Afalino(Cenobamate)
Therapeutic Group: Drugs of Nervous System, Antiepileptic
Presentation
Afalinoâ„¢ 12.5: Each film coated tablet contains Cenobamate INN 12.5 mg.
Afalinoâ„¢ 25: Each film coated tablet contains Cenobamate INN 25 mg.
Afalinoâ„¢ 50: Each film coated tablet contains Cenobamate INN 50 mg.
Description
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 (GABAA) ion channel.
Indications
Cenobamate is indicated for the treatment of partial-onset seizures in adult patients.
Dosage & Administration
Recommended Dosage for Partial-Onset Seizures in Adults-
Initial Dosage:
For Week 1 and 2 dose is 12.5 mg once daily
Titration Regimen:
For Week 3 and 4 dose is 25 mg once daily
For Week 5 and 6 dose is 50 mg once daily
For Week 7 and 8 dose is 100 mg once daily
For Week 9 and 10 dose is 150 mg once daily
Maintenance Dosage:
For Week 11 and thereafter dose is 200 mg once daily
Maximum Dosage:
Dose is 400 mg once daily
Side Effects
The most common side-effects of Cenobamate include-somnolence, dizziness, fatigue, diplopia, headache etc.
Precautions
• Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) / Multi-Organ Hypersensitivity: Discontinue if no alternate etiology.
• QT Shortening: Use caution when administering Cenobamate with other drugs that shorten the QT interval
• Suicidal Behavior and Ideation: Monitor patients for suicidal behavior and ideation.
• Neurological Adverse Reactions: Monitor for somnolence and fatigue and advise patients not to drive or operate
machinery until they have gained sufficient experience on Cenobamate. Concomitant use with other CNS depressants or alcohol may have additive effects.
• Withdrawal of Antiepileptic Drugs: Cenobamate should be gradually withdrawn to minimize the potential of increased seizure frequency.
Use in Pregnancy & Lactation
Pregnancy: There are no adequate and well-controlled studies in pregnant women with the use of Cenobamate. But it may cause fetal harm when administered to a pregnant woman. It should be used during
pregnancy only if the potential benefits justify the potential risk to the fetus.
Lactation: There are no data on the presence of Cenobamate in human milk, the effects of Cenobamate on the breastfed infant, or the effects of Cenobamate on milk production.
Use in special population
Pediatric use: Safety and effectiveness of Cenobamate has not been established in pediatric patients.
Geriatric use: Start at the low end of the dosing range.
Renal impairment: Cenobamate should be used with caution and dosage reduction may be considered in patients with mild to moderate (CLcr 30 to less than 90 mL/min) and severe (CLcr less than 30 mL/min) renal
impairment. Use in patients with end-stage renal disease undergoing dialysis is not recommended.
Hepatic impairment: Cenobamate should be used with caution and in patients with mild to moderate hepatic impairment
Drug Interaction
• Phenytoin: Gradually decrease phenytoin dosage by up to 50%
• Phenobarbital and Clobazam: Reduce dosage as needed when used concomitantly with Cenobamate.
• Lamotrigine, Carbamazepine: Increase dosage as needed when used concomitantly with Cenobamate.
• CYP2B6 and CYP3A Substrates: Increase dosage as needed when used concomitantly with Cenobamate.
• CYP2C19 Substrates: Reduce dosage as needed when used concomitantly with Cenobamate.
• Oral Contraceptives: Effectiveness of hormonal oral contraceptives may be reduced when administered concomitantly with Cenobamate. Women should use additional or alternative non-hormonal birth control.
Over Dose
In the event of overdose, Cenobamate should be discontinued and general supportive treatment given until clinical toxicity has been diminished or resolved.
Storage
Do not store above 30 degree C. Keep away from light and out of the reach of children.
Commercial Pack
Afalinoâ„¢ 12.5: Each box contains 3 blister strips of 10 tablets.
Afalinoâ„¢ 25: Each box contains 2 blister strips of 10 tablets.
Afalinoâ„¢ 50: Each box contains 1 blister strip of 10 tablets.
