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[肝脏去神经支配状态下药物的药代动力学特征]

[Pharmacokinetic characteristics of drug substance in liver denervation].

作者信息

Ashirmetov A Kh, Krakovskiĭ M E

出版信息

Farmakol Toksikol. 1989 Jan-Feb;52(1):77-80.

PMID:2707429
Abstract

In experiments on male rats the pharmacokinetics of antipyrine, hexenal and phenylbutazone was studied 7 days after the liver denervation produced by subdiaphragmatic vagotomy, sympathotomy and their combination. It was found that in all variants of the liver denervation there occurs an increase of the period of half-life and a decrease of clearance of the drugs. As the liver denervation practically does not change the degree of protein binding and the hepatic blood flow velocity, it is thought that suppression of the drug biotransformation in hepatocytes due to suppression of the activity of enzymes of their microsomal oxidative system underlies changes in the pharmacokinetics of drugs.

摘要

在雄性大鼠实验中,研究了经膈下迷走神经切断术、交感神经切断术及其联合手术造成肝脏去神经支配7天后安替比林、己醛和保泰松的药代动力学。结果发现,在肝脏去神经支配的所有情况下,药物的半衰期延长,清除率降低。由于肝脏去神经支配实际上并未改变蛋白质结合程度和肝血流速度,因此认为药物微粒体氧化系统酶活性受到抑制,进而导致肝细胞中药物生物转化受到抑制,是药物药代动力学发生变化的原因。

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