Singh B N
Department of Cardiology, Wadsworth Veterans Administration Hospital, Los Angeles, California 90073.
Am J Cardiol. 1993 Aug 12;72(4):8A-18A. doi: 10.1016/0002-9149(93)90020-d.
Although synthesized as a nonselective beta-adrenergic blocking compound, sotalol has emerged as the prototype of the so-called class III antiarrhythmic compounds. It delays cardiac repolarization by inhibiting the delayed rectifier potassium current, having a lesser effect on the inward rectifying potassium current with little or no effect on the inward calcium or sodium currents. This property of prolonging repolarization with an accompanying increase in the effective refractory period is not due to blockade of the beta-adrenergic receptors. The major electrophysiologic profile of sotalol constitutes the summed effects of beta blockade and prolonged repolarization. Sotalol exerts a potent antifibrillatory action modulated by its antiadrenergic effects. It suppresses premature ventricular contractions and nonsustained ventricular tachycardia while preventing inducible ventricular tachycardia and fibrillation in patients with advanced structural heart disease. The compound is therefore likely to exert a broad spectrum of antiarrhythmic actions in ventricular arrhythmias.
虽然索他洛尔最初是作为一种非选择性β肾上腺素能阻滞剂合成的,但它已成为所谓Ⅲ类抗心律失常化合物的原型。它通过抑制延迟整流钾电流来延迟心脏复极化,对内向整流钾电流的影响较小,对内向钙电流或钠电流几乎没有影响。这种延长复极化并伴随有效不应期增加的特性并非由于β肾上腺素能受体的阻断。索他洛尔的主要电生理特征是β受体阻断和复极化延长的综合作用。索他洛尔通过其抗肾上腺素能作用发挥强大的抗纤颤作用。它可抑制室性早搏和非持续性室性心动过速,同时预防晚期结构性心脏病患者的诱发性室性心动过速和纤颤。因此,该化合物可能对室性心律失常发挥广泛的抗心律失常作用。