Verdier Marie-Clémence, Tribut Olivier, Bentué-Ferrer Danièle
CHU Pontchaillou, Laboratoire de Pharmacologie Biologique, Rennes, France.
Therapie. 2012 Mar-Apr;67(2):157-60. doi: 10.2515/therapie/2012014. Epub 2012 Aug 2.
Stiripentol is a third generation antiepileptic, marketed since 2007 under the name of Diacomit(®). It is indicated, always in combination, in the treatment of severe myoclonic epilepsy in infancy or Dravet syndrome. Its pharmacokinetics is not linear. It is a potent inhibitor of CYP3A4, 1A2 and 2C19 and increases the plasma concentrations of many other antiepileptic drugs. Without this being considered as a validated therapeutic range, the trough plasma concentrations at steady-state, corresponding to the usual doses are between 10 and 15 mg/L. The concentration-efficacy relationship is not established, but there is some evidence for a concentration-related toxicity. However, because of its non-linear kinetics, stiripentol should be a good candidate for therapeutic drug monitoring (TDM). Nonetheless, the current level of evidence for the advantage of TDM is "remains to be estimated".
司替戊醇是第三代抗癫痫药物，自2007年以来以Diacomit（®）的名称上市。它总是与其他药物联合使用，用于治疗婴儿严重肌阵挛性癫痫或德雷维特综合征。其药代动力学是非线性的。它是CYP3A4、1A2和2C19的强效抑制剂，并会增加许多其他抗癫痫药物的血浆浓度。在未将其视为有效治疗范围的情况下，对应于常用剂量的稳态谷血浆浓度在10至15毫克/升之间。浓度-疗效关系尚未确立，但有一些证据表明存在与浓度相关的毒性。然而，由于其非线性动力学，司替戊醇应该是治疗药物监测（TDM）的良好候选药物。尽管如此，目前关于TDM优势的证据水平为“有待评估”。
