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[美托洛尔缓释片/长效片:经典β受体阻滞剂的先进剂型]

[Metoprolol CR/XL: advanced formulation of a classical beta-blocker].

作者信息

Kobalava Zh D, Gudkov K M

机构信息

Russian University of Peoples Friendship, ul. Vavilova 61, 117292 Moscow, Russia.

出版信息

Kardiologiia. 2003;43(9):91-100.

Abstract

Metoprolol is a selective beta(1)-adrenergic antagonist extensively used in major fields of cardiology since 1975. Metoprolol has proven its efficacy in reducing cardiovascular events and mortality in patients with hypertension and coronary heart disease in large clinical trials. Recently developed controlled release/extended release (CR/XL) formulation of metoprolol succinate was designed to provide relatively constant metoprolol plasma concentrations and beta(1)-blockade while retaining the convenience of once daily administration. The avoidance of high peak plasma concentrations with metoprolol succinate is associated with lesser degree of adverse effects and may improve patients compliance. This formulation of metoprolol has demonstrated efficacy in reducing cardiovascular events and mortality in patients with heart failure. More recently evidence for antiatherogenic activity of metoprolol succinate has been also obtained.

摘要

美托洛尔是一种选择性β(1)肾上腺素能拮抗剂,自1975年以来广泛应用于心脏病学的主要领域。在大型临床试验中,美托洛尔已证明其在降低高血压和冠心病患者心血管事件及死亡率方面的疗效。最近开发的琥珀酸美托洛尔控释/缓释(CR/XL)制剂旨在提供相对恒定的美托洛尔血浆浓度和β(1)受体阻滞作用,同时保持每日一次给药的便利性。避免琥珀酸美托洛尔出现高血浆峰浓度与较低程度的不良反应相关,并可能提高患者的依从性。这种美托洛尔制剂已证明在降低心力衰竭患者心血管事件及死亡率方面有效。最近还获得了琥珀酸美托洛尔具有抗动脉粥样硬化活性的证据。

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