Tutka Piotr, Barczynski Bartlomiej, Wielosz Marian
Department of Pharmacology and Toxicology, Medical University of Lublin, Jaczewskiego 8, PL-20-090 Lublin, Poland.
Eur J Pharmacol. 2004 Sep 19;499(1-2):117-20. doi: 10.1016/j.ejphar.2004.07.105.
This study demonstrated that bupropion hydrochloride, an effective antidepressant and a commonly used smoking cessation aid, dose-dependently caused clonic convulsions in mice, with the CD50 (convulsive dose50, i.e., the dose producing convulsions in 50% of mice) at 119.7 mg kg(-1). An evaluation for anticonvulsant effects showed that bupropion in the doses of 15-30 mg kg(-1) protected against convulsions induced by maximal electroshock with the ED50 (effective dose50, i.e., the dose protected 50% of mice against convulsions) being 19.4 mg kg(-1). Bupropion had no effect on pentylenetetrazole- and kainic acid-induced convulsions. It is possible that the anticonvulsant activity of bupropion may be exploited for use in the treatment of epilepsy but it requires further investigations.
本研究表明,盐酸安非他酮作为一种有效的抗抑郁药和常用的戒烟辅助药物,在小鼠中可引起剂量依赖性的阵挛性惊厥,其半数惊厥剂量(CD50,即导致50%小鼠惊厥的剂量)为119.7 mg·kg⁻¹。抗惊厥作用评估显示,15 - 30 mg·kg⁻¹剂量的安非他酮可保护小鼠免受最大电休克诱导的惊厥,其半数有效剂量(ED50,即保护50%小鼠免受惊厥的剂量)为19.4 mg·kg⁻¹。安非他酮对戊四氮和 kainic 酸诱导的惊厥无影响。安非他酮的抗惊厥活性有可能被用于癫痫治疗,但这需要进一步研究。