Generic
Perampanel
2 brands available in the market
At a glance
Perampanel is an anti-epileptic drug used for the treatment of partial-onset seizures with or without secondarily generalized seizures in patients from 4 years of age and older, and as adjunctive therapy for primary generalized tonic-clonic seizures in patients from 12 years of age and older.
Description
Perampanel is a non-competitive antagonist of the ionotropic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor on post-synaptic neurons. Glutamate is the primary excitatory neurotransmitter in the central nervous system and is implicated in neurological disorders caused by neuronal over-excitation.
Indications
- Partial-onset seizures with or without secondarily generalized seizures in patients from 4 years of age and older
- Adjunctive therapy for primary generalized tonic-clonic seizures in patients from 12 years of age and older
Therapeutic class
Adjunct anti-epileptic drugs
Pharmacological class
AMPA Receptor Antagonist (Non-competitive)
Pharmacology
Perampanel is a non-competitive antagonist of the AMPA glutamate receptor on post-synaptic neurons. Glutamate is the primary excitatory neurotransmitter in the CNS. Perampanel reduces neuronal over-excitation by inhibiting AMPA receptors, helping to control seizures.
Mechanism of action
Non-competitively inhibits AMPA glutamate receptors, reducing neuronal excitation.
Dosage
Adult Dose (Oral):
- Starting dose: 2 mg once daily at bedtime
- May increase by increments of 2 mg weekly based on clinical response and tolerability
- Maintenance dose for partial-onset seizures: 8-12 mg once daily at bedtime
- Maintenance dose for primary generalized tonic-clonic seizures: 8 mg once daily at bedtime
- Mild hepatic impairment: Max 6 mg/day; Moderate: 4 mg/day
- Severe hepatic or renal impairment: Not recommended
- Elderly: Increase dose no more frequently than every 2 weeks
Administration
- May be taken with or without food
- Take once daily at bedtime
- Swallow tablet whole
- Follow the prescribed dose
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Side Effects:
- Serious psychiatric and behavioral reactions
- Suicidal behavior and ideation
- Dizziness
- Somnolence
- Fatigue
- Irritability
- Falls
- Nausea
- Ataxia
- Balance disorder
Precautions & warnings
- Monitor for suicidal thoughts or behavior
- Monitor for dizziness, gait disturbance, somnolence, and fatigue
- Monitor for falls and injuries
- DRESS/Multi-organ hypersensitivity: Discontinue if no alternate etiology
- Withdrawal of antiepileptic drugs may increase seizure frequency
Contraindications
None.
Drug interactions
- Carbamazepine, oxcarbazepine, phenytoin (CYP3A4 inducers): Increase clearance and decrease plasma concentrations of Perampanel
- Hormonal contraceptives (levonorgestrel): May decrease effectiveness (at 12 mg/day)
Food interactions
Food does not affect absorption; it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: Based on animal data, may cause fetal harm; no data on presence in human milk.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No data on the presence of perampanel in human milk, effects on the breastfed child, or effects on milk production.
Pediatric use
Safety and efficacy not established in children under 4 years.
Geriatric use
Elderly patients: Increase dose no more frequently than every 2 weeks.
Renal / hepatic impairment
Renal Impairment: Severe renal impairment: Not recommended; consult your doctor.
Hepatic Impairment: Mild: Max 6 mg/day; Moderate: 4 mg/day; Severe: Not recommended.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Protect from light and moisture; store below 30°C; keep out of reach of children.
Chemical structure
Perampanel