N S A I D s NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AN OVERVIEW , , N S A I D s NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AN OVERVIEW Swarnlata Saraf Reader Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur (C.G) - 492010 . • ·::::::' ill.........•...•...•...•.. .. PharmaMed Press 1t1.=-::= .•••••••••••••...,, An Imprint of Pharma Book Syndicate 4-4-316, Giriraj Lane, .-lA/mpri"'''f Sultan Bazar, Hyderabad -500 095, Phanna Book Syndicate Copyright © 2008, by Author All rights reserved No part of this book or parts thereof may be reproduced, stored in a retrieval system or transmitted in any language or by any means, electronic, mechanical, photocopying, recording or otherwise without the prior written permission of the publishers. • Published by : • PharmaMed Press . ........:....•:....•:....•:.....•:....: ..... An Imprint of Pharma Book Syndicate 4-4-316, Giriraj Lane, Sultan Bazar, Hyderabad -500 095. , Phone: 040-23445605,23445688; Fax: 91+40-23445611 \ . < E-mail: [email protected] www.pharmamedpress.com/pharmamedpress.net Printed at Adithya Art Printers Hyderabad I I t ISBN : 978-81-88449-39-3 Preface It gives us immense pleasure in bringing out the first edition of the book NSAIDs: An Overview Musculoskeletal disorders presents a serious socioeconomic burden that has and will continue to attract major research and development efforts aimed at elucidating the basis of the disease as well as developing effective new drug molecules as well as therapies. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequently prescribed drugs worldwide in musculoskeletal disorders. These are categorized as 'over-the counter' (OTe) inavailability, and are also consumed on a non-prescription basis as well. The approach and purpose of th is books are di fferent from those of the several excellent books on the NSAIDs. No single book is available which covers all the different aspects of NSAIDs. Many drug molecules are available in the market but complete information on those molecules is not available in one book especially the recently invented molecules. Drug professionals, research scholars, graduate and undergraduate students of pharmacy all over the world face problems in knowing all about such molecules. We have made the efforts to compile information about NSAIDs at one place in this book. This book will be beneficial to all professionals working in hospitals, clinics, academia, nursing, drug stores, PG and research students of medicine and pharmacy. The salient features of the book are • It covers different areas of information viz; drug interactions, contrainuications, warnings and combination of drugs • FDA regulations for use of NSAlDs in clinics, hospitals and dispensaries to help in preparing and dispensing as well as nursing of NSAIDs. • The physico-chemical properties with current literature review make this manuscript helpful to researcher of medical and pharmacy. • The generic names of the drugs are given with brand names which are important and useful for physicians. (VI) Preface • Besides, all current information of individual drugs has been covered which make it useful in the drug information centre of different states as suggested by the WHO. • Clinical aspects ofNSAIDs This book consists of6 chapters. Chapter [-Introduction, consists of general information ofNSAIDs such as properties, classifications, brand names of drugs available all over the world, combinations, side effects, mechanism of action, warning and contraindications etc. Chapter II, HI, IV and V consist of specific physicochemical properties of individual drugs based on their chemical classification which covers interactions, clinical values and trade names etc. Chapter VI consists of tabular information about individual drugs which is a ready reconer of NSAIDs. There is no book for NSAIDs available in the market which has all information at one place; hence, this manuscript will cater the need of all interested professionals working in the field ofNSAIDs. We have tried to make this book as informative and exhaustive as possible within the constraints of time allotted to the subject in the curriculum of different universities. This book provides copious information about NSAIDs and points out their interactions and side effects. We hope this book will be informative, beneficial and will fulfil the demands of the undergraduate and graduate students, budding researchers of the pharmacy, paramedical students as well as medical practitioners. We are particularly indepted to our colleagues Mr. KamIesh Dashora and Mr. Gopal Garg for their constant support to make this book. -Author Contents Preface ................................................................................................ (v) Chapterl Introduction eyc looxygenase Enzyme ................................................................. 2 Mechanism of Action ofNSAIDs ................................................... 3 Classification ofNSAIDs ................................................................ 6 Therapeutic Effects ......................................................................... 9 Side Effects ................................................................................... 10 Other Effects ................................................................................. 13 Drug Interactions ........................................................................... 16 NSAIDs in Varying Clinical Situations .......................................... 18 Marketed Dosage F orrn ........... ........................................ ............. 19 Warnings ........................................................................................ 24 Symptoms ofNSAID Overdose .................................................... 24 FDA Medication Guidelines ........................................................... 25 Drugs Information for Pharrnacist.. ............................................... 28 Chapter 2 Carboxylic Acid Derivative Compounds Asprin ............................................................................................ 37 Diflunisal ........................................................................................ 42 Benorylate ..................................................................................... 44 Salsalate ......................................................................................... 45 Sodium salicylate ........................................................................... 51 Trisalicylate .................................................................................... 54 (viii) Contents Aceclofenac ............................................................................ :. .... 58 Diclofenac ..................................................................................... 58 Tolmetin ......................................................................................... 66 Zomepirac ...................................................................................... 74 Carprofen ....................................................................................... 76 Ketorolac ....................................................................................... 79 Tromethamine ................................................................................ 83 Mefenamic ..................................................................................... 86 Flufenamic ..................................................................................... 90 Pirprofen ........................................................................................ 91 Fenbufen ........................................................................................ 93 Flurbiprofen .................................................................................... 97 Ketoprofen .................................................................................... 101 Oxaprozin ...................................................................................... 105 F enoprofen .................................................................................... 109 Indoprofen .................................................................................... 113 Naproxen ...................................................................................... 115 Suprofen ....................................................................................... 120 Niflumic ........................................................................................ 122 Chapter 3 EnolicAcid Compounds Phenylbutazone ............................................................................. 125 Oxyphenbutazone ......................................................................... 127 Piroxicam ...................................................................................... 130 Isoxicam ....................................................................................... 134 Meloxicam .................................................................................... 135 Chapter 4 Non-Acidic Compounds Nabumetone ................................................................................. 139 Tiaramide ...................................................................................... 140 Fluproquazone .............................................................................. 143 Proquazone ................................................................................... 146 Contents (Ix) Chapter 5 Miscellaneous Celecoxib ...................................................................................... 148 Etoricoxib ...................................................................................... 149 Nimesulide .................................................................................... 153 Valdecoxib .................................................................................... 154 Chapter 6 Tabular Infonnation ................................................................ 157 Bibliography ......................................................................................... 171 Some FAQ's .......................................................................................... 175