Eslicarbazepine Acetate

Eslicarbazepine acetate is a sodium channel blocker (IC₅₀ = 138 nM in a radioligand binding assay).¹ It inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes at concentrations ranging from 30-300 μM. In vivo, oral and i.p. administration of eslicarbazepine acetate is protective against seizures induced by maximal electroshock (MES) in mice with ED₅₀ values of 4.7 and 6.3 mg/kg, respectively, which are well below the median toxic dose (TD₅₀) values of 358.7 and 78.6 mg/kg for oral and i.p. administration respectively. High-dose administration (30 mg/kg) of eslicarbazepine acetate prevents picrotoxin-induced seizures in rats.² Low-dose administration (10 mg/kg) does not suppress picrotoxin-induced seizures, however, it reduces seizure number and duration. Formulations containing eslicarbazepine acetate have been used for the treatment of partial-onset seizures.³

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1. Benes, J., Parada, A., Figueiredo, A.A., et al. Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. J. Med. Chem. 42(14), 2582-2587 (1999).

2. Sierra-Paredes, G., Núñez-Rodriguez, A., Vázquez-López, A., et al. Anticonvulsant effect of eslicarbazepine acetate (BIA 2-093) on seizures induced by microperfusion of picrotoxin in the hippocampus of freely moving rats. Epilepsy Res. 72(2-3), 140-146 (2006).

3. Toledano, R., Jovel, C.E., Jiménez-Huete, A., et al. Efficacy and safety of eslicarbazepine acetate monotherapy for partial-onset seizures: Experience from a multicenter, observational study. Epilepsy Behav. 73, 173-179 (2017).