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使用氨己烯酸治疗期间的药代动力学和药效学药物相互作用。

Pharmacokinetic and pharmacodynamic drug interactions during treatment with vigabatrin.

作者信息

Richens A

机构信息

Department of Pharmacology and Therapeutics, University of Wales College of Medicine, Cardiff.

出版信息

Acta Neurol Scand Suppl. 1995;162:43-6. doi: 10.1111/j.1600-0404.1995.tb00500.x.

DOI:10.1111/j.1600-0404.1995.tb00500.x
PMID:7495190
Abstract

Pharmacokinetic drug interactions take place when one drug interacts with another at the level of metabolism, absorption or excretion. Pharmacodynamic interactions take place at the level of receptor sites, where they may have additive or potentiating effects. Vigabatrin is relatively free of pharmacokinetic interactions, and though it is associated with about a 20% decrease in serum levels of concomitantly administered phenytoin, the reduction is of little clinical significance. The mechanism underlying this effect is unknown. Because vigabatrin increases GABA-mediated inhibition in the brain (an action that is believed to account for its anticonvulsant effects), it might be expected to potentiate the CNS effects of benzodiazepines and alcohol. However, very sensitive eye movement studies have failed to detect any evidence of such an interaction. Overall, vigabatrin appears to be remarkably free of drug interactions. As a result, it is easier to use in clinical practice than older anti-epilepsy agents. Perhaps the most important finding of the interaction studies with vigabatrin is that there is no need for patients receiving the drug to be told to avoid alcohol.

摘要

当一种药物在代谢、吸收或排泄水平上与另一种药物相互作用时,就会发生药代动力学药物相互作用。药效学相互作用发生在受体部位,在那里它们可能具有相加或增强作用。氨己烯酸相对不存在药代动力学相互作用,尽管它会使同时服用的苯妥英血清水平降低约20%,但这种降低在临床上意义不大。这种作用的潜在机制尚不清楚。由于氨己烯酸会增加大脑中γ-氨基丁酸(GABA)介导的抑制作用(据信这种作用是其抗惊厥作用的原因),因此可能会增强苯二氮䓬类药物和酒精对中枢神经系统的作用。然而,非常敏感的眼球运动研究未能发现任何这种相互作用的证据。总体而言,氨己烯酸似乎极少发生药物相互作用。因此,与 older anti-epilepsy agents 相比,它在临床实践中使用起来更容易。与氨己烯酸相互作用研究中最重要的发现可能是,无需告知服用该药物的患者避免饮酒。 (注:原文中“older anti-epilepsy agents”表述不太准确规范,推测可能是指传统抗癫痫药物,但需结合更多原文背景信息准确理解。)

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