Essentials of Pharmacology for Dentistry Essentials of Pharmacology for Dentistry 2ND EDITION KD TRIPATHI MD Ex-Director-Professor and Head of Pharmacology Maulana Azad Medical College and associated LN and GB Pant Hospitals New Delhi, India ® JAYPEE BROTHERS MEDICAL PUBLISHERS (P) LTD New Delhi • Panama City (cid:129) London ® Jaypee Brothers Medical Publishers (P) Ltd. Headquarter Jaypee Brothers Medical Publishers (P) Ltd 4838/24, Ansari Road, Daryaganj New Delhi 110 002, India Phone: +91-11-43574357 Fax: +91-11-43574314 Email: [email protected] Overseas Offices J.P. Medical Ltd., Jaypee-Highlights Medical Publishers Inc. 83 Victoria Street London City of Knowledge, Bld. 237, Clayton SW1H 0HW (UK) Panama City, Panama Phone: +44-2031708910 Phone: 507-317-0160 Fax: +02-03-0086180 Fax: +50-73-010499 Email: [email protected] Email: [email protected] Website: www.jaypeebrothers.com Website: www.jaypeedigital.com © 2011 KD Tripathi All rights reserved. No part of this book may be reproduced in any form or by any means without the prior permission of the publisher. Inquiries for bulk sales may be solicited at: [email protected] This book has been published in good faith that the contents provided by the author contained herein are original, and is intended for educational purposes only. While every effort is made to ensure accuracy of information, the publisher and the author specifically disclaim any damage, liability, or loss incurred, directly or indirectly, from the use or application of any of the contents of this work. If not specifically stated, all figures and tables are courtesy of the author. Where appropriate, the readers should consult with a specialist or contact the manufacturer of the drug or device. Publisher: Jitendar P Vij Publishing Director: Tarun Duneja Managing Editor: M. Tripathi Essentials of Pharmacology for Dentistry First Edition: 2005 Second Edition: 2011 ISBN-13: 978-93-5025-385-4 Printed at Replika Press, Kundli Preface to the Second Edition With phenomenal growth of information on mechanism of action and clinical application of drugs, as well as rapid introduction of new drugs, pharmacology, the science of drugs (medicines), has become increasingly important to all health professionals who prescribe/administer drugs. Practice of dentistry utilizes drugs both as primary treatment modality as well as facilitator of dental procedures. Dentists may have to manage a medical emergency arising in their clinic. Moreover, many dental patients could be receiving other medication that may have orodental implications, or may interact with drugs prescribed by the dentist. As such, a broad knowledge of pharmacology with emphasis on certain aspects is needed by the dentist. This book is divided into three sections. The first describes the general pharmacological principles with which all professionals involved in drug therapy must be conversant. The second on systemic pharmacology presents a brief account of drugs acting on various organ systems and used in the treatment of common disorders affecting the systems. Each chapter is organised systematically. The opening sentence defines the class of drugs, followed by their classification. The ‘prototype’ approach is followed by describing the representative drug of the class. In these chapters, matters particularly relevant to dental therapeutics have been highlighted by italicizing. Wherever applicable, the implications in dentistry are prominently elaborated, e.g. drugs and diseases affecting postextraction haemostasis, dental procedures in patients on corticosteroid therapy or in diabetics, oral complications of cancer chemotherapy, conscious sedation in dentistry, etc. Management of medical emergencies like anaphylactic shock, seizures, angina, or asthmatic attack during dental treatment is outlined. The third section covers antimicrobials and other drugs which the dentists prescribe or administer themselves. However, the allocation of topics in sections two and three does not indicate water- tight distinction, which is impossible, but has been done with a view to focus attention on drugs that have greater relevance in dentistry. To mention a few, the application of analgesics and NSAIDs in dental pain, dental anaesthesia, role of each class of antimicrobials in orodental infections, prophylaxis of postextraction infection and endocarditis in patients at special risk are emphasized. The highlight of this 2nd edition is a new chapter on drugs and aids having specific application in dental disorders and in dental care. Drugs for dental plaque, caries tooth, dentine sensitivity alongwith aids like dentifrices, bleaching agents, disclosing agents, etc. are described pointing out their current role in practice. The last chapter on drug interactions highlights those that may be encountered in dental practice. All chapters in the present edition have been thoroughly updated to include latest information and new drugs. Presentation and illustrations have been improved. Leading trade names and dosage forms of drugs generally prescribed by dentists are mentioned distinctively. Thus, the book is oriented vi Essentials of Pharmacology for Dentistry to provide core and contemporary pharmacological knowledge based on understanding of the rationale. It is designed to meet the specific needs of dental students and practitioners. I am indebted to my colleagues in pharmacology and dentistry as well as to readers of the 1st edition for their comments and suggestions which helped in orienting the 2nd edition. As always, the motivational influence of Shri J.P. Vij, Chairman and Managing Director, Jaypee Brothers, was crucial. The meticulous preparation of the manuscript and illustrations by Ms Sunita Katla, Mr Manoj Pahuja and others in the editorial section is highly appreciated. The participation and cooperation of my wife is sincerely acknowledged. June, 2011 KD Tripathi Contents 1. Introduction, Routes of Drug Administration............................................................3 Introduction 3 Routes of Drug Administration 5 2. Pharmacokinetics.............................................................................................................10 Drug Transport 11 Drug Absorption 14 Drug Distribution 16 Drug Biotransformation (Metabolism) 20 Drug Excretion 25 Kinetics of Elimination 26 3. Pharmacodynamics..........................................................................................................31 Principles of Drug Action 31 Mechanism of Drug Action 31 Combined Effect of Drugs 45 Drug Dosage 48 Factors Modifying Drug Action 50 4. Adverse Drug Effects......................................................................................................56 5. Drugs Acting on Autonomic Nervous System..........................................................67 (General Considerations, Cholinergic and Anticholinergic Drugs) General Considerations 67 Cholinergic Drugs (Cholinomimetic, Parasympathomimetic) 72 viii Essentials of Pharmacology for Dentistry Anticholinesterases 74 Anticholinergic Drugs (Parasympatholytic) 76 Drugs Acting on Autonomic Ganglia 80 6. Drugs Acting on Autonomic Nervous System..........................................................81 (Adrenergic and Antiadrenergic Drugs) Adrenergic Transmission 81 Adrenergic Drugs (Sympathomimetics) 83 Antiadrenergic Drugs (Adrenergic Receptor Antagonists) 90 7. Autacoids and Related Drugs.......................................................................................98 Histamine 98 H Antagonists (Conventional Antihistaminics) 101 1 5-hydroxytryptamine (5-HT, Serotonin) 105 Drug Therapy of Migraine 107 Prostaglandins and Leukotrienes (Eicosanoids) 109 Platelet Activating Factor (PAF) 115 8. General Anaesthetics and Skeletal Muscle Relaxants........................................117 General Anaesthetics 117 Preanaesthetic Medication 125 Skeletal Muscle Relaxants 126 9. Drugs Acting on Central Nervous System...............................................................133 (Sedative-Hypnotics, Alcohols, Antiepileptics and Antiparkinsonian Drugs) Sedative-hypnotics 133 Ethyl Alcohol (Ethanol) 139 Antiepileptic Drugs 143 Antiparkinsonian Drugs 149 10. Drugs Acting on Central Nervous System...............................................................155 (Psychopharmacological Agents) Psychopharmacological Agents 155 Antipsychotic Drugs (Neuroleptics) 156 Antimanic (Mood Stabilizing) Drugs 160 Antidepressant Drugs 163 Antianxiety Drugs 168 11. Cardiovascular Drugs...................................................................................................171 (Drugs Affecting Renin-Angiotensin System, Calcium Channel Blockers, Drugs for Hypertension, Angina Pectoris and Myocardial Infarction) Angiotensin 171 Angiotensin Converting Enzyme Inhibitors 173 Calcium Channel Blockers 176 Antihypertensive Drugs 178 Antianginal Drugs 183 Drug Therapy in Myocardial Infarction 188 Contents ix 12. Cardiovascular Drugs...................................................................................................190 (Drugs for Heart Failure and Cardiac Arrhythmia) Cardiac Glycosides 190 Treatment of Congestive Heart Failure 195 Antiarrhythmic Drugs 197 13. Drugs Acting on Kidney...............................................................................................203 Relevant Physiology of Urine Formation 203 Diuretics 205 Antidiuretics 212 14. Hormones and Related Drugs ....................................................................................215 (Anterior Pituitary Hormones, Antidiabetic Drugs, Corticosteroids) Introduction 215 Anterior Pituitary Hormones 216 Antidiabetic Drugs 219 Insulin 220 Oral Hypoglycaemic Drugs 224 Corticosteroids 228 15. Hormones and Related Drugs ....................................................................................235 (Sex Hormones, Contraceptives, Drugs Acting on Uterus) Androgens (Male Sex Hormones) 235 Estrogens 237 Progestins 239 Hormonal Contraceptives 241 Uterine Stimulants (Oxytocics, Abortifacients) 243 Uterine Relaxants (Tocolytics) 245 16. Hormones and Related Drugs ....................................................................................246 (Thyroid Hormone and Thyroid Inhibitors, Hormones Regulating Calcium Balance) Thyroid Hormone 246 Thyroid Inhibitors 249 Hormones Regulating Calcium 250 17. Drugs Affecting Blood..................................................................................................256 Haematinics 256 Coagulants 260 Anticoagulants 264 Fibrinolytics (Thrombolytics) 268 Antifibrinolytics 269 Antiplatelet Drugs (Antithrombotic Drugs) 269 Hypolipidaemic Drugs 271 x Essentials of Pharmacology for Dentistry 18. Drugs for Gastrointestinal Disorders.......................................................................274 Drugs for Peptic Ulcer 274 Antiemetics 280 Treatment of Gastroesophageal Reflux Disease 284 Laxatives (Aperients, Purgatives, Cathartics) 285 Treatment of Diarrhoeas 288 19. Drugs for Respiratory Disorders................................................................................291 Drugs for Cough 291 Drugs for Bronchial Asthma 292 20. Vitamins...........................................................................................................................299 Fat-soluble Vitamins 300 Water-soluble Vitamins 301 21. Anticancer and Immunosuppressant Drugs...........................................................305 Anticancer Drugs 305 Immunosuppressant Drugs 313 22. Antirheumatoid and Antigout Drugs........................................................................317 Antirheumatoid Drugs 317 Drugs Used in Gout 319 23. Nonsteroidal Antiinflammatory Drugs and Antipyretic-Analgesics...............325 Analgesic/NSAIDs in Dentistry 339 24. Opioid Analgesics and Antagonists..........................................................................341 Opioid Analgesics 341 Complex Action Opioids and Opioid Antagonists 350 25. Local Anaesthetics.........................................................................................................354 Uses and Techniques of Local Anaesthesia 361 Local Anaesthesia in Dentistry 362 26. Antimicrobial Drugs: General Considerations......................................................364 Drug Resistance 367 Superinfection 369 Choice of an Antimicrobial Agent 370 Combined Use of Antimicrobials 373 Prophylactic Use of Antimicrobials 375