Perampanel: a selective AMPA antagonist for treating seizures.
نویسنده
چکیده
Perampanel is a selective, noncompetitive AMPA receptor antagonist that has recently been approved for treating localization-related epilepsy. This article reviews the pharmacology, clinical development, efficacy, and safety/tolerability of perampanel.
منابع مشابه
Preclinical pharmacology of perampanel, a selective non-competitive AMPA receptor antagonist.
Perampanel [2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile; E2007] is a potent, selective, orally active non-competitive AMPA receptor antagonist developed for the treatment of epilepsy. Perampanel has a 2,3'-bipyridin-6'-one core structure, distinguishing it chemically from other AMPA receptor antagonist classes. Studies in various physiological systems indicate that per...
متن کاملClinical efficacy of perampanel for partial-onset and primary generalized tonic–clonic seizures
BACKGROUND AND PURPOSE Perampanel, a selective noncompetitive antagonist at the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, is highly effective in a wide range of experimental models. Although initially licensed as adjunctive therapy for partial seizures with or without secondary generalization in patients aged 12 years or older, the US Food and Drug Administration has...
متن کاملPsychiatric and behavioral adverse events in randomized clinical studies of the noncompetitive AMPA receptor antagonist perampanel
OBJECTIVE Perampanel, a selective, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor antagonist, is indicated for adjunctive treatment of partial seizures in patients ≥12 years based on three phase III clinical studies. The perampanel U.S. Prescribing Information includes a boxed warning for serious psychiatric and behavioral adverse reactions. To pro...
متن کاملPerampanel, an Antagonist of α-amino-3-hydroxy-5- methyl-4-isoxazolepropionic acid (AMPA) Receptors for the Treatment of Epilepsy: Studies in Human Epileptic Brain, Non-Epileptic Brain, and in Rodent Models
Perampanel (Fycompa®) is an AMPA receptor antagonist used as an adjunctive treatment of partial-onset seizures. We asked whether perampanel has AMPA receptor antagonist activity in both cerebral cortex and hippocampus, associated with antiepileptic efficacy, and also in cerebellum, associated with motor side-effects, in rodent and human brain. We also asked if epileptic and non-epileptic human ...
متن کاملPerampanel Inhibition of AMPA Receptor Currents in Cultured Hippocampal Neurons
Perampanel is an aryl substituted 2-pyridone AMPA receptor antagonist that was recently approved as a treatment for epilepsy. The drug potently inhibits AMPA receptor responses but the mode of block has not been characterized. Here the action of perampanel on AMPA receptors was investigated by whole-cell voltage-clamp recording in cultured rat hippocampal neurons. Perampanel caused a slow (τ∼1 ...
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ورودعنوان ژورنال:
- Epilepsy currents
دوره 13 6 شماره
صفحات -
تاریخ انتشار 2013