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马来酸依那普利(MK-421),一种强效非巯基血管紧张素转换酶抑制剂:人体中的吸收、分布及代谢

Enalapril maleate (MK-421), a potent, nonsulfhydryl angiotensin-converting enzyme inhibitor: absorption, disposition, and metabolism in man.

作者信息

Ulm E H

出版信息

Drug Metab Rev. 1983;14(1):99-110. doi: 10.3109/03602538308991383.

Abstract

Animal studies (particularly in dogs) on enalapril maleate have served to predict the patterns of absorption and elimination observed in man. Enalapril is more readily absorbed in man than the active inhibitor form MK-422. Estimates of minimum absorption of enalapril are of the order of 60-70%, based on urinary recovery. Metabolism of enalapril to MK-422 appears to be largely a postabsorptive process. From urinary recovery data, a minimum of 43% of a 10-mg dose of enalapril is available as MK-422. Excretion of enalapril and MK-422 is principally renal. The excellent mass balance obtained in human studies precludes extensive metabolism beyond hydrolysis to MK-422. Data in hand suggest that any metabolism other than to MK-422 is of a trace nature.

摘要

对马来酸依那普利进行的动物研究(尤其是在狗身上)有助于预测在人体中观察到的吸收和消除模式。依那普利在人体中的吸收比活性抑制剂形式的MK - 422更容易。根据尿液回收率估计,依那普利的最低吸收率约为60 - 70%。依那普利代谢为MK - 422似乎主要是一个吸收后过程。根据尿液回收率数据,10毫克剂量的依那普利至少有43%可转化为MK - 422。依那普利和MK - 422的排泄主要通过肾脏。人体研究中获得的出色质量平衡排除了除水解为MK - 422之外的广泛代谢。现有数据表明,除了转化为MK - 422之外的任何代谢都是微量的。

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