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次要物种中的药物代谢与处置比较

Comparative drug metabolism and disposition in minor species.

作者信息

Short C R, Barker S A, Flory W

机构信息

Louisiana State University, School of Veterinary Medicine, Baton Rouge 70803.

出版信息

Vet Hum Toxicol. 1988;30 Suppl 1:2-8.

PMID:3212936
Abstract

The disposition of fenbendazole (FBZ) was studied in vivo in cattle (steers), goats, chickens, ducks, turkeys and rabbits, and in vitro in hepatic enzyme preparations from cattle, sheep, goats, rabbits, rats, chickens, ducks, turkeys and catfish. The major excretory metabolite when FBZ was administered either iv or po (5 mg/kg) was p-hydroxyfenbendazole (FBZ-OH). The sulfoxide (FBZ-SO) and sulfone (FBZ-SO2) appeared in plasma but were recovered in only trace amounts in urine or feces, and the amine (FBZ-NH2) was a minor metabolite appearing only occasionally in plasma. The greatest species differences were seen among the avian species, and differences in metabolite excretion correlated well with the ability of the species to metabolize the drug (especially to FBZ-OH) in vitro. Other in vitro studies measured the rate of oxidative, hydrolytic, and conjugative (glucuronide, acetate, sulfate) pathways in liver preparations.

摘要

研究了芬苯达唑(FBZ)在牛(阉牛)、山羊、鸡、鸭、火鸡和兔子体内的处置情况,以及在牛、绵羊、山羊、兔子、大鼠、鸡、鸭、火鸡和鲶鱼肝酶制剂中的体外处置情况。静脉注射或口服(5毫克/千克)FBZ后,主要的排泄代谢产物是对羟基芬苯达唑(FBZ-OH)。亚砜(FBZ-SO)和砜(FBZ-SO2)出现在血浆中,但在尿液或粪便中仅以痕量回收,而胺(FBZ-NH2)是一种次要代谢产物,仅偶尔出现在血浆中。在鸟类物种之间观察到最大的物种差异,代谢产物排泄的差异与该物种在体外代谢药物(尤其是转化为FBZ-OH)的能力密切相关。其他体外研究测量了肝制剂中氧化、水解和结合(葡糖醛酸、乙酸盐、硫酸盐)途径的速率。

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