Color profile: Disabled Composite Default screen Macrocyclic Lactones in Antiparasitic Therapy 1 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:54 AM Color profile: Disabled Composite Default screen 2 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:54 AM Color profile: Disabled Composite Default screen Macrocyclic Lactones in Antiparasitic Therapy Edited by J. VERCRUYSSE Faculty of Veterinary Medicine Department of Virology, Parasitology, Immunology Ghent University Belgium and R.S. REW Pfizer Animal Health Exton Pennsylvania USA CABI Publishing 3 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:54 AM Color profile: Disabled Composite Default screen CABI Publishing is a division of CAB International CABI Publishing CABI Publishing CAB International 10E 40th Street Wallingford Suite 3203 Oxon OX10 8DE New York, NY 10016 UK USA Tel: +44 (0)1491 832111 Tel: +1 212 481 7018 Fax: +44 (0)1491 833508 Fax: +1 212 686 7993 E-mail: [email protected] E-mail: [email protected] Website: www.cabi-publishing.org ©CAB International 2002. All rights reserved. No part of this publication may be reproduced in any form or by any means, electronically, mechanically, by photocopying, recording or otherwise, without the prior permission of the copyright owners. A catalogue record for this book is available from the British Library, London, UK. Library of Congress Cataloging-in-Publication Data Macrocyclic lactones in antiparasitic therapy / edited by J. Vercruysse and R.S. Rew p. cm. Includes bibliographical references (p. ). ISBN 0-85199-617-5 (alk. paper) 1. Avermectins. 2. Lactones. 3. Macrocyclic compounds. 4. Antiparasitic agents. I. Vercruysse, J. (Jozef) II. Rew, Robert S. RM412 .M33 2002 616.9′6061--dc21 2002004075 ISBN 0 85199 617 5 Typeset by AMA DataSet Ltd, UK Printed and bound in the UK by Cromwell Press, Trowbridge 4 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:55 AM Color profile: Disabled Composite Default screen Contents Contributors ix Preface xiii 1. Chemistry, Pharmacology and Safety of the Macrocyclic Lactones 1 1.1. Ivermectin, Abamectin and Eprinomectin 1 W. Shoop and M. Soll 1.2. Doramectin and Selamectin 30 G.A. Conder and W.J. Baker 1.3. Milbemycin Oxime 51 M. Jung, A. Saito, G. Buescher, M. Maurer and J.-F. Graf 1.4. Moxidectin 75 D.W. Rock, R.L. DeLay and M.J. Gliddon 2. Pharmacokinetics of the Macrocyclic Lactones: Conventional Wisdom and New Paradigms 97 D.R. Hennessy and M.R. Alvinerie 3. Mode of Action of the Macrocyclic Lactones 125 R.J. Martin, A.P. Robertson and A.J. Wolstenholme 4. Ecological Impact of Macrocyclic Lactones on Dung Fauna 141 J.W. Steel and K.G. Wardhaugh 5. Resistance Against Macrocyclic Lactones 163 R.K. Prichard v 5 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:55 AM Color profile: Disabled Composite Default screen vi Contents 6. The Use of Macrocyclic Lactones to Control Parasites of Cattle 183 6.1. General Efficacy of the Macrocyclic Lactones to Control Parasites of Cattle 185 J. Vercruysse and R. Rew 6.2. Use of Macrocyclic Lactones to Control Cattle Parasites in Europe 223 J. Vercruysse and R. Rew 6.3. Use of Macrocyclic Lactones to Control Cattle Parasites in the USA and Canada 248 R. Rew and J. Vercruysse 6.4. Use of Macrocyclic Lactones to Control Cattle Parasites in South America 262 C. Eddi, A. Nari and J. Caracostantogolo 6.5. Use of Macrocyclic Lactones to Control Cattle Parasites in Australia and New Zealand 288 P.A. Holdsworth 7. The Use of Macrocyclic Lactones to Control Parasites of Sheep and Goats 303 R.L. Coop, I. Barger and F. Jackson 8. The Use of Macrocyclic Lactones to Control Parasites of Horses 323 C.M. Monahan and T.R. Klei 9. The Use of Macrocyclic Lactones to Control Parasites of Pigs 339 J. Arends and J. Vercruysse 10. The Use of Macrocyclic Lactones in the Control and Prevention of Heartworm and Other Parasites in Dogs and Cats 353 J. Guerrero, J.W. McCall and C. Genchi 11. The Use of Macrocyclic Lactones to Control Parasites of Domesticated Wild Ruminants 371 S.E. Marley and G.A. Conder 12. The Use of Macrocyclic Lactones to Control Parasites of Exotic Pets 395 S.E. Little, C.B. Greenacre and R.M. Kaplan 13. The Use of Macrocyclic Lactones to Control Parasites of Humans 405 K.R. Brown 6 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:55 AM Color profile: Disabled Composite Default screen Contents vii 14. Macrocyclic Lactones as Antiparasitic Agents in the Future 413 T.G. Geary Index 425 7 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:55 AM Color profile: Disabled Composite Default screen 8 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:55 AM Color profile: Disabled Composite Default screen Contributors M.R. Alvinerie, INRA Laboratoire de Phamacologie, 180 Chemin de Tournefeuille, F-31931 Toulouse, France. J. Arends, S&J Farms Animal Health, 2340 Sanders Road, Willow Springs, NC 27592, USA. W.J. Baker, Pfizer Central Research, Eastern Point Road, Mailstop 8200-40, Groton, CT 06340, USA. I. Barger, 597 Rockvale Road, Armidale, NSW 2350, Australia. K.R. Brown, 8111 Winston Road, Philadelphia, PA 19118, USA. G. Buescher, Novartis Animal Health Inc., CH-4002 Basel, Switzerland. J. Caracostantogolo, Jose Paula Rodriguez Alvez 794, 1408 Ciudad de Buenos Aires, Argentina. G.A. Conder, Pfizer Central Research, Eastern Point Road, Mailstop 8200-40, Groton, CT 06340, USA. R.L. Coop, Moredun Research Institute, Pentlands Science Park, Bush Loan, Penicuik, Midlothian EH26 0PZ, UK. R.L. DeLay, Fort Dodge Animal Health, Agricultural Research Center, PO Box 400, Princeton, NJ 08543-0400, USA. C. Eddi, Alberti 664, 1714 Ituzalogo, Argentina. New address: Animal Production and Health Division, Room C-528, FAO, Vialle delle Terme di Caracalla-00100, Rome, Italy. ix 9 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Thursday, October 31, 2002 10:12:56 AM Color profile: Disabled Composite Default screen x Contributors T.G. Geary, Pharmacia & Upjohn Co., 301 Henrietta Street, Kalamazoo, MI 49007-4940, USA. C. Genchi, Dipartimento di Patologia Animale, Igiene e Sanita Pubblica Veterinaria, Sezione di Patologia generale e Parassitologia, Universitá degli Studi di Milano, Via Celoria 10, I-20122 Milan, Italy. M.J. Gliddon, Fort Dodge Animal Health, Agricultural Research Center, PO Box 400, Princeton, NJ 08543-0400, USA. J.-F. Graf, Novartis Animal Health Inc., CH-4002 Basel, Switzerland. C.B. Greenacre, Department of Comparative Medicine, College of Veterinary Medicine, University of Tennessee, PO Box 1071, Knoxville, TN 37902-1071, USA. J. Guerrero, Department of Pathobiology, School of Veterinary Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA. D.R. Hennessy, CSIRO Animal Production McMaster Laboratory, Clunies Ross St., Private Bag 1, Delivery Center Blacktown, Sydney, NSW 2148, Australia. New address: Veterinary Health Research Pty Ltd, 1 Rivett Rd, Riverside Corporate Park, North Ryde, NSW 2113, Australia. P.A. Holdsworth, Director Scientific & Regulatory Affairs, Avcare, Locked Bag 916, Canberra, ACT 2601, Australia. F. Jackson, Moredun Research Institute, Pentlands Science Park, Bush Loan, Penicuik, Midlothian EH26 0PZ, UK. M. Jung, Novartis Centre de Recherche Santé Animal SA, CH-1566 St.-Aubin, Switzerland. R.M. Kaplan, Department of Medical Microbiology and Parasitology, College of Veterinary Medicine, University of Georgia, Athens, GA 30602-7387, USA. T.R. Klei, Department of Veterinary Microbiology and Parasitology, School of Veterinary Medicine, Louisiana State University, Baton Rouge, LA 70803, USA. S.E. Little, Department of Medical Microbiology and Parasitology, College of Veterinary Medicine, University of Georgia, Athens, GA 30602-7387, USA. S.E. Marley, Merial, 3239 Satellite Blvd, Duluth, GA 30096, USA. 10 Z:\Customer\CABI\A4325 - Vercruysse - Macrocyclic Lactones\A4414 - Vercruysse - Vouchers #A.vp Friday, November 08, 2002 4:49:37 PM Color profile: Disabled Composite Default screen Contributors xi R.J. Martin, Department of Biomedical Sciences, College of Veterinary Medicine, Iowa State University, Ames, IA 50011, USA. M. Maurer, Novartis Centre de Recherche Santé Animal SA, CH-1566 St.-Aubin, Switzerland. J.W. McCall, Department of Medicine, Microbiology and Parasitology, College of Veterinary Medicine, University of Georgia, Athens, GA 300602, USA. C.M. Monahan, College of Veterinary Medicine, Ohio State University, 1900 Coffey Rd, Columbus, Ohio 43210, USA. A. Nari, Via Odoardo Beccari 14 apt. 6, I-00154 Rome, Italy. R.K. Prichard, Institute of Parasitology, McGill University, MacDonald Campus, 21111 Lakeshore Road, Ste-Anne-DeBellevue, Quebec H9X3V9, Canada. R.S. Rew, formerly Pfizer Animal Health, 812 Springdale Drive, Exton, PA 19341, USA, now at Rewsearch Inc., 400 N Wawaset Road, West Chester, PA 19382, USA. D.W. Rock, Fort Dodge Animal Health, Agricultural Research Center, PO Box 400, Princeton, NJ 08543-0400, USA. A.P. Robertson, Department of Biomedical Sciences, College of Veterinary Medicine, Iowa State University, Ames, IA 50011, USA. A. Saito, Sankyo Co. Ltd, Tokyo 104, Japan. W.L. Shoop, Merck & Co., PO Box 2000, Rahway, NJ 07065, USA. M.D. Soll, Merial 3239 Satellite Boulevard, Duluth, GA 30096, USA. J.W. Steel, CSIRO Animal Production McMaster Laboratory, Clunies Ross St., Private Bag 1, Delivery Centre, Blacktown, Sydney, NSW 2148, Australia. New address: CSIRO Livestock Industries, 5 Julius Avenue (off Delhi Road), Riverside Corporate Park, North Ryde, NSW 1670, Australia. J. Vercruysse, Faculty of Veterinary Medicine, Department of Virology, Parasitology, Immunology, Ghent University, Salisbury Laan 133, B-9820 Merelbeke, Belgium.