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[两种β受体阻滞剂的药代动力学:一种药物遗传学异常的检测]

[Pharmacokinetics of two beta blocking drugs: detection of a pharmacogenetic abnormality].

作者信息

Balant L, Gorgia A, Tschopp J M, Revillard C, Fabre J

出版信息

Schweiz Med Wochenschr. 1976 Oct 9;106(41):1403-7.

PMID:12563
Abstract

10 healthy male volunteers received orally either 100 mg tolamolol or 20 mg bufuralol. These experiments were repeated by intravenous administration of 10 and 5 mg respectively of these two drugs. Plasma levels of the parent drugs and their main metabolite were measured. In one subject, the apparent half-life of elimination was increased from 2.5 h (normal subjects) to 5 h for both drugs. This prolongation of the half-life is associated with low plasma levels of the metabolites, a peculiarity which can be explanined by a decreased rate of metabolism for these two drugs. This anomaly may explain the marked orthostatic hypotension observed only in this subject. The likelihood of a pharmacogenetic defect is discussed.

摘要

10名健康男性志愿者口服了100毫克托拉洛尔或20毫克布呋洛尔。这两种药物分别静脉注射10毫克和5毫克后重复了这些实验。测定了母体药物及其主要代谢物的血浆水平。在一名受试者中,两种药物的表观消除半衰期从2.5小时(正常受试者)增加到了5小时。半衰期的这种延长与代谢物的低血浆水平有关,这一特性可以用这两种药物代谢速率降低来解释。这种异常情况可能解释了仅在该受试者中观察到的明显体位性低血压。讨论了药物遗传学缺陷的可能性。

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