Eslicarbazepine

Products

Eslicarbazepine has been approved in tablet form in the EU since 2009, in the United States since 2013, and in many countries in 2020 (Zebinix, Aptiom).

Structure and properties

Eslicarbazepine (C15H14N2O2, Mr = 254.3 g/mol) is present in drugs in the form of the prodrug eslicarbazepine acetate, which is hydrolyzed in the body after absorption to eslicarbazepine. Eslicarbazepine acetate is acetylated at the hydroxyl group. It exists as a white, odorless, crystalline substance and is sparingly soluble in water. Eslicarbazepine is a carboxamide and dibenzazepine derivative and is closely structurally related to carbamazepine and oxcarbazepine.

Effects

Eslicarbazepine (ATC N03AF04) has antiepileptic properties and prevents seizures and convulsions. The effects are due to blockade of voltage-gated sodium channels, inhibiting neuronal discharges. Eslicarbazepine has a half-life of up to 24 hours.

Indications

For adjunctive treatment of partial epileptic seizures with or without secondary generalization.

Dosage

According to the SmPC. Tablets are taken once daily, independent of meals. Therapy is started gradually.

Contraindications

  • Hypersensitivity
  • AV block

For complete precautions, see the drug label.

Interactions

Eslicarbazepine is an inducer of CYP3A4 and an inhibitor of CYP2C19, and corresponding drug-drug interactions are possible.

Adverse effects

The most common potential adverse effects include dizziness and somnolence.