降血脂化合物n -双-(对氯苯氧基)-乙酰脲在人和大鼠体内的酶诱导作用。

A Gógl, K Simon, D Müller, W Klinger, C Ruzsa, Z Vezekényi
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引用次数: 0

摘要

新型纤维酸衍生物n -双-(对氯苯氧基)-乙酰脲除具有降脂作用外,还具有酶诱导作用。给药(100 mg/kg口服)雄性Wistar大鼠3天。治疗后肝脏重量增加,肝微粒体蛋白和细胞色素p-450含量增加,六巴比妥睡眠时间缩短。体外实验发现,肝匀浆上清9000 g细胞色素p-450依赖性生物转化增加。I型底物(乙基吗啡、氨基吡啶)的生物转化量增加,硝基苯的还原量急剧增加。我们没有发现ii型底物苯胺的生物转化有任何变化。在16例吉尔伯特综合征患者中,该药以150mg /天口服治疗3周后,血清胆红素水平下降,尿中d -葡萄糖酸输出量和溴磺胺吡啶转运量最大。在此治疗后,γ -谷氨酰胺转肽类的水平没有改变。作者强烈建议在临床应用中认真考虑代谢相互作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Enzyme-inductive effect of a hypolipidemic compound N-bis-(p-chlorophenoxy)-acetyl-urea in man and rat.

Besides its antilipidaemic effect, the new clofibric acid derivative (N-bis-(p-chlorohenoxy)-acetyl-urea) has an enzyme-inductive effect. The drug was administered (100 mg/kg orally) to male, Wistar rats for three days. The treatment raised the weight of the liver, the content of liver microsomal protein and cytochrome p-450 and shortened the hexobarbital sleeping time. The increase of cytochrome p-450 dependent biotransformation was found by in vitro methods in 9000-g supernatant of liver homogenate. There was a growth in biotransformation of substrates of type I (ethylmorphine, aminopyrine) and an extreme increase in reduction of nitrobenzene. We did not find any change in biotransformation of the type-II substrate aniline. In 16 patients suffering from Gilbert's syndrome, there was a decrease in the level of serum bilirubin, and increase of D-glucuric-acid output in urine and bromsulphophthalein transport maximum following the treatment of this drug given in 150 mg/day orally for three weeks. After this treatment, the level of gamma-glutamyl-transpeptides did not change. The authors highly recommend the serious consideration of metabolic interaction during the clinical application.

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