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抗癫痫治疗中的活性代谢产物。关于一种药理学上的“百搭牌”的思考。

Active metabolites in antiepileptic therapy. Reflections on a pharmacological joker.

作者信息

Hvidberg E F

出版信息

Acta Neurol Scand Suppl. 1983;94:9-13.

PMID:6410677
Abstract

Treatment with drugs that produce active metabolites in the organism may sometimes resemble playing cards that includes a joker. Both kinetically and dynamically the metabolites may be different from their parent compound, and antiepileptic drugs are no exception. Primidone, carbamazepine and valproate all have active metabolites, and the various problems which these mean for the treatment of epileptic patients are briefly discussed. Models for studying a parent compound and its active metabolite parallelly in man have been proposed for diazepam. These and other may be applied to antiepileptic drugs in order to increase the quality of their clinical use and the development of new drugs.

摘要

使用在生物体内产生活性代谢物的药物进行治疗,有时可能类似于玩包含百搭牌的纸牌游戏。无论是在动力学还是动态方面,代谢物可能都与其母体化合物不同,抗癫痫药物也不例外。扑米酮、卡马西平和丙戊酸盐都有活性代谢物,本文将简要讨论这些代谢物给癫痫患者治疗带来的各种问题。已针对地西泮提出了在人体中并行研究母体化合物及其活性代谢物的模型。这些模型以及其他模型可应用于抗癫痫药物,以提高其临床使用质量和新药研发水平。

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