Keren G, Tepper D, Butler B, Miura D, Aogaichi K, Somberg J
J Clin Pharmacol. 1984 Oct;24(10):466-72. doi: 10.1002/j.1552-4604.1984.tb01821.x.
The electrophysiologic effects of cibenzoline were studied using programmed electrical stimulation (PES) techniques and were compared to those of quinidine. Cibenzoline, like the conventional class 1 agent quinidine, was effective in preventing arrhythmia induction. Twelve dogs were given 0.02 mg/kg digoxin intravenously for seven days to achieve a steady-state digoxin level. On the eighth day, cibenzoline was administered in incremental doses (0.5 to 10.5 mg/kg) and PES was performed at 30-minute intervals. A mean dose of 2.6 +/- 0.8 mg/kg cibenzoline prevented ventricular tachycardia induction. At this dose, cibenzoline had no significant effect on mean arterial blood pressure, but PR interval increased by 17 +/- 9 per cent, QRS duration by 27 +/- 14 per cent, and the ventricular refractory period (ERP) for the first extra stimulus increased by 35 +/- 9 per cent. A gradual decrease in heart rate and an increase in PR interval and QRS duration was caused by incremental doses of cibenzoline. In six additional animals, quinidine was administered in incremental doses (1 to 30 mg/kg) and PES performed at 30-minute intervals. A mean of 15 +/- 5 mg/kg prevented induction of ventricular tachycardia in five animals. No significant change in heart rate, PR, QRS, and ERP was found at the effective dose.
采用程控电刺激（PES）技术研究了西苯唑啉的电生理效应，并与奎尼丁进行了比较。西苯唑啉与传统的Ⅰ类药物奎尼丁一样，能有效预防心律失常的诱发。给12只犬静脉注射0.02mg/kg地高辛，连续7天以达到地高辛稳态血药浓度。在第8天，递增剂量（0.5至10.5mg/kg）给予西苯唑啉，并每隔30分钟进行一次PES。平均剂量2.6±0.8mg/kg的西苯唑啉可预防室性心动过速的诱发。在此剂量下，西苯唑啉对平均动脉血压无显著影响，但PR间期增加了17±9%，QRS时限增加了27±14%，第一个额外刺激的心室不应期（ERP）增加了35±9%。递增剂量的西苯唑啉可导致心率逐渐下降，PR间期和QRS时限增加。在另外6只动物中，递增剂量（1至30mg/kg）给予奎尼丁，并每隔30分钟进行一次PES。平均15±5mg/kg可预防5只动物诱发室性心动过速。在有效剂量下，未发现心率、PR、QRS和ERP有显著变化。
