Gabapentinoids

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Gabapentinoids are a class of chemical compounds that are derivatives of gamma-aminobutyric acid which block α2δ subunit-containing voltage-dependent calcium channels. While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.

Diagram showing the structural similarities of pregabalin, gabapentin and gamma-aminobutyric acid.

Gabapentinoids are commonly used for epilepsy, neuropathic pain, and restless legs syndrome. Gabapentinoids are often sedating, have anticonvulsant effects, and suppress anxiety. Drugs in this class include gabapentin, F-phenibut, phenibut and, pregabalin. Gabapentinoids can be dangerous when mixed with other depressants such as benzodiazepines, alcohol and opioids.

See also

• Responsible use
• Depressants
• Gabapentin
• Phenibut
• Pregabalin