abortion. Vaginal gel (1 mg or 2 mg in 2.5 ml) 1 mg inserted into posterior fornix, followed by 1–2 mg after 6 hour if required. Vaginal tab (3 mg) 3 mg inserted into posterior fornix, followed by another 3 mg if labour does not start within 6 hour. Extraamniotic solution (10 mg/ml in 0.5 ml amp.) infrequently used. Intravenous solution (1 mg/ml in 0.75 ml amp., 10 mg/ml in 0.5 ml amp) rarely used. Oral tablet PRIMIPROST 0.5 mg tab, one tab. hourly till induction, max 1.5 mg per hr; rarely used. Cervical gel CERVIPRIME (0.5 mg in 2.5 ml prefilled syringe) 0.5 mg inserted into cervical canal for preinduction cervical softening and dilatation in patients with poor Bishop’s score. 2. Gemeprost: CERVAGEM 1 mg vaginal pessary: for softening of cervix in first trimester–1 mg 3 hr before attempting dilatation; for 2nd trimester abortion/molar gestation—1 mg every 3 hours, max. 5 doses. 3. PGF 2α (Dinoprost): PROSTIN F 2 ALPHA intraamniotic injection, 5 mg/ml in 4 ml amp. for midterm abortion/ induction of labour (rarely used). 4. 15-methyl PGF2α (Carboprost): PROSTODIN 0.25 mg in 1 ml amp; 0.25 mg i.m. every 30–120 min for PPH, midterm abortion, missed abortion. 5. Misoprostol (methyl–PGE1 ester): 200 μg oral 6 hourly; CYTOLOG 200 μg tab, MISOPROST 100, 200 μg tab. T-PILL + MISO Mifepristone 200 mg tab (3 tabs) + misoprostol 200 μg (2 tabs); mifepristone 3 tab orally followed 2 days later by misoprostol 2 tab orally for termination of pregnancy of upto 49 days. 6. PGE1 (Alprostadil): 0.5 mg by slow i.v. infusion; PROSTIN–VR, BIOGLANDIN 0.5 mg in 1 ml inj. 18 Autacoids and Related Drugs 7. Latanoprost (PGF2α analogue): 0.005% topically in eye OD in the evening; LACOMA, XALATAN, LATOPROST 50 μg/ml eye drops. 8. PGI2 (Prostacyclin, Epoprostenol): 0.5 mg by i.v. infusion or injection in extracorporial circulation; FLOLAN 0.5 mg per vial for reconstitution. Antipyretic-Analgesics and Nonsteroidal Antiinflammatory Drugs (NSAIDs) A. Nonselective COX inhibitors (conventional NSAIDs) 1. Salicylates: Aspirin. 2. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen. 3. Anthranilic acid derivative: Mephenamic acid. 4. Aryl-acetic acid derivatives: Diclofenac, Aceclofenac. 5. Oxicam derivatives: Piroxicam, Tenoxicam. 6. Pyrrolo-pyrrole derivative: Ketorolac. 7. Indole derivative: Indomethacin. 8. Pyrazolone derivatives: Phenylbutazone, Oxyphen- butazone. B. Preferential COX-2 inhibitors Nimesulide, Meloxicam, Nabumetone, Etodolac. C. Selective COX-2 inhibitors Celecoxib, Etoricoxib, Parecoxib. D. Analgesic-antipyretics with poor antiinflammatory action 1. Paraaminophenol derivative: Paracetamol (Aceta- minophen). 2. Pyrazolone derivatives: Metamizol (Dipyrone), Propiphenazone. 3. Benzoxazocine derivative: Nefopam.  Antipyretic-Analgesics and NSAIDs 19 Preparations 1. Aspirin: Antiinflammatory dose 3–5 g/day (75–100 mg/kg/ day); analgesic-antipyretic dose 0.3–0.6 g 6–8 hourly; antiplatelet dose 75–150 mg/day. ASPIRIN 350 mg tab, COLSPRIN 100, 325, 650 mg tabs, ECOSPRIN 75, 150, 325 mg tabs, DISPRIN 350 mg tab, LOPRIN 75, 162.5 mg tabs. BIOSPIRIN: Lysine acetylsalicylate 900 mg + glycine 100 mg/vial for dissolving in 5 ml water and i.v. injection. 2. Indomethacin: 25–50 mg BD–QID. Those not tolerating the drug orally may be given nightly suppository. IDICIN, INDOCAP 25 mg cap, 75 mg SR cap, ARTICID 25, 50 mg cap, INDOFLAM 25, 75 mg caps, 1% eye drop. RECTICIN 50 mg suppository. 3. Ibuprofen: 400–800 mg TDS; BRUFEN, EMFLAM, IBUSYNTH 200, 400, 600 mg tab, IBUGESIC also 100 mg/5 ml susp. 4. Naproxen: 250 mg BD–TDS; NAPROSYN, NAXID, ARTAGEN, XENOBID 250 mg tab., NAPROSYN also 500 mg tab. 5. Ketoprofen: 50–100 mg BD–TDS; KETOFEN 50, 100 mg tab; OSTOFEN 50 mg cap. RHOFENID 100 mg tab, 200 mg SR tab; 100 mg/2 ml amp. 6. Flurbiprofen: 50 mg BD–QID; ARFLUR 50, 100 mg tab, 200 mg SR tab, FLUROFEN 100 mg tab., OCUFLUR 0.03% eye drops. 7. Mephenamic acid: 250–500 mg TDS; MEDOL 250, 500 mg cap; MEFTAL 250, 500 mg tab, 100 mg/5 ml susp. PONSTAN 125, 250, 500 mg tab, 50 mg/ml syrp. 8. Diclofenac: 50 mg TDS, then BD oral, 75 mg deep i.m.; VOVERAN, DICLONAC, MOVONAC 50 mg enteric coated tab, 100 mg S.R. tab, 25 mg/ml in 3 ml amp. for i.m. inj. DICLOMAX 25, 50 mg tab, 75 mg/3 ml inj. Diclofenac potassium: VOLTAFLAM 25, 50 mg tab, ULTRA-K 50 mg tab; VOVERAN 1% topical gel. 9. Aceclofenac: 100 mg BD; ACECLO, DOLOKIND 100 mg tab, 200 mg SR tab. 10. Piroxicam: 20 mg BD for two days followed by 20 mg OD; DOLONEX, PIROX 10, 20 mg cap, 20 mg dispersible tab, 20 mg/ ml inj in 1 and 2 ml amps; PIRICAM 10, 20 mg cap. 11. Tenoxicam: 20 mg OD; TOBITIL 20 mg tab. 20 Autacoids and Related Drugs 12. Ketorolac: 10–20 mg oral 6 hourly, 15–30 mg i.m./i.v. 6 hourly (max 90 mg/day); KETOROL, ZOROVON, KETANOV, TOROLAC 10 mg tab, 30 mg in 1 ml amp., KETLUR, ACULAR 0.5% eye drops. 13. Nimesulide: 100 mg BD; NIMULID, NIMEGESIC, NIMODOL 100 mg tab, 50 mg/5 ml susp. 14. Meloxicam: 7.5–15 mg OD; MELFLAM, MEL–OD, MUVIK, M–CAM 7.5 mg, 15 mg tabs. 15. Nabumetone: 500 mg OD; NABUFLAM 500 mg tab. 16. Etodolac: 200-400 mg BD-TDS; ETOVA 200, 300, 400 mg tabs. 17. Celecoxib: 100–200 mg BD; CELACT, CELCOX, COLCIBRA, COBIX 100, 200 mg tabs. 18. Etoricoxib: 60–120 mg OD; ETODY, ETOXIB, ETOSHINE, NUCOXIA 60, 90, 120 mg tabs. 19. Parecoxib: 40 mg oral/i.m./i.v. repeated after 6–12 hours (max. 80 mg/day); PAROXIB 40 mg tab, REVALDO, VALTO-P 40 mg/ vial inj. 20. Paracetamol: 0.5–1 g TDS; infants 50 mg; children 15 mg/kg (1–3 years 80–160 mg, 4–8 years 240–320 mg, 9–12 years 300–600 mg); CROCIN 0.5 g tab, 125 mg/5 ml and 250 mg/5 ml syr, 100 mg/ml pediatric drops, CROCIN PAIN RELIEF 650 mg with caffeine 50 mg tab; METACIN, PARACIN 500 mg tab, 125 mg/ 5 ml syrup, 150 mg/ml ped. drops, ULTRAGIN, PYRIGESIC, CALPOL 500 mg tab, 125 mg/5 ml syrup, NEOMOL, FEVASTIN, FEBRINIL 300 mg/2 ml inj. 21. Metamizol: 0.5–1.5 g oral/i.m./i.v.; ANALGIN 0.5 g tab; NOVALGIN, BARALGAN 0.5 g tab, 0.5 g/ml in 2 ml and 5 ml amps; ULTRAGIN 0.5 g/ml inj in 2 ml amp and 30 ml vial. 22. Propiphenazone: 300–600 mg TDS; marketed only in combi- nation in several ‘over the counter’ preparations–in SARIDON, ANAFEBRIN: propiphenazone 150 mg + paracetamol 250 mg tab, DART: propiphenazone 150 mg + paracetamol 300 mg + caffeine 50 mg tab. 23. Nefopam: 30–60 mg TDS oral, 20 mg i.m. 6 hourly; NEFOMAX 30 mg tab, 20 mg in 1 ml amp. Topical NSAIDs 1. Diclofenac 1% gel: VOVERAN, EMULGEL, RELAXYL GEL, DICLONAC GEL  Antirheumatoid Drugs 21 2. Ibuprofen 10% gel: RIBUFEN GEL 3. Naproxen 10% gel: NAPROSYN GEL 4. Ketoprofen 2.5% gel: RHOFENID GEL 5. Flurbiprofen 5% gel: FROBEN GEL 6. Nimesulide 1% gel: NIMULID TRANS GEL, ZOLANDIN GEL, NIMEGESIC-T-GEL 7. Piroxicam 0.5% gel: DOLONEX GEL, MOVON GEL, PIROX GEL, MINICAM GEL Antirheumatoid Arthritis Drugs A. Disease Modifying Antirheumatic Drugs (DMARDs) 1. Immunosuppressants: Methotrexate, Azathioprine, Cyclosporine 2. Sulfasalazine 3. Chloroquine or Hydroxychloroquine 4. Leflunomide 5. Gold sod, thiomalate, Auranofin 6. d-Penicillamine B. Biologic Response Modifiers (BRMs) 1. TNF α inhibitors: Etanercept, Infliximab, Adalimumab 2. IL-1 antagonist: Anakinra c. Adjuvant Drugs Corticosteroids: Prednisolone and others. Preparations 1. Auranofin: 6 mg/day in 1–2 doses, RIDURA, GOLDAR 3 mg tab. 2. Chloroquine: 150 mg (base) per day; LARIAGO, RESOCHIN, NIVAQUIN-P 250 mg as phosphate (150 mg base) tab. 3. Hydroxychloroquine: initially 200 mg BD followed by 200 mg OD for maintenance; ZHQUINE, ZYQ 200 mg tab. 4. Sulfasalazine: 1–3 g/day in 2–3 divided doses; SALAZOPYRIN, SAZO-EN 0.5 g tab. 22 Autacoids and Related Drugs 5. Leflunomide: 100 mg/day for 3 days loading dose followed by 20 mg OD; LEFRA 10 mg, 20 mg tabs. 6. Methotrexate: 7.5–15 mg weekly oral; NEOTREXATE, BIOTREXATE 2.5 mg tab. 7. Azathioprine: 50–150 mg/day; IMURAN 50 mg tab. 8. d-Penicillamine: 125-250 mg OD (max 250 mg BD); ARTIN 150, 200 mg caps, CILAMIN 250 mg cap. 9. Etanercept: 25-50 mg s.c. twice weekly; ENBREL, ENBROL 25 mg/ 0.5 ml and 50 mg/1 ml inj. Note: For preparations of corticosteroids – See Index. Antigout Drugs For acute gout NSAIDs Colchicine Corticosteroids For chronic gout/hyperuricaemia Uricosurics Synthesis inhibitor Probenecid Allopurinol Sulfinpyrazone Preparations 1. Colchicine: For control of acute attack – 0.5 mg 1–3 hourly to a total of 3 doses; maintenance dose 0.5–1 mg/day; for prophylaxis 0.5–1.5 mg/day; ZYCOLCHIN, GOUTNIL 0.5 mg tab. 2. Probenecid: 0.25–1.0 g BD; BENEMID, BENCID 0.5 g tab. 3. Sulfinpyrazone: 100–200 mg BD (max. 800 mg/day); ANTURANE, ARTIRAN 200 mg cap. 4. Allopurinol: Start with 100 mg OD, gradually increase to maintenance dose of 300 mg/day; maximum 600 mg/day. ZYLORIC, 100, 300 mg tabs., ZYLOPRIM, CIPLORIC 100 mg cap.  Drugs for 3 Respiratory Disorders Drugs for Cough 1. Pharyngeal Demulcents Lozenges, cough drops, linctuses containing Syrup, Glycerine, Liquorice. 2. Expectorants (Mucokinetics) (a) Bronchial secretion enhancers Sodium or Potassium citrate, Potassium iodide, Guaiphenesin (Glyceryl guaiacolate), balsum of Tolu, Vasaka, Ammonium chloride. (b) Mucolytics Bromhexine, Ambroxol, Carbocisteine, Acetylcysteine. 3. Antitussives (Cough centre suppressants) (a) Opioids Codeine, Pholcodeine, Ethylmorphine. (b) Nonopioids Noscapine, Dextromethorphan, Chlophedianol. (c) Antihistamines Chlorpheniramine, Diphenhydra- mine, Promethazine. 4. Adjuvant Antitussives Bronchodilators Salbutamol, Terbutalin. Preparations 1. Sod./Pot. citrate/acetate: 0.3–1.0 g TDS. 2. Pot. iodide: 0.2–0.3 g TDS. 3. Guaiphenesin: 100–200 mg TDS. 4. Tolu balsum: 0.3–0.6 g TDS. 5. Vasaka syrup: 2–4 ml TDS. 6. Ammonium chloride: 50-200 mg TDS. 24 Drugs for Respiratory Disorders 7. Bromhexine: 8 mg TDS, child 1–5 yr 4 mg BD, 5–10 yr 4 mg TDS; BROMHEXINE 8 mg tab, 4 mg/5 ml elixer. 8. Ambroxol: 15–30 mg TDS; AMBRIL, AMBROLITE, AMBRODIL, MUCOLITE 30 mg tab, 30 mg/5 ml liq, 7.5 mg/ml drops. 9. Carbocisteine: 250–750 mg TDS; MUCODYNE 375 mg cap, 250 mg/5 ml syr. 10. Acetylcysteine: 200 mg/ml solution by nebulization or instillation through tracheostomy tube; MUCOMIX 200 mg/ml inj in 1, 2, 5 ml amps. 11. Codeine: 15–30 mg TDS; children 2–6 years 7.5 mg, 6–12 years 15 mg; CODINE 15 mg tab, 15 mg/5 ml linctus. 12. Ethylmorphine: 10-30 mg TDS; DIONINDON 16 mg tab. 13. Pholcodeine: 10–15 mg BD–TDS. 14. Noscapine: 15–30 mg, children 2–6 years 7.5 mg, 6–12 years 15 mg; COSCOPIN 7 mg/5 ml syrup, COSCOTABS 25 mg tab. 15. Dextromethorphan: 10–20 mg TDS, child 2–6 yr 2.5–5 mg, 6–10 yrs 5–10 mg. 16. Chlophedianol: 20–40 mg BD–TDS; DETIGON, TUSSIGON 20 mg/5 ml linctus with Ammon. chloride 50 mg and menthol 0.25 mg. Some combined formulations ASTHALIN EXPECTORANT: Salbutamol 2 mg, guaiphenesin 100 mg per 10 ml syr; dose 10–20 ml. ASCORIL-C: Codeine 10 mg, chlorpheniramine 4 mg per 5 ml syr. AXALIN: Ambroxol 15 mg, guaiphenesin 50 mg, salbutamol 1 mg, menthol 1 mg per 5 ml syr. BRONCHOSOLVIN: Guaiphenesin 100 mg, terbutalin 2.5 mg, bromhexine 8 mg per 10 ml susp. CADICOFF, GRILINCTUS: Dextromethorphan 5 mg, chlorpheniramine 2.5 mg, guaiphenesin 50 mg, amm. chloride 60 mg per 5 ml syr.  Drugs for Cough 25 BENADRYL COUGH FORMULA: Diphenhydramine 14 mg, amm. chlor. 138 mg, sod. citrate 57 mg, menthol 1.1 mg per 5 ml syrup; dose 5–10 ml, children 2.5–5 ml. BRO-ZEDEX: Bromhexine 8 mg, guaiphenesin 100 mg, terbutaline 2.5 mg, menthol 5 mg per 10 ml syrup; dose 10 ml. CADISTIN EXPECTORANT: Chlorpheniramine 2 mg, glyceryl guaiacolate 80 mg, amm. chlor. 100 mg, sod. citrate 44 mg, menthol 0.8 mg, terpin hydrate 4 mg, tolu balsum 6 mg, vasaka syrup 0.13 ml per 5 ml syrup; dose 10 ml. CLISTIN: Dextromethorphan 10 mg, Carbinoxamine 4 mg, amm. chlor. 240 mg, sod. citrate 240 mg per 10 ml syrup. COREX: Chlorpheniramine 4 mg, codeine phos. 10 mg, menthol 0.1 mg per 5 ml syrup; dose 5 ml, children 1.25–2.5 ml. COSCOPIN LINCTUS: Noscapine 7 mg, chlorpheniramine 2 mg, citric acid 29 mg, sod. citrate 3 mg, amm. chlor. 28 mg per 5 ml syrup; dose 10–20 ml. COSOME: Bromhexine 8 mg, phenylephrine 10 mg, chlorpheniramine 4 mg per 10 ml syr; dose 10 ml. SOLVIN EXPECTORANT: Bromhexine 4 mg, pseudoephedrine 30 mg tablet and in 10 ml liquid; dose 1 tablet or 5 ml liquid. TOSSEX: Codeine phos 10 mg, chlorpheniramine 4 mg, menthol 1.5 mg, sod. citrate 75 mg per 5 ml liquid; dose 5 ml. VENTORLIN EXPECTORANT: Salbutamol 2 mg, guaiphenesin 100 mg per 10 ml syrup; dose 10 ml, children 2.5–7.5 ml. ZEET EXPECTORANT: Diphenhydramine 8 mg, amm. chlor. 100 mg, guaiphenesin 50 mg, bromhexine 4 mg, menthol 1 mg per 5 ml syr. ZEET LINCTUS: Dextromethorphan 10 mg, guaiphenesin 50 mg, phenylpropanolamine 25 mg per 5 ml syr; dose 5 ml. 26 Drugs for Respiratory Disorders Drugs for Bronchial Asthma A. Bronchodilators 1. β2 Sympathomimetics: Salbutamol, Terbutaline, Bambuterol, Salmeterol, Formoterol, Ephedrine. 2. Methylxanthines: Theophylline (anhydrous), Aminophylline, Choline theophyllinate, Hydroxy- ethyl theophylline, Theophylline ethanolate of piperazine, Doxophylline. 3. Anticholinergics: Ipratropium bromide, Tiotropium bromide. B. Leukotriene antagonists Montelukast, Zafirlukast. C. Mast cell stabilizers Sodium cromoglycate, Ketotifen. D. Corticosteroids 1. Systemic: Hydrocortisone, Prednisolone and others. 2. Inhalational: Beclomethasone dipropionate, Budesonide, Fluticasone propionate, Flunisolide, Ciclesonide. E. Anti-IgE antibody Omalizumab. Preparations 1. Salbutamol (Albuterol): 2–4 mg oral, 0.25–0.5 mg i.m./s.c., 100–200 μg by inhalation; ASTHALIN 2, 4 mg tab., 8 mg SR tab., 2 mg/5 ml syrup, 100 µg metered dose inhaler; 5 mg/ml respirator soln., 200 µg rota caps; CROYSAL 0.5 mg/ml inj, SALOL 2.5 mg/3 ml inj; VENTORLIN 2 mg/5 ml syr, 4 mg, 8 mg CR caps., DERIHALER 100 μg metered dose inhaler. 2. Terbutaline: 5 mg oral, 0.25 mg s.c., 250 µg by inhalation; TERBUTALINE, BRICAREX 2.5, 5 mg tab., 3 mg/5 ml syrup, 0.5 mg/ml inj; MISTHALER 250 µg/metered dose, 10 mg/ml nebulizing soln.; BRICANYL 0.5 mg/ml inj, 2.5 mg, 5 mg tabs, 1.5 mg/5 ml syr.  Drugs for Bronchial Asthma 27 3. Bambuterol: 10–20 mg OD in the evening; BAMBUDIL 10 mg, 20 mg tabs, 5 mg/5 ml oral soln; BETADAY 10, 20 mg tabs. 4. Salmeterol: 50–100 μg by inhalation; SALMETER, SEROBID 25 µg per metered dose inhaler; 2 puffs BD; severe cases 4 puffs BD; also SEROBID ROTACAPS 50 µg; 1–2 caps BD by inhalation. SEROFLO—100/250/500 ROTACAPS: Salmeterol 50 µg + fluticasone 100 µg/250 µg/500 µg per rotacap SEROFLO—125/250, COMBITIDE—125/250, INHALERS: Salmeterol 25 µg + fluticasone 125 µg or 250 µg per puff. 5. Formoterol: 12–24 µg by inhalation twice daily; FORATEC 12 µg rotacaps. 6. Theophylline (Anhydrous): 100–300 mg TDS (15 mg/kg/ day), THEOLONG 100, 200 mg SR cap., DURALYN-CR 400 mg continuous release cap, UNICONTIN 400 mg, 600 mg CR tabs. 7. Aminophylline (Theophylline-ethylenediamine; 85% theophylline) water soluble, can be injected i.v. but not i.m. or s.c., 250–500 mg oral or slow i.v. injection; children 7.5 mg/kg i.v.; AMINOPHYLLINE 100 mg tab, 250 mg/10 ml inj. 8. Hydroxyethyl theophylline (Etophylline, 80% theophylline) water soluble; can be injected i.v. and i.m. (but not s.c.), 250 mg oral/i.m./i.v.; DERIPHYLLIN 100 mg tab., 300 mg SR tab., 220 mg/2 ml inj. 9. Choline theophyllinate (Oxtriphylline; 64% theophylline) 250–500 mg oral, CHOLIPHYLLINE 125 mg cap., 125 mg/5 ml elixir. 10. Theophylline ethanolate of piperazine: 250–500 mg oral or i.v.; CADIPHYLLATE, 80 mg/5 ml elixir; ETOPHYLATE 125 mg/5 ml syrup. 11. Doxophylline: 400 mg OD-BD, Children 12 mg/kg/day; DOXORIL 400 mg tab, 100 mg/5 ml syr. 12. Ipratropium bromide: 40–80 μg by inhalation; IPRAVENT 20 μg/puff metered dose inhaler, 2 puffs 3–4 times daily; 250 μg/ ml respirator soln., 0.4–2 ml nebulized in conjunction with a β2 agonist 2–4 times daily. 13. Tiotropium bromide: 18 μg by inhalation; TIOVA 18 μg rotacaps; 1 rotacap by inhalation OD. 28 Drugs for Respiratory Disorders 14. Montelukast: 10 mg OD; children 2–5 yr 4 mg OD, 6–14 yr 5 mg OD; EMLUKAST, MONTAIR, VENTAIR 4 mg, 5 mg, 10 mg tabs. 15. Zafirlukast: 20 mg BD; children 5–11 yr 10 mg BD; ZUVAIR 10 mg, 20 mg tabs. 16. Sodium cromoglycate: 2–10 mg by inhalation 3–4 times a day; FINTAL inhaler: 1 mg metered dose aerosol; 2 puffs 4 times daily. CROMAL-5 INHALER: 5 mg metered dose aerosol, 2 puffs 4 times daily. 17. Ketotifen: 1–2 mg BD; children 0.5 mg BD; ASTHAFEN 1 mg tab, 1 mg/5 ml syrup; KETOVENT 1 mg tab. 18. Beclomethasone dipropionate: Initially 100–200 μg BD by inhalation, increase as needed upto 400 μg QID; BECLATE INHALER 50 µg, 100 µg, 200 µg per metered dose, 200 doses inhaler, BECORIDE 50, 100, 250 µg per puff inhaler. BECLATE ROTACAPS (with rotahaler) 100, 200, 400 µg powder per cap. AEROCORT INHALER 50 µg/metered aerosol dose with salbutamol 100 µg. AEROCORT ROTACAPS 100 µg with salbutamol 200 µg rotacaps (with rotahaler). 19. Budesonide: 200–400 µg BD–QID by inhalation in asthma; 200– 400 µg/day by intranasal spray for allergic rhinitis. PULMICORT 100, 200, 400 µg/metered dose inhaler, BUDECORT 100 µg/metered dose inhaler. FORACORT: Formoterol 6 µg + Budesonide 100 µg/200 µg rotacaps. RHINOCORT 50 µg per metered dose nasal spray; BUDENASE AQ 100 µg/metered dose aqueous nasal spray; for prophylaxis and treatment of seasonal and perennial allergic or vasomotor rhinitis, nasal polyposis; initially 2 puffs in each nostril every morning, maintenance 1 puff in each nostril in the morning. 20. Fluticasone propionate: 100–250 μg BD (max 1000 μg/day) by inhalation; FLOHALE INHALER 25 µg, 50 µg, 125 µg per actuation. FLOHALE ROTACAPS 50 µg, 100 µg, 250 µg rotacaps. FLOMIST 50 µg per actuation nasal spray.  Drugs for Bronchial Asthma 29 21. Flunisolide: 25 μg by local spray in each nostril BD-TDS; SYNTARIS 25 μg per actuation nasal spray (for allergic rhinitis). 22. Ciclesonide: 80-160 μg by inhalation OD in the evening; CICLEZ 80 μg and 160 μg per metered dose inhaler. Note: For preparations of systemic corticosteroids –see Index. Some combined formulations BRONKOPLUS: Salbutamol 2 mg, anhydrous theophylline 100 mg tab., also per 5 ml syrup. BRONKOTUS: Bromhexine 8 mg, salbutamol 2 mg tab., also syrup— bromhexine 4 mg, salbutamol 2 mg per 5 ml. DUOLIN INHALER Salbutamol 100 μg + ipratropium 20 μg per metered dose inhaler. DUOLIN ROTACAP salbutamol 200 μg + ipratropium 40 μg per rotacap. DUOLIN RESPULES salbutamol 2.5 mg + ipratropium 500 μg in 2.5 ml respirator solution. TERPHYLIN: Terbutaline 2.5 mg, etophylline 100 mg tab. THEO ASTHALIN: Salbutamol 2 mg, theophylline anhydrous 100 mg tab. THEO ASTHALIN-SR: Salbutamol 4 mg, theophylline 300 mg SR tab, also syrup—Salbutamol 2 mg, theophylline 100 mg per 10 ml. THEO BRIC: Terbutaline 2.5 mg, theophylline 100 mg tab. THEOBRIC SR: Terbutaline 5 mg, theophylline 300 mg SR tab. 30 Hormones and Related Drugs Hormones and 4 Related Drugs Anterior Pituitary Hormones and Related Drugs A. Anterior pituitary hormones Growth hormone (GH), Prolactin (Prl.) Thyroid stimulating hormone (TSH, Thyrotropin) Adrenocorticotropic hormone (ACTH, Corticotropin) Gonadotropins (Gns): Follicle stimulating hormone (FSH), Luteinizing hormone (LH) B. Drugs altering anterior pituitary hormone secretion 1. Drugs inhibiting GH release: Somatostatin, Octreotide 2. Drugs inhibiting Prl release: Bromocriptine, Cabergoline, Apomorphine 3. Drugs enhancing Prl release: Chlorpromazine (and other neuroleptics), Metoclopramide, Reserpine 4. Superactive/long acting GnRH agonists: Nafarelin, Triptorelin, Buserelin, Goserelin, Leuprolide Preparations 1. Growth hormone (Somatropin: recombinant human GH): 0.03–0.07 mg/kg (0.06-0.16 IU/kg) i.m./s.c. 3 times a week; GENOTROPIN, NORDITROPIN 4 IU, 12 IU, 16 IU, 36 IU, SAIZEN 10 IU vials for injection (12 IU = 5 mg). 2. Corticotropin: ACTHAR inj. 5 ml vial (40 IU/ml on reconstitution) ACTH INJ 25 IU/ml, 50 IU/ml inj. 3. Menotropins (FSH + LH) obtained from urine of menopausal women:  Anterior Pituitary Hormones and Related Drugs 31 PREGNORM, PERGONAL, GYNOGEN 75/150; 75 IU FSH + 75 IU LH activity per amp, also 150 IU FSH + 150 IU LH per amp. 4. Urofollitropin or Menotropin (pure FSH): METRODIN, ENDOGEN, FOLICULIN, PUREGON 75 IU and 150 IU per amp. 5. Human chorionic gonadotropin (HCG) derived from urine of pregnant women. CORION, PROFASI, PUBERGEN 1000 IU, 2000 IU, 5000 IU, 10,000 IU, all as dry powder with separate solvent for injection. 6. Somatostatin: For upper g.i.bleeding 250 µg slow i.v. injection over 3 min followed by 3 mg i.v. infusion over 12 hours. STILMEN, SOMATOSAN 250 µg and 3 mg amps. 7. Octreotide: 100 μg i.v. followed by 25 μg/hour; SANDOSTATIN, OCTRIDE 50 μg, 100 μg in 1 ml amp. 8. Bromocriptine: Start with 1.25 mg BD, titrate upward upto 10 mg BD; PROCTINAL, PARLODEL, SICRIPTIN, BROMOGEN 1.25 mg, 2.5 mg tabs. 9. Cabergoline: Start with 0.25 mg twice weekly, increase upto 1 mg twice weekly as needed; CABERLIN 0.5 mg tab, CAMFORTE 0.5, 1 mg tabs. 10. Nafarelin: For endometriosis 200 μg intranasal spray BD; For precocious puberty 800 μg intranasal spray BD; NASAREL 2 mg/ ml solution for nasal spray, 200 μg per actuation. 11. Triptorelin: For endometriosis and carcinoma prostate: 2.5-3.75 mg of depot injection i.m. every 4 weeks; For female infertility: 0.1 mg s.c. daily for 10-12 days starting on 2nd day of menstruation; For precocious puberty: 50 μg/kg i.m. of depot injection every 4 weeks. DECAPEPTYL DAILY 0.1 mg inj, DECAPEPTYL DEPOT 3.75 mg inj, TRYPTOLOG 2.5 mg/5 ml inj. 12. Leuprorelin: For palliative treatment of advanced carcinoma prostate—1 mg s.c. OD or 3.75 mg i.m./s.c. once a month of depot preparation; LUPRIDE 1 mg inj, 3.75 mg depot inj, PROGTASE 1 mg/ml inj. Thyroid Hormone Thyroxine (T4) Triiodothyronine (T3, Liothyronine) 32 Hormones and Related Drugs Preparations l-Thyroxine sod: Adult hypothyroidism—start with 50 μg/day, increase every 2–3 weeks by 25–50 μg to the optimum dose of 100–200 μg/day adjusted by the clinical response and serum TSH level. Cretinism—6–8 μg/kg/day; ELTROXIN, ROXIN 100 μg tab, THYRONORM, THYROX 25 μg, 50 μg, 100 μg tabs. Thyroid Inhibitors 1. Inhibit hormone synthesis (Antithyroid drugs) Propylthiouracil, Methimazole, Carbimazole 2. Inhibit iodide trapping (Ionic inhibitors) Thiocyanates (–SCN), Perchlorates (–ClO4), Nitrates (–NO3) 3. Inhibit hormone release Iodine, Iodides of Na and K, Organic iodide. 4. Destroy thyroid tissue Radioactive iodine (131I, I, 125 123 I). Preparations 1. Propylthiouracil: 50–150 mg TDS followed by 25–50 mg BD–TDS for maintenance. PTU 50 mg tab. 2. Methimazole: 5–10 mg TDS initially, maintenance dose 5–15 mg daily in 1–2 divided doses. 3. Carbimazole: 5–15 mg TDS initially, maintenance dose 2.5–10 mg daily in 1–2 divided doses, NEO MERCAZOLE, THYROZOLE, ANTITHYROX 5 mg tab. 4. Lugol’s solution (5% iodine in 10% Pot. iodide solution): LUGOL’S SOLUTION, COLLOID IODINE 10%: 5–10 drops/day. COLLOSOL 8 mg iodine/5 ml liq. 5. Iodide (Sod./Pot.): 100–300 mg/day—therapeutic, 5–10 mg/ day prophylactic for endemic goiter.  Antidiabetic Drugs 33 Antidiabetic Drugs (Hypoglycaemic Drugs) INSULIN A. Rapid Acting 1. Insulin lispro 2. Insulin aspart 3. Insulin glulisine B. Short Acting 1. Regular (soluble) Insulin 2. Prompt Insulin Zinc Suspension (amorphous) or Semilente C. Intermediate Acting 1. Insulin Zinc Suspension or Lente (Ultra: Semi: 7:3) 2. Neutral Protamine Hagedorn (NPH) or Isophane Insulin D. Long Acting 1. Extended Insulin Zinc Suspension (crystalline) or Ultralente 2. Protamine Zinc Insulin (PZI) 3. Insulin glargine Preparations (Dose to be individualized according to requirement) I. Highly purified insulins (pork/beef) 1. ACTRAPID, RAPIDICA: Highly purified pork regular insulin; 40 U/ml. 2. LENTARD, ZINULIN: Highly purified pork lente insulin; 40 U/ml. 3. ACTRAPHANE, RAPIMIX, MIXTARD: Highly purified pork regular insulin (30%) and isophane insulin (70%) 40 U/ml. 4. ILETIN-NPH: Highly purified bovine-porcine isophane insulin 40 U/ml. 5. ACTRAPID MC: Monocomponent pork regular insulin; 40 U/ml, 100 U/ml. 6. MONOTRAD MC: Monocomponent pork lente insulin; 40 U/ml. 34 Hormones and Related Drugs II. Human insulins 1. HUMAN ACTRAPID: Human regular insulin; 40 U/ml, 100 U/ml, ACTRAPID HM PENFIL 100 U/ml pen inj., WOSULIN-R 40 U/ml inj and 100 U/ml pen injector cartridges. 2. HUMAN MONOTRAD: Human lente insulin; 40 U/ml, 100 U/ml. 3. HUMAN INSULATARD, HUMINSULIN-N: Human isophane insulin 40 U/ml, WOSULIN-N 40 U/ml inj and 100 U/ml cartridges. 4. HUMAN ACTRAPHANE, HUMINSULIN 30/70, HUMAN MIXTARD: Human soluble insulin (30%) and isophane insulin (70%), 40 U/ml, WOSULIN-30/70 40 U/ml inj and 100 U/ml cartridges. 5. ACTRAPHANE HM PENFIL: Human soluble insulin 30% + isophane insulin 70% 100 U/ml pen injector. 6. INSUMAN 50/50: Human soluble insulin 50% + isophane insulin 50% 40 U/ml inj; WOSULIN 50/50 40 U/ml inj. and 100 U/ml cartridges. III. Insulin analogues 1. Insulin Lispro (rDNA origin): HUMALOG 100 U/ml inj; to be injected s.c. within 15 min before or immediately after a meal. 2. Insulin Aspart: NOVOLOG, NOVORAPID 100 U/ml inj; NOVOMIX 30 FLEXPEN inj (biphasic insulin aspart). 3. Insulin Glargine: LANTUS OPTISET 100 U/ml prefilled pen injector 3 ml and vial 5 ml. ORAL HYPOGLYCAEMIC DRUGS 1. Sulfonylureas First generation Second generation Tolbutamide Glibenclamide (Glyburide) Chlorpropamide Glipizide Gliclazide Glimepiride 2. Biguanide Metformin 3. Meglitinide/Phenylalanine analogues Repaglinide Nateglinide 4. Thiazolidinediones Rosiglitazone Pioglitazone  Antidiabetic Drugs 35 5. α Glucosidase inhibitors Acarbose Miglitol 6. Dipeptidyl peptidase-4 (DPP-4) inhibitor Sitagliptin Vildagliptin Preparations 1. Tolbutamide: 0.5–3 g/day in 2–3 divided doses; RASTINON 0.5 g tab. 2. Chlorpropamide: 0.1–0.5 g OD; DIABINESE 0.1, 0.25 g tab. 3. Glibenclamide (Glyburide): 5–15 mg/day in 1–2 doses; DAONIL, EUGLUCON, BETANASE 2.5, 5 mg tab. 4. Glipizide: 5–20 mg/day in 1–2 doses; GLYNASE, GLIDE, MINIDIAB 5 mg tab. 5. Gliclazide: 40–240 mg/day in 1–2 doses; DIAMICRON 80 mg tab, DIAZIDE 20, 80 mg tab, GLIZID 30, 40, 80 mg tab. 6. Glimepiride: 1–6 mg OD; AMARYL, GLYPRIDE, GLIMER 1, 2 mg tab. 7. Metformin: 0.5–2.5 g/day in 2–4 doses; GLYCIPHAGE, GLYCOMET 0.5, 0.85 g tab. 8. Repaglinide: 1.5–8 mg/day in 3–4 doses; EUREPA, REGAN, RAPLIN 0.5, 1, 2 mg tab. 9. Nateglinide: 180–480 mg/day in 3–4 doses; GLINATE 60, 120 mg tab. 10. Rosiglitazone: 4–8 mg/day in 1–2 doses; REGLIT, ROSINORM, ROSS 2, 4, 8 mg tab. 11. Pioglitazone: 15–45 mg OD; PIONORM, PIOREST, PIOZONE 15, 30 mg tab. 12. Acarbose: 50–100 mg TDS taken just before each major meal; GLUCOBAY 50, 100 mg tabs, ASUCROSE, GLUCAR 50 mg tab. 13. Sitagliptin: 100 mg OD-BD before meals; JANUVIA 100 mg tab. 14. Vildagliptin: 50 mg OD-BD before meals; GALVUS 50 mg tab. 36 Hormones and Related Drugs Corticosteroids I. GLUCOCORTICOIDS A. Short acting Hydrocortisone (cortisol), Cortisone B. Intermediate acting Prednisolone, Methyl-prednisolone, Triamcinolone C. Long acting Dexamethasone, Betamethasone, Deflazacort II. MINERALOCORTICOIDS Desoxycorticosterone acetate (DOCA), Fludrocortisone, Aldosterone Preparations 1. Cortisone: 20–100 mg/day oral/i.m. 2. Hydrocortisone: 20–30 mg/day oral for replacement therapy; 100 mg i.v. 8 hourly (as hemisuccinate); 100–200 mg i.m./ intraarticular (as acetate), 2.0 g as retention enema; LYCORTIN-S, EFCORLIN SOLUBLE 100 mg/2 ml vial (as hemisuccinate for i.v. inj.) WYCORT, EFCORLIN 25 mg/ml vial (as acetate for i.m./intraarticualr inj.). PRIMACORT 100, 200, 400 mg/vial inj; ENTOFOAM 2 g in 20 g foam cream (10%) for retention enema. 3. Prednisolone: 5–60 mg/day oral, 10–40 mg i.m./intraarticular; DELTACORTRIL, HOSTACORTIN-H, 5, 10 mg tab, 20 mg/ml (as acetate) for i.m., intraarticular inj., WYSOLONE, NUCORT, 5, 10, 20, 40 mg tab. 4. Methyl prednisolone: 4–32 mg/day oral, 0.5–1.0 g slow i.v. injection for pulse therapy; SOLU-MEDROL Methylprednisolone (as sod. succinate) 4 mg tab; 40 mg, 125 mg, 0.5 g (8 ml) and 1.0 g (16 ml) vial, for i.m. or slow i.v. inj., DEESOLONE 4 mg, 16 mg tab, 0.5 g, 1.0 g inj. 5. Triamcinolone: 4–32 mg/day oral, 5–40 mg i.m./intraarticular; KENACORT, TRICORT 1, 4, 8 mg tab., 10 mg/ml, 40 mg/ml (as acetonide) for i.m., intraarticular inj., LEDERCORT 4 mg tab., KENALOG-S EYE 0.1% with neomycin 0.25% and gramicidin 0.025% eye oint.  Corticosteroids 37 6. Dexamethasone: 0.5–5 mg/day oral, 4–20 mg i.v. or i.m.; DECADRON, DEXONA 0.5 mg tab, 4 mg/ml (as sod. phosphate) for i.v., i.m. inj, 0.5 mg/ml oral drops; WYMESONE, DECDAN 0.5 mg tab, 4 mg/ml inj, OCUDEX, MINIDEX, DEXONA 0.1% eye drops. 7. Betamethasone: 0.5–5 mg/day oral, 4–20 mg i.v./i.m. inj; BETNESOL, BETACORTRIL, CELESTONE 0.5 mg, 1 mg tab, 4 mg/ml (as sod. phosphate) for i.v., i.m. inj., 0.5 mg/ml oral drops. BETNELAN 0.5 mg, 1 mg tabs, BETNESOL EYE/EAR 0.1% drops and oint. 8. Deflazacort: Initially 60-120 mg/day, maintenance 6-18 mg/ day, children 0.25-1.5 mg/kg on alternate days. DEFLAR, DEFZA, DFZ 1, 6, 30 mg tabs, DEFGLU 6, 30 mg tabs. 9. Desoxycorticosterone acetate (DOCA): 2–5 mg sublingual, 10–20 mg i.m. once or twice weekly; in DOCABOLIN 10 mg/ml inj. (along with nandrolone). 10. Fludrocortisone: Replacement therapy in Addison’s disease 50–200 μg daily. Congenital adrenal hyperplasia in patients with salt wasting 50–200 μg/day. Idiopathic postural hypotension 100–200 μg/day. FLORICORT 100 μg tab. TOPICAL STEROIDS A. Potent 1. Beclomethasone 0.025% BECLATE cream dipropionate 2. Betamethasone benzoate 0.025% TOPICASONE cream, oint. 3. Betamethasone valerate 0.12% BETNOVATE cream, oint., BETASONE cream 4. Halcinonide 0.1% CORTILATE, HALOG cream 5. Clobetasol propionate 0.05% LOBATE, TENOVATE, DERMOTYL cream 38 Hormones and Related Drugs 6. Dexamethasone 0.1% DECADRON cream sod. phosphate (with Neomycin 0.35%) 7. Dexamethasone 0.1% MILLICORTENOL trimethyl-acetate cream 8. Fluocinolone acetonide 0.025% FLUCORT oint., LUCI oint. 9. Fluocortolone 0.5% ULTRALAN oint. 10. Triamcinolone acetonide 0.1% LEDERCORT oint. Moderately potent 1. Fluocinolone acetonide 0.01% FLUCORT-H oint. and skin lotion 2. Clobetasol butyrate 0.05% EUMOSONE cream 3. Fluocortolone 0.25% COLSIPAN oint. 4. Mometasone 0.1% MOMATE, CUTIZONE oint, cream 5. Fluticasone propionate 0.05% FLUTIVATE, MOLIDERM cream 6. Hydrocortisone 1% COTARYL-H + urea 12% cream. 7. Hydrocortisone acetate 2.5% WYCORT oint. Mild 1. Hydrocortisone acetate 0.1– LYCORTIN 1% oint., 1.0% in CORTOQUINOL 1% with quiniodochlor 4% cream, GENTACYN-HC TOPICAL 1% with gentamicin 0.1%, CORTISON- KEMICETINE 0.5% with chlorampheni- col 0.5%. 2. Hydrocortisone butyrate 0.001% LOCOID cream  Androgens and Related Drugs 39 Androgens and Related Drugs Natural Androgens Testosterone, Dihydrotestosterone Synthetic Androgens Methyl testosterone, Fluoxymesterone, Mesterolone Preparations 1. Testosterone (free): 25 mg i.m. daily to twice weekly; AQUAVIRON 25 mg in 1 ml inj. 2. Testosterone propionate: 25–50 mg i.m. daily to twice weekly: TESTOVIRON, PARENDREN, TESTANON 25, 50 mg/ml inj. 3. TESTOVIRON DEPOT 100: testo. propionate 25 mg + testo. enanthate 100 mg in 1 ml amp; 1 ml i.m. weekly. 4. TESTOVIRON DEPOT 250: testo. propionate 250 mg + testo. enanthate 250 mg in 1 ml amp; i.m. every 2–4 weeks. 5. SUSTANON ‘100’: testo. propionate 20 mg + testo. phenyl propionate 40 mg + testo. isocaproate 40 mg in 1 ml amp; 1 ml i.m. every 2–3 weeks. 6. SUSTANON ‘250’: testo. propionate 30 mg + testo. phenylpropionate 60 mg + testo. isocaproate 60 mg + testo. decanoate 100 mg in 1 ml amp; 1 ml i.m. every 3–4 weeks. 7. Testosterone undecanoate: NUVIR 40 mg cap, 1–3 cap daily for male hypogonadism, osteoporosis. 8. Mesterolone: 25 mg OD–TDS oral; PROVIRONUM, MESTILON 25 mg tab. 9. Dihydrotestosterone: 100–250 mg cutaneous application daily; ANDRACTIM 25 mg/g gel for application over nonscrotal skin once daily. Anabolic Steroids 1. Methandienone: 2–5 mg OD–BD oral; children 0.04 mg/kg/day, 25 mg i.m. weekly; ANABOLEX 2, 5 mg tab, 2 mg/ml drops, 25 mg/ml inj. 2. Nandrolone phenyl propionate: 10–50 mg; children 10 mg; i.m. once or twice weekly; DURABOLIN 10, 25 mg/ml inj. 40 Hormones and Related Drugs 3. Nandrolone decanoate: 25–100 mg i.m. every 3 weeks, DECADURABOLIN, 25, 100 mg/ml inj. 4. Oxymetholone: 5–10 mg, children 0.1 mg/kg, OD; ADROYD 5 mg tab. 5. Stanozolol: 2–6 mg/day; MENABOL, NEURABOL 2 mg tab. Impeded Androgen 1. Danazol: 200–800 mg/day; DANAZOL, LADOGAL, DANOGEN, GONABLOK 50, 100, 200 mg cap. Antiandrogens Cyproterone acetate Flutamide Bicalutamide Nilutamide 1. Flutamide: 250 mg TDS; PROSTAMID, FLUTIDE, CYTOMID 250 mg tab. 2. Bicalutamide: 50 mg OD; BIPROSTA, CALUTIDE, TABI 50 mg tab. α -Reductase Inhibitor 5α 1. Finasteride: For benign hypertrophy of prostate (BHP) 5 mg OD, review after 6 months; for male pattern baldness 1 mg/day. FINCAR, FINARA, FINAST 5 mg tab, FINPECIA, ASTIFINE 1 mg tab. 2. Dutasteride: For BHP 0.5 mg/day. DUPROST, DURIZE 0.5 mg tab. Drugs for Erectile Dysfunction 1. Androgens 2. Phosphodiesterase-5 (PDE-5) inhibitors Sildenafil Tadalafil Vardenafil 3. Papaverine/phentolamine (intracavernosal injection) 4. Prostaglandin E1 (PGE1): Alprostadil (intracavernosal injection)  Estrogens and Related Drugs 41 Preparations 1. Sildenafil: 50 mg (max. 100 mg) 1 hour before intercourse; elderly 25 mg. PENEGRA, CAVERTA, EDEGRA 25, 50, 100 mg tabs. 2. Tadalafil: 10 mg (max. 20 mg) at least ½ hr before intercourse. MEGALIS, TADARICH, TADALIS 10, 20 mg tab, MANFORCE 10 mg tab. Estrogens and Related Drugs Natural Estrogens Estradiol, Estrone, Estriol, Equilin Synthetic Estrogens 1. Steroidal: Ethinylestradiol, Mestranol, Tibolone. 2. Nonsteroidal: Diethylstilbestrol, Hexestrol, Dienestrol. Preparations 1. Estradiol benzoate/cypionate/enanthate/valarate: 2.5–10 mg i.m.; OVOCYCLIN-P 5 mg inj, PROGYNON DEPOT 10 mg/ml inj. 2. Conjugated estrogens: 0.625–1.25 mg/day oral; PREMARIN 0.625 mg, 1.25 mg tab, 25 mg inj (for dysfunctional uterine bleeding). 3. Ethinylestradiol: for menopausal syndrome 0.02–0.2 mg/day oral; LYNORAL 0.01, 0.05, 1.0 mg tab, PROGYNON-C 0.02 mg tab. 4. Mestranol: 0.1–0.2 mg/day oral; in OVULEN 0.1 mg tab, with ethynodiol diacetate 1 mg. 5. Estriol succinate: 4–8 mg/day initially, maintenance dose in menopause 1–2 mg/day oral: EVALON 1, 2 mg tab, 1 mg/g cream for vaginal application in atrophic vaginitis 1–3 times daily. 6. Fosfestrol tetrasodium: initially 600–1200 mg slow i.v. inj for 5 days, maintenance dose 120–240 mg/day oral or 300 mg 1– 3 times a week i.v.; HONVAN 120 mg tab, 60 mg/ml inj 5 ml amp. 7. Dienestrol: 0.01% topical; DIENESTROL 0.01% vaginal cream. 42 Hormones and Related Drugs 8. Estradiol transdermal: ESTRADERM-MX: Estradiol 25, 50 or 100 μg per 24 hr transdermal patches; apply to nonhairy skin below waist, replace every 3–4 days using a different site; add an oral progestin for last 10–12 days every month. 9. Estradiol dermal gel: 1–2.5 mg/day; OESTRAGEL 3 mg/ 5 g gel in 80 g tube; apply 1.5-4 g gel over arms & shoulder daily. 10. Tibolone: 2.5 mg/day without interruption in postmenopausal women; LIVIAL, TIBOFEM 2.5 mg tab. Antiestrogen Clomiphene citrate: for infertility in women—50 mg/day for 5 days starting from 5th day of cycle, increase to 100 mg/day after 2–3 unsuccessful cycles (max. 200 mg/day); for oligozoospermia in men— 25 mg daily for 24 days in a month upto 6 months; CLOMID, FERTOMID 25, 50 mg tabs, CLOFERT, CLOME 25, 50, 100 mg tabs. Selective Estrogen Receptor Down Regulator/ Pure Estrogen Antagonist Fulvestrant: 250 mg i.m. (in gluteal region) monthly. Selective Estrogen Receptor Modulators (SERMs) 1. Tamoxifen citrate: 10–20 mg BD. TAMOXIFEN, MAMOFEN, TAMODEX 10, 20 mg tabs. 2. Toremifene: 60 mg OD. 3. Raloxifene: 60 mg/day; OSRAL, BONMAX, RALOTAB, ESSERM 60 mg tab. Aromatase Inhibitors 1. Letrozole: 2.5 mg/day oral; FEMARA, ONCOLET, LETOVAL, LETROZ 2.5 mg tab. 2. Anastrozole: 1 mg/day oral; ARMOTRAZ, ALTRAZ 1 mg tab. 3. Exemestane: 25 mg/day oral.  Progestins 43 Progestins Progesterone derivatives Medroxyprogesterone Hydroxyprogesterone acetate caproate Megestrol acetate Nomegestrol acetate Dydrogesterone 19-Nortestosterone derivatives Older compounds Newer compounds (Gonanes) Norethindrone Desogestrel (Norethisterone) Norgestimate Lynestrenol (Ethinylestrenol) Gestodene Allylestrenol Levonorgestrel (Gonane) Preparations 1. Progesterone: 10–100 mg i.m. (as oily solution) OD; PROGEST, PROLUTON, GESTONE 50 mg/ml inj., 1 and 2 ml amp; 100–400 mg OD oral: NATUROGEST, OGEST, DUBAGEST 100, 200, 400 mg caps containing micronized oily suspension. 2. Hydroxyprogesterone caproate: 250–500 mg i.m. at 2–14 days intervals; PROLUTON DEPOT, MAINTANE INJ, PROCAPRIN 250 mg/ml in 1 and 2 ml amp. 3. Medroxyprogesterone acetate: 5–20 mg OD–BD oral, 50–150 mg i.m. at 1–3 month interval; FARLUTAL 2.5, 5, 10 mg tab., PROVERA, MEPRATE, MODUS 10 mg tab, DEPOT-PROVERA 150 mg in 1 ml inj. (as contraceptive). 4. Dydrogesterone: 5–10 mg OD/TDS oral; DUPHASTON 5 mg tab. 5. Norethindrone (Norethisterone): 5–10 mg OD–BD oral; PRIMOLUT-N, STYPTIN, REGESTRONE, NORGEST 5 mg tab; REGESTRONE HRT, NORETA HRT 1 mg tab (for HRT); 44 Hormones and Related Drugs NORISTERAT 200 mg/ml inj (as enanthate) for contraception 1 ml i.m every 2 months. 6. Lynestrenol (Ethinylestrenol): 5–10 mg OD oral; ORGAMETRIL 5 mg tab. 7. Allylestrenol: 10–40 mg/day; GESTANIN, FETUGARD, MAINTANE 5 mg tab, PROFAR 25 mg tab. 8. Levonorgestrel: 0.1–0.5 mg/day; DUOLUTON-L, OVRAL 0.25 mg + ethinylestradiol 0.05 mg tab. 9. Desogestrel: 150 µg + ethinylestradiol 30 µg (NOVELON) tab, 1 tab OD, 3 weeks on 1 week off cyclic therapy. Antiprogestin 1. Mifepristone: 200–600 mg single oral dose; MIFEGEST, MIFEPRIN 200 mg tab. 2. Onapristone 3. Gestinone Oral Contraceptives Combined Pills 1. Norgestrel 0.3 mg + Ethinylestradiol 30 µg; MALA-D (21 tabs + 7 ferrous sulfate 60 mg tabs) 2. Norgestrel 0.5 mg + Ethinylestradiol 50 µg; OVRAL-G 3. Levonorgestrel 0.25 mg + Ethinylestradiol 50 µg; OVRAL, DUOLUTON-L 4. Levonorgestrel 0.15 mg + Ethinylestradiol 30 µg; OVRAL-L, BANDHAN 5. Desogestrel 0.15 mg + Ethinylestradiol 30 µg; NOVELON 6. Desogestrel 0.15 mg + Ethinylestradiol 20 µg; FEMILON Phased Pills 1. Levonorgestrel 50–75–125 µg + Ethinylestradiol 30–40–30 µg; TRIQUILAR (6 + 5 + 10 tablets) 2. Norethindrone 0.5–0.75–1.0 mg + Ethinylestradiol 35–35–35 µg; ORTHONOVUM 7/7/7 (7+7+7 tabs)  Uterine Stimulants 45 Postcoital Pills 1. Levonorgestrel 0.25 mg + Ethinylestradiol 50 µg; OVRAL, DUOLUTON-L (2 + 2 tabs) 2. Levonorgestrel 0.75 mg; NORLEVO, ECEE2 (1 + 1 tab) 3. Levonorgestrel 1.5 mg iPILL (1 tab). 4. Mifepristone 600 mg; MIFEGEST, MIFEPRIN 200 mg (3 tabs) Mini Pills 1. Norethindrone 0.35 mg 2. Norgestrel 75 µg Anti implantation SERM Centchroman (Ormeloxifene); 30 mg twice weekly for 12 weeks and then 30 mg weekly; CENTRON, SAHELI 30 mg tab. Injectable contraceptives 1. Depot medroxyprogesterone acetate (DMPA): 150 mg i.m. at 3 month intervals. DEPOT-PROVERA 150 mg in 1 ml vial for deep i.m. injection during first 5 days of menstrual cycle. Repeat every 3 months. 2. Norethindrone (Norethisterone) enanthate (NEE): 200 mg i.m. at 2 month intervals. NORISTERAT 200 mg in 1 ml vial for deep i.m. injection during first 5 days of menstrual cycle. Repeat every 2 months. Uterine Stimulants (Oxytocics, Abortifacients) 1. Posterior pituitary hormone: Oxytocin; Desamino- oxytocin 2. Ergot alkaloids: Ergometrine (Ergonovine), Methylergo- metrine 3. Prostaglandins: PGE 2 , PGF 2α, 15-methyl PGF 2α , Misoprostol 4. Miscellaneous: Ethacridine, Quinine. 46 Hormones and Related Drugs Preparations 1. Oxytocin: for induction/augmentation of labour 2–10 milli IU/ min i.v. infusion (total 2–4 IU); for postpartum haemorrhage 5 IU i.m. or i.v. infusion; OXYTOCIN, SYNTOCINON 2 IU/2 ml and 5 IU/ml inj., PITOCIN 5 IU/0.5 ml inj. 2. Desamino-oxytocin: for induction 50 IU buccal every 30 min, for uterine inertia 25 IU buccal every 30 min; for breast engorgement 25–50 IU just before breast feeding; BUCTOCIN 50 IU buccal tab. 3. Ergometrine: 0.2–0.5 mg i.m./i.v., 0.25–0.5 mg TDS oral; ERGOMETRINE 0.25, 0.5 mg tab, 0.5 mg/ml inj. 4. Methylergometrine: 0.2–0.5 mg i.m./i.v., 0.125–0.25 mg TDS oral; METHERGIN, METHERONE, ERGOMET 0.125 mg tab, 0.2 mg/ml inj. 5. Ethacridine: 150 mg extra-amniotic infusion; EMCREDIL, VECREDIL 50 mg/50 ml inj. (Note: For preparations of prostaglandins See p. 17) Uterine Relaxants (Tocolytics) 1. β-Adrenergic agonists: Ritodrine, Salbutamol, Terbu- taline, Isoxsuprine 2. Calcium channel blockers: Nifedipine (and other dihydropyridines) 3. Magnesium sulfate 4. Progesterone 5. Oxytocin antagonist: Atosiban 6. Miscellaneous drugs: Nitrates, Diazoxide, Atropine, Ethyl alcohol, Chlorpromazine, Halothane, PG synthesis inhibitors. (Note: For preparations – See Index)  Drugs Acting on 5 Peripheral (somatic) Nervous System Skeletal Muscle Relaxants PERIPHERALLY ACTING MUSCLE RELAXANTS I. Neuromuscular blocking agents A. Nondepolarizing (Competitive) blockers 1. Long acting: d-Tubocurarine, Pancuronium, Doxacurium, Pipecuronium 2. Intermediate acting: Vecuronium, Atracurium, Cisatracurium, Rocuronium, Rapacuronium 3. Short acting: Mivacurium B. Depolarizing blockers Succinylcholine (SCh., Suxamethonium), Decamethonium (C-10) II. Directly acting agents Dantrolene sodium Quinine CENTRALLY ACTING MUSCLE RELAXANTS 1. Mephenesin congeners: Mephenesin, Carisoprodol, Chlorzoxazone, Chlormezanone, Methocarbamol 2. Benzodiazepines: Diazepam and others 3. GABA derivative: Baclofen 4. Central α2 agonist: Tizanidine 48 Drugs Acting on Peripheral Nervous System Preparations (Note: Doses of neuromuscular blocking agents given below are initial paralysing doses for nitrous oxide- oxygen/opioid anaesthesia. These doses are to be reduced to 1/3–1/2 in patients anaesthetised with ether/ halothane/isoflurane etc.) 1. d-Tubocurarine: 0.2–0.4 mg/kg i.v. 2. Pancuronium: 0.04–0.1 mg/kg i.v.; PAVULON, PANURON, NEOCURON 2 mg/ml in 2 ml amp. 3. Doxacurium: 0.03–0.08 mg/kg i.v. 4. Pipecuronium: 0.05–0.08 mg/kg i.v.; ARDUAN 4 mg/2 ml inj. 5. Vecuronium: 0.08–0.1 mg/kg i.v.; NORCURON, NEOVEC 4 mg amp. and 10 mg vial; dissolve in 1–2.5 ml solvent supplied. 6. Atracurium: 0.3–0.6 mg/kg i.v.; TACRIUM 10 mg/ml in 2 ml vial. 7. Cisatracurium: 0.15–0.2 mg/kg i.v. 8. Rocuronium: 0.6–0.9 mg/kg i.v.; CUROMID, ROCUNIUM 50 mg/5 ml, 100 mg/10 ml vials. 9. Mivacurium: 0.07–0.15 mg/kg i.v. 10. Succinylcholine (Suxamethonium): 0.5–0.8 mg/kg i.v.; MIDARINE, SCOLINE, MYORELEX, ENTUBATE 50 mg/ml in 2 ml amp. 11. Dantrolene: 25–100 mg QID oral, 1 mg/kg i.v. repeated as required. 12. Carisoprodol: 350 mg TDS–QID oral; CARISOMA 350 mg tab; SOMAFLAM 175 mg + ibuprofen 400 mg tab. 13. Chlorzoxazone: 500 mg BD–TDS; PARAFON DSC 500 mg tab; MOBIZOX 500 mg + diclofenac 50 mg + paracetamol 500 mg tab; PARAFON: 250 mg + paracetamol 300 mg tab; FLEXON-MR 250 mg + ibuprofen 400 mg + paracetamol 325 mg tab. 14. Chlormezanone: 100–200 mg TDS–QID; WINTRAC 100 mg tab; DOLOBAK 100 mg + paracetamol 450 mg tab. 15. Methocarbamol: 400–800 mg TDS oral, 100–200 mg i.m./i.v.; ROBINAX 0.5 g tab, 1 TDS: 100 mg/ml inj. for i.v. or i.m. use.  Local Anaesthetics 49 ROBIFLAM 750 mg + ibuprofen 200 mg tab; FLEXINOL 400 mg + paracetamol 325 mg tab. 16. Baclofen: 10 mg BD–25 mg TDS oral; LIORESAL, LIOFEN 10, 25 mg tabs. 17. Tizanidine: 2 mg TDS; max 24 mg/day; SIRDALUD 2 mg tab; TIZAN 2, 4 mg tab; TIZAFEN 2 mg + ibuprofen 400 mg tab; TIZANAC 2 mg + diclofenac 50 mg tab., PROXIVON-MR 2 mg + nimesulide 100 mg cap. Local Anaesthetics A. Injectable anaesthetic 1. Low potency, short duration Procaine Chloroprocaine 2. Intermediate potency and duration Lidocaine (Lignocaine) Prilocaine 3. High potency, long duration Tetracaine (Amethocaine) Bupivacaine Ropivacaine Dibucaine (Cinchocaine) B. Surface anaesthetic Soluble Insoluble Cocaine Benzocaine Lidocaine Butylaminobenzoate Tetracaine (Butamben) Benoxinate Oxethazaine Preparations 1. Lidocaine (lignocaine): 0.5–2% for nerve block, 1–5% topically; XYLOCAINE, GESICAIN 4% topical solution, 2% jelly, 2% viscous, 5% ointment, 1% and 2% injection (with or without 50 Drugs Acting on Peripheral Nervous System adrenaline), 5% heavy (for spinal anaesthesia); 100 mg/ml spray (10 mg per puff) 2. Bupivacaine: 0.25–0.5% for nerve block, 0.5–0.75% for spinal anaesthesia; MARCAIN 0.5%, 1% (hyperbaric for spinal anaesthesia). SENSORCAINE 0.25%, 0.5% inj, 0.5% heavy inj. 3. Tetracaine (Amethocaine): 0.25% for nerve block, 0.25–0.5% for spinal anaesthesia, 1% topically; ANETHANE powder for preparing solution, 1% oint. 4. Eutectic Lidocaine-prilocaine: 5% for cutaneous anaesthesia; PRILOX 5% cream 5. Dibucaine: 0.25–0.5% for nerve block and spinal anaesthesia, 1% for surface anaesthesia; NUPERCAINE 0.5% inj, NUPERCAINAL 1% oint, in OTOGESIC 1% ear drops. 6. Benzocaine: 5–20% topically; in PROCTOQUINOL 5% oint., ZOKEN 20% gel. 7. Butylaminobenzoate: 1–5% topically; in PROCTO SEDYL- M 1% oint with framycetin and hydrocortisone for anal application. 8. Benoxinate: 0.4% for corneal anaesthesia; BENDZON 0.4% eye drops. 9. Oxethazaine: 0.2% for gastric mucosal anaesthesia; MUCAINE 0.2% in alumina gel + magnesium hydroxide suspension; 5–10 ml orally. TRICAINE-MPS: Oxethazaine 10 mg with methyl polysiloxane 125 mg, alum. hydroxide gel 300 mg, mag. hydroxide 150 mg per 5 ml gel.  6 Drugs Acting on Central Nervous System General Anaesthetics Inhalational Gas Volatile liquids Nitrous oxide Ether Halothane Enflurane Isoflurane Desflurane Sevoflurane Intravenous Inducing agents Slower acting drugs Thiopentone sod. Benzodiazepines Methohexitone sod. Diazepam Propofol Lorazepam Etomidate Midazolam Dissociative anaesthesia Ketamine Opioid analgesia Fentanyl Preparations 1. Thiopentone sod.: 3–5 mg/kg i.v. for induction; PENTOTHAL, INTRAVAL SODIUM 0.5, 1.0 g for preparing injectable solution freshly. 2. Propofol: 2 mg/kg bolus i.v. injection for induction, 9 mg/kg/ hr for maintenance; PROPOVAN 10 mg/ml and 20 mg/ml in 10, 20 ml vials. 52 Drugs Acting on Central Nervous System 3. Diazepam: 0.25–0.5 mg/kg by slow injection in a running i.v. drip; VALIUM, CALMPOSE 10 mg/2 ml inj. 4. Lorazepam: 0.04 mg/kg (2–4 mg total for adult) i.v.; CALMESE 4 mg/2 ml inj. 5. Midazolam: 1–2.5 mg i.v. bolus injection, 0.02–0.1 mg/kg/hour i.v. infusion for maintenance; MEZOLAM, FULSED, SHORTAL 1 mg/ml and 5 mg/ml inj. 6. Ketamine: 1–3 mg/kg i.v., 5 mg/kg i.m.; KETMIN, KETAMAX, ANEKET 50 mg/ml in 2 ml amp, 10 ml vial. 7. Fentanyl: 2–4 μg/kg i.v.; TROFENTYL, FENT 50 μg/ml in 2 ml amp, 10 ml vial. Preanaesthetic Medication 1. Opioids: Morphine, Pethidine, Fentanyl 2. Sedative-antianxiety drugs: Diazepam, Lorazepam, Midazolam, Promethazine 3. Anticholinergics: Atropine, Hyoscine, Glycopyrrolate 4. Neuroleptics: Chlorpromazine, Triflupromazine, Haloperidol 5. Histamine H2 blockers: Ranitidine, Famotidine, etc. 6. Proton pump inhibitors: Omeprazole, Pantoprazole, etc. 7. Antiemetics: Metoclopramide, Domperidone, Ondan- setron. (Note: See Index for preparations) Sedative-Hypnotics 1. Barbiturates Long acting Short acting Ultra short acting Phenobarbitone Butobarbitone Thiopentone Pentobarbitone Methohexitone 2. Benzodiazepines Hypnotic Antianxiety Anticonvulsant Diazepam Diazepam Diazepam  Sedative-Hypnotics 53 Flurazepam Chlordiazepoxide Lorazepam Nitrazepam Oxazepam Clonazepam Alprazolam Lorazepam Clobazam Temazepam Alprazolam Triazolam 3. Newer nonbenzodiazepine hypnotics Zopiclone, Zolpidem, Zaleplon 4. Other CNS depressants Chloral hydrate, Triclophos, Paraldehyde, Glutethimide, Methyprilone, Methaqualone, Meprobamate, Promethazine, Chlorpromazine, Amitriptyline, Morphine, Hyoscine Preparations 1. Phenobarbitone: 30–60 mg OD–TDS (as antiepileptic) 100–200 mg i.m./i.v.; GARDENAL 30, 60 mg tab; LUMINAL 30 mg tab; PHENOBARBITONE SOD 200 mg/ml inj. 2. Diazepam: 2.5–10 mg (as hypnotic), 5–30 mg/day (as antianxiety); VALIUM 2, 5, 10 mg tab., 10 mg/2 ml inj., CALMPOSE 5, 10 mg tab, 2 mg/5 ml syr, 10 mg/2 ml inj. 3. Flurazepam: 15–30 mg (as hypnotic); NINDRAL, FLURAZ 15 mg cap. 4. Nitrazepam: 5–10 mg (as hypnotic); SEDAMON, HYPNOTEX, NITRAVET 5, 10 mg tab/cap. 5. Alprazolam: 0.25–1.0 mg (hypnotic dose), 0.25–1.0 mg TDS for anxiety; ALPRAX 0.25, 0.5, 1.0 mg tabs., 0.5, 1.0, 1.5 mg SR tabs; ALZOLAM 0.25, 0.5, 1.0 mg tabs; 1.5 mg SR tab, RESTYL 0.25, 0.5, 1.0 mg tab, RESTYL-SR 0.5, 1.0, 1.5 mg SR tab. 6. Temazepam: 10–20 mg (as hypnotic). 7. Triazolam: 0.125–0.25 mg (as hypnotic). 8. Zopiclone: 7.5 mg (hypnotic dose), elderly 3.75 mg; ZOPICON, ZOLIUM, ZOPITRAN 7.5 mg tab. 9. Zolpidem: 10–20 mg (hypnotic dose), elderly and liver disease patients 5–10 mg; NITREST, ZOLDEM, DEM 5, 10 mg tabs. 54 Drugs Acting on Central Nervous System 10. Zaleplon: 5–10 mg (max 20 mg) hypnotic dose; ZAPLON, ZASO, ZALEP 5, 10 mg tabs. (Note: See Index for preparations of other drugs). Antiepileptic Drugs 1. Barbiturate: Phenobarbitone 2. Deoxybarbiturate: Primidone 3. Hydantoin: Phenytoin, Fosphenytoin 4. Iminostilbene: Carbamazepine, Oxcarbazepine 5. Succinimide: Ethosuximide 6. Aliphatic carboxylic acid: Valproic acid (sodium valproate), Divalproex 7. Benzodiazepines: Clonazepam, Diazepam, Lorazepam, Clobazam 8. Phenyltriazine: Lamotrigine 9. Cyclic GABA analogue: Gabapentin, Pregabalin 10. Newer drugs: Vigabatrin, Topiramate, Tiagabine, Zonisamide, Levetiracetam Preparations 1. Phenobarbitone: 60 mg OD–TDS (child 3–6 mg/kg/day), 100–200 mg i.m./i.v.; GARDENAL 30, 60 mg tab; LUMINAL 30 mg tab; PHENOBARBITONE SOD 200 mg/ml inj. 2. Primidone: 250–500 mg BD (child 10–20 mg/kg/day); MYSOLINE 250 mg tab. 3. Phenytoin: 100–200 mg BD (child 5–8 mg/kg/day) oral, 25 mg/min slow i.v. injection (max 1.0 g); DILANTIN 25 mg, 100 mg cap., 100 mg/4 ml oral suspension, 100 mg/2 ml inj.; EPTOIN 50, 100 mg tab, 25 mg/ml syr; FENTOIN-ER 100 mg extended release cap. 4. Fosphenytoin: 25-100 mg (as phenytoin sod. equivalent)/min i.v. injection (max 1.0 g) for generalized convulsive status epilepticus; FOSOLIN 50 mg/ml inj in 2 ml and 10 ml amp. 5. Carbamazepine: 200–400 mg TDS, children 15–30 mg/kg/ day; TEGRETOL, MAZETOL 100, 200, 400 mg tab, 100 mg/5 ml  Antiepileptic Drugs 55 syr; CARBATOL 100, 200, 400 mg tab; MAZETOL-SR, TEGRITAL-CR 200, 400 mg sustained release tabs. 6. Oxcarbazepine: 300–600 mg BD; OXCARB, OXEP, OXETOL 150, 300, 600 mg tabs. 7. Ethosuximide: 20–30 mg/kg/day; ZARONTIN 250 mg/5 ml syr. 8. Valproic acid (Sodium valproate): Adults—start with 200 mg TDS, maximum 800 mg TDS; children—15–30 mg/kg/day; VALPARIN CHRONO 200, 300, 500 mg tabs, 200 mg/5 ml syr, ENCORATE 200, 300, 500 mg regular and controlled release tabs, 200 mg/5 ml syr, 100 mg/ml inj. 9. Divalproex: Epilepsy—initially 15 mg/kg/day, increase gradually as required (max 60 mg/kg/day); Bipolar disorder 250–500 mg TDS; Migraine 250–500 mg BD; DIPROEX, VALANCE, DEPAKOTE 125, 250, 500 mg tabs. 10. Clonazepam: Adults 0.5–5 mg TDS, children 0.02–0.2 mg/kg/ day; status epilepticus 1–2 mg slow i.v. inj; LONAZEP, CLONAPAX, RIVOTRIL 0.5, 1.0, 2.0 mg tab. 11. Diazepam: for status epilepticus—10 mg (0.2–0.5 mg/kg) slow i.v. injection (2 mg/min), repeat fractional doses as required (max 100 mg/day); for febrile convulsions 0.5 mg/kg rectal instillation, repeat 12 hourly for 48 hours; VALIUM, CALMPOSE, PLACIDOX 10 mg/2 ml inj. 12. Lorazepam: for status epilepticus—0.04–0.1 mg/kg slow i.v. injection (2 mg/min); CALMESE 4 mg/2 ml inj. 13. Clobazam: start with 10–20 mg at bed time, can be increased upto 60 mg/day; FRISIUM, LOBAZAM, CLOZAM 5, 10, 20 mg cap. 14. Lamotrigine: 50 mg/day initially, increase upto 300 mg/day as needed. LAMITOR, LAMETEC, LAMIDUS 25, 50, 100 mg tabs. 15. Gabapentin: start with 300 mg OD, increase to 300–600 mg TDS as required; NEURONTIN, GABANTIN 300 mg, 400 mg cap, GABAPIN 100, 300, 400 mg cap. 16. Pregabalin: 75-150 mg BD, max. 600/day (used primarily for neuropathic pain). PREEGA, TRUGABA 75, 150 mg caps. 17. Vigabatrin: 2–4 g/day, child 40–100 mg/kg/day. 18. Topiramate: Initially 25 mg OD, increase weekly upto 100–200 mg BD as required, child 5–10 mg/kg/day. TOPEX, EPITOP, TOPAMATE, NEXTOP 25, 50, 100 mg tabs. 56 Drugs Acting on Central Nervous System 19. Zonisamide: 25-100 mg BD; ZONISEP, ZONICARE, ZONIT 50, 100 mg cap. 20. Levetiracetam: 250-750 mg BD; child > 4 year 10 mg/kg BD. EPIFAST, TORLEVA, LEVROXA 250, 500, 750 mg tabs. Antiparkinsonian Drugs 1. Drugs Affecting Brain Dopaminergic System (a) Dopamine precursor : Levodopa (l–dopa) (b) Peripheral decarboxylase inhibitors: Carbidopa, Benserazide (c) Dopaminergic agonists: Bromocriptine, Ropinirole, Pramipexole (d) MAO-B inhibitor: Selegiline (e) COMT inhibitors: Entacapone, Tolcapone (f) Dopamine facilitator: Amantadine 2. Drugs Affecting Brain Cholinergic System (a) Central anticholinergics: Trihexyphenidyl (Benzhexol), Procyclidine, Biperiden (b) Antihistaminics: Orphenadrine, Promethazine. Preparations 1. Levodopa: Start with 0.25 g BD after meals, gradually increase till adequate response is obtained. Usual dose is 2–3 g/day. LEVOPA, BIDOPAL 0.5 g tab. 2. Carbidopa/Benserazide + Levodopa combination: Usual daily maintenance dose of levodopa is 0.4–0.8 g along with 75–100 mg carbidopa or 100–200 mg benserazide, given in 3–4 divided