Medical University of Lublin, Department of Pathophysiology, Jaczewskiego 8, 20-090 Lublin, Poland.
Expert Opin Drug Discov. 2008 Apr;3(4):453-60. doi: 10.1517/17460441.3.4.453.
As 20 - 30% of patients are refractory to the presently available antiepileptic drugs, there is a strong need for the development of newer antiepileptics.
A question arises whether stiripentol fulfills the criteria for a promising newer antiepileptic drug.
A literature search, including experimental and clinical studies, with no time limit was performed.
RESULTS/CONCLUSION: Stiripentol represents a group of drugs indirectly enhancing GABA-ergic neurotransmission and it exerts a protective activity in some experimental seizure models, including maximal electroshock (MES)-, pentylenetetrazol-, bicuculline-, strychnine-, and cocaine-induced convulsions. The drug potently inhibits metabolism of other antiepileptic drugs, significantly elevating their plasma and brain concentrations. This requires dosage adjustments of the concomitant antiepileptic drugs used in combination. In the form of an add-on therapy, stiripentol has proved to be effective in partial and atypical absence epilepsies. Considering its particular efficacy against severe myoclonic seizures in infancy (Dravet's syndrome), stiripentol has been awarded an orphan drug status for an adjunctive therapy of this difficult-to-treat condition.
目前可用的抗癫痫药物有 20%-30%的患者对此没有反应,因此强烈需要开发新的抗癫痫药物。
一种疑问是,司替戊醇是否符合有前途的新型抗癫痫药物的标准。
进行了一项文献检索,包括实验和临床研究,没有时间限制。
结果/结论:司替戊醇代表了一组间接增强 GABA 能神经传递的药物,它在一些实验性癫痫模型中具有保护作用,包括最大电休克(MES)、戊四氮、印防己毒素、士的宁和可卡因诱发的惊厥。该药物能强烈抑制其他抗癫痫药物的代谢,显著提高其血浆和脑浓度。这需要调整同时使用的伴随抗癫痫药物的剂量。作为附加治疗,司替戊醇已被证明对部分性和非典型性失神性癫痫有效。鉴于其对婴儿严重肌阵挛性癫痫(Dravet 综合征)的特殊疗效,司替戊醇已被授予孤儿药地位,用于治疗这种难以治疗的疾病的辅助治疗。