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各种正性肌力药物的药理作用。

Pharmacological actions of various inotropic agents.

作者信息

Scholz H

出版信息

Eur Heart J. 1983 Jan;4 Suppl A:161-72. doi: 10.1093/eurheartj/4.suppl_a.161.

Abstract

The aim of this paper is to describe various positive inotropic drugs (except the cardiac glycosides) and to attempt a classification according to their mechanism of action. The most important drugs with established positive inotropic effect are summarized first. Present interest focuses on the development of new agents with sufficiently high oral bioavailability and long duration of action. Prenalterol is a beta 1-adrenergic drug which appears to fulfil these criteria. Of increasing importance are drugs which combine a positive inotropic and a vasodilator effect. These include mainly the methylxanthines and possibly also the beta 2-adrenoceptor stimulating agents salbutamol, terbutaline, fenoterol and pirbuterol. A positive inotropic and vasodilator effect is also produced by the new compounds amrinone and AR-L 115 BS. These drugs appear to resemble theophylline and other methylxanthines in that they also act mainly as phosphodiesterase inhibitors with a subsequent increase in cAMP without interference with alpha- or beta-adrenoceptors. The mechanism of the as yet only experimentally established positive inotropic effect of alpha-adrenoceptor stimulating agents, e.g. phenylephrine, is unknown. However, it is independent of the cAMP system and is not accompanied by changes in frequency.

摘要

本文旨在描述各类正性肌力药物(不包括强心苷),并尝试根据其作用机制进行分类。首先总结已确定具有正性肌力作用的最重要药物。目前的研究兴趣集中在开发具有足够高口服生物利用度和长效作用的新型药物。普瑞特罗是一种β1肾上腺素能药物,似乎符合这些标准。兼具正性肌力和血管舒张作用的药物越来越重要。这些药物主要包括甲基黄嘌呤类,可能还包括β2肾上腺素能受体激动剂沙丁胺醇、特布他林、非诺特罗和吡布特罗。新型化合物氨力农和AR-L 115 BS也具有正性肌力和血管舒张作用。这些药物似乎与茶碱和其他甲基黄嘌呤类相似,因为它们也主要作为磷酸二酯酶抑制剂起作用,随后使环磷酸腺苷(cAMP)增加,而不干扰α或β肾上腺素能受体。α肾上腺素能受体激动剂(如去氧肾上腺素)目前仅在实验中确定的正性肌力作用机制尚不清楚。然而,它独立于cAMP系统,且不伴有频率变化。

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