Kocsis Pál, Tarnawa István, Kovács Gyula, Szombathelyi Zsolt, Farkas Sándor
Richter Gedeon Rt., Budapest.
Acta Pharm Hung. 2002;72(1):49-61.
Since its introduction in 1959 tolperisone hydrochloride (Mydeton) is still one of the leading products of Gedeon Richter Ltd. It has been successfully applied for treating different painful muscle spasms. The compound is successfully marketed also by several foreign, mostly Japanese, pharmaceutical companies, as a central muscle relaxant agent. The present summary overviews the pharmacology of tolperisone, with special emphasize on its still partly understood way of action. Data from the scientific literature as well as our own experimental results strongly support the hypothesis that inhibition of voltage gated sodium channels is a major component of the mechanism of action of tolperisone. The paper also summarizes the clinical results with tolperisone and the perspectives of the therapeutic use of centrally acting muscle relaxants.
自1959年引入以来,盐酸托哌酮(Mydeton)仍是吉德昂·里奇特有限公司的主导产品之一。它已成功应用于治疗各种疼痛性肌肉痉挛。该化合物还被几家外国制药公司,主要是日本的制药公司成功地作为中枢性肌肉松弛剂推向市场。本综述概述了托哌酮的药理学,特别强调了其作用方式仍部分未明的情况。科学文献数据以及我们自己的实验结果有力地支持了这样一种假说,即抑制电压门控钠通道是托哌酮作用机制的主要组成部分。本文还总结了托哌酮的临床结果以及中枢性肌肉松弛剂治疗应用的前景。