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

Gabapentinoids are a chemical class of psychoactive substances derived from gamma-aminobutyric acid (GABA).[citation needed] Members of this class include gabapentin, F-phenibut, phenibut, baclofen and pregabalin.

Gabapentinoids are commonly prescribed for epilepsy, neuropathic pain, and restless legs syndrome. Subjective effects include sedation, muscle relaxation, and anxiety suppression.

Gabapentinoids can be dangerous when mixed with other depressants such as benzodiazepines, alcohol and opioids.



Gabapentinoids are 3-substituted derivatives of GABA. Hence, they are GABA analogues, as well as γ-amino acids.[1][2]


Gabapentinoids act by blocking α2δ subunit-containing voltage-dependent calcium channels (VGCCs).[citation needed] While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.[citation needed]


See also

External links


  1. Elaine Wyllie; Gregory D. Cascino; Barry E. Gidal; Howard P. Goodkin (17 February 2012). Wyllie's Treatment of Epilepsy: Principles and Practice. Lippincott Williams & Wilkins. p. 423. ISBN 978-1-4511-5348-4.
  2. Honorio Benzon; James P. Rathmell; Christopher L. Wu; Dennis C. Turk; Charles E. Argoff; Robert W Hurley (11 September 2013). Practical Management of Pain. Elsevier Health Sciences. p. 1006. ISBN 978-0-323-17080-2.