Department of Anesthesiology and Intensive Care, Medical University, Staszica 16, PL 20-081 Lublin, Poland.
Pharmacol Rep. 2011;63(3):690-6. doi: 10.1016/s1734-1140(11)70580-1.
Nefopam is a centrally acting non-opioid analgesic with a mechanism of action that is not completely understood. Adverse effects associated with the therapeutic use and overdose of nefopam are mainly associated with the central nervous system, such as hallucinations, cerebral edema and convulsions. The aim of this study was to assess the effect of nefopam on the electrical threshold and its influence on the protective activity of antiepileptic drugs in the maximal electroshock test in mice. A 5 mg/kg dose of nefopam significantly elevated the electric seizure threshold, while a dose of 1 mg/kg failed to protect mice against electroconvulsion. At a subthreshold dose of 1 mg/kg, nefopam significantly enhanced the anticonvulsant activity of valproate against electroconvulsions. The protective activity of phenobarbital and phenytoin was significantly enhanced by co-administration of nefopam at the 5 mg/kg dose, but this same dose of nefopam failed to affect the protective activity of carbamazepine. In conclusion, nefopam exerts an anticonvulsive effect when given alone and significantly enhances the protective activity of certain antiepileptic agents against electroconvulsions induced in mice.
奈福泮是一种中枢作用的非阿片类镇痛药，其作用机制尚未完全阐明。奈福泮在治疗用途和过量使用时出现的不良反应主要与中枢神经系统有关，如幻觉、脑水肿和惊厥。本研究旨在评估奈福泮对电阈值的影响及其在最大电休克试验中对抗癫痫药物保护活性的影响。奈福泮 5mg/kg 剂量可显著提高电惊厥阈值，而 1mg/kg 剂量不能保护小鼠免受电惊厥。在亚阈值剂量 1mg/kg 时，奈福泮可显著增强丙戊酸钠对电惊厥的抗惊厥活性。奈福泮 5mg/kg 剂量与苯巴比妥和苯妥英合用时，可显著增强其对电惊厥的保护活性，但相同剂量的奈福泮不能影响卡马西平的保护活性。总之，奈福泮单独使用具有抗惊厥作用，并显著增强某些抗癫痫药物对小鼠电惊厥的保护活性。
