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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Eslicarbazepine acetate is rapidly and extensively biotransformed to its major active metabolite eslicarbazepine by hydrolytic first-pass metabolism. Minor metabolites in plasma are R-licarbazepine and oxcarbazepine, which were shown to be active, and the glucuronic acid conjugates of eslicarbazepine acetate, eslicarbazepine, R-licarbazepine and oxcarbazepine.
Melting point depression for enhanced dissolution rate of eslicarbazepine acetate
Published in Drug Development and Industrial Pharmacy, 2023
Ebtehal M. Dorgham, Gamal M. El Maghraby, Ebtessam A. Essa, Mona F. Arafa
Eslicarbazepine acetate (ESL) is antiepileptic agent which is approved for use as single therapy or in combination with other drugs [1]. However, the drug suffers from poor oral bioavailability and erratic intestinal absorption. This poor oral bioavailability was attributed mainly to its poor solubility and slow dissolution rate [1]. The drug is classified as class II compound according to biopharmaceutical classification system (BCS) with solubility value of less than 1 mg/ml [2]. Accordingly, this drug is challengeable for pharmaceutical formulators to develop oral delivery system with enhanced oral bioavailability. Limited research work was conducted to augment eslicarbazepine acetate dissolution rate and hence its oral bioavailability. The available literature reports utilized solid dispersion technique using hydrophilic polymers as drug carrier [3] and cyclodextrin inclusion complex formation [1].
Eslicarbazepine acetate in epilepsies with focal and secondary generalised seizures: systematic review of current evidence
Published in Expert Review of Clinical Pharmacology, 2018
Laurent M. Willems, Johann Philipp Zöllner, Esther Paule, Susanne Schubert-Bast, Felix Rosenow, Adam Strzelczyk
Eslicarbazepine acetate shows promising results in clinical trials and post-marketing case series.Currently, eslicarbazepine acetate is approved as adjunctive therapy and initial monotherapy in patients suffering from focal epilepsies with and without secondary generalisation.An immediate switch from oxcarbazepine to eslicarbazepine acetate is feasible without titration and might alleviate adverse events.Main adverse events are dizziness and somnolence.Changes in serum sodium levels should be closely monitored.
Initial monotherapy with eslicarbazepine acetate for the management of adult patients with focal epilepsy in clinical practice: a meta-analysis of observational studies
Published in International Journal of Neuroscience, 2023
Silvia Fernández-Anaya, Vicente Villanueva, José M. Serratosa, Fernando Rico-Villademoros, Rosa Rojo, Pilar Sarasa
Eslicarbazepine acetate (ESL) is a ASM of the dibenzazepine carboxamide family that inhibits voltage-gated sodium channels [4]. ESL (Zebinix® in non-US countries, and Aptiom® in the US) was first approved for the adjunctive treatment of adults with partial seizures (currently called focal-onset seizures) and, more recently, as monotherapy for that population. The efficacy of ESL monotherapy in patients with newly diagnosed focal-onset seizures is based on the results of a randomized, double-blind, multicenter study that demonstrated the noninferiority of once-daily ESL compared to twice-daily controlled-release carbamazepine in terms of seizure freedom for the entire 6-month evaluation phase; retention rates were also similar for ESL and controlled-release carbamazepine [5]. Efficacy results with ESL were maintained during a 2-year open-label extension both in patients kept on ESL monotherapy and those who switched from controlled-release carbamazepine to ESL, with a good tolerability and safety profile [6]. Head-to-head comparisons of ESL monotherapy with other second- or third-generation ASMs are lacking; however, the result of a network meta-analysis that included 4 randomized trials comparing levetiracetam, zonisamide, lacosomide and ESL with controlled-release carbamazepine found no differences among the studied drugs in the 6- and 12-month seizure freedom rates [7]. ESL provides some advantages over some other ASMs, such as limited pharmacokinetic and pharmacodynamic interactions, a once-daily administration, and a potentially improved tolerability profile, more specifically regarding psychiatric and metabolic adverse reactions [8,9], that may contribute to enhanced treatment compliance [10].