Xue Y, Tanabe S, Nabuchi Y, Hashimoto K
Department of Pharmacology, Yamanashi Medical University, Japan.
J Cardiovasc Pharmacol. 1998 Aug;32(2):239-47. doi: 10.1097/00005344-199808000-00011.
KCB-328 is a newly synthesized class III drug. To determine whether this drug has antiarrhythmic or proarrhythmic effects, we used canine ventricular arrhythmia models induced by coronary ligation and reperfusion, programmed electrical stimulation (PES), two-stage coronary ligation, digitalis, or epinephrine. KCB-328, in an intravenous infusion of 0.5 mg/kg/30 min, prolonged the QTc interval only 11%, but had antiarrhythmic effects on the reentry arrhythmias induced by PES (12 of 12 dogs with old myocardial infarction; p < 0.05). KCB-328, in an infusion of 1 mg/kg/h, suppressed the occurrence of fatal ventricular fibrillation (VF) induced by coronary ligation and reperfusion under either halothane anesthesia (p < 0.05) or pentobarbital anesthesia (p < 0.05). Under the halothane anesthesia, KCB-328 alone showed proarrhythmic effects [i.e., induction of ventricular premature contractions (VPCs)], but it did not induce a more severe effect such as torsades de pointes-type ventricular tachycardia (VT). In addition, KCB-328 had weak antiarrhythmic effects on the automaticity arrhythmias induced by 24-h coronary ligation but was effective neither on 48-h coronary ligation arrhythmias nor on the digitalis- and epinephrine-induced arrhythmias. Our results indicate that KCB-328 has powerful antiarrhythmic effects with fewer proarrhythmic potencies.
KCB - 328是一种新合成的III类药物。为了确定该药物是否具有抗心律失常或促心律失常作用,我们使用了冠状动脉结扎和再灌注、程序电刺激(PES)、两阶段冠状动脉结扎、洋地黄或肾上腺素诱导的犬室性心律失常模型。以0.5毫克/千克/30分钟的静脉输注剂量使用KCB - 328时,QTc间期仅延长了11%,但对PES诱导的折返性心律失常具有抗心律失常作用(12只陈旧性心肌梗死犬中的12只;p < 0.05)。以1毫克/千克/小时的输注剂量使用KCB - 328时,在氟烷麻醉(p < 0.05)或戊巴比妥麻醉(p < 0.05)下,均可抑制冠状动脉结扎和再灌注诱导的致命性室颤(VF)的发生。在氟烷麻醉下,单独使用KCB - 328显示出促心律失常作用[即诱发室性早搏(VPC)],但未诱发更严重的效应,如尖端扭转型室性心动过速(VT)。此外,KCB - 328对24小时冠状动脉结扎诱导的自律性心律失常具有较弱的抗心律失常作用,但对48小时冠状动脉结扎心律失常以及洋地黄和肾上腺素诱导的心律失常均无效。我们的结果表明,KCB - 328具有强大的抗心律失常作用,且促心律失常潜力较小。