avermectin-b(1)a and Intestinal-Diseases--Parasitic

Three groups of horses and ponies (N = 13, 13 and 12) were treated with ivermectin paste (0.2 mg/kg p.o.), avermectin B1 solution (0.2 mg/kg p.o.), or fenbendazole suspension (10 mg/kg via nasogastric tube). The avermectin B1 was a 1% solution in a propylene glycolglycerol formal base. Faecal strongyle egg counts were performed before, and 14, 28, 42, 56 and 70 d, after treatment. Full-thickness skin biopsies from the neck, pectoral and umbilical regions were examined for Onchocera microfilaria before treatment, and again 14 and 70 d later. Ivermectin therapy produced a significant (P less than 0.01) decrease in mean strongyle egg counts 14, 28, 42 and 56 d after treatment. Avermectin B1 therapy resulted in significant (P less than 0.01) decreases in mean strongyle egg counts 14, 28 and 42 d after treatment. All horses given ivermectin or avermectin B1 had zero strongyle egg counts 14 and 28 d after treatment. Fenbendazole failed to significantly decrease strongyle egg counts. Both ivermectin and avermectin B1 resulted in zero microfilaria counts in all horses 14 d after treatment. On day 70 the percentage decrease in microfilaria counts were 100% and 99.6% respectively. Fenbendazole failed to significantly decrease microfilaria counts. The oral administration of this formulation of avermectin B1 appeared to be highly efficacious against intestinal strongyles and Onchocera microfilaria. The duration of anti-strongyle activity was, however, significantly (P less than 0.01) shorter than that of ivermectin paste.

Topics: Administration, Oral; Animals; Anthelmintics; Antiparasitic Agents; Feces; Female; Fenbendazole; Horse Diseases; Horses; Intestinal Diseases, Parasitic; Ivermectin; Male; Microfilariae; Ointments; Onchocerca; Onchocerciasis; Parasite Egg Count; Skin Diseases, Parasitic; Strongyle Infections, Equine

Doramectin, 25-cyclohexyl-5-O-demethyl-25-de(l-methylpropyl)avermectin A1a, was selected as the best of a series of novel avermectins prepared by mutational biosynthesis. The primary evaluation of its in vivo antiparasitic activity was carried out using a rat Trichostrongylus colubriformis model and a rabbit Psoroptes cuniculi model. In each case the new avermectin performed favourably relative to dihydroavermectin B1a (DHAVM), the major component of ivermectin. Doramectin was extensively evaluated in cattle using an experimental micelle formulation, proving highly effective in cattle infected with Ostertagia ostertagi, Cooperia oncophora and Dictyocaulus viviparus when administered subcutaneously at 200 micrograms kg-1. The plasma pharmacokinetic characteristics of doramectin in cattle following intravenous administration revealed a plasma half-life of approximately 89 h. In the micelle formulation, doramectin administered subcutaneously at 400 micrograms kg-1 provided persistent activity against infection of cattle with C. oncophora and O. ostertagi for at least 8 and 12 days respectively.

Topics: Administration, Oral; Animals; Anthelmintics; Cattle; Cattle Diseases; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation; Female; Injections, Subcutaneous; Insecticides; Intestinal Diseases, Parasitic; Ivermectin; Male; Micelles; Mite Infestations; Mites; Nematode Infections; Rabbits; Random Allocation; Rats; Rats, Wistar; Trichostrongylosis

In a critical study, 40 female mixed-breed lambs with experimental infections of Cooperia spp, Trichostrongylus colubriformis, Ostertagia circumcincta, T axei, and Haemonchus contortus were allocated to 8 groups in 1977. Groups 1 and 5 served as controls. Groups 2 to 4 were treated orally with avermectin B1a at dosage levels of 25, 50, and 100 micrograms/kg of body weight, respectively. Groups 6 to 8 were given oral dihydroavermectin B1a at dosage levels of 50, 100, and 200 micrograms/kg, respectively. The lambs were euthanatized and necropsied 6 days after treatment. The compounds were greater than 99% effective at all dosage levels.

Topics: Animals; Anthelmintics; Drug Evaluation; Female; Gastrointestinal Diseases; Haemonchiasis; Intestinal Diseases, Parasitic; Ivermectin; Lactones; Ostertagiasis; Sheep; Sheep Diseases; Trichostrongyloidiasis; Trichostrongylosis

22,23-Dihydroavermectin B1, ivermectin, derived from avermectin B1 by selective hydrogenation using Wilkinson's homogenous catalyst [Ph3P)3RhCl], was shown to be a highly effective drug for the treatment of a wide variety of metazoan parasitic diseases in animals.

Topics: Animals; Anthelmintics; Cattle; Disaccharides; Helminthiasis; Intestinal Diseases, Parasitic; Ivermectin; Lactones; Sheep