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Aspirin and related Drugs - K. Rainsford (CRC, 2004) WW PDF

773 Pages·2004·5.19 MB·English
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CRC PR ESS Boca Raton London New York Washington, D.C. EDITED BY K. D. Rainsford PhD, FRCP Edin, FRCPath, FRSC, FIBiol, FIBMS, Dr(hc) Biomedical Research Centre Sheffield Hallam University Sheffield, UK ASPIRIN AND RELATED DRUGS © 2004 K.D. Rainsford Aspirin and Related Drugs © 2004 K.D. Rainsford Aspirin and Related Drugs K.D. Rainsford PhD, FRCP Edin, FRCPath, FRSC, FIBiol, FIBMS, Dr(hc) Biomedical Research Centre Sheffield Hallam University Sheffield, UK © 2004 K.D. Rainsford First published 2004 by Taylor & Francis 11 New Fetter Lane, London EC4P 4EE Simultaneously published in the USA and Canada by Taylor & Francis Inc, 29 West 35th Street, New York, NY 10001 Taylor & Francis is an imprint of the Taylor & Francis Group © 2004 K.D. Rainsford Typeset in Baskerville by Wearset Ltd, Boldon, Tyne and Wear Printed and bound in Great Britain by TJ International Ltd, Padstow, Cornwall All rights reserved. No part of this book may be reprinted or reproduced or utilised in any form or by any electronic, mechanical, or other means, now known or hereafter invented, including photocopying and recording, or in any information storage or retrieval system, without permission in writing from the publishers. Every effort has been made to ensure that the advice and information in this book is true and accurate at the time of going to press. However, neither the publisher nor the authors can accept any legal responsibility or liability for any errors or omissions that may be made. In the case of drug administra- tion, any medical procedure or the use of technical equipment mentioned within this book, you are strongly advised to consult the manufacturer’s guidelines. British Library Cataloguing in Publication Data A catalogue record for this book is available from the British Library Library of Congress Cataloging in Publication Data A catalog record for this book has been requested ISBN 0–7484–0885–1 © 2004 K.D. Rainsford ‘To those who have gone before’ In recognition of those who have contributed so much to the explosion of science and clinical practice on the actions and uses of aspirin and the salicylates as well as other related analgesic/anti-inflammatory/ antipyretic drugs © 2004 K.D. Rainsford Contents Contributors Preface Abbreviations and nomenclature 1 HISTORY AND DEVELOPMENT OF THE SALICYLATES K.D. Rainsford Introduction Early Use of Salicylate-containing Plants Chemical Development of Salicylates Clinical Observations on the Use of Salicylates in the Nineteenth Century Early Clinical Studies with Salicylates in the Treatment of Rheumatoid Arthritis Chemical Development and Early Clinical Studies with Aspirin Aspects of the Commercial Development of Aspirin Other Salicylates References 2 THE INDUSTRIAL HISTORY OF ANALGESICS: THE EVOLUTION OF ANALGESICS AND ANTIPYRETICS J.R. McTavish Recognition of Pain Therapeutic Nihilism and Fevers The Organic Chemical Industry The Salicylates The Value of a Good Name Conclusion References 3 OCCURRENCE, PROPERTIES AND SYNTHETIC DEVELOPMENTS OF THE SALICYLATES K.D. Rainsford Introduction Naturally Occurring Salicylates Chemical Properties Commercial Synthesis and Properties of the Salicylates Experimental Drugs © 2004 K.D. Rainsford Various Chemical Applications Conclusions References 4 PHARMACOKINETICS AND METABOLISM OF THE SALICYLATES G.G. Graham, M.S. Roberts, R.O. Day and K.D. Rainsford Introduction Absorption of Aspirin and Salicylate Distribution of Aspirin and Salicylate Elimination of Aspirin Elimination of Salicylate Metabolic Pathways of Salicylate Factors Controlling the Elimination of Aspirin and Salicylate Kinetics of Elimination of Salicylate Pro-Drugs Analytical Methods for the Salicylates Salicylate Derivatives Diflunisal Salicylamide References 5 METABOLISM AND PHARMACOKINETICS OF IBUPROFEN G.G. Graham and K.M. Williams Introduction Absorption Distribution Elimination Half-life and Clearance Factors Affecting the Elimination of Ibuprofen Pharmacokinetics, Plasma Concentrations and Clinical Response Analytical Methods References 6 PHARMACOKINETICS AND METABOLISM OF PARACETAMOL (ACETAMINOPHEN) G.G. Graham and M. Hicks Introduction Absorption Distribution © 2004 K.D. Rainsford Elimination Half-life and Clearance Factors Affecting the Elimination of Paracetamol Metabolism of Pro-drugs Analytical Methods References 7 PHARMACOLOGY AND BIOCHEMISTRY OF SALICYLATES AND RELATED DRUGS K.D. Rainsford Introduction Anti-inflammatory Effects Biochemical Effects of Salicylates in Relation to their Anti-inflammatory Actions Analgesic Activity Antipyresis References Appendix to Chapter 7 8 SIDE EFFECTS AND TOXICOLOGY OF THE SALICYLATES K.D. Rainsford Introduction Occurrence of Adverse Events from NSAIDs, including Aspirin Gastrointestinal Side Effects Hepatotoxicity Nephropathy Hypersensitivity Reactions and Asthma Teratogenesis and Pregnancy Miscellaneous Side Effects Acute Salicylate Poisoning Conclusions References 9 REYE’S SYNDROME AND ASPIRIN J.F.T. Glasgow and S.M. Hall Introduction Background Definition Clinical Features Investigations © 2004 K.D. Rainsford Differential Diagnosis Aetiology and Pathogenesis Management Principles The Future Conclusion Acknowledgements References 10 SALICYLATES IN THE TREATMENT OF ACUTE PAIN K.D. Rainsford Introduction Concepts of the Mode of Action in Acute Pain Early Observations in Various Pain States Efficacy in Various Pain Conditions Comparative Effects in Acute Pain States References 11 ACETYLSALICYLIC ACID FOR THE PREVENTION AND TREATMENT OF THROMBOEMBOLIC DISEASES K.E. Webert and J.G. Kelton The Role of Platelets in Haemostasis and Thrombosis The Role of Platelets in Acute and Chronic Vascular Injury Effects of Acetylsalicylic Acid on Platelet Function Pharmacokinetics of ASA Dose–Effect Relationships of ASA The Effects of ASA on Coagulation Factors, other than Platelets ASA for the Prevention of Vascular Thromboembolic Disease: Epidemiological Studies ASA for the Treatment of Acute Vascular Thromboembolic Events Novel Analogues of Salicylates and Further Developments References 12 USE OF SALICYLATES IN RHEUMATIC AND RELATED CONDITIONS W.W. Buchanan, W.F. Kean and K.D. Rainsford Introduction History Rheumatoid Arthritis Osteoarthritis Miscellaneous musculoskeletal disorders Drug Kinetics and Monitoring © 2004 K.D. Rainsford Adverse Events in Rheumatic Patients Factors Affecting Side Effects and Therapeutic Effects Toxicity Conclusions References . 13 ASPIRIN AND NSAIDs IN THE PREVENTION OF CANCER, ALZHEIMER’S DISEASE AND OTHER NOVEL THERAPEUTIC ACTIONS K.D. Rainsford Introduction Prevention of Colorectal and Other Cancers Alzheimer’s Disease and Related Dementias Copper Salicylates in the Treatment of Inflammatory Diseases and Cancer Therapeutic Uses of Aspirin in Pregnancy Kawasaki Disease Perturbed Metabolic States Immunological Effects Other Possible Uses Miscellaneous References © 2004 K.D. Rainsford

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