title: [Therapeutic drug monitoring of rufinamide].
abstract: Rufinamide is a third-generation antiepileptic           drug, available since early 2010 in France. It is indicated in combination           therapy in the Lennox-Gastaut syndrome from the age of 4. It has           orphan drug status. The bioavailability of rufinamide is high, but           decreases with the dose and increases with food intake. Rufinamide           is not metabolized by cytochromes but hydrolyzed by a carboxylesterase in           an inactive carboxylic derivative. Elimination is mainly renal.           The half-life varies from 6 to 10h. Although established from relatively           few studies, exposure efficacy and exposure toxicity relationships are           argued. A plasma concentration of 15 mg/L, obtained with a standard           regimen, reduces the number of seizures of 25%. Few factors of intrinsic variability           are described. There are few clinically significant pharmacokinetic           interactions and they concern combinations with other antiepileptic           drugs, especially valproate. Although there is no validated therapeutic           range, the level of evidence for this therapeutic drug monitoring           has been estimated at "possibly useful".
authors: CHU Pontchaillou, Laboratoire de Pharmacologie Biologique Rennes France. dbentueferrer@gmail.com
authors: Danièle
authors: D
authors: Bentué-Ferrer
authors: Olivier
authors: O
authors: Tribut
authors: Marie-Clémence
authors: MC
authors: Verdier
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; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D016903:Drug Monitoring; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism; D008107:Liver Diseases / Q000378:metabolism; D014230:Triazoles / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics / Q000627:therapeutic use*
chemical_list: D000927:Anticonvulsants; D014230:Triazoles; C079703:rufinamide