Perampanel, a newer antiepileptic approved as adjunctive therapy for focal and generalized tonic-clonic seizures, acts by which unique mechanism that distinguishes it from all older antiepileptics?
- A Selective blockade of voltage-gated sodium channels (Nav1.1 preferring)
- B Non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonism ✓
- C Enhancement of GABAergic inhibition via GABA-A receptor positive allosteric modulation
- D Inhibition of synaptic vesicle glycoprotein 2A (SV2A) reducing vesicle exocytosis
Correct answer: B. Non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonism
Explanation
Perampanel is the first and only non-competitive AMPA receptor antagonist approved for epilepsy. It blocks the AMPA subtype of ionotropic glutamate receptors at a non-competitive (negative allosteric modulator) site, reducing excitatory glutamatergic neurotransmission. This is mechanistically distinct from sodium channel blockers (carbamazepine, phenytoin), GABA enhancers (benzodiazepines, barbiturates), and SV2A binders (levetiracetam). Its unique mechanism makes it useful as add-on therapy when other agents have failed.
Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.
High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP
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