title: The AMPA receptor antagonist perampanel is a new hope in the treatment for epilepsy.
abstract: Perampanel is a novel drug recently approved as adjunctive therapy in epileptic patients aged 12 years and older who have drug-resistant partial epilepsy with and without secondary generalization. Pharmacological researches revealed that perampanel reduces neuronal excitability by a non-competitive antagonistic activity against the ionotropic alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors causing modulation of glutamatergic neurotransmission. The pharmacological profile of the drug showed complete absorption following oral administration, and extensive metabolism in the liver by oxidation followed by glucuronidation with an elimination half-life of approximately 53-165 h (average: 105 h), allowing once-daily administration. Randomized placebo-controlled trials demonstrated an effective dose range of the drug, between 4 and 12 mg/day, to significantly reduce seizure frequency in patients with partial-onset seizure that are pharmacoresistant with a favorable tolerability profile. The most frequent adverse events of the drug reported in phase III clinical trials were dizziness, somnolence, fatigue, and headache. However, the data raised from the studies can give a hope that perampanel offers a valuable option as an adjuvant therapy for pharmacoresistant partial-onset and secondarily generalized seizures.
authors.affiliation: Department of Pharmacology, Faculty of Medicine, Assiut University, 71515, Assiut, Egypt.
authors.forename: Ehab S
authors.initials: ES
authors.lastname: El Desoky
mesh_terms: D000927:Anticonvulsants / Q000627:therapeutic use*; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D009570:Nitriles; D011728:Pyridones / Q000627:therapeutic use*; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*
chemical_list: D000927:Anticonvulsants; D009570:Nitriles; D011728:Pyridones; D018091:Receptors, AMPA; C551441:perampanel
keywords: clinical background; epilepsy; perampanel; pharmacodynamics; pharmacokinetics