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人体内乙妥英的饱和代谢途径。

Saturable metabolic pathways for ethotoin in man.

作者信息

Naestoft J, Hvidberg E F, Sjö O

出版信息

Clin Exp Pharmacol Physiol. 1976 Sep-Oct;3(5):453-9. doi: 10.1111/j.1440-1681.1976.tb00623.x.

Abstract
  1. The urinary excretion pattern of ethotoin and five metabolites were examined in three patients receiving continuous treatment with ethotoin at two dose levels, in order to investigate the mechanism behind the dose-dependent kinetics of this anticonvulsant drug. 2. The results suggest a partial saturation in the dealkylation process at high dose levels in three patients. 3. A rough approximation of the Michaelis-Menten constants for different enzymatic processes was attempted. On the basis of the results obtained, the p-hydroxylation may be a saturable process. 4. The dose-dependent kinetics of ethotoin in man seem to be explicable by the existence of partly saturable enzymatic pathways.
摘要
  1. 为研究这种抗惊厥药物剂量依赖性动力学背后的机制,对三名接受两种剂量水平乙苯妥英持续治疗的患者的乙苯妥英及其五种代谢物的尿排泄模式进行了研究。2. 结果表明,三名患者在高剂量水平下脱烷基过程存在部分饱和。3. 尝试对不同酶促过程的米氏常数进行粗略估算。根据所得结果,对羟基化可能是一个可饱和过程。4. 乙苯妥英在人体内的剂量依赖性动力学似乎可以通过部分可饱和酶促途径的存在来解释。

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