title: Perampanel: a new agent for adjunctive treatment of partial seizures.
abstract: OBJECTIVE
  The pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of perampanel are reviewed.
  
  
  CONCLUSIONS
  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-isoxazole-propionate (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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Michele A. Faulkner, Pharm.D., is Associate Professor of Pharmacy Practice, School of Pharmacy and Health Professions, and Associate Professor of Medicine, Department of Neurology, School of Medicine, Creighton University, Omaha, NE (faulkner@creighton.edu).
authors.forename: Michele A
authors.initials: MA
authors.lastname: Faulkner
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000927:Anticonvulsants / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D001682:Biological Availability; D004347:Drug Interactions; D004348:Drug Labeling; D004828:Epilepsies, Partial / Q000188:drug therapy* / Q000503:physiopathology; D006207:Half-Life; D006801:Humans; D009570:Nitriles; D011728:Pyridones / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors
chemical_list: D000927:Anticonvulsants; D009570:Nitriles; D011728:Pyridones; D018091:Receptors, AMPA; C551441:perampanel