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倍他洛尔:一种新型长效β1选择性肾上腺素能阻滞剂。

Betaxolol: a new long-acting beta 1-selective adrenergic blocker.

作者信息

Frishman W H, Tepper D, Lazar E J, Behrman D

机构信息

Department of Medicine, Albert Einstein College of Medicine, Bronx, New York.

出版信息

J Clin Pharmacol. 1990 Aug;30(8):686-92. doi: 10.1002/j.1552-4604.1990.tb03627.x.

Abstract

Betaxolol (Searle, Skokie, Illinois) is a new beta 1-selective adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity. Its pharmacokinetic profile is characterized by a long serum half-life and excellent oral bioavailability, with little first-pass metabolism. The mean 16-hour half-life of betaxolol has been shown to provide full 24-hour control of blood pressure and heart rate. Betaxolol has been proven to be a safe and effective antihypertensive agent, and was recently approved for clinical use in the United States for this indication.

摘要

倍他洛尔(先灵公司,伊利诺伊州斯科基)是一种新型的β1选择性肾上腺素能阻滞剂,无部分激动剂作用,膜稳定活性极小。其药代动力学特征为血清半衰期长,口服生物利用度极佳,首过代谢少。倍他洛尔平均16小时的半衰期已被证明可对血压和心率提供24小时的完全控制。倍他洛尔已被证明是一种安全有效的抗高血压药物,最近在美国被批准用于该适应症的临床治疗。

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