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Pharmacology · CNS drugs and antiepileptics: pregabalin mechanism
Sample itemA patient with post-herpetic neuralgia is started on pregabalin. Through which target does it reduce neuropathic pain?
Original practice item, not a recalled exam question. Nothing here is recorded.
The answer and the reasoning
D. The alpha-2-delta subunit of presynaptic voltage-gated calcium channels
Pregabalin and gabapentin bind the alpha-2-delta subunit of voltage-gated calcium channels, reducing calcium entry and the release of glutamate and substance P. Despite being GABA analogues, they do not act on GABA receptors. Dizziness, sedation and weight gain are common adverse effects.
Option by option
A. Inactivation of voltage-gated sodium channels
Sodium channel inactivation is the action of phenytoin and carbamazepine.
B. Inhibition of GABA transaminase
GABA transaminase inhibition is the action of vigabatrin.
C. Positive allosteric modulation of the GABA-A receptor
GABA-A receptor modulation is the action of benzodiazepines, not of pregabalin.
D. The alpha-2-delta subunit of presynaptic voltage-gated calcium channels (correct)
Correct. Binding alpha-2-delta reduces calcium influx and excitatory transmitter release.
Source note: Original NextPrep sample item — pending expert review. This item is original practice material awaiting independent expert review, so confirm important facts in a standard textbook.
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