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奈必洛尔的药理学

Pharmacology of nebivolol.

作者信息

Mangrella M, Rossi F, Fici F, Rossi F

机构信息

Institute of Pharmacology and Toxicology, Faculty of Medicine and Surgery, 2nd University of Naples, Italy.

出版信息

Pharmacol Res. 1998 Dec;38(6):419-31. doi: 10.1006/phrs.1998.0387.

Abstract

Nebivolol is a new selective beta 1-adrenergic blocking agent, that possesses a peculiar pharmacodynamic profile and an original chemical structure, by which it differs from traditional beta 1-blockers. Nebivolol is a racemic mixture of two enantiomers in equal ratios. It is endowed with a highly selective beta 1-blocking activity, and does not show an intrinsic sympathomimetic activity. Nebivolol is endowed with peripheral vasodilating properties mediated by the modulation of the endogenous production of nitric oxide. It does not significantly decrease airway conductance compared with atenolol and propranolol. Nebivolol does not compromise the left ventricular function, but it may increase stroke volume, and does not reduce heart inotropism during exertion. Nebivolol is quite safe and is well tolerated, also when compared to traditional beta-blockers. The most common adverse effects are dizziness, headache and fatigue. Owing to its combined dual mechanism of action, nebivolol leads to a unique haemodynamic and therapeutic profile by which it may be advantageous in essential hypertension, ischaemic heart disease and congestive heart failure.

摘要

奈必洛尔是一种新型选择性β1肾上腺素能阻滞剂,具有独特的药效学特征和原始化学结构,与传统β1阻滞剂不同。奈必洛尔是两种对映体按等比例组成的外消旋混合物。它具有高度选择性的β1阻断活性,且不表现出内在拟交感活性。奈必洛尔具有通过调节内源性一氧化氮产生介导的外周血管舒张特性。与阿替洛尔和普萘洛尔相比,它不会显著降低气道传导。奈必洛尔不会损害左心室功能,但可能增加心搏量,且在运动时不会降低心肌收缩力。奈必洛尔相当安全且耐受性良好,与传统β阻滞剂相比也是如此。最常见的不良反应是头晕、头痛和疲劳。由于其双重作用机制,奈必洛尔产生独特的血流动力学和治疗特性,这使其在原发性高血压、缺血性心脏病和充血性心力衰竭中可能具有优势。

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