Sugiyama Atsushi
Department of Pharmacology, Interdisciplinary Graduate School of Medicine and Engineering, University of Yamanashi, Nakakoma-gun, Japan.
Nihon Yakurigaku Zasshi. 2003 Jun;121(6):393-400. doi: 10.1254/fpj.121.393.
The proarrhythmic effects of class III antiarrhythmic agents and non-cardiovascular drugs, which have been shown to prolong QT interval, were assessed using two types of in vivo canine models. First, electrophysiological effects of dofetilide, nifekalant, amiodarone, cisapride, astemizole, sulpiride, haloperidol, and sparfloxacin were assessed using halothane-anesthetized dogs. Each drug prolonged the monophasic action potential (MAP) duration and effective refractory period (ERP) at clinically recommended daily doses. The extent of increase was greater in the refractoriness than in the repolarization only for amiodarone, indicating abbreviation of the terminal repolarization period. The reverse was true for the other drugs. Next, torsadogenic action of sematilide, nifekalant, amiodarone, cisapride, terfenadine, sulpiride, and sparfloxacin was assessed using chronic complete atrioventricular block dogs with Holter ECG monitoring in the conscious state. Oral administration of 1-10 times higher doses than the clinically relevant doses of the drugs induced polymorphic ventricular tachycardia torsades de pointes (TdP), except for amiodarone. These results indicate that the prolongation and backward shift of the terminal repolarization period may be closely related to the drug-induced TdP and suggest that these in vivo models can be used to screen proarrhythmic potential of new drugs.
已证实可延长QT间期的Ⅲ类抗心律失常药物和非心血管药物的促心律失常作用,使用两种体内犬类模型进行了评估。首先,在氟烷麻醉的犬类中评估了多非利特、尼非卡兰、胺碘酮、西沙必利、阿司咪唑、舒必利、氟哌啶醇和司帕沙星的电生理作用。每种药物在临床推荐的每日剂量下均延长了单相动作电位(MAP)持续时间和有效不应期(ERP)。仅胺碘酮的不应期延长程度大于复极化,表明终末复极化期缩短。其他药物则相反。接下来,在清醒状态下使用慢性完全性房室传导阻滞犬并进行动态心电图监测,评估了司美利特、尼非卡兰、胺碘酮、西沙必利、特非那定、舒必利和司帕沙星的致扭转型室性心动过速作用。口服剂量比临床相关剂量高1 - 10倍的这些药物,除胺碘酮外,均诱发了多形性室性心动过速尖端扭转型室速(TdP)。这些结果表明,终末复极化期的延长和后移可能与药物诱导的TdP密切相关,并提示这些体内模型可用于筛选新药的促心律失常潜力。