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

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.

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