Perampanel

A new agent for adjunctive treatment of partial seizures

Research output: Contribution to journalReview article

7 Citations (Scopus)

Abstract

Purpose. The pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of perampanel are reviewed. Summary. Perampanel, a first-in-class antiepileptic agent, was recently approved for use as adjunctive therapy for the treatment of resistant partial seizures in patients 12 years of age and older. It acts as a selective, noncompetitive antagonist at postsynaptic α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionate (AMPA) receptors. Perampanel exhibits linear pharmacokinetics and has a half-life of approximately 105 hours. The drug is rapidly and nearly completely absorbed after oral administration, achieving its maximum serum concentration in approximately 1 hour. Its bioavailability is nearly complete. Several efficacy studies have consistently demonstrated the utility of perampanel as adjunctive therapy for the treatment of refractory partial seizures with or without secondary generalization. Drug interactions have been noted with agents that induce cytochrome P-450 hepatic enzymes, including other antiepileptics, and alterations in perampanel dosing may be necessary when these medications are used concurrently. Adverse effects associated with perampanel use are primarily related to the central nervous system, and slow dosage adjustment and bedtime administration are recommended to maximize patient tolerance. The drug's labeling includes a boxed warning about the possible induction of serious adverse psychiatric and behavioral reactions that necessitate close monitoring. Perampanel is not recommended for individuals with severe liver disease or severely compromised kidney function, including those undergoing hemodialysis. Conclusion. Perampanel is a novel antiepileptic agent specifically designed to exhibit selective noncompetitive antagonist activity at AMPA receptors. Perampanel has consistently demonstrated the ability to control treatment-refractory partial seizures in many patients.

Original languageEnglish
Pages (from-to)191-198
Number of pages8
JournalAmerican Journal of Health-System Pharmacy
Volume71
Issue number3
DOIs
StatePublished - Feb 1 2014

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Seizures
Drug Labeling
Anticonvulsants
AMPA Receptors
Therapeutics
Pharmacokinetics
perampanel
Drug Interactions
Hydroxyl Radical
Cytochrome P-450 Enzyme System
Biological Availability
Oral Administration
Psychiatry
Half-Life
Renal Dialysis
Liver Diseases
Central Nervous System
Pharmacology
Kidney
Safety

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Health Policy
  • Medicine(all)

Cite this

Perampanel : A new agent for adjunctive treatment of partial seizures. / Faulkner, Michele A.

In: American Journal of Health-System Pharmacy, Vol. 71, No. 3, 01.02.2014, p. 191-198.

Research output: Contribution to journalReview article

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