犬单次服用异戊巴比妥后的酶诱导作用。

Enzyme induction following a single dose of amobarbital in dogs.

作者信息

Reilly P A, Inaba T, Kadar D, Endrenyi L

出版信息

J Pharmacokinet Biopharm. 1978 Aug;6(4):305-13. doi: 10.1007/BF01060094.

Abstract

The elimination of amobarbital in dogs was investigated by injecting various doses of amobarbital into a given animal. At low doses (3 mg/kg) serum levels declined in a first-order fashion. Superficially, at high doses (20 mg/kg) the relationship between serum concentration and time could be quantitatively characterized by simple one-compartment saturable kinetics. Indeed, qualitatively, saturation of the amobarbital-metabolizing enzymes was indicated by a shallower initial slope of the semilogarithmic concentration--time profile at the high than at the low dose. However, in addition, an acute enzyme induction phenomenon was observed which was indicated by a shorter terminal half-life of amobarbital at the high dose than after the low dose and also by a shortening in antipyrine half-life.

摘要

通过给特定动物注射不同剂量的异戊巴比妥来研究其在犬体内的消除情况。低剂量（3毫克/千克）时，血清水平呈一级动力学下降。表面上看，高剂量（20毫克/千克）时，血清浓度与时间的关系可用简单的单室饱和动力学进行定量表征。实际上，定性来看，高剂量时半对数浓度-时间曲线的初始斜率比低剂量时更平缓，这表明异戊巴比妥代谢酶出现了饱和。然而，此外还观察到一种急性酶诱导现象，这表现为高剂量时异戊巴比妥的终末半衰期比低剂量时更短，同时安替比林半衰期也缩短。