Oxcarbazepine

Products

Oxcarbazepine is available in the form of film-coated tablets, sustained-release tablets, and as a suspension and commercially (Trileptal, Apydan extent). It has been approved in many countries since 1997.

Structure and properties

Oxcarbazepine (C15H12N2O2, Mr = 252.3 g/mol) exists as a white to faint orange crystalline powder and is practically insoluble in water. Oxcarbazepine is the lipophilic 10-keto analog of carbamazepine (Tegretol, generics) and is structurally closely related to it. It is a prodrug and is biotransformed in the body to the active 10-monohydroxymetabolite (MHD).

Effects

Oxcarbazepine (ATC N03AF02) has antiepileptic properties. It protects against seizures and reduces their frequency. Its effects are primarily due to blockade of voltage-sensitive sodium channels, which stabilizes neuronal membranes, inhibits discharges, and slows conduction of synaptic impulses.

Indications

For treatment of partial seizures with or without secondary generalized tonic-clonic seizures and generalized tonic-clonic seizures.

Dosage

According to the SmPC. The drug is taken once twice daily, depending on the dosage form. Discontinuation should be gradual to avoid adverse effects.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Oxcarbazepine and its active metabolite are CYP2C19 inhibitors and, unlike carbamazepine, are only weak inducers of CYP3A. Corresponding drug-drug interactions are possible. Other interactions have been described with oral contraceptives, calcium channel blockers, other antiepileptic drugs, and lithium.

Adverse effects

The most common possible adverse effects include drowsiness, headache, dizziness, visual disturbances (double vision), nausea, vomiting, and feeling weak.