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[实践中剂量确定的示例。一种抗心律失常药物的药理学(作者译)]

[Example of dose finding in practice. Pharmacology of an antiarrhythmic agent (author's transl)].

作者信息

Oberdorf A, Raschack M

出版信息

Arzneimittelforschung. 1977 Feb;27(2A):281-3.

PMID:577176
Abstract

Results of the pharmacological investigation of a new antiarrhythmic drug are presented. In the isolated guinea pig ileum the substance of the procainamide-quinidine type reveals strong activity in prolonging the relative refractory period. The safety index as to antiarrhythmic and negative-inotropic properties in relatively high. In the aconitine arrhythmia of the rat the substance is effective after i.v. or oral administration. Furthermore, in these experiments it shows a long-lasting action with these two modes of application. From experimental data in the conscious and anesthetized dog the oral efficacy can also be derived. An oral dose of the new substance for the first application in humans is proposed which refers to its pharmacological activity compared with procainamide and to the human dose of this latter substance.

摘要

本文介绍了一种新型抗心律失常药物的药理学研究结果。在离体豚鼠回肠中,普鲁卡因胺-奎尼丁类型的该物质在延长相对不应期方面显示出强大活性。其抗心律失常和负性肌力特性的安全指数相对较高。在大鼠乌头碱心律失常模型中,该物质经静脉注射或口服给药均有效。此外,在这些实验中,两种给药方式均显示出持久的作用。从清醒和麻醉犬的实验数据中也可得出其口服疗效。根据该新型物质与普鲁卡因胺相比的药理活性以及后者的人体剂量,提出了该新型物质在人体首次应用的口服剂量。

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