Zicha S, Tsuji Y, Shiroshita-Takeshita A, Nattel S
Montreal Heart Institute, 5000 Belanger East, Montreal Quebec, HIT 1C8, Canada.
Handb Exp Pharmacol. 2006(171):235-66.
Drugs that suppress beta-adrenergic signaling by competitively inhibiting agonist binding to beta-adrenergic receptors ("beta-blockers") have important antiarrhythmic properties. They differ from most other antiarrhythmic agents by not directly modifying ion channel function; rather, they prevent the arrhythmia-promoting actions of beta-adrenergic stimulation. beta-Blockers are particularly useful in preventing sudden death due to ventricular tachyarrhythmias associated with acute myocardial ischemia, congenital long QT syndrome, and congestive heart failure. They are also quite valuable in controlling the ventricular rate in patients with atrial fibrillation. This chapter reviews the properties of beta-adrenoceptor signaling, the basic mechanisms of cardiac arrhythmias on which beta-blockers act, the ion channel mediators of beta-adrenergic responses, the evidence for clinical antiarrhythmic indications for beta-blocker therapy and the specific pharmacodynamic and pharmacokinetic properties of beta-blockers that differentiate the various agents of this class.
通过竞争性抑制激动剂与β-肾上腺素能受体结合来抑制β-肾上腺素能信号传导的药物（“β受体阻滞剂”）具有重要的抗心律失常特性。它们与大多数其他抗心律失常药物不同，不会直接改变离子通道功能；相反，它们可预防β-肾上腺素能刺激引起的促心律失常作用。β受体阻滞剂在预防与急性心肌缺血、先天性长QT综合征和充血性心力衰竭相关的室性快速心律失常导致的猝死方面特别有用。它们在控制房颤患者的心室率方面也非常有价值。本章回顾了β-肾上腺素能受体信号传导的特性、β受体阻滞剂作用的心律失常基本机制、β-肾上腺素能反应的离子通道介质、β受体阻滞剂治疗临床抗心律失常适应症的证据以及区分该类各种药物的β受体阻滞剂的具体药效学和药代动力学特性。
