Small molecule · CNS / Neurology

Gabapentin

Neurontin
Small moleculeAlpha-2-delta calcium channel subunit modulator

PubChem CID 3446 · 3D model

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Calms overactive nerve signals by damping down a calcium-channel doorway that nerve cells use to release pain and seizure signals.

How it works

Gabapentin attaches to a specific docking site on calcium channels in nerve cells throughout the brain and spinal cord. Even though its chemical structure resembles a natural calming brain chemical called GABA, it doesn't actually interact with GABA at all. Instead, by binding to this calcium-channel docking site, it appears to reduce how many of these channels show up at nerve endings, which turns down the release of chemical signals that drive seizures and nerve pain. That said, doctors don't fully know why this translates into fewer seizures and less pain in practice — the exact mechanism is still not completely understood, even though the drug clearly works.

What it’s used for

Used to relieve the lingering nerve pain that can follow a shingles outbreak in adults. Also used alongside other medications to help control partial (focal) seizures in adults and children age 3 and up who have epilepsy.

Mechanism
Alpha-2-delta subunit
Drug class
Therapeutic area
CNS / Neurology

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