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[安替比林的代谢相互作用]

[Metabolic interactions of propyphenazone].

作者信息

Borchert H H, Schuster S, Pfeifer S

出版信息

Pharmazie. 1983 Jan;38(1):48-50.

PMID:6405401
Abstract

Pretreatment of female Wistar rats with propyphenazone produces a slight shortening of the hexobarbital sleeping time, and high doses of this drug cause a small increase in the relative liver weight, but there occurs no significant change in the N-demethylation of aminophenazone, the O-demethylation of codeine phosphate, the hydroxylation of aniline, the glucuronidation of p-nitrophenol, the cytochrome P-450 concentration and the NADPH-cytochrome c reductase activity in the 9.000 supernatant of liver homogenates. The differences between these properties of propyphenazone and those of aminophenazone and phenazone are discussed with reference to partition coefficients and biotransformation. The findings obtained do not justify the expectation of metabolic drug-drug interactions in case of repeated application of propyphenazone in the framework of a combined therapy.

摘要

用安替比林预处理雌性Wistar大鼠会使己巴比妥睡眠时间稍有缩短,高剂量该药物会使相对肝脏重量略有增加,但在肝脏匀浆9000g上清液中,氨基比林的N-去甲基化、磷酸可待因的O-去甲基化、苯胺的羟基化、对硝基苯酚的葡萄糖醛酸化、细胞色素P-450浓度以及NADPH-细胞色素c还原酶活性均未发生显著变化。参照分配系数和生物转化讨论了安替比林与氨基比林和非那宗这些特性之间的差异。所得结果并不支持在联合治疗框架内重复应用安替比林时会出现药物代谢性相互作用的预期。

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