Browne T R, Feldman R G, Buchanan R A, Allen N C, Fawcett-Vickers L, Szabo G K, Mattson G F, Norman S E, Greenblatt D J
Neurology. 1983 Apr;33(4):414-8. doi: 10.1212/wnl.33.4.414.
Methsuximide (MSM; Celontin) was administered for 8 weeks to 26 patients with complex partial seizures (CPS) refractory to phenytoin and carbamazepine and phenobarbital or primidone. A 50% or greater reduction in CPS frequency was obtained in eight patients. MSM therapy was continued chronically in these eight patients, and five continued to have a 50% or greater reduction in CPS frequency after 3 to 34 months of follow-up. Drowsiness, gastrointestinal disturbance, hiccups, irritability, and headache were the common side effects of MSM. No serious toxicity occurred. N-desmethylmethsuximide was the principal substance detected in plasma and had the following pharmacokinetic values: accumulation half-life, 49.7 hours; time to steady state, 10.4 days; elimination half-life, 72.2 hours; therapeutic range of plasma concentration, 10 to 30 mg per liter. Plasma concentrations of phenytoin and phenobarbital derived from primidone rose significantly (p less than 0.05) after addition of MSM.
对26例对苯妥英、卡马西平、苯巴比妥或扑米酮治疗无效的复杂部分性发作（CPS）患者给予甲琥胺（MSM；赛伦丁）治疗8周。8例患者的CPS发作频率降低了50%或更多。这8例患者继续长期接受MSM治疗，其中5例在随访3至34个月后CPS发作频率持续降低50%或更多。嗜睡、胃肠道不适、呃逆、易怒和头痛是MSM的常见副作用。未发生严重毒性反应。N-去甲基甲琥胺是血浆中检测到的主要物质，其药代动力学值如下：蓄积半衰期49.7小时；达到稳态时间10.4天；消除半衰期72.2小时；血浆浓度治疗范围为每升10至30毫克。添加MSM后，由扑米酮转化而来的苯妥英和苯巴比妥的血浆浓度显著升高（p<0.05）。
