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Chemical structure of pregabalin, gabapentin, and GABA

Gabapentinoids are a class of drugs that are derivatives of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) which block α2δ subunit-containing voltage-dependent calcium channels.[1][2] This site has been referred to as the gabapentin receptor (α2δ subunit), as it is the target of the drugs gabapentin and pregabalin.[3] Clinically-used gabapentinoids include gabapentin (Neurontin) and pregabalin (Lyrica)[1][2][4] as well as a gabapentin prodrug, gabapentin enacarbil (Horizant).[5] Another analogue mirogabalin is in clinical trials but has not yet been approved.[6] Other compounds from this family used in research but not developed for medical use include phenibut (Noofen), atagabalin, 4-methylpregabalin and PD-217,014.

Gabapentinoids are used clinically in the treatment of conditions including epilepsy, neuropathic pain, fibromyalgia, generalized anxiety disorder, and restless legs syndrome.[1][5][7] Some off-label uses include migraine, social phobia, panic disorder, mania, bipolar disorder, and alcohol withdrawal.[5][8]

See also[edit]


  1. ^ a b c 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. ^ a b 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. ^
  4. ^ Zvejniece, Liga; Vavers, Edijs; Svalbe, Baiba; Veinberg, Grigory; Rizhanova, Kristina; Liepins, Vilnis; Kalvinsh, Ivars; Dambrova, Maija (2015). "R-phenibut binds to the α2–δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects". Pharmacology Biochemistry and Behavior. 137: 23–29. doi:10.1016/j.pbb.2015.07.014. ISSN 0091-3057. PMID 26234470. 
  5. ^ a b c Douglas Kirsch (10 October 2013). Sleep Medicine in Neurology. John Wiley & Sons. p. 241. ISBN 978-1-118-76417-6. 
  6. ^ Vinik A, Rosenstock J, Sharma U, Feins K, Hsu C, Merante D, et al. (Dec 2014). "Efficacy and safety of mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study". Diabetes Care. 37 (12): 3253–61. doi:10.2337/dc14-1044. PMID 25231896. 
  7. ^ Alan F. Schatzberg; Charles B. Nemeroff (2009). The American Psychiatric Publishing Textbook of Psychopharmacology. American Psychiatric Pub. pp. 767–777. ISBN 978-1-58562-309-9. 
  8. ^