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[乙胺噻嗪:药理特性及临床应用前景]

[Ethacizin: pharmacologic properties and prospects for clinical application].

作者信息

Kaverina N V, Lyskovtsev V V, Senova Z P, Grigor'eva E K

出版信息

Kardiologiia. 1984 May;24(5):52-7.

PMID:6748472
Abstract

The study of the regularities between the chemical structure and pharmacologic action of phenathiazine dialkylaminoacyl derivatives led to the identification and investigation of a new drug called ethacizine-phenothiazin-2-carbethoxyamino-10 (beta-diethylamino-propionyl) hydrochloride. Ethacizine exceeds its structural analogue ethmozin by two times in terms of intensity and by 4-5 times in terms of the duration of antiarrhythmic effect. Ethacizine has marked antianginal properties. It shows a prolonged inhibitory effect on the average elevation of the ST interval at multiple leads of the epicardial electrogram during coronary occlusion, increases the threshold of myocardial ischemia development, and reduces the size of experimental infarction. The combination of potent antiarrhythmic activity, already confirmed by clinical observations, with antianginal properties and a capacity to limit the size of infarction makes in possible to consider ethacizine a promising means for treating coronary heart disease.

摘要

对吩噻嗪二烷基氨基酰基衍生物的化学结构与药理作用之间规律的研究,促成了一种名为盐酸乙卡嗪 - 吩噻嗪 - 2 - 乙氧羰基氨基 - 10(β - 二乙氨基丙酰基)的新药的鉴定与研究。就抗心律失常作用的强度而言,乙卡嗪比其结构类似物乙吗噻嗪强两倍,就作用持续时间而言则强4至5倍。乙卡嗪具有显著的抗心绞痛特性。在冠状动脉闭塞期间,它对心外膜心电图多导联ST段平均抬高具有延长的抑制作用,提高心肌缺血发展的阈值,并减小实验性梗死的面积。临床观察已证实的强效抗心律失常活性,与抗心绞痛特性以及限制梗死面积的能力相结合,使得乙卡嗪有可能被视为治疗冠心病的一种有前景的手段。

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