Gabapentinoids - PsychonautWiki



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

Gabapentinoids are a relatively small chemical class of psychoactive substances derived from gamma-aminobutyric acid (GABA).[citation needed] Members of this class include gabapentin, F-phenibut, phenibut 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 close structural relatives, and are all 3-substituted derivatives of GABA, the differences being the addition of a cyclohexyl group on the GABA chain in the case of gabapentin, the substitution of that cyclohexyl group for an isobutyl group in the case of pregabalin, and the substitution of that isobutyl group with a cyclic phenyl ring in the case of phenibut. Hence, they are GABA analogues, as well as γ-amino acids.[1][2]


Gabapentinoids act by inhibiting the α2δ subunit-containing voltage-dependent calcium channels (VGCCs).[3] While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.[4]


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.
  3. Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).
  4. Goldlust, A., Su, T. Z., Welty, D. F., Taylor, C. P., & Oxender, D. L. (1995). Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA. Epilepsy research, 22(1), 1-11.