El-Sherif Nabil, Turitto Gioia
SUNY Downstate Medical Center 450 Clarkson Avenue, Box 1199, Brooklyn, NY 11203, USA.
Pacing Clin Electrophysiol. 2005 Sep;28(9):985-90. doi: 10.1111/j.1540-8159.2005.00200.x.
The cardiovascular drug carvedilol is characterized by multiple pharmacological actions, which translate into a wide-spectrum therapeutic potential. Its major molecular targets are membrane adrenoceptors, ion channels, and reactive oxygen species. Carvedilol's favorable hemodynamic effects are due to the fact that the drug competitively blocks beta(1)-, beta(2)-, and alpha(1)- adrenoceptors. Several additional properties have been documented and may be clinically important, including antioxidant, antiproliferative/antiatherogenic, anti-ischemic, and antihypertrophic effects. The antiarrhythmic action of carvedilol may be related to a combination of its beta-blocking effects with its modulating effects on a variety of ion channels and currents. Several studies suggest that the drug may be useful in reducing cardiac death in high-risk patients with prior myocardial infarction and/or heart failure, as well as for primary and secondary prevention of atrial fibrillation. This article will review experimental data available on the electrophysiologic properties of carvedilol, with a focus on their clinical relevance.
心血管药物卡维地洛具有多种药理作用，这使其具有广泛的治疗潜力。其主要分子靶点是膜肾上腺素能受体、离子通道和活性氧。卡维地洛良好的血流动力学效应归因于该药物竞争性阻断β(1)-、β(2)-和α(1)-肾上腺素能受体。已证实卡维地洛还有其他几种特性，可能具有临床重要性，包括抗氧化、抗增殖/抗动脉粥样硬化、抗缺血和抗肥厚作用。卡维地洛的抗心律失常作用可能与其β受体阻断作用以及对多种离子通道和电流的调节作用有关。多项研究表明，该药物可能有助于降低既往有心肌梗死和/或心力衰竭的高危患者的心源性死亡风险，以及用于心房颤动的一级和二级预防。本文将综述有关卡维地洛电生理特性的实验数据，重点关注其临床相关性。
