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癫痫患者中丙二酸二正丙酯的药代动力学

Pharmacokinetics of di-n-propylacetate in epileptic patients.

作者信息

Schobben F, van der Kleijn E, Gabreëls F J

出版信息

Eur J Clin Pharmacol. 1975 Feb 28;8(2):97-105. doi: 10.1007/BF00561557.

Abstract

The pharmacokinetics of the anti-epileptic drug di-n-propylacetate (DepakineR) have been studied in 7 patients, in whom plasma concentrations were determined during and following subchronic treatment. Elimination of the drug appeared to follow a monophasic exponential course; biological half lives were 8 to 15 hours. The data supported the assumption that an open one-compartment model can be used to describe the kinetics of dipropylacetate in man. The drug appeared to have a relatively restricted distribution: calculated relative distribution volumes ranged from 0.15 to 0.40 1/kg. There were large interindividual differences in clearance rate. The therapeutic range was considered to be between 50 and 100 mg/1 plasma. Plasma levels of phenobarbital were markedly raised during treatment with dipropylacetate for an unknown reason. Determination of the plasma concentrations of drugs at accurately fixed times appears to be a reliable method for pharmacotherapeutic monitoring of epileptic patients.

摘要

在7名患者中研究了抗癫痫药物二正丙基乙酸酯(德巴金®)的药代动力学,在亚慢性治疗期间及之后测定了他们的血浆浓度。药物消除似乎遵循单相指数过程;生物半衰期为8至15小时。数据支持这样的假设,即开放一室模型可用于描述二正丙基乙酸酯在人体内的动力学。该药物的分布似乎相对受限:计算得出的相对分布容积范围为0.15至0.40升/千克。清除率存在较大的个体间差异。治疗范围被认为是血浆中50至100毫克/升。在用二正丙基乙酸酯治疗期间,苯巴比妥的血浆水平因不明原因显著升高。在准确固定的时间测定药物的血浆浓度似乎是癫痫患者药物治疗监测的可靠方法。

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