Gabapentin
- Class: Anticonvulsant / neuropathic pain
- Used for: nerve pain
- Say it: GAB-uh-pen-tin
- Forms: capsule, tablet, oral liquid
GABAPENTIN quiets the screaming nerve PAIN — the burning, shooting kind that ordinary painkillers never touch.
Careful with the GABA at the front: despite the name it does not act on GABA receptors. It binds the alpha-2-delta subunit of a calcium channel. The name remembers the indication, not the mechanism.
Despite the name, it binds the alpha-2-delta subunit of a calcium channel on nerve endings and cuts excess neurotransmitter release. The name is a trap set for exam candidates.
Side effects
Common: drowsiness, dizziness, leg swelling
Serious: breathing depression with opioids, misuse
Typical dose
300 mg at night, titrated to 900–3600 mg daily in three doses
Titrate over days: 300 mg on day one, twice daily on day two, three times daily on day three. Reduce in renal impairment.
Check yourself
Despite its name, Gabapentin works by...
- binding a calcium-channel subunit on nerve endings
- activating GABA receptors directly
- blocking sodium channels
- blocking NMDA receptors
Show answer
A. binding a calcium-channel subunit on nerve endings
It was designed as a GABA analogue and named accordingly, but it does not act at the GABA receptor at all. Reducing calcium entry at the nerve terminal is what cuts the pain signal.
See it, don't memorize it
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