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Mechanisms of Action of Carbamazepine and Its Derivatives, Oxcarbazepine, BIA 2-093, and BIA 2-024

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Abstract

Carbamazepine (CBZ) has been extensively used in the treatment of epilepsy, as well as in the treatment of neuropathic pain and affective disorders. However, the mechanisms of action of this drug are not completely elucidated and are still a matter of debate. Since CBZ is not very effective in some epileptic patients and may cause several adverse effects, several antiepileptic drugs have been developed by structural variation of CBZ, such as oxcarbazepine (OXC), which is used in the treatment of epilepsy since 1990. (S)-(−)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (BIA 2-093) and 10,11-dihydro-10-hydroxyimino-5H-dibenz[b,f]azepine-5-carboxamide (BIA 2-024), which were recently developed by BIAL, are new putative antiepileptic drugs, with some improved properties. In this review, we will focus on the mechanisms of action of CBZ and its derivatives, OXC, BIA 2-093 and BIA 2-024. The available data indicate that the anticonvulsant efficacy of these AEDs is mainly due to the inhibition of sodium channel activity.

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Authors and Affiliations

  1. Department of Cell Biology, Center for Neuroscience of Coimbra, Department of Zoology, University of Coimbra, 3004-517, Coimbra

    António F. Ambrósio, Caetana M. Carvalho & Arsélio P. Carvalho

  2. Department of Research & Development, Bial, 4745-457, S. Mamede do Coronado, Portugal

    Patrício Soares-da-Silva

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  1. António F. Ambrósio
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  2. Patrício Soares-da-Silva
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  3. Caetana M. Carvalho
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  4. Arsélio P. Carvalho
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Ambrósio, A.F., Soares-da-Silva, P., Carvalho, C.M. et al. Mechanisms of Action of Carbamazepine and Its Derivatives, Oxcarbazepine, BIA 2-093, and BIA 2-024. Neurochem Res 27, 121–130 (2002). https://doi.org/10.1023/A:1014814924965

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