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氯胺酮及其代谢产物在肾功能正常和受损兔体内的动力学。

Kinetics of ketamine and its metabolites in rabbits with normal and impaired renal function.

作者信息

Pedraz J L, Lanao J M, Dominguez-Gil A

出版信息

Eur J Drug Metab Pharmacokinet. 1985 Jan-Mar;10(1):33-9. doi: 10.1007/BF03189695.

Abstract

The plasma levels of ketamine, an anaesthetic, and its metabolites were studied in 10 rabbits with normal renal function and in 9 rabbits with varying degrees of experimentally induced renal impairment. All the animals received a single bolus type i.v. dose of 10 mg/kg of the drug. The results obtained reveal an apparent inhibition of the biotransformation of ketamine in rabbits with renal impairment in which the drug is accumulated. The plasma half-life of ketamine ranged from 0.74 h in rabbits with normal renal function to 2.6 h in the animals with severe renal impairment. The plasma levels of norketamine (metabolite I) did not alter significantly in states of renal impairment. However, the kinetics of the other metabolite (II), dehydronorketamine, did change significantly in renal impairment, due to its high renal excretion capacity.

摘要

在10只肾功能正常的兔子和9只不同程度实验性诱导肾损伤的兔子中,研究了麻醉剂氯胺酮及其代谢物的血浆水平。所有动物均接受10mg/kg药物的单次静脉推注剂量。获得的结果显示,在肾损伤且药物蓄积的兔子中,氯胺酮的生物转化明显受到抑制。氯胺酮的血浆半衰期在肾功能正常的兔子中为0.74小时,在严重肾损伤的动物中为2.6小时。去甲氯胺酮(代谢物I)的血浆水平在肾损伤状态下没有显著变化。然而,另一种代谢物(II),即脱氢去甲氯胺酮的动力学在肾损伤时确实发生了显著变化,这是由于其高肾排泄能力。

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