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新型Ⅰ类抗心律失常药物AN-132对比格犬室性心律失常的抗心律失常作用

Antiarrhythmic effect of a new class 1 antiarrhythmic drug, AN-132, on ventricular arrhythmias in beagles.

作者信息

Hashimoto K, Watanabe K, Mitsuhashi H

机构信息

Department of Pharmacology, Yamanashi Medical College, Tamaho-cho, Japan.

出版信息

Cardiovasc Drugs Ther. 1989 Oct;3(5):683-9. doi: 10.1007/BF01857620.

Abstract

Using two-stage coronary-ligation-, digitalis- and adrenaline-induced ventricular arrhythmias in beagles, antiarrhythmic effects of AN-132 were examined, and the minimum effective plasma concentration for each arrhythmia model was determined. AN-132 suppressed all the arrhythmias, and the minimum effective plasma concentrations for arrhythmias induced by 24-hour coronary ligation, 48-hour coronary ligation, digitalis, and adrenaline were 3.4-4.6, 1.5-2.3, 0.83, and 9.3 micrograms/ml, respectively. The concentration for adrenaline-induced arrhythmia was significantly higher than that of 24-hour coronary ligation arrhythmia, and it was also higher than that of digitalis arrhythmia. This pharmacologic profile is similar to those of pirmenol and mexiletine. Since AN-132 had no deleterious effects on the hemodynamics and the central nervous system, it may become a clinically useful antiarrhythmic drug.

摘要

在比格犬身上利用两阶段冠状动脉结扎、洋地黄和肾上腺素诱发的室性心律失常,研究了AN-132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。AN-132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3.4 - 4.6、1.5 - 2.3、0.83和9.3微克/毫升。肾上腺素诱发心律失常的浓度显著高于24小时冠状动脉结扎诱发心律失常的浓度,也高于洋地黄诱发心律失常的浓度。这种药理学特征与吡美诺和美西律相似。由于AN-132对血流动力学和中枢神经系统没有有害影响,它可能成为一种临床上有用的抗心律失常药物。

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