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在兔心律失常模型中评估 HCN 通道阻滞剂伊伐布雷定的致扭转型作用。

Torsadogenic Potential of HCN Channel Blocker Ivabradine Assessed in the Rabbit Proarrhythmia Model.

机构信息

Department of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Toho University.

出版信息

Biol Pharm Bull. 2021;44(11):1796-1799. doi: 10.1248/bpb.b21-00605.

Abstract

Torsadogenic effects of ivabradine, an inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, were assessed in an in vivo proarrhythmia model of acute atrioventricular block rabbit. Ivabradine at 0.01, 0.1, and 1 mg/kg was intravenously administered to isoflurane-anesthetized rabbits (n = 5) in the stable idioventricular rhythm. Ivabradine at 0.01 and 0.1 mg/kg hardly affected the atrial and ventricular automaticity, QT interval, or the monophasic action potential duration of the ventricle. Additionally administred ivabradine at 1 mg/kg decreased the atrial and ventricular rate significantly but increased the QT interval and duration of the monophasic action potential. Meanwhile, torsade de pointes arrhythmias were detected in 1 out of 5 animals and in 2 out of 5 animals after the administration of 0.1 and 1 mg/kg, respectively. Importantly, torsade de pointes arrhythmias could be observed only in 2 rabbits showing more potent suppressive effects on ventricular automaticity. These results suggest that the torsadogenic potential of ivabradine may become evident when its expected bradycardic action appears more excessively.

摘要

在急性房室传导阻滞兔的体内致心律失常模型中评估了伊伐布雷定(一种超极化激活环核苷酸门控(HCN)通道抑制剂)的致扭转型作用。在异氟烷麻醉的兔子(n=5)稳定的自身节律下,静脉内给予伊伐布雷定 0.01、0.1 和 1mg/kg。伊伐布雷定 0.01 和 0.1mg/kg 几乎不影响心房和心室自动性、QT 间期或心室单相动作电位的持续时间。此外,给予 1mg/kg 的伊伐布雷定可显著降低心房和心室率,但增加 QT 间期和单相动作电位的持续时间。同时,在 5 只动物中有 1 只,在给予 0.1 和 1mg/kg 后有 2 只动物中检测到尖端扭转型室性心动过速。重要的是,尖端扭转型室性心动过速仅在 2 只显示对心室自动性更强烈抑制作用的兔子中观察到。这些结果表明,当伊伐布雷定预期的缓慢性作用表现得更加过度时,其致扭转型作用的可能性就会变得明显。

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