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Ⅲ类抗心律失常活性重要吗?

Is class III antiarrhythmic activity important?

作者信息

Singh B N

机构信息

VA Medical Center WLA, CA 90073.

出版信息

Cardiovasc Drugs Ther. 1990 Jun;4 Suppl 3:597-602. doi: 10.1007/BF00357037.

Abstract

The beginning of thought about a discrete Class III antiarrhythmic action stemmed from the observation that sotalol produced a very marked increase in the time course of repolarization with little or no change in conduction velocity in cardiac muscle. It is known that in patients with hypothyroidism or hypocalcemia, both of which are associated with a marked lengthening of the cardiac action potential, arrhythmias are exceedingly rare. The acetyl metabolite of procainamide also produces, as its sole action, a marked increase in the action-potential duration, and it has antiarrhythmic activity. It is clear that lengthening the action-potential duration is antiarrhythmic. Sotalol is a unique beta blocker in not only antagonizing sympathetic stimulation competitively, but also in exerting a potent antiarrhythmic effect by prolonging repolarization. Because of the augmented tension that is associated with the increase in action-potential duration, sotalol produces a less negative inotropic effect than that seen with other beta blockers. Sotalol is a potent broad-spectrum antiarrhythmic agent because of its Class III properties, resulting from an increase in the length of cardiac repolarization, a property that is modulated by its beta-adrenergic blocking actions.

摘要

关于离散的III类抗心律失常作用的思考始于这样的观察:索他洛尔使复极化的时间过程显著延长,而心肌传导速度几乎没有变化。已知在甲状腺功能减退或低钙血症患者中,这两种情况都与心脏动作电位的显著延长有关,但心律失常极为罕见。普鲁卡因酰胺的乙酰代谢产物也仅产生动作电位持续时间的显著延长这一唯一作用,并且它具有抗心律失常活性。显然,延长动作电位持续时间具有抗心律失常作用。索他洛尔是一种独特的β受体阻滞剂,不仅能竞争性拮抗交感神经刺激,还能通过延长复极化发挥强大的抗心律失常作用。由于与动作电位持续时间增加相关的张力增强,索他洛尔产生的负性肌力作用比其他β受体阻滞剂小。索他洛尔是一种强效的广谱抗心律失常药物,因其III类特性,这是由心脏复极化长度增加导致的,该特性受其β肾上腺素能阻断作用调节。

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