title: [Therapeutic drug monitoring of stiripentol].
abstract: 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".
authors: CHU Pontchaillou, Laboratoire de Pharmacologie Biologique, Rennes, France.
authors: Marie-Clémence
authors: MC
authors: Verdier
authors: Olivier
authors: O
authors: Tribut
authors: Danièle
authors: D
authors: Bentué-Ferrer
mesh_terms: D000375:Aging / Q000378:metabolism; D000927:Anticonvulsants / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002851:Chromatography, High Pressure Liquid; D016638:Critical Illness; D004148:Dioxolanes / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D016903:Drug Monitoring; D004831:Epilepsies, Myoclonic / Q000188:drug therapy; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism; D008107:Liver Diseases / Q000378:metabolism
chemical_list: D000927:Anticonvulsants; D004148:Dioxolanes; C021092:stiripentol