Macrocyclic Lactone (macrocyclic + lactone)

Distribution by Scientific Domains


Selected Abstracts


Insect nicotinic acetylcholine receptor agonists as flea adulticides in small animals

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 4 2010
D. T. VO
Vo, D. T., Hsu, W. H., Abu-Basha, E. A., Martin, R. J. Insect nicotinic acetylcholine receptor agonists as flea adulticides in small animals. J. vet. Pharmacol. Therap. doi: 10.1111/j.1365-2885.2010.01160.x. Fleas are significant ectoparasites of small animals. They can be a severe irritant to animals and serve as a vector for a number of infectious diseases. In this article, we discuss the pharmacological characteristics of four insect nicotinic acetylcholine receptor (nAChR) agonists used as flea adulticides in dogs and cats, which include three neonicotinoids (imidacloprid, nitenpyram, and dinotefuran) and a macrocyclic lactone (spinosad). Insect nAChR agonists are one of the most important classes of insecticides, which are used to control sucking insects on both plants and animals. These novel compounds provide a new approach for practitioners to safely and effectively eliminate adult fleas. [source]


Economic management of anthelmintic resistance: model and application,

AUSTRALIAN JOURNAL OF AGRICULTURAL & RESOURCE ECONOMICS, Issue 4 2009
Caris L. Pech
The increasing prevalence of anthelmintic (drench) resistance in gastrointestinal parasite populations is decreasing the profitability of the Australian sheep industry. Refugia management can delay its development by not exposing a proportion of the worm population to chemical control. A dynamic-optimisation model is used to assess the economic value of refugia for management of the worm species Teladorsagia circumcincta and macrocyclic lactone drenches in an application to Western Australian sheep flocks. A low rate of refugia (2 per cent) is most profitable under standard circumstances because it slows the development of resistance, but also reduces the proportion of the flock not exposed to chemical control. Frequent drench application should remain the primary method of control. However, its efficacy should be preserved through refugia management, rather than greatly reducing treatment frequency. [source]


A review of the use of moxidectin in horses

EQUINE VETERINARY EDUCATION, Issue 10 2008
J. Schumacher
Summary Moxidectin has broad-spectrum anti-nematodal and anti-arthropodal activities in the horse but is not effective against tapeworms or flukes. Moxidectin and ivermectin have the same efficacy against internal, adult parasites of horses. Moxidectin, however, is highly effective in eliminating encysted and hypobiotic larval stages of cyathostomins, whereas ivermectin is not. Treatment of horses with moxidectin results in an egg-reappearance period (ERP) of 15,24 weeks. Because of its long ERP, moxidectin is labelled to be used at 12 week intervals. Moxidectin may provide protection against infection by ingested cyathostomin larvae for 2,3 weeks after it is administered. The larvicidal activity of moxidectin has often been compared to that of fenbendazole administered at either 7.5 or 10 mg/kg bwt for 5 consecutive days. The efficacy of fenbendazole, when administered daily for 5 consecutive days at 7.5 or 10 mg/kg bwt, against all stages of cyathostomins is often less than that of moxidectin because resistance of cyathostomins to benzimidazoles is prevalent worldwide, and the 5 day course of fenbendazole does not overcome this resistance. There are now reports of resistance of ascarids to moxidectin. Overt resistance of cyathostomins and a shortened egg re-emergence period after treatment with moxidectin have been reported. Rapid removal of manure by natural fauna can significantly reduce larval nematode concentrations and thereby reduce intervals of anthelmintic treatment. Of the macrocyclic lactones, moxidectin has the least deleterious effect on faecal fauna. [source]


Moxidectin and ivermectin metabolic stability in sheep ruminal and abomasal contents

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 5 2005
A. LIFSCHITZ
The oral administration of macrocyclic lactones to sheep leads to poorer efficacy and shorter persistence of the antiparasitic activity compared to the subcutaneous treatment. Gastrointestinal biotransformation occurring after oral treatment to ruminant species has been considered as a possible cause of the differences observed between routes of administration. The current work was addressed to evaluate on a comparative basis the in vitro metabolism of moxidectin (MXD) and ivermectin (IVM) in sheep ruminal and abomasal contents. Both compounds were incubated under anaerobic conditions during 2, 6 and 24 h in ruminal and abomasal contents collected from untreated adult sheep. Drug concentrations were measured by high-performance liquid chromatography with fluorescence detection after sample clean up and solid phase extraction. Neither MXD nor IVM suffered metabolic conversion and/or chemical degradation after 24-h incubation in ruminal and abomasal contents collected from adult sheep. Unchanged MXD and IVM parent compounds represented between 95.5 and 100% of the total drug recovered in the ruminal and abomasal incubation mixtures compared with those measured in inactive control incubations. The partition of both molecules between the solid and fluid phases of both sheep digestive contents was assessed. MXD and IVM were extensively bound (>90%) to the solid material of both ruminal and abomasal contents collected from sheep fed on lucerne hay. The results reported here confirm the extensive degree of association to the solid digestive material and demonstrates a high chemical stability without evident metabolism and/or degradation for both MXD and IVM in ruminal and abomasal contents. [source]