Eslicarbazepine: A Comprehensive Monograph on its Pharmacology, Clinical Application, and Safety Profile

1.0 Executive Summary

Eslicarbazepine is a third-generation antiepileptic drug (AED) belonging to the dibenzazepine carboxamide class, representing a significant pharmacological refinement of its predecessors, carbamazepine and oxcarbazepine.[1] It is indicated for the treatment of partial-onset seizures, both as monotherapy and as an adjunctive therapy, in adults and children aged four years and older.[4] The therapeutic rationale for Eslicarbazepine is rooted in its unique mechanism of action and favorable pharmacokinetic profile. Its primary pharmacodynamic effect is the stabilization of the inactive state of voltage-gated sodium channels (VGSCs), with a notable and selective affinity for the slow-inactivated state.[6] This state-dependent action allows for targeted inhibition of the rapid, repetitive neuronal firing characteristic of an epileptic focus, while minimizing interference with normal physiological neuronal activity, potentially contributing to its efficacy and tolerability.

Clinically, Eslicarbazepine is administered as a prodrug, eslicarbazepine acetate, which undergoes rapid and extensive first-pass hydrolysis to its single active metabolite, eslicarbazepine, also known as S-licarbazepine.[2] This metabolic pathway is a key advantage, as it avoids the formation of the potentially toxic epoxide metabolites associated with carbamazepine and the racemic mixture of active metabolites produced by oxcarbazepine.[2] The resulting pharmacokinetic profile is predictable and linear, with a long elimination half-life that supports a convenient once-daily dosing regimen, a factor that can significantly enhance patient adherence in the long-term management of epilepsy.[10]