Grant A O, Hondeghem L M, Katzung B G
J Pharmacol Exp Ther. 1978 Apr;205(1):193-203.
The neuroleptic drug droperidol has been shown to have clinically useful antiarrhythmic activity. Prior reports have resulted in conflicting conclusions regarding actions on ventricular myocardial fibers. The present study was carried out to determine whether droperidol did in fact affect the electrophysiological properties of guinea-pig papillary muscle fibers. By means of microelectrode recordings from preparations mounted in a single sucrose gap, the effects of concentrations from 10(-6) to 4 X 10(-5) M were studied on depolarization-induced automaticity, and on Vmax and its recovery time under several conditions of membrane potential, stimulation rate and external ion concentration. The results showed that at clinically relevant concentrations, droperidol significantly slows ventricular pacemaker activity, a depression reversible by epinephrine. Furthermore, Vmax was decreased and the time constant for Vmax recovery was significantly prolonged under several conditions which pertain to clinical arrhythmias, i.e., reduced membrane potential, elevated extracellular potassium concentrations and increased stimulation rate.
已证明神经安定药氟哌利多具有临床上有用的抗心律失常活性。先前的报告对于其对心室肌纤维的作用得出了相互矛盾的结论。本研究旨在确定氟哌利多是否确实影响豚鼠乳头肌纤维的电生理特性。通过在单个蔗糖间隙中安装的制剂进行微电极记录,研究了浓度从10(-6)到4×10(-5)M对去极化诱导的自律性以及在几种膜电位、刺激速率和外部离子浓度条件下的Vmax及其恢复时间的影响。结果表明,在临床相关浓度下,氟哌利多显著减慢心室起搏器活动,这种抑制作用可被肾上腺素逆转。此外,在与临床心律失常相关的几种条件下,即膜电位降低、细胞外钾浓度升高和刺激速率增加时,Vmax降低且Vmax恢复的时间常数显著延长。