Introduction
Perampanel is a noncompetitive AMPA glutamate receptor antagonist. It is indicated as an adjunct in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures.
Uses
Perampanel is a non-competitive AMPA glutamate receptor antagonist used to treat partial-onset seizures with or without secondarily generalized seizures, and as adjunctive treatment of primary generalized tonic-clonic seizures in patients with epilepsy.
Used in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures.
Associated Conditions
Pharmacodynamics
Perampanel is involved in inhibiting neuronal excitation in the central nervous system leading to such effects as decreased pyschomotor performance.
Mechanism of Action
The exact mechanism of action of perampanel in seizures is not yet determined, but it is known that perampanel decreases neuronal excitation by non-competitive ihibition of the AMPA receptor.
Absorption
After oral adminitration, perampanel is absorbed rapidly and completely.
Volume of Distribution
The volume of distribution of perampanel was not quantified.
Protein Binding
Perampanel is 95-96% plasma protein bound with most binding to the plasma proteins α1-acid glycoprotein and albumin.
Route of Elimination
Perampanel is eliminated mostely in the feces (48%) and to a lesser exten in the urine (22%).
Half Life
Perampanel has a long elmination half-life of about 105 hours.
Clearance
In healthy patients, perampanel has a clearance of about 12 mL/min.
Toxicity
The FDA label includes an important warning of serious or life-threatening behavioral and psychiatric adverse reactions including aggression, hostility, irritability, anger, and homicidal thoughts in patients taking perampanel.
Food Interactions
- Take with or without food. Food slows the rate of absorption but not the extent.
Dosage
- 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.
Severe Hepatic Impairment: Not recommended.
Severe Renal Impairment: Not recommended.
Elderly: Increase dose no more frequently than every 2 weeks.
