Perampanel, a third-generation antiepileptic, has a novel mechanism compared to classical agents. It is best classified as:
- A Voltage-gated sodium channel blocker
- B Non-competitive AMPA receptor antagonist ✓
- C GABA-B receptor positive allosteric modulator
- D Selective HCN channel (Ih current) blocker
Explanation
Perampanel is the first and only non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist approved for epilepsy. It binds to an allosteric site on the AMPA receptor — the major mediator of fast excitatory glutamate neurotransmission — blocking glutamate-driven neuronal hyperexcitability without affecting the agonist binding site (hence non-competitive). This mechanism is distinct from all older antiepileptics. GABA-B modulation is the mechanism of baclofen; HCN channel (Ih) block is the mechanism of ZD7288 (investigational); sodium channel block is the mechanism of phenytoin/carbamazepine.
Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.
High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP
Written and medically reviewed by the StethoPrep medical team.