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Indications

Perampanel an anti-epileptic drug is indicated for:

  • Treatment of partial-onset seizures with or without secondarily generalized seizures in patients with epilepsy from 4 years of age and older.
  • Adjunctive therapy in the treatment of primary generalized tonic-clonic seizures in patients with epilepsy from 12 years of age and older.

Pharmacology

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 a number of neurological disorders caused by neuronal over excitation. The precise mechanism by which Perampanel exerts its antiepileptic effects in humans is unknown.

Dosage And Administration

Perampanel can be taken without regard to food. The dosage of Perampanel is as follows-

  • Starting dose: 2 mg once daily at bedtime. May increase dose based on clinical response and tolerability by increments of 2 mg once daily no more frequently than at weekly intervals.
  • Recommended maintenance dose in monotherapy or adjunctive therapy for partial-onset seizures: 8 mg to 12 mg once daily at bedtime.
  • Recommended maintenance dose in adjunctive therapy for primary generalized tonic-clonic seizures: 8 mg once daily at bedtime.

Mild and Moderate Hepatic Impairment: Maximum recommended daily dose is 6 mg (mild) and 4 mg (moderate) once daily at bedtime.

Severe Hepatic Impairment: Not recommended.

Severe Renal Impairment: Not recommended.

Elderly: Increase dose no more frequently than every 2 weeks.

Interaction

  • Contraceptives: 12 mg once daily may decrease the effectiveness of hormonal contraceptives containing levonorgestrel.
  • Moderate and Strong CYP3A4 Inducers (including carbamazepine, oxcarbazepine, and phenytoin): increase the clearance of Perampanel and decrease Perampanel plasma concentrations.

Contraindications

None.

Side Effects

Perampanel may cause Serious Psychiatric and Behavioral Reactions, Suicidal Behavior and Ideation, Dizziness, Somnolence, Fatigue, Irritability, Falls, Nausea, Ataxia, Balance Disorder etc.

Pregnancy And Lactation

Based on animal data, may cause fetal harm. There are no data on the presence of perampanel in human milk, the effects on the breastfed child, or the effects of the drug on milk production.

Precautions And Warnings

  • Suicidal Behavior and Ideation: Monitor for suicidal thoughts or Behaviour.
  • Neurologic Effects: Monitor for dizziness, gait disturbance, somnolence and fatigue.
  • Falls: Monitor for falls and injuries.
  • Drug Reaction with Eosinophilia and Systemic Symptoms/Multi-organ Hypersensitivity: Discontinue if no alternate etiology.
  • Withdrawal of Antiepileptic Drugs: In patients with epilepsy, there may be an increase in seizure frequency.

Therapeutic Class

Adjunct anti-epileptic drugs.

Storage Conditions

Protect from light and moisture, store below 30°C. Keep out of the reach of children.