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新型抗心律失常药物氟卡尼(R 818)对人体的电生理效应(作者译)

[Electrophysiological effects of the new antiarrhythmic drug flecainide (R 818) in man (author's transl)].

作者信息

Seipel L, Abendroth R R, Breithardt G

出版信息

Z Kardiol. 1981 Jul;70(7):524-9.

PMID:7269731
Abstract

The electrophysiological effects of the new antiarrhythmic drug Flecainide (R 818) was tested in altogether 27 patients with and without disturbances of sinus node function and intraventricular conduction. Flecainide was given intravenously in a dose of 1 mg/kg and 2 mg/kg. Constant "therapeutic" plasma levels were reached by application of 1 mg/kg as a bolus and an additional infusion of 1 mg/kg during the test period of 20 min. The drug had no significant effects on sinus node function even in patients with sinus node dysfunction tested so far. Intracardiac conduction time was prolonged within all compartments of the heart in a dose-dependent manner. After bolus injection of 1 mg/kg, the HRA-A interval lengthened by 10.4%, the A-H interval by 13.5%, the H-V time by 15.7% and the V-RVA interval by 29.1% of the control value. In addition, the QRS complex widened by 8.1%. After 2 mg/kg Flecainide the HRA-A interval was prolonged by 9.0%, the A-H interval by 24.4%, the H-V time by 40.2%, and the V-RVA interval by 16.5% of the control value. The QRS complex widened by 24.2%. In contrast, there was only a small and often insignificant increase in the refractoriness of the different compartments of the heart (5-15% increase of the control value). In two patients with bundle branch block, a higher degree A-V block distal the H potential occurred after 2 mg/kg Flecainide. These electrophysiological effects may explain some antiarrhythmic actions of Flecainide. In addition, possible side effects of the drug can be assessed. In patients with intraventricular conduction defects the drug should be used with caution especially when given iv in higher doses.

摘要

对27例有或无窦房结功能及室内传导障碍的患者,测试了新型抗心律失常药物氟卡尼(R 818)的电生理效应。静脉注射氟卡尼的剂量为1mg/kg和2mg/kg。通过静脉推注1mg/kg并在20分钟的测试期内额外输注1mg/kg,达到恒定的“治疗性”血浆水平。即使在迄今为止测试的窦房结功能障碍患者中,该药物对窦房结功能也无显著影响。心脏各腔室的心脏内传导时间以剂量依赖性方式延长。静脉推注1mg/kg后,高位右房-心房(HRA-A)间期延长了对照值的10.4%,心房-希氏束(A-H)间期延长了13.5%,希氏束-心室(H-V)时间延长了15.7%,心室-右室心尖(V-RVA)间期延长了29.1%。此外,QRS波群增宽了8.1%。给予2mg/kg氟卡尼后,HRA-A间期延长了对照值的9.0%,A-H间期延长了24.4%,H-V时间延长了40.2%,V-RVA间期延长了16.5%。QRS波群增宽了24.2%。相比之下,心脏不同腔室的不应期仅有轻微且通常不显著的增加(对照值增加5%-15%)。在2例束支传导阻滞患者中,给予2mg/kg氟卡尼后,在希氏束电位远端出现了更高程度的房室传导阻滞。这些电生理效应可能解释了氟卡尼的一些抗心律失常作用。此外,还可以评估该药物可能的副作用。对于有室内传导缺陷的患者,尤其是静脉给予较高剂量时,应谨慎使用该药物。

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