Hashimoto K, Akiyama K, Mitsuhashi H
J Cardiovasc Pharmacol. 1987 Feb;9(2):148-53. doi: 10.1097/00005344-198702000-00004.
Using two-stage coronary ligation-, digitalis-, and adrenaline-induced canine ventricular arrhythmias, antiarrhythmic effects of cibenzoline were examined and the minimum effective plasma concentration for each arrhythmia model was determined. Cibenzoline suppressed all the arrhythmias, and the minimum effective plasma concentrations for arrhythmias induced by 24-h coronary ligation, 48-h coronary ligation, digitalis, and adrenaline were 1.9 +/- 0.9 (by 8 mg/kg i.v.), 1.6 +/- 0.5 (by 8 mg/kg i.v.), 0.6 +/- 0.2 (by 2 mg/kg i.v.), and 3.5 +/- 1.3 (by 5 mg/kg i.v.) micrograms/ml, respectively (mean +/- SDM, n = 6-7). The concentration for adrenaline-induced arrhythmia was significantly higher than those for the other types of arrhythmias. This pharmacological profile is similar to those of mexiletine and tocainide, and all three drugs have central nervous system (CNS) stimulant action. Because cibenzoline had only weak hypotensive and sinus node depressive effects and was found to be orally active when given to coronary ligation arrhythmia dogs, its clinical usefulness is expected.
利用两阶段冠状动脉结扎、洋地黄和肾上腺素诱发的犬室性心律失常,研究了西苯唑啉的抗心律失常作用,并确定了每种心律失常模型的最低有效血浆浓度。西苯唑啉抑制了所有心律失常,24小时冠状动脉结扎、48小时冠状动脉结扎、洋地黄和肾上腺素诱发的心律失常的最低有效血浆浓度分别为1.9±0.9(静脉注射8mg/kg)、1.6±0.5(静脉注射8mg/kg)、0.6±0.2(静脉注射2mg/kg)和3.5±1.3(静脉注射5mg/kg)μg/ml(平均值±标准差,n=6-7)。肾上腺素诱发心律失常的浓度显著高于其他类型的心律失常。这种药理学特征与美西律和妥卡尼相似,这三种药物都有中枢神经系统(CNS)兴奋作用。由于西苯唑啉只有微弱的降压和窦房结抑制作用,并且在给予冠状动脉结扎性心律失常犬时发现其口服有效,因此预期其具有临床应用价值。