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eslicarbazepine acetate + ethinylestradiol + levonorgestrel

Development stage
Unknown
Lead developer
Bial
Modality
Small Molecules
Administration
Oral
01

Overview

This entry refers to the co-administration of eslicarbazepine acetate (BIA 2-093) and a combined oral contraceptive (COC) containing ethinylestradiol and levonorgestrel. Eslicarbazepine acetate is a small molecule voltage-gated sodium channel blocker developed by Bial - Portela C S.A. for the treatment of partial-onset seizures in patients with epilepsy. It acts by stabilizing the inactivated state of voltage-gated sodium channels, thereby preventing repetitive neuronal firing. The combination was evaluated in clinical trials (such as NCT00898560) to assess the impact of eslicarbazepine acetate on the pharmacokinetics of hormonal contraceptives. Eslicarbazepine acetate is a weak inducer of the CYP3A4 enzyme, which can lead to increased metabolism and reduced plasma concentrations of ethinylestradiol and levonorgestrel, potentially compromising contraceptive efficacy in women with epilepsy.

Brand names
AptiomZebinixMicroginon
Other names
eslicarbazepine acetateethinylestradiollevonorgestrelcombined oral contraceptive
02

Targets

CaV3 (Caveolin-3)PR (Progesterone receptor)ER (Estrogen receptor)NaV (Voltage-gated sodium channels)

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