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克拉维坦(M-71)的药理特性。

Pharmacological properties of Craviten (M-71).

作者信息

Maj J, Kulig D, Myśliwiec D, Bugielska Z, Tomsa E, Zaczyńska-Kostrakiewicz M

出版信息

Pol J Pharmacol Pharm. 1980 Nov-Dec;32(6):855-75.

PMID:7243682
Abstract

The preparation Craviten (M-71) produced by POLFA Pharmaceutical Works in Cracow (2S, 2'S) N, N'-dimethyl-N, N'-bis-[1-(3',4',5'-trimethoxybenzoyloxy)-butyl]-2-ethylenediamine dihydrochloride) prevents and abolishes heart rhythm disturbance induced in the rat with BaCl2, CaCl2, adrenaline or aconitine. The doses effectively preventing arrhythmia development were in the range from 0.035 to 0.175 mg/kg. They are many times lower than the doses of lidocaine, hexobendine, procaine amide and D,L-propranolol producing a similar effect. Craviten has a much more favourable therapeutic index than these antiarrhythmic agents. Craviten causes sinus bradycardia and slows down myocardial conduction. It exerts a spasmolytic effect about 70 times as strong as papaverine. It has no influence on the central nervous system, on urine excretion, and after topical application it has no irritating or local anaesthetic effect. The 2R, 2'R isomer of Craviten has a similar profile of pharmacological action but its antiarrhythmic and spasmolytic effects are many times weaker.

摘要

克拉维亭(M - 71)由克拉科夫的POLFA制药厂生产,其化学成分为(2S,2'S)N,N'-二甲基 - N,N'-双 - [1 - (3',4',5'-三甲氧基苯甲酰氧基)-丁基]-2-乙二胺二盐酸盐,可预防和消除由氯化钡、氯化钙、肾上腺素或乌头碱诱发的大鼠心律失常。有效预防心律失常发生的剂量范围为0.035至0.175毫克/千克。这些剂量比产生类似效果的利多卡因、己氧苯啶、普鲁卡因酰胺和D,L - 普萘洛尔的剂量低很多倍。克拉维亭的治疗指数比这些抗心律失常药物更有利。克拉维亭可引起窦性心动过缓并减慢心肌传导。其解痉作用比罂粟碱强约70倍。它对中枢神经系统、尿液排泄无影响,局部应用后无刺激或局部麻醉作用。克拉维亭的2R,2'R异构体具有相似的药理作用,但抗心律失常和解痉作用要弱很多倍。

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