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Chemotherapy of Gastrointestinal Helminths

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Chemotherapy of Gastrointestinal Helminths Contributors J. H. Arundel • J. H. Boersema • C. F. A. Bruyning • J. H. Cross A. Davis • A. De Muynck • P. G. Janssens • W. S. Kammerer IF. Michel • M.H. Mirck • M.D. Rickard F. Rochette M. M. H. Sewell • H. Vanden Bossche Editors H. Vanden Bossche • D.Thienpont • P.G. Janssens UNIVERSITATS- BlfiUOTHElC Springer-Verlag Berlin Heidelberg New York Tokyo Contents CHAPTER 1 Introduction. A. DAVIS A. Pathogenic Mechanisms in Man 1 B. Modes of Transmission 2 C. Clinical Sequelae of Infection 3 D. Epidemiological Considerations 3 E. Chemotherapy 4 F. Conclusion 5 References 5 CHAPTER 2 Epidemiology of Gastrointestinal Helminths in Human Populations C. F. A. BRUYNING A. Introduction 7 B. Epidemiological or "Mathematical" Models and Control 8 C. Nematodes 11 I. Angiostrongylus costaricensis 11 II. Anisakis marina 12 III. Ascaris lumbricoides 14 IV. Capillaria philippinensis 21 V. Enterobius vermicularis 23 VI. Gnathostoma spinigerum 25 VII. Hookworms: Ancylostoma duodenale and Necator americanus . 26 VIII. Oesophagostoma spp 32 IX. Strongyloides stercoralis 33 X. Ternidens deminutus 34 XI. Trichinella spiralis 35 XII. Trichostrongylus spp 38 XIII. Trichuris trichiura 39 D. Trematodes 41 I. Echinostoma spp 41 II. Fasciolopsis buski 42 III. Gastrodiscoides hominis 44 IV. Heterophyes heterophyes 44 V. Metagonimus yokogawai 46 X Contents E. Cestodes 47 I. Diphyllobothrium latum 47 II. Dipylidium caninum 50 III. Hymenolepis diminuta 51 IV. Hymenolepis nana 52 V. Taenia saginata 54 VI. Taenia solium 57 VII. Cysticercosis cellulosae 58 References 60 CHAPTER 3 Epidemiology and Control of Gastrointestinal Helminths in Domestic Animals J. F. MICHEL. With 20 Figures A. Introduction 67 I. Effect of Worm Infection on Production 68 II. Economic Effects 71 B. Spontaneous Regulation of Worm Burdens in the Host 72 I. Self-cure and Protection 73 II. Resistance to the Establishment of Worms 74 III. The Loss of Worms 76 IV. Arrested Development 79 V. Stunting and Morphological Effects 85 VI. Regulation of Egg Output 86 VII. Effect of Parturition and Lactation on Host Resistance .... 88 C. The Free-Living Stages 90 I. Development 92 II. Migration 93 III. Survival 94 IV. Herbage Infestations 95 D. Epidemiology of Gastrointestinal Nematode Infections ....... 98 I. Cattle 98 II. Sheep 101 III. Intraspecific Variation 104 E. The Control of Gastrointestinal Nematode Infections of Sheep and Cattle 107 I. Eradication 107 II. Suppressive Dosing 107 III. Monitoring and Forecasting 108 IV. Control Strategies 109 V. Dairy Followers Ill VI. Beef 113 VII. Sheep 114 VIII. Integration of Sheep and Cattle Grazing 115 F. Conclusions 117 References 118 Contents XI CHAPTER 4 Pharmacology of Anthelmintics. H. VANDEN BOSSCHE. With 37 Figures A. Introduction 125 B. Albendazole 125 I. Pharmacokinetics 125 II. Toxicology 127 III. Mode of Action 127 C. Amoscanate 127 I. Pharmacokinetics 127 II. Toxicology 128 III. Mode of Action 128 D. Amidantel 128 Toxicology 129 E. Avermectins 129 Mode of Action 130 F. Bephenium Hydroxynaphthoate 131 I. Pharmacokinetics 132 II. Toxicology 132 III. Mode of Action 132 G. Bithionol 132 I. Toxicology 132 II. Mode of Action 133 H. Bitoscanate 133 I. Pharmacokinetics 133 II. Toxicology 133 I. Bromoxanide 133 J. Brotianide 134 K. Cambendazole 134 I. Pharmacokinetics 134 II. Toxicology 134 III. Mode of Action .134 L. Ciclobendazole 135 I. Pharmacokinetics 135 II. Toxicology 136 M. Closantel 136 I. Pharmacokinetics 136 II. Toxicology 136 III. Mode of Action 137 N. Dichlorophen 138 I. Toxicology 138 II. Mode of Action 138 O. Diphetarsone 138 P. Disophenol 139 I. Toxicology 139 II. Mode of Action 139 XII Contents Q. Febantel 140 I. Pharmacokinetics 140 II. Toxicology 141 III. Mode of Action 141 R. Fenbendazole 141 I. Pharmacokinetics 141 II. Toxicology 143 III. Mode of Action 143 S. Flubendazole 143 I. Pharmacokinetics 144 II. Toxicology 144 III. Mode of Action 145 T. Levamisole and Tetramisole 145 I. Pharmacokinetics 146 II. Pharmacology 146 III. Toxicology 147 IV. Mode of Action 148 U. Mebendazole 148 I. Pharmacokinetics 149 II. Toxicology 150 III. Mode of Action 151 V. Metrifonate 152 I. Pharmacokinetics 152 II. Toxicology 153 III. Mode of Action 153 W. Morantel 153 I. Pharmacokinetics 154 II. Toxicology 154 III. Mode of Action 154 X. Niclosamide 154 I. Pharmacokinetics 154 II. Toxicology • ... 154 III. Mode of Action 155 Y. Oxantel 155 Z. Oxfendazole 156 I. Pharmacokinetics 156 II. Toxicology 157 III. Mode of Action 157 AA. Oxibendazole 157 I. Pharmacokinetics 158 II. Toxicology 158 III. Mode of Action 158 BB. Parbendazole 158 I. Pharmacokinetics 158 II. Toxicology 159 III. Mode of Action 159 CC. Paromomycin 159 Contents XIII DD. Piperazine 160 I. Pharmacokinetics 160 II. Toxicology 161 III. Mode of Action 161 EE. Praziquantel 162 I. Pharmacokinetics 162 II. Toxicology 162 III. Mode of Action 163 FF. Pyrantel 164 I. Pharmacology 165 II. Toxicology 165 III. Mode of Action 165 GG. Pyrvinium Pamoate 166 HH. Rafoxanide 166 I. Toxicology 166 II. Mode of Action 166 II. Tetrachloroethylene 167 JJ. Tiabendazole 167 I. Pharmacokinetics 168 II. Toxicology 169 III. Mode of Action 169 KK. Thiophanate 170 I. Pharmacokinetics 171 II. Toxicology 171 References 171 CHAPTER 5 Chemotherapy of Gastrointestinal Nematodiasis in Man. P. G. JANSSENS A. Introduction 183 The Methodology of Drug Trials 188 B. Ancylostomiasis . 191 I. Introduction 191 II. Drugs 196 III. Drug Combinations 232 IV. General Comments 235 C. Anisakiasis 236 Introduction : 236 D. Ascariasis 240 I. Introduction 240 II. Drugs 250 III. Drug Combinations 276 E. Enterobiasis 277 I. Introduction 277 II. Drugs 281 III. Drug Combinations 293 IV. Comments 294 XIV Contents F. Gnathostomiasis 294 I. Introduction 294 II. Drugs 296 G. Intestinal Angiostrongyliasis 296 I. Introduction 296 II. Drugs 298 III. Angiostrongyliasis 298 H. Intestinal Capillariasis 299 I. Introduction 299 II. Drugs 301 HI. General Comments 304 J. Oesophagostomiasis 304 I. Introduction 304 II. Drugs 306 K. Strongyloidiasis 307 I. Introduction 307 II. Drugs 314 III. Drug Combinations 327 L. Ternidens or False Hookworm Infection 328 I. Introduction 328 II. Drugs 329 III. Comments 329 M. Trichinosis 330 I. Introduction 330 II. Drugs 333 III. Comments 337 N. Trichostrongyliasis 337 I. Introduction 337 II. Drugs 339 O. Trichuriasis 342 I. Introduction 342 II. Drugs 347 III. Drug Combinations 367 References 368 CHAPTER 6 Chemotherapy of Gastrointestinal Nematodiasis in Ruminants J. H. BOERSEMA A. Introduction 407 B. Factors and Circumstances Influencing the Choice of Anthelmintic . 407 I. Diagnosis 407 II. Toxicity at the Therapeutic Dose and Drug Interactions . 408 III. Formulation 409 IV. Presence of Inhibited Larvae 411 V. Ovicidal Effect 412 VI. Resistance 412 Contents XV C. The Anthelmintics 413 I. Phenothiazine 413 II. Bephenium 413 III. Organic Phosphorus Compounds 418 IV. Metyridine 420 V. Nitrophenols 420 VI. Benzimidazoles 421 VII. Salicyclanilides 427 VIII. Tetrahydropyrimidines 428 IX. Imidazothiazoles 429 X. Probenzimidazoles 431 XI. Avermectins 432 References 433 CHAPTER 7 Chemotherapy of Gastrointestinal Nematodiasis in Equines. M. H. MIRCK A. Introduction 443 B. Strongylidae 443 I. Epidemiology 444 II. Prevention and Treatment 444 III. Drug Resistance 447 C. Other Important Nematodes 448 D. Anthelmintics 449 I. Phenothiazine 449 II. Piperazine 449 III. Organophosphates 449 IV. Tetrahydropyrimidines 450 V. Imidazothiazoles 451 VI. Benzimidazoles 452 VII. Benzimidazole Carbamates 452 VIII. Febantel . 455 IX. Avermectins 455 E. Conclusions 456 References 456 CHAPTER 8 Chemotherapy of Gastrointestinal Nematodiasis in Pigs. F. ROCHETTE A. Introduction 463 B. Pig Nematodes 464 I. Ascaris suum 464 II. Strongyloides ransomi 465 III. Hyostrongylus rubidus 466 IV. Oesophagostomum dentatum, O. quadrispinulatum 466 XVI Contents V. Trichuris suis 467 VI. Spiruroidea 467 VII. Trichinella spiralis 467 C. Pen Hygiene and Pasture Management 468 D. Herd Deworming 469 E. Anthelmintics 471 I. Piperazines 471 II. Organophosphates 471 III. Tetrahydropyrimidines 474 IV. Imidazothiazoles 474 V. Benzimidazoles 475 VI. Benzimidazole Carbamates 476 VII. Probenzimidazoles 478 VIII. Avermectins 479 References 479 CHAPTER 9 Chemotherapy of Gastrointestinal Nematodiasis in Carnivores F. ROCHETTE A. Introduction 487 B. Gastrointestinal Nematodes of Dogs and Cats 487 I. Ascarids 488 II. Hookworms 489 III. Whipworms 489 C. Prevention and Treatment 490 D. Older and Superseded Anthelmintics 491 I. Piperazine 491 II. Diethylcarbamazine 492 III. Methylbenzene 492 IV. Dithiazanine 492 V. Disophenol \ 492 VI. Thenium 493 VII. Metyridine 493 VIII. Nitrodan 493 E. Organophosphates 493 Dichlorvos 493 F. Tetrahydropyrimidines 494 Pyrantel, Morantel 494 G. Imidazothiazoles 495 Tetramisole, Levamisole 495 H. Nitroscanate 496 J. Benzimidazoles 496 I. Tiabendazole 496 II. Mebendazole 496 III. Fenbendazole 499 IV. Albendazole 499 Contents XVII K. Avermectins 500 L. Ticarbodine 500 M. Tioxidazole 500 N. Conclusions 500 References 500 CHAPTER 10 Chemotherapy of Gastrointestinal Nematodiasis in Birds. J. H. BOERSEMA A. Introduction 505 B. Nematodes in Domestic Birds 505 I. Ascaridia 505 II. Heterakis 505 III. Capillaria 506 IV. Amidostonum 506 C. General Remarks 506 D. The Anthelmintics 506 I. Phenothiazine 510 II. Piperazine 510 III. Metyridine 510 IV. Organic Phosphorus Compounds 511 V. Nitrophenols 512 VI. Benzimidazoles 512 VII. Tetrahydropyrimidines 515 VIII. Imidazothiazoles 515 IX. Probenzimidazoles 516 X. Avermectins 517 References
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  • Anthelmintic Resistance of Ostertagia Ostertagi and Cooperia Oncophora to Macrocyclic Lactones in Cattle from the Western United States

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    Veterinary Parasitology 170 (2010) 224–229 Contents lists available at ScienceDirect Veterinary Parasitology journal homepage: www.elsevier.com/locate/vetpar Anthelmintic resistance of Ostertagia ostertagi and Cooperia oncophora to macrocyclic lactones in cattle from the western United States M.D. Edmonds, E.G. Johnson, J.D. Edmonds ∗ Johnson Research LLC, 24007 Highway 20-26, Parma, ID, 83660, USA article info abstract Article history: In June 2008, 122 yearling heifers with a history of anthelmintic resistance were obtained Received 15 October 2009 from pastures in northern California and transported to a dry lot facility in southwest- Received in revised form 28 January 2010 ern Idaho, USA. Fifty heifers with the highest fecal egg counts were selected for study Accepted 24 February 2010 enrollment. Candidates were equally randomized to treatment with either injectable iver- mectin (Ivomec®, Merial, 0.2 mg kg−1 BW), injectable moxidectin (Cydectin®, Fort Dodge, Keywords: 0.2 mg kg−1 BW), oral fenbendazole (Safe-Guard®, Intervet, 5.0 mg kg−1 BW), oral oxfenda- Anthelmintic resistance zole (Synanthic®, Fort Dodge, 4.5 mg kg−1 BW), or saline. At 14 days post-treatment, Cattle Bovine nematodes were recovered from the abomasum, small intestine, and large intestine. Par- Nematodes asitism was confirmed in the control group when 10/10 animals were infected with Efficacy adult Ostertagia ostertagi and 9/10 animals with both developing and early L4 stages of Cooperia O. ostertagi. Similarly, 9/10 animals were parasitized with adult Cooperia spp. Fenbenda- Ostertagia zole and oxfendazole efficacy verses controls were >90% against adult Cooperia spp., while moxidectin caused an 88% parasite reduction post-treatment (P < 0.05).
  • NON-HAZARDOUS CHEMICALS May Be Disposed of Via Sanitary Sewer Or Solid Waste

    NON-HAZARDOUS CHEMICALS May Be Disposed of Via Sanitary Sewer Or Solid Waste

    NON-HAZARDOUS CHEMICALS May Be Disposed Of Via Sanitary Sewer or Solid Waste (+)-A-TOCOPHEROL ACID SUCCINATE (+,-)-VERAPAMIL, HYDROCHLORIDE 1-AMINOANTHRAQUINONE 1-AMINO-1-CYCLOHEXANECARBOXYLIC ACID 1-BROMOOCTADECANE 1-CARBOXYNAPHTHALENE 1-DECENE 1-HYDROXYANTHRAQUINONE 1-METHYL-4-PHENYL-1,2,5,6-TETRAHYDROPYRIDINE HYDROCHLORIDE 1-NONENE 1-TETRADECENE 1-THIO-B-D-GLUCOSE 1-TRIDECENE 1-UNDECENE 2-ACETAMIDO-1-AZIDO-1,2-DIDEOXY-B-D-GLYCOPYRANOSE 2-ACETAMIDOACRYLIC ACID 2-AMINO-4-CHLOROBENZOTHIAZOLE 2-AMINO-2-(HYDROXY METHYL)-1,3-PROPONEDIOL 2-AMINOBENZOTHIAZOLE 2-AMINOIMIDAZOLE 2-AMINO-5-METHYLBENZENESULFONIC ACID 2-AMINOPURINE 2-ANILINOETHANOL 2-BUTENE-1,4-DIOL 2-CHLOROBENZYLALCOHOL 2-DEOXYCYTIDINE 5-MONOPHOSPHATE 2-DEOXY-D-GLUCOSE 2-DEOXY-D-RIBOSE 2'-DEOXYURIDINE 2'-DEOXYURIDINE 5'-MONOPHOSPHATE 2-HYDROETHYL ACETATE 2-HYDROXY-4-(METHYLTHIO)BUTYRIC ACID 2-METHYLFLUORENE 2-METHYL-2-THIOPSEUDOUREA SULFATE 2-MORPHOLINOETHANESULFONIC ACID 2-NAPHTHOIC ACID 2-OXYGLUTARIC ACID 2-PHENYLPROPIONIC ACID 2-PYRIDINEALDOXIME METHIODIDE 2-STEP CHEMISTRY STEP 1 PART D 2-STEP CHEMISTRY STEP 2 PART A 2-THIOLHISTIDINE 2-THIOPHENECARBOXYLIC ACID 2-THIOPHENECARBOXYLIC HYDRAZIDE 3-ACETYLINDOLE 3-AMINO-1,2,4-TRIAZINE 3-AMINO-L-TYROSINE DIHYDROCHLORIDE MONOHYDRATE 3-CARBETHOXY-2-PIPERIDONE 3-CHLOROCYCLOBUTANONE SOLUTION 3-CHLORO-2-NITROBENZOIC ACID 3-(DIETHYLAMINO)-7-[[P-(DIMETHYLAMINO)PHENYL]AZO]-5-PHENAZINIUM CHLORIDE 3-HYDROXYTROSINE 1 9/26/2005 NON-HAZARDOUS CHEMICALS May Be Disposed Of Via Sanitary Sewer or Solid Waste 3-HYDROXYTYRAMINE HYDROCHLORIDE 3-METHYL-1-PHENYL-2-PYRAZOLIN-5-ONE
  • PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1

    PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1

    Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known.
  • Review Article a BRIEF REVIEW on the MODE of ACTION of ANTINEMATODAL DRUGS

    Review Article a BRIEF REVIEW on the MODE of ACTION of ANTINEMATODAL DRUGS

    Acta Veterinaria-Beograd 2017, 67 (2), 137-152 UDK: 615.284.03 DOI: 10.1515/acve-2017-0013 Review article A BRIEF REVIEW ON THE MODE OF ACTION OF ANTINEMATODAL DRUGS ABONGWA Melanie, MARTIN Richard J., ROBERTSON Alan P.* Department of Biomedical Sciences, College of Veterinary Medicine, Iowa State University, Ames, IA 50011, USA (Received 01 May, Accepted 24 May 2017) Anthelmintics are some of the most widely used drugs in veterinary medicine. Here we review the mechanism of action of these compounds on nematode parasites. Included are the older classes of compounds; the benzimidazoles, cholinergic agonists and macrocyclic lactones. We also consider newer anthelmintics, including emodepside, derquantel and tribendimidine. In the absence of vaccines for most parasite species, control of nematode parasites will continue to rely on anthelmintic drugs. As a consequence, vigilance in detecting drug resistance in parasite populations is required. Since resistance development appears almost inevitable, there is a continued and pressing need to fully understand the mode of action of these compounds. It is also necessary to identify new drug targets and drugs for the continued effective control of nematode parasites. Key words: anthelmintic, parasite, benzimidazoles, avermectins, cholinergic, emodepside, derquantel INTRODUCTION Anthelmintics are drugs that are used to treat infections caused by parasitic worms (helminths) [1]. There are three major groups of helminths namely: nematodes (roundworms), trematodes (fl ukes) and cestodes (tapeworms). These groups of helminths are divided into two phyla; nematodes (roundworms) and platyhelminths (trematodes and cestodes) [2]. Anthelmintics either kill worms or cause their expulsion from the body, without causing any signifi cant damage to the host [3].