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[血管紧张素转换酶抑制剂的临床药理学]

[Clinical pharmacology of ACE inhibitors].

作者信息

Hitzenberger G

机构信息

I. Medizinische Universitätsklinik, Abteilung für Klinische Pharmakologie, Wien.

出版信息

Wien Med Wochenschr. 1990 Jan 31;140(1-2):12-8.

PMID:2408245
Abstract

The main effect of the ACE-inhibitors is a reduction of the peripheral resistance and according to that an increase of blood-flow to the organs. Direct effects on the heart are of minor importance. The exact mechanism of action is not fully understood; the main role plays obviously the inhibition of the angiotensin converting enzyme itself; in addition may be effects on the kallikrein-bradykinin-prostaglandin-system are of importance. The pharmacodynamical effects depend on the plasma-concentration and therefore on the pharmacokinetics. These are different with Captopril and Enalapril: Captopril acts directly whereas Enalapril is a "prodrug". With the nowadays used doses Captopril and Enalapril are widely free of side-effects. With the exception of patients with negative sodium-balance (salt-poor diet and/or treatment with diuretics) or patients with renal insufficiency (sometimes increase of creatinine and potassium). In the first group of patients the first dose of ACE-inhibitors should be administered in the evening before going to bed, in the second group creatinine and potassium must be checked 5 to 7 days after an initiation of treatment.

摘要

血管紧张素转换酶抑制剂的主要作用是降低外周阻力,从而增加器官的血流量。对心脏的直接作用相对较小。其确切作用机制尚未完全明确;显然主要作用是抑制血管紧张素转换酶本身;此外,对激肽释放酶-缓激肽-前列腺素系统的影响也很重要。药效学效应取决于血浆浓度,因此也取决于药代动力学。卡托普利和依那普利在这方面有所不同:卡托普利直接起作用,而依那普利是一种“前体药物”。以目前使用的剂量,卡托普利和依那普利基本无副作用。除了钠平衡为负的患者(低盐饮食和/或使用利尿剂治疗)或肾功能不全的患者(有时肌酐和钾会升高)。对于第一组患者,血管紧张素转换酶抑制剂的首剂应在晚上睡前服用,对于第二组患者,治疗开始后5至7天必须检查肌酐和钾。

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