Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy

Renato Tambucci,1 Claudia Basti,1 Maria Maresca,1 Giangennaro Coppola,2 Alberto Verrotti11Department of Pediatrics, University of L’Aquila, L’Aquila, Italy; 2Child and Adolescent Neuropsychiatry Unit, University of Salerno, Salerno, ItalyAbstract: Eslicarbazepine acetate...

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Main Authors: Tambucci R, Basti C, Maresca M, Coppola G, Verrotti A
Format: Article
Language:English
Published: Dove Medical Press 2016-05-01
Series:Neuropsychiatric Disease and Treatment
Subjects:
Online Access:https://www.dovepress.com/update-on-the-role-of-eslicarbazepine-acetate-in-the-treatment-of-part-peer-reviewed-article-NDT
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spelling doaj-15e3e34c47e24dbfaef04045081c49bc2020-11-25T01:16:09ZengDove Medical PressNeuropsychiatric Disease and Treatment1178-20212016-05-012016Issue 11251126027076Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsyTambucci RBasti CMaresca MCoppola GVerrotti ARenato Tambucci,1 Claudia Basti,1 Maria Maresca,1 Giangennaro Coppola,2 Alberto Verrotti11Department of Pediatrics, University of L’Aquila, L’Aquila, Italy; 2Child and Adolescent Neuropsychiatry Unit, University of Salerno, Salerno, ItalyAbstract: Eslicarbazepine acetate (ESL) is a once daily new third generation antiepileptic drug that shares the basic chemical structure of carbamazepine and oxcarbazepine – a dibenzazepine nucleus with the 5-carboxamide substituent, but is structurally different at the 10,11-position. ESL is a pro-drug metabolized to its major active metabolite eslicarbazepine. Despite the fact that the exact mechanism of action has not been fully elucidated, it is thought to involve inhibition of voltage-gated sodium channels (VGSC). ESL inhibits sodium currents in a voltage-dependent way by an interaction predominantly with the inactivated state of the VGSC, thus selectively reducing the activity of rapidly firing (epileptic) neurons. ESL reduces VGSC availability through enhancement of slow inactivation. In Phase III studies, adjunctive therapy with ESL 800 or 1,200 mg/day leads to a significant decrease in the seizure frequency in adults with refractory partial onset epilepsy. Based on these results, ESL has been approved in Europe (by the European Medicines Agency) and in the United States (by the US Food and Drug Administration) as add-on therapy. Data on efficacy and safety have been confirmed by 1-year extension and real life observational studies. Recently, based on results from two randomized, double-blind, historical control Phase III trials, ESL received US Food and Drug Administration approval also as a monotherapy for patients with partial onset epilepsy. In the pediatric setting, encouraging results have been obtained suggesting its potential role in the management of epileptic children. Overall ESL was generally well tolerated. The most common adverse events were dizziness, somnolence, headache, nausea, diplopia, and vomiting. Adverse events can be minimized by appropriate titration. In conclusion, ESL seems to overcome some drawbacks of the previous antiepileptic drugs, suggesting a major role of ESL in the management of focal onset epilepsy for both new onset and refractory cases, either as monotherapy or as adjunctive treatment.Keywords: eslicarbazepine, partial-onset epilepsy, antiepileptic drugs, refractory epilepsyhttps://www.dovepress.com/update-on-the-role-of-eslicarbazepine-acetate-in-the-treatment-of-part-peer-reviewed-article-NDTEslicarbazepinepartial-onset epilepsyantiepileptic drugsrefractory epilepsy.
collection DOAJ
language English
format Article
sources DOAJ
author Tambucci R
Basti C
Maresca M
Coppola G
Verrotti A
spellingShingle Tambucci R
Basti C
Maresca M
Coppola G
Verrotti A
Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
Neuropsychiatric Disease and Treatment
Eslicarbazepine
partial-onset epilepsy
antiepileptic drugs
refractory epilepsy.
author_facet Tambucci R
Basti C
Maresca M
Coppola G
Verrotti A
author_sort Tambucci R
title Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
title_short Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
title_full Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
title_fullStr Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
title_full_unstemmed Update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
title_sort update on the role of eslicarbazepine acetate in the treatment of partial-onset epilepsy
publisher Dove Medical Press
series Neuropsychiatric Disease and Treatment
issn 1178-2021
publishDate 2016-05-01
description Renato Tambucci,1 Claudia Basti,1 Maria Maresca,1 Giangennaro Coppola,2 Alberto Verrotti11Department of Pediatrics, University of L’Aquila, L’Aquila, Italy; 2Child and Adolescent Neuropsychiatry Unit, University of Salerno, Salerno, ItalyAbstract: Eslicarbazepine acetate (ESL) is a once daily new third generation antiepileptic drug that shares the basic chemical structure of carbamazepine and oxcarbazepine – a dibenzazepine nucleus with the 5-carboxamide substituent, but is structurally different at the 10,11-position. ESL is a pro-drug metabolized to its major active metabolite eslicarbazepine. Despite the fact that the exact mechanism of action has not been fully elucidated, it is thought to involve inhibition of voltage-gated sodium channels (VGSC). ESL inhibits sodium currents in a voltage-dependent way by an interaction predominantly with the inactivated state of the VGSC, thus selectively reducing the activity of rapidly firing (epileptic) neurons. ESL reduces VGSC availability through enhancement of slow inactivation. In Phase III studies, adjunctive therapy with ESL 800 or 1,200 mg/day leads to a significant decrease in the seizure frequency in adults with refractory partial onset epilepsy. Based on these results, ESL has been approved in Europe (by the European Medicines Agency) and in the United States (by the US Food and Drug Administration) as add-on therapy. Data on efficacy and safety have been confirmed by 1-year extension and real life observational studies. Recently, based on results from two randomized, double-blind, historical control Phase III trials, ESL received US Food and Drug Administration approval also as a monotherapy for patients with partial onset epilepsy. In the pediatric setting, encouraging results have been obtained suggesting its potential role in the management of epileptic children. Overall ESL was generally well tolerated. The most common adverse events were dizziness, somnolence, headache, nausea, diplopia, and vomiting. Adverse events can be minimized by appropriate titration. In conclusion, ESL seems to overcome some drawbacks of the previous antiepileptic drugs, suggesting a major role of ESL in the management of focal onset epilepsy for both new onset and refractory cases, either as monotherapy or as adjunctive treatment.Keywords: eslicarbazepine, partial-onset epilepsy, antiepileptic drugs, refractory epilepsy
topic Eslicarbazepine
partial-onset epilepsy
antiepileptic drugs
refractory epilepsy.
url https://www.dovepress.com/update-on-the-role-of-eslicarbazepine-acetate-in-the-treatment-of-part-peer-reviewed-article-NDT
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