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[雌激素对非那宗及N-乙酰对氨基酚药代动力学的影响]

[Effect of estrogens on pharmacokinetics of phenazone and N-acetyl-p-aminophenol].

作者信息

Kwiatkowski A

机构信息

Zakładu Farmakologii Klinicznej Instytutu Farmakologii, Pomorskiej Akademii Medycznej.

出版信息

Ann Acad Med Stetin. 1991;37:35-47.

PMID:1816754
Abstract

The aim of the paper was to determine the effect of estrogens on the pharmacokinetics of drugs. The experimental models were made up of female rabbits with bilaterally removed ovaries or those being given mestranol for a long time . N-acetyl-p-amino-phenol and phenazone were the model substances. The effect of surplus as well as deficiency of estrogens on the pharmacokinetics of drugs was ascertained. The surface area under the curve of paracetamol concentration changes was found to diminish after the bilateral removal of ovaries; there was a shortening of the half-life period for the elimination phase, and also an increase of the total clearance. The application of mestranol has made the mentioned parameters behave adversely. The bilateral ovariectomy has led to an increase in the surface area under the curve for phenazone concentration changes, elongation of its half-life period for the elimination phase, and the diminution of the total clearance. These parameters followed the course in a manner being inverse to that in animals receiving mestranol. It may be concluded that estrogens induce the microsomal system of oxidases with mixed function, and exert inhibitory action on enzymes mediating in reactions of coupling.

摘要

本文的目的是确定雌激素对药物药代动力学的影响。实验模型由双侧卵巢切除的雌性兔子或长期服用炔雌醇甲醚的兔子组成。对乙酰氨基酚和非那宗为模型物质。确定了雌激素过多和不足对药物药代动力学的影响。发现双侧卵巢切除后,对乙酰氨基酚浓度变化曲线下的面积减小;消除相的半衰期缩短,总清除率增加。炔雌醇甲醚的应用使上述参数出现相反变化。双侧卵巢切除术导致非那宗浓度变化曲线下的面积增加,其消除相的半衰期延长,总清除率降低。这些参数的变化趋势与接受炔雌醇甲醚的动物相反。可以得出结论,雌激素可诱导具有混合功能的微粒体氧化酶系统,并对介导偶联反应的酶发挥抑制作用。

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