Winslow E, Marshall R J, Hope F G
J Cardiovasc Pharmacol. 1987 Mar;9(3):267-75. doi: 10.1097/00005344-198703000-00002.
The potential antiarrhythmic and electrophysiological effects of prolonged oral dosing with amiodarone (20 mg/kg/day) or disopyramide (25 or 50 mg/kg b.i.d.) were compared in normokalaemic (NK) and diet-induced hypokalaemic (HK) anaesthetised rats. In NK rats, amiodarone reduced the number of electrical deaths consequent upon coronary artery ligation and prolonged action potential duration (APD50) of papillary muscle. Disopyramide conferred marked protection against arrhythmias in NK animals, prolonged APD50, reduced the maximum rate of depolarisation, and induced bradycardia. Hypokalaemia inhibited both the antiarrhythmic efficacy and these electrophysiological actions of amiodarone and disopyramide. However, prolongation of APD90 by both drugs was little affected by hypokalaemia. Amiodarone prolonged QTc both in NK and HK rats, whilst disopyramide only prolonged QTc in NK rats and only at the higher dose. It is concluded that reduced antiarrhythmic efficacy of the two drugs by hypokalaemia may be due to altered electrophysiological responses. QTc prolongation per se appears to be associated with antiarrhythmic, not arrhythmogenic, actions in this experimental model.
在正常血钾(NK)和饮食诱导的低钾血症(HK)麻醉大鼠中,比较了长期口服胺碘酮(20毫克/千克/天)或丙吡胺(25或50毫克/千克,每日两次)的潜在抗心律失常和电生理作用。在NK大鼠中,胺碘酮减少了冠状动脉结扎后电死亡的数量,并延长了乳头肌的动作电位持续时间(APD50)。丙吡胺对NK动物的心律失常有显著的保护作用,延长了APD50,降低了最大去极化速率,并诱发了心动过缓。低钾血症抑制了胺碘酮和丙吡胺的抗心律失常疗效及这些电生理作用。然而,低钾血症对两种药物延长APD90的影响很小。胺碘酮在NK和HK大鼠中均延长了QTc,而丙吡胺仅在NK大鼠中且仅在较高剂量时延长了QTc。得出的结论是,低钾血症降低这两种药物的抗心律失常疗效可能是由于电生理反应改变所致。在该实验模型中,QTc延长本身似乎与抗心律失常作用而非致心律失常作用相关。