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Cenobamate - Antiepileptic Drug for Focal Seizures

Cenobamate is an antiepileptic drug used to treat focal seizures in adults. It acts on sodium channels and GABA-A receptors in the brain.

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Things worth knowing about "Cenobamate"

Cenobamate is an antiepileptic drug used to treat focal seizures in adults. It acts on sodium channels and GABA-A receptors in the brain.

What is Cenobamate?

Cenobamate is a prescription antiepileptic drug (AED) approved for the treatment of focal (partial) seizures in adults. It is marketed under the brand name Xcopri in the United States and Ontozry in Europe. Cenobamate is indicated as add-on therapy for patients whose seizures have not been adequately controlled by other antiepileptic medications.

Indication

Cenobamate is approved for:

Focal seizures with or without secondary generalization in adults
Drug-resistant epilepsy, meaning cases where at least two prior antiepileptic treatments have failed to provide sufficient seizure control

Mechanism of Action

Cenobamate works through two distinct mechanisms simultaneously, which distinguishes it from many other antiepileptic drugs:

Sodium channel blockade: Cenobamate inhibits voltage-gated sodium channels in the brain, particularly the persistent sodium current. This reduces the excessive electrical activity in neurons that triggers epileptic seizures.
GABA-A receptor modulation: Cenobamate enhances the activity of GABA (gamma-aminobutyric acid), the brain's primary inhibitory neurotransmitter, by binding to a specific site on the GABA-A receptor. This increases neuronal inhibition and reduces seizure activity.

This dual mechanism of action may explain why cenobamate can be effective even in patients with treatment-resistant epilepsy.

Dosage and Administration

Cenobamate is taken orally as a tablet. The dose is titrated gradually to reduce the risk of adverse reactions:

Starting dose: 12.5 mg once daily for 2 weeks
Dose increases every 2 weeks: 25 mg, then 50 mg, then 100 mg
Maintenance dose: typically 200 mg once daily; up to 400 mg once daily depending on tolerability and response

The slow titration schedule is critical to minimize the risk of serious adverse effects, particularly Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS syndrome).

Side Effects

Common side effects of cenobamate include:

Dizziness and coordination problems
Fatigue and somnolence
Headache
Diplopia (double vision) or blurred vision
Nausea

Rare but serious adverse effects include:

DRESS syndrome: A potentially life-threatening hypersensitivity reaction characterized by skin rash, fever, and organ involvement. The risk is significantly reduced by slow dose titration.
QT interval shortening on ECG (cardiac rhythm changes)
Elevated liver enzymes

Drug Interactions

Cenobamate can affect the plasma concentrations of other medications, as it is metabolized by hepatic enzymes including CYP3A4 and others. Clinically relevant interactions include:

Other antiepileptic drugs such as phenytoin, phenobarbital, and clobazam
Hormonal contraceptives (cenobamate may reduce their effectiveness)
Other drugs metabolized by CYP enzymes

Contraindications

Known hypersensitivity to cenobamate or any excipient
Familial Short QT syndrome
Pregnancy and breastfeeding (use only after careful benefit-risk assessment)

References

European Medicines Agency (EMA): Ontozry (cenobamate) - Summary of Product Characteristics and Assessment Report. EMA/CHMP, 2021. Available at: www.ema.europa.eu
Krauss GL et al. - Randomized Phase 2 Study of Cenobamate (YKP3089) as Adjunctive Treatment for Uncontrolled Focal Seizures. Neurology. 2020;91(14):e1289-e1298.
Biton V et al. - Cenobamate for Uncontrolled Focal Seizures: A Randomized, Double-Blind, Placebo-Controlled Trial. Lancet Neurology. 2019;18(12):1027-1037.

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