抗心律失常药物的分类:电药理学基础和临床相关性。

Cardiovascular clinics Pub Date : 1992-01-01
J Coromilas
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引用次数: 0

摘要

只有具有I类活性的抗心律失常药物才能延长QRS持续时间,IC类药物能显著延长QRS持续时间,其次是IA和IB。这与这三种亚类药物与钠通道相互作用的动力学一致。胺碘酮对QRS持续时间的影响介于IB和IA药物之间,符合其1.5秒的tau值。Moricizine对QRS持续时间的影响比预期的2.6秒更明显,但可能是由于失活阻滞的缓慢开始。IC类药物和胺碘酮抑制VPC的效果最好。虽然胺碘酮和索他洛尔被归为III类,但胺碘酮具有显著的IB类活性,而索他洛尔是更有效的-肾上腺素能阻滞剂。这两种药物在抑制VPCs方面的不同作用可以用胺碘酮的I类作用来解释。令人惊讶的是,鉴于可能产生VPC的机制存在明显的异质性,每个亚类中的药物在VPC抑制中都存在相关性。具有III类活性的抗心律失常药物似乎对诱导性持续性室性心动过速患者最有效。除了具有III类活性的I类药物,即IA类药物外,所有I类药物仅对10% - 15%的诱导性室性心动过速患者有效。索他洛尔和胺碘酮之间的不一致是无法解释的。正如预期的那样,室性心动过速周期长度延长最明显的是IC类药物,其次是IA类和IB类药物。在室性心动过速的快速发生时,即使是“快速IB”药物也会发生频率依赖性钠通道阻滞,室性心动过速周期长度延长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Classification of antiarrhythmic agents: electropharmacologic basis and clinical relevance.

Only antiarrhythmic agents with class I activity prolong QRS duration The most marked QRS prolongation is produced by the IC agents, followed by IA and IB. This is consistent with the kinetics of interaction of each of these three subclasses with the sodium channel. Amiodarone's effect on QRS duration is between that of the IB and IA agents consistent with its tau rec of 1.5 seconds. Moricizine's effects on QRS duration are more marked than would be expected from its tau rec of 2.6 seconds but may be explained by the slow onset of inactivation block. The greatest efficacy in VPC suppression is exhibited by the class IC agents and amiodarone. Although amiodarone and sotalol are included in class III, amiodarone has marked class IB activity and sotalol is a more potent beta-adrenergic blocker. The disparate effects of these two drugs in suppressing VPCs may be explained by the class I action of amiodarone. It is surprising that drugs within each subclass correlate at all in VPC suppression in view of the marked heterogeneity of mechanisms potentially producing VPCs. Antiarrhythmic agents with class III activity seem to be the most effective in patients with inducible sustained ventricular tachyarrhythmias. Except for the class I agents with class III activity, that is, IA agents, all class I agents are effective in only 10% to 15% of patients with inducible ventricular tachycardia. The discordance between sotalol and amiodarone is unexplained. As expected, the most marked prolongation of ventricular tachycardia cycle length occurs with the class IC agents, followed by class IA and IB. At the rapid rates of the ventricular tachycardia, frequency-dependent sodium channel block occurs even with the "fast IB" drugs, and ventricular tachycardia cycle length is prolonged.

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