[新型复方抗心律失常制剂美他西嗪的药理学]

[The pharmacology of the new combined anti-arrhythmia preparation metatsizin].

作者信息

Kaverina N V, Chichkanov G G, Bugriĭ E M, Vititnova M B, Tolmacheva E A, Turilova A I, Kryzhanovskiĭ S A, Lyskovtsev V V, Rodionov A P, Beloborodov V L

机构信息

Laboratory of Blood Circulation Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia.

出版信息

Eksp Klin Farmakol. 1998 Mar-Apr;61(2):33-6.

PMID:9621171

Abstract

The combined antiarrhythmic effect of ethmosin and ethacisin in various dose ratios was studied in conscious dogs with two-stage ligation of the coronary artery (after Harris). A 6:1 ratio was found to be optimal for manifestation of the antiarrhythmic effect. In such a ratio of the doses the antiarrhythmic effect of a combination of ethmosin and ethacisin is essentially higher than the activity of each component. On the grounds of these data a combined antiarrhythmic drug methacisin was developed. It possesses a broad spectrum of antiarrhythmic activity. The drug is effective on models of arrhythmias specific of class I, III, and IV antiarrhythmics. Metacisin does not change hemodynamics and activity of the heart. Study of metacisin pharmacokinetics showed that it possesses bioavailability twice that of ethmosin tablets taken separately and four times that of ethasicin.

摘要

在冠状动脉两阶段结扎的清醒犬（按照哈里斯方法）中，研究了不同剂量比的乙吗噻嗪和乙卡噻嗪的联合抗心律失常作用。发现6:1的比例对于抗心律失常作用的表现最为理想。在此剂量比下，乙吗噻嗪和乙卡噻嗪组合的抗心律失常作用实质上高于各组分的活性。基于这些数据，研发了一种联合抗心律失常药物甲卡噻嗪。它具有广泛的抗心律失常活性。该药物在I类、III类和IV类抗心律失常药物特有的心律失常模型上有效。甲卡噻嗪不改变血流动力学和心脏活性。甲卡噻嗪的药代动力学研究表明，其生物利用度是单独服用乙吗噻嗪片的两倍，是乙卡噻嗪的四倍。