Topical Corticosteroids

Transcription

1 Topical Corticosteroids

2

3 Topical Cοrt cοsterοids Editors Howard L Maibach, San Francisco, Calif. Christian Surber, Basel 83 figures and 91 tables, 1992 KARG E R. Basel München Paris London NewYork New Delhi Bangkok Singapore Tokyo Sydney

4 The Editors Howard L Maibach, MD, is Professor 0f Dermatology at the School of Medicine, University of California, San Francisco, Calif. Dr. Maibach graduated from Tulane University, New Orleans, La. (AB and MD). He interned at William Beaumont Army Hospital, and after additional training at Walter Reed Army Hospital, he practiced medicine in neurology and psychiatry in the US Army in France. He received his dermatological research and clinical training at the University of Pennsylvania, Philadelphia, Pa. He received an honorary doctorate from the University of Paris Sud in Dr. Maibach is a member of the International Contact Dermatitis Research Group, the North American Contact Dermatitis Group, and the European Environmental Contact Dermatitis Group. Dr. Maibach is the author, co-author and editor of some 800 articles and 35 textbooks. Christian Surber, PhD, is Research Associate at the Department of Dermatology, University of Basel and Head of the Department of Pharmacy of the St. Clara Hospital, Basel, Switzerland. Dr. Surber obtained his PharmD degree (Switzerland) from the University of Basel and received his PhD degree in 1984 at the same University for investigations on local tissue tolerance of injectable drugs. Subsequently, he joined Hoffmann-La Roche Basel, for 4 years and then the University of California, San Francisco, Calif., for 3 years. His major areas of interest are skin pharmacology and skin pharmacokinetics. Dr. Surber is a member of the American Association of Pharmaceutical Scientist, Skin Pharmacology Society and the American, European and the Swiss Society of Hospital Pharmacists. Drug Dosage The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any change in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Copyright 1992 by S. Karger AG, P.O. Box, CH-4009 Basel (Switzerland) Printed in Switzerland on acid-free paper by Thíír AG Offsetdruck, Pratteln ISBN

5 Contents Preface VIII Historical Aspects Witten, V.H. (Miami, Fia.): History 1 Pharmacological Aspects Niedner, R. (Freiburg í.br.): Animal Models 7 Niedner, R. (Freiburg i.br.): Human Models 17 Lubach, D.; Kíetzmann, M. (Hannover): Anti-Inflammatory Effect and Thinning of the Skin: Models for Testing Topically Applied Corticosteroids on Human Skin 26 Stoughton, R.B. (La Jolla, Calif.): Vasoconstrictor Assay Specific Applications. 42 Stoughton, R.B. (La Jolla, Calif.): Generic Copies of Innovator Formulations of Topical Glucocorticoids 54 Smith, E.W.; Meyer, E.; Haigh, J.M. (Grahamstown): Accuracy and Reproducibility of the Multiple-Reading Skin Blanching Assay 65 Gibson, J.R. (Buffalo, Ν.Υ.); Hough, J.E.; Marks, P.M. (London): Effect of Concentration on the Clinical Pharmacology of Corticosteroid Ointment Formulations 74 Stouch, T.R. (Princeton, N.J.): Structure-Activity Relationships Using Multivariate Analysis Techniques: Application to Topical Corticosteroids 93 Wester, R.C.; Maibach, H.I. (San Francisco, Calif.): Percutaneous Absorption in Diseased Skin 128 Milioni, K. (San Francisco, Calif.): Topical Anti-Inflammatory Thiosteroids 142 Clinical Aspects Cornell, R.C.; Maibach, H.I. (La Jolla, Calif.): Clinical Indications: Real and Assumed 154 Robertson, D.B.; Maíbach, H.I. (Atlanta, Ga.): Adverse Systemic Effects of Topical Corticoids 163 Marks, R. (Cardiff): Adverse Side Effects from the Use of Topical Corticosteroids 170

6 Contents VI Elsner, P. (Würzburg): Gynecology 184 Sillevis Smitt, J.H.; Winterberg, D.H. (Amsterdam): Topical Corticosteroids in Children: Local and Systemic Effects 196 Lee, K.C.; Jackler, R.K. (San Francisco, Calif.): Topical Corticosteroids in Otology 210 Future Aspects Surber, Ch. (Basel); Maibach, H.I. (San Francisco, Calif.): The Future 227 Topical Corticosteroids: Application Tung, J.P. (San Francisco, Calif.): List of Generic and Brand Names of Corticosteroids 235 Pakes, G.E.; Kamm, A.R. (Research Triangle Park, N.C.): Topical Alclometasone Dipropionate 269 Ellis, C.N. (Ann Arbor, Mich.): Amcinonide Cyclocort Comparative Efficacy, Safety, and Tolerability 286 Samson, C.; Peets, E.; Winter-Sperry, R.; Wolkoff, H. (Kenilworth, N.J.): Augmented Betamethasone Dipropionate Díprolene Enhancement of Topical Activity Through Vehicle Formulation 302 Samson, C.; Peets, E.; Winter-Sperry, R.; Wolkoff, H. (Kenilworth, N.J.): Clotrimazole/Betamethasone Dipropionate Lotrisone An Antifungal/Steroid Combination for Treatment of Cutaneous Dermatophyte Infections 318 Samson, C.; Peets, E.; Winter-Sperry, R.; Wolkoff, H. (Kenilworth, N.J.): Betamethasone Valerate Valisone Establishment of a New Standard for Topical Corticosteroid Potency 335 Richter, J.R. (Leiderdorp): Budesonide Preferid A New, Nonfluorinated Acetal Type of Steroid 349 Pakes, G.E.; Kamm, A.R. (Research Triangle Park, N.C.): Topical Clobetasol Propionate 370 Forster, J.R.; Abrams, B. (Somerville, N.J.): Desoximetasone 388 Packman, A.M. (Blue Bell, Pa.): Diflorasone Diacetate 403 Stanfield, J.W.; Gibson, J.R. (Buffalo, Ν.Υ.); White, R.J. (Ickenham): Halcinonide 415 Loder, J.S.; Gibson, J.R. (Buffalo, Ν.Υ.); Yawalkar, S.J. (Basel); White, R.J. (Ickenham): Halobetasol Propionate 423 Korstanje, C.; Dijkman, J.H.M. (Delft): Hydrocortisone 17-Butyrate 435 Loder, J.S.; Gibson, J.R. (Buffalo, Ν.Υ.): Hydrocortisone Valerate 451 Samson, C.; Peets, E.; Winter-Sperry, R.; Wolkoff, H. (Kenilworth, N.J.): Mometasone Furoate Elocon A Medium Potency Topical Corticosteroid with Favorable Efficacy/Safety Profile 462 Drebinger, K.; Hoehler, Th. (Frankfurt/M): Prednicarbate 480 Stanfield, J.W.; Gibson, J.R. (Buffalo, Ν.Υ.); White, R.J. (Ickenham): Triamcinolone Acetonide 494 Fairbrother, J.E.; Hollingsbee, D.A.; White, R.J. (Deeside): Hydrocolloid Dermatological Patches Corticosteroid Combinations 503 Subject Index 513

7 Preface Topical corticosteroids are the most widely used preparations in dermatology. The introduction of topical hydrocortisone in the early 1950s represented a great advance on previously available therapies, but it was the first of the halogenated corticosteroids, triamcinolone acetonide, that began the revolution which cumulated in the appearance of the very potent agents now available. Enthusiasm for these highly effective agents was at its peak during the 1960s and 1970s and perhaps inevitably, the more potent corticosteroids were often used inappropriately and indiscriminately. Adverse effects became apparent and the subsequent backlash of opinion against topical corticosteroids has created confusion and prejudice against all steroid-containing preparations is today still of considerable concern. Of recent years, much care has been taken to re-establish the image and certainly much effort has been taken to improve the understanding of pharmacological and clinical aspects of topical corticosteroids. This book is designed to provide the readers with comprehensive essays on Topical Corticosteroids written by experts who are scientifically active within the specific research fields. The chapters are divided into two main sections: The first section deals with pharmacological and clinical aspects of topical corticosteroids surrounded by two short chapters on historical and future aspects of these remedies. The second section, Topical Corticosteroids: Applications, includes a total of 18 chapters. It starts with a complete list of all generic and brand names of topical corticosteroids available. It follows a series of chapters dealing with specific properties of a selection of topical corticosteroids.

8 Preface VIII The concept of Topical Corticosteroids is unique. It combines information on an unparalleled class of remedy which is published in a vast range of medical and pharmaceutical journals that can hardly be mastered by a single individual. Researchers with medical and/or pharmaceutical backgrounds have helped with their contributions to further improve the mutual understanding of clinical, experimental and laboratory issues of topical corticosteroids. It is hoped that the book will be useful as a source of ideas, references and critical reviews to those engaged in the development and use of topical corticosteroids. We are thankful for the cooperation provided by the coauthors. Howard I. Maibach, MD Christian Surber, PhD