氯巴占及其N-去甲基代谢物的血浆浓度；对小鼠戊四氮诱发惊厥的保护作用。

Plasma concentrations of clobazam and its N-desmethyl metabolite; protection against pentetrazol-induced convulsions in mice.

作者信息

Haigh J R, Gent J P, Calvert R

出版信息

J Pharm Pharmacol. 1984 Sep;36(9):636-8. doi: 10.1111/j.2042-7158.1984.tb04917.x.

DOI:10.1111/j.2042-7158.1984.tb04917.x

Abstract

The anticonvulsant effects of acute administration of clobazam and its principal metabolite N-desmethylclobazam were studied in mice. Pentetrazol, given by slow intravenous infusion 1 or 2 h after the anticonvulsant dose, was used as the convulsant stimulus. Log dose response relationships for both clobazam and N-desmethylclobazam appeared linear, but there was no correlation between plasma concentrations of clobazam and protection. However, correlation between plasma concentrations of N-desmethylclobazam and protection was significant in both cases.

摘要

研究了急性给予氯巴占及其主要代谢产物N-去甲基氯巴占对小鼠的抗惊厥作用。在给予抗惊厥剂量1或2小时后，通过缓慢静脉输注给予戊四氮作为惊厥刺激物。氯巴占和N-去甲基氯巴占的对数剂量反应关系均呈线性，但氯巴占的血浆浓度与保护作用之间无相关性。然而，在两种情况下，N-去甲基氯巴占的血浆浓度与保护作用之间的相关性均显著。