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β-肾上腺素能阻滞剂作为抗心律失常和抗纤颤化合物:综述。

Beta-Adrenergic blockers as antiarrhythmic and antifibrillatory compounds: an overview.

作者信息

Singh Bramah N

机构信息

Department of Cardiology, VA Medical Center, West Los Angeles, David Geffen School of Medicine at UCLA, Los Angeles 90073, USA.

出版信息

J Cardiovasc Pharmacol Ther. 2005 Jun;10 Suppl 1:S3-S14. doi: 10.1177/10742484050100i402.

Abstract

Beta-Adrenergic blockers have a wide spectrum of action for controlling cardiac arrhythmias that is larger than initially thought. Data from the past several decades indicate that, as an antiarrhythmic class, beta-blockers remain among the very few pharmacologic agents that reduce the incidence of sudden cardiac death, prolong survival, and ameliorate symptoms caused by arrhythmias in patients with cardiac disease. As a class of compounds, beta-blockers have a fundamental pharmacologic property that attenuates the effects of competitive adrenergic receptors. However, the net clinical effects of the different beta-receptor blockers may vary quantitatively because of variations in associated intrinsic sympathomimetic agonism and in their intrinsic potency for binding to beta-receptors. These individual compounds also differ in their selectivity for beta(1)- and beta(2)-receptors. Metoprolol is a beta(1)-selective blocker, whereas carvedilol is a nonselective beta(1)- and beta(2)-blocker, an antioxidant, and has a propensity to inhibit alpha(1)-receptors and endothelin. Evolving data from controlled and uncontrolled clinical trials suggest that there are clinically significant differences among this class of drugs. Recent evidence also suggests that the antiarrhythmic actions of certain beta-receptor blockers such as carvedilol and metoprolol extend beyond the ventricular tissue to encompass atrial cells and help maintain sinus rhythm in patients with atrial fibrillation, especially in combination with potent antifibrillatory agents such as amiodarone. This introduction provides a current perspective on these newer developments in the understanding of the antiarrhythmic and antifibrillatory actions of beta-blockers.

摘要

β-肾上腺素能阻滞剂在控制心律失常方面具有比最初认为的更广泛的作用谱。过去几十年的数据表明,作为一类抗心律失常药物,β-阻滞剂仍然是极少数能够降低心源性猝死发生率、延长生存期并改善心脏病患者心律失常所致症状的药物之一。作为一类化合物,β-阻滞剂具有一种基本的药理特性,即减弱竞争性肾上腺素能受体的作用。然而,由于相关内在拟交感神经活性及与β受体结合的内在效能存在差异,不同β受体阻滞剂的临床净效应在数量上可能有所不同。这些个别化合物对β1和β2受体的选择性也存在差异。美托洛尔是一种β1选择性阻滞剂,而卡维地洛是一种非选择性β1和β2阻滞剂,具有抗氧化作用,且有抑制α1受体和内皮素的倾向。来自对照和非对照临床试验的不断发展的数据表明,这类药物之间存在临床上的显著差异。最近的证据还表明,某些β受体阻滞剂如卡维地洛和美托洛尔的抗心律失常作用不仅限于心室组织,还包括心房细胞,并有助于维持房颤患者的窦性心律,尤其是与胺碘酮等强效抗纤颤药物联合使用时。本引言提供了关于β阻滞剂抗心律失常和抗纤颤作用理解方面这些新进展的当前观点。

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