Hashimoto K, Watanabe K, Sugiyama A
Department of Pharmacology, Yamanashi Medical College, Japan.
Jpn J Pharmacol. 1988 Oct;48(2):273-82. doi: 10.1254/jjp.48.273.
Using two-stage coronary ligation-, digitalis- and adrenaline-induced canine ventricular arrhythmias, antiarrhythmic effects of pirmenol were examined, and the minimum effective plasma concentration for each arrhythmia model was determined. Pirmenol suppressed all the arrhythmias, and the minimum effective plasma concentrations for arrhythmias induced by 24 hr coronary ligation, 48 hr coronary ligation, digitalis and adrenaline were 1.1 +/- 0.3 (by 3 mg/kg, i.v.), 1.1 +/- 0.3 (by 3 mg/kg, i.v.), 1.1 +/- 0.2 (by 3 mg/kg, i.v.) and 2.5 +/- 1.5 (by 3 mg/kg, i.v.) microgram/ml, respectively (mean +/- S.D.M., 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, tocainide and cibenzoline. Since pirmenol had no deleterious effects on the blood pressure and sinus node activity, 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,研究了吡美诺的抗心律失常作用,并确定了每种心律失常模型的最低有效血浆浓度。吡美诺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1.1±0.3(静脉注射3mg/kg)、1.1±0.3(静脉注射3mg/kg)、1.1±0.2(静脉注射3mg/kg)和2.5±1.5(静脉注射3mg/kg)微克/毫升(平均值±标准差,n = 6 - 7)。肾上腺素诱发的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、妥卡尼和西苯唑啉相似。由于吡美诺对血压和窦房结活动没有有害影响,因此预期其具有临床应用价值。