Pregabalin
LyricaPubChem CID 5486971 · 3D model
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Calms overactive nerve signals the same way gabapentin does, by damping down a calcium-channel doorway nerve cells use to release pain and seizure signals — but pregabalin absorbs into the body more predictably at higher doses.
How it works
Pregabalin plugs into the same calcium-channel docking site as gabapentin, also on this site, turning down the release of chemical signals that drive nerve pain and seizures. It shares gabapentin's chemical resemblance to the calming brain chemical GABA, but, like gabapentin, doesn't actually act on GABA itself. Where the two drugs really differ is in how reliably the body absorbs them: gabapentin relies on a saturable gut-absorption process, so a smaller fraction of a high dose gets absorbed the more you take — its bioavailability can drop from about 60% down to under 30% at high doses. Pregabalin doesn't have that ceiling; roughly 90% of an oral dose gets absorbed no matter the dose size, so its effect scales more predictably with dose than gabapentin's does.
What it’s used for
Used to relieve nerve pain from diabetic nerve damage, lingering nerve pain after shingles, and nerve pain following spinal cord injury; as an add-on medicine to help control certain seizures in patients as young as 1 month old; and to manage fibromyalgia, a chronic condition involving widespread muscle pain and tenderness. That fibromyalgia use is one pregabalin has that gabapentin, also on this site, does not.
- Mechanism
- Alpha-2-delta calcium channel subunit modulator
- Drug class
- Small molecule
- Therapeutic area
- CNS / Neurology