Lacosamide is an orally active anticonvulsant that blocks voltage-gated sodium channels (VGSCs) selectively in their inactivated state (IC50 = 16 μM/Nav1.8, 182 μM/Nav1.7, 415 μM/Nav1.3) over resting state by enhancing slow inactivation. In addition to in vivo anticonvulsant activity (ED50 = 4.5 mg/kg in mice via i.p., 3.9 mg/kg in rats via p.o. by maximal electroshock seizure test), lacosamide also shows therapeutic efficacy in various pain models (10-30 mg/kg in rats via i.p.).
Orally active anticonvulsant that blocks voltage-gated sodium channels (VGSCs) selectively in inactivated over resting state by enhancing slow inactivation.