Drug intelligence / Profile preview

eslicarbazepine acetate + topiramate

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

Overview

This is a combination of two anticonvulsant (antiepileptic) drugs, eslicarbazepine acetate and topiramate. Both are used primarily in the management of epilepsy, particularly for partial-onset seizures that are not adequately controlled with monotherapy. Eslicarbazepine acetate is a prodrug rapidly converted to eslicarbazepine, which inhibits voltage-gated sodium channels and T-type calcium channels, stabilizing hyperexcitable neuronal membranes and reducing repetitive neuronal firing. Topiramate acts through multiple mechanisms including inhibition of voltage-dependent sodium channels, enhancement of GABAergic activity at GABA-A receptors, antagonism of AMPA/kainate subtype glutamate receptors, and inhibition of carbonic anhydrase isoenzymes. The combination has been studied for pharmacokinetic interactions; co-administration does not significantly alter exposure to eslicarbazepine but may decrease topiramate exposure by about 18%, likely due to reduced bioavailability[1][2][5]. No dose adjustment is generally required when these drugs are used together[1].

02

Targets

CA2 (Carbonic Anhydrase 2)Kainate-type ionotropic glutamate receptorCaV3 (Caveolin-3)AMPAR (AMPA receptor)GABAA (Gamma-aminobutyric acid receptor)NaV (Voltage-gated sodium channels)

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