Perampanel, a newer antiepileptic, has a unique mechanism among approved antiepileptics in that it:

• A Selectively blocks T-type calcium channels on thalamic relay neurons
• B Is the only non-competitive AMPA receptor antagonist approved for focal seizures ✓
• C Inhibits carbonic anhydrase II and IV in brain parenchyma
• D Activates GABA-B receptors to produce pre- and post-synaptic inhibition

Explanation

Perampanel (Fycompa) is the first and only non-competitive antagonist of AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid) glutamate receptors. AMPA receptors mediate fast excitatory neurotransmission; their blockade reduces neuronal hyperexcitability. Because it is non-competitive (acting at an allosteric site), its efficacy is not overcome by elevated glutamate levels during seizures — an advantage over competitive antagonists. T-type channel blockade is the mechanism of ethosuximide/zonisamide; carbonic anhydrase inhibition characterizes acetazolamide/topiramate/zonisamide.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.