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原发性高血压患者短期和长期服用依那普利后的血浆依那普利水平及激素效应

Plasma enalapril levels and hormonal effects after short- and long-term administration in essential hypertension.

作者信息

Johnston C I, Jackson B J, Larmour I, Cubella R, Casley D

出版信息

Br J Clin Pharmacol. 1984;18 Suppl 2(Suppl 2):233S-239S, 241S. doi: 10.1111/j.1365-2125.1984.tb02602.x.

Abstract

Enalapril lowers blood pressure both acutely and during long-term therapy in patients with essential hypertension. After a single 10 mg dose of enalapril a close relationship between plasma enalaprilic acid (MK-422) levels, angiotensin converting enzyme (ACE) inhibition and the acute hypotensive and hormonal effects was demonstrated. During long-term administration of enalapril, a similar relationship between the plasma enalaprilic acid level, ACE inhibition and the hypotensive effect was shown, although the dose-response curve for plasma enalaprilic acid to ACE inhibition was displaced to the right compared to the acute dose-response curve. Several weeks' administration of enalapril was needed to reach stable plateau levels of plasma enalaprilic acid and ACE inhibition. During long-term treatment with enalapril in essential hypertension, there was sustained inhibition of ACE and the associated hormonal changes.

摘要

依那普利在原发性高血压患者的急性治疗期和长期治疗过程中均可降低血压。单次服用10毫克依那普利后,血浆依那普利酸(MK-422)水平、血管紧张素转换酶(ACE)抑制作用与急性降压及激素效应之间呈现出密切关系。在依那普利长期给药期间,血浆依那普利酸水平、ACE抑制作用与降压效果之间也表现出类似关系,尽管与急性剂量反应曲线相比,血浆依那普利酸对ACE抑制作用的剂量反应曲线向右偏移。需要数周的依那普利给药才能使血浆依那普利酸和ACE抑制作用达到稳定的平台水平。在原发性高血压患者长期使用依那普利治疗期间,ACE受到持续抑制,同时伴有相关的激素变化。

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