XCOPRI Dosage & Rx Info | Uses, Side Effects

Xcopri Generic Name & Formulations

Legal Class

General Description

Cenobamate 12.5mg, 25mg, 50mg, 100mg, 150mg, 200mg; tabs.

Pharmacological Class

Antiepileptic.

How Supplied

Tabs 50mg, 100mg, 150mg, 200mg—30; Blister packs (Titration)—14; (Maintenance)—28

Manufacturer

SK Life Science, Inc.

Generic Availability

Mechanism of Action

The precise mechanism by which cenobamate exerts its therapeutic effects in patients with partial-onset seizures is unknown. Cenobamate has been demonstrated to reduce repetitive neuronal firing by inhibiting voltage-gated sodium currents. It is also a positive allosteric modulator of the γ-aminobutyric acid (GABA_A) ion channel.

Xcopri Indications

Indications

Partial-onset seizures.

Xcopri Dosage and Administration

Adult

Tabs can be swallowed whole or be crushed. Mix crushed tabs with water (25mL) and administered as an oral susp or via NG tube. Initially (Weeks 1 & 2): 12.5mg once daily. Titration regimen (Weeks 3 & 4): 25mg once daily; (Weeks 5 & 6): 50mg once daily; (Weeks 7 & 8): 100mg once daily; (Weeks 9 & 10): 150mg once daily. Maintenance (Week 11 & thereafter): 200mg once daily. Maximum dose (if needed based on response and tolerability, may increase by increments of 50mg/day every 2 weeks): 400mg once daily. Mild to moderate hepatic impairment: max 200mg once daily. Withdraw gradually over ≥2 weeks, if discontinuation needed.

Children

Not established.

Xcopri Contraindications

Contraindications

Familial short QT syndrome.

Xcopri Boxed Warnings

Not Applicable

Xcopri Warnings/Precautions

Warnings/Precautions

Permanently discontinue if multiorgan hypersensitivity/DRESS occurs. Monitor for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes. Monitor for CNS depression, neurological reactions. Avoid abrupt cessation. Drug abuse. Mild to moderate hepatic impairment: see Adult dose. Severe hepatic impairment: not recommended. Renal impairment. ESRD on dialysis: not recommended. Elderly. Pregnancy. Advise females of reproductive potential to use additional or alternative non-hormonal contraceptive. Nursing mothers.

Xcopri Pharmacokinetics

Absorption

Median T_max: range 1–4 hours.

Distribution

Volume of distribution: ~40–50 L. Plasma protein bound: 60%.

Metabolism

Primarily glucuronidation (UGT2B7, UGT2B4); oxidation (CYP2E1, CYP2A6, CYP2B6, CYP2C19, CYP3A4/5.

Elimination

Renal (87.8%), fecal (5.2%). Half-life: 50–60 hours.

Xcopri Interactions

Interactions

May antagonize lamotrigine, carbamazepine, oral contraceptives, CYP2B6 and CYP3A substrates. May potentiate phenytoin (reduce phenytoin dose by up to 50%), phenobarbital, clobazam, CYP2C19 substrates. Caution with other drugs that shorten the QT interval. Increased risk of neurological reactions with other CNS depressants, including alcohol.

Xcopri Adverse Reactions

Adverse Reactions

Somnolence, dizziness, fatigue, diplopia, headache; multiorgan hypersensitivity/DRESS.

Xcopri Clinical Trials

See Literature

Xcopri Note