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The AMPA receptor antagonist perampanel
is a new hope in the treatment for epilepsy

مؤلف البحث
Ehab S. El Desoky
مجلة البحث
Fundamental & Clinical Pharmacology 28 (5): 473-80
المشارك في البحث
تصنيف البحث
1
عدد البحث
Vol 28, No 5
سنة البحث
2014
صفحات البحث
PP.473-480
ملخص البحث

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.