Pharmacokinetic Features of the Antiparasitic Macrocyclic Lactones

作者: Quintin A. McKellar , Cengiz Gokbulut

DOI: 10.2174/138920112800399194

关键词:

摘要: The macrocyclic lactones have pharmacokinetic properties which enhance their use against endo- and ectoparasites in animals man. most consistent physico-chemical feature of the group contributes to kinetic characteristics is high lipid solubility. This appears be necessary for pharmacodynamic action as well common features such large volumes distribution influence body fat composition on disposition. They are used all domestic animal species undoubtedly influenced by anatomical physiological differences these species, however also exert a major distribution, metabolism persistence between breeds individuals. A myriad formulations been developed convenience administration different delivered orally, subcutaneously topically good effect. Lipid based excipients "depot" extend period effective prevention parasite re-infection. Subtle structural changes made lactone molecules reduce central nervous system mammary gland, thus allowing some compounds selamectin (SLM) "toxicity sensitive" collie dog lack P-glycoprotein efflux systems eprinomectin (EPM) dairy cattle with nil-milk withdrawal period. Gender exist pharmacokinetics may associated (fat) or metabolism. Feeding availability bind particulate digestive material parasitism impact kinetics drugs because parasitized altered pathophysiological processes, especially gastro intestinal tract but condition (and deposition) animals. affected coadministration interfere transporters interactions explored possible mechanisms enhancing effectiveness antiparasitics. objective this article provide comprehensive review interpret where that information prove clinically useful.

参考文章(158)
Sutra Jf, Galtier P, Alvinerie M, Ivermectin in goat plasma and milk after subcutaneous injection. Veterinary Research. ,vol. 24, pp. 417- 421 ,(1993)
R. S. Rew, J. Vercruysse, Macrocyclic Lactones in Antiparasitic Therapy ,(2003)
J. Dupuy, C. Eeckhoutte, J.F. Sutra, C. Mage, M. Alvinerie, Lack of sex-influence on the in vitro metabolism of ivermectin by hepatic microsomal preparations from cattle. Veterinary Research Communications. ,vol. 23, pp. 223- 227 ,(1999) , 10.1023/A:1006249009553
J A Bogan, S E Marriner, Pharmacokinetics of fenbendazole in sheep. American Journal of Veterinary Research. ,vol. 42, pp. 1146- 1148 ,(1981)
Ming Xu, Marcelo Molento, William Blackhall, Paula Ribeiro, Robin Beech, Roger Prichard, Ivermectin resistance in nematodes may be caused by alteration of P-glycoprotein homolog. Molecular and Biochemical Parasitology. ,vol. 91, pp. 327- 335 ,(1998) , 10.1016/S0166-6851(97)00215-6
M. BALLENT, A. LIFSCHITZ, G. VIRKEL, L. MATE, C. LANUSSE, Pretreatment with the inducers rifampicin and phenobarbital alters ivermectin gastrointestinal disposition. Journal of Veterinary Pharmacology and Therapeutics. ,vol. 33, pp. 252- 259 ,(2009) , 10.1111/J.1365-2885.2009.01129.X
H. Van den Bossche, Biochemistry of parasites and host-parasite relationships. Biochemistry of parasites and host-parasite relationships.. ,(1976)
R. PÉREZ, C. PALMA, M. J. NÚÑEZ, J. COX, M. ARBOIX, Pharmacokinetics of ivermectin in pregnant and nonpregnant sheep. Journal of Veterinary Pharmacology and Therapeutics. ,vol. 31, pp. 71- 76 ,(2007) , 10.1111/J.1365-2885.2007.00926.X
P J Cripps, S Love, T S Mair, L V de Westerlaken, Diarrhoea in adult horses: a survey of clinical cases and an assessment of some prognostic indices Veterinary Record. ,vol. 126, pp. 479- 481 ,(1990) , 10.1136/VR.126.19.479
Eeckhoutte C, Sutra Jf, Galtier P, Alvinerie M, Escudero E, The pharmacokinetics of moxidectin after oral and subcutaneous administration to sheep. Veterinary Research. ,vol. 29, pp. 113- 118 ,(1998)