A Comprehensive Monograph on Oxcarbazepine (DB00776)

1.0 Executive Summary

This report provides a comprehensive analysis of the anticonvulsant medication Oxcarbazepine (DrugBank ID: DB00776), a small molecule drug belonging to the dibenzazepine class. Developed as a second-generation analogue of carbamazepine, Oxcarbazepine was engineered to retain the therapeutic efficacy of its predecessor while offering a significantly improved safety and tolerability profile. Its primary mechanism of action involves the blockade of voltage-gated sodium channels, an effect mediated almost entirely by its active metabolite, the 10-monohydroxy derivative (MHD). This action stabilizes hyperexcited neuronal membranes, thereby reducing the frequency of epileptic seizures.

Clinically, Oxcarbazepine is established as a first- or second-line therapy for partial-onset seizures, with or without secondary generalization, in both adult and pediatric populations. Its pharmacokinetic profile is a key differentiator from carbamazepine; as a prodrug, it undergoes rapid reductive metabolism to MHD, largely bypassing the cytochrome P450 system. This metabolic pathway minimizes the potential for drug-drug interactions, eliminates the issue of autoinduction, and reduces the risk of certain severe adverse events associated with carbamazepine.

Despite its favorable profile, Oxcarbazepine is associated with notable risks, including clinically significant hyponatremia, which necessitates serum sodium monitoring, particularly during the initial phase of treatment. Severe, life-threatening dermatological reactions, such as Stevens-Johnson Syndrome (SJS) and Toxic Epidermal Necrolysis (TEN), can occur, with a markedly increased risk in individuals of Asian descent carrying the HLA-B*1502 genetic allele.