Rufinamide: Pharmacology, clinical trials, and role in clinical practice.
Rufinamide is a structurally novel compound with anticonvulsant activity that is undergoing evaluation through the European Medicines Agency and the American Food and Drug Administration. Its mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. Absorption of the drug is significantly enhanced in the fed state. The drug is extensively metabolised by non-CYP450 systems with a half-life of 8-12 h. Most common adverse effects noted are somnolence, fatigue and tremor. Efficacy against partial seizures in adults and adolescents has been demonstrated in three randomised, placebo-controlled trials. Efficacy against seizures of Lennox-Gastaut syndrome, a severe, disabling childhood onset epilepsy syndrome, was shown in a single randomised, placebo-controlled trial. Efficacy against partial onset seizures in children has been suggested in an open-label trial. Should rufinamide become commercially available, reserving the drug as a second- or third-line agent should be considered.
Cheng-Hakimian
A
A
Department of Neurology, Regional Epilepsy Center, University of Washington, Seattle, WA 98104, USA.
Anderson
G D
GD
Miller
J W
JW
D000293:Adolescent; D000328:Adult; D000927:Anticonvulsants / Q000009:adverse effects / Q000494:pharmacology*; D002648:Child; D002675:Child, Preschool; D002986:Clinical Trials as Topic; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D014230:Triazoles / Q000009:adverse effects / Q000494:pharmacology*
D000927:Anticonvulsants; D014230:Triazoles; C079703:rufinamide