Gabapentinoid

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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] In addition, phenibut (Noofen) has been found to act as a gabapentinoid in addition to its primary mechanism of action.[4][6] Another analogue mirogabalin is in clinical trials but has not yet been approved.[7] Other compounds from this family used in research but not developed for medical use include 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][8] Some off-label uses include migraine, social phobia, panic disorder, mania, bipolar disorder, and alcohol withdrawal.[5][9]

See also[edit]

References[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. ^ Eroglu, Çagla; Allen, Nicola J.; Susman, Michael W.; O'Rourke, Nancy A.; Park, Chan Young; Özkan, Engin; Chakraborty, Chandrani; Mulinyawe, Sara B.; Annis, Douglas S.; Huberman, Andrew D.; Green, Eric M.; Lawler, Jack; Dolmetsch, Ricardo; Garcia, K. Christopher; Smith, Stephen J.; Luo, Z. David; Rosenthal, Arnon; Mosher, Deane F.; Barres, Ben A. (2009). "Gabapentin Receptor α2δ-1 is a Neuronal Thrombospondin Receptor Responsible for Excitatory CNS Synaptogenesis". Cell. 139 (2): 380–92. doi:10.1016/j.cell.2009.09.025. PMC 2791798Freely accessible. PMID 19818485. 
  4. ^ a b 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: 23–9. doi:10.1016/j.pbb.2015.07.014. 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. ^ Vavers, Edijs; Zvejniece, Liga; Svalbe, Baiba; Volska, Kristine; Makarova, Elina; Liepinsh, Edgars; Rizhanova, Kristina; Liepins, Vilnis; Dambrova, Maija (2015). "The neuroprotective effects of R-phenibut after focal cerebral ischemia". Pharmacological Research. doi:10.1016/j.phrs.2015.11.013. ISSN 1043-6618. 
  7. ^ Vinik, Aaron; Rosenstock, Julio; Sharma, Uma; Feins, Karen; Hsu, Ching; Merante, Domenico (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. 
  8. ^ Frye, Mark; Moore, Katherine (2009). "Gabapentin and Pregabalin". In Schatzberg, Alan F.; Nemeroff, Charles B. The American Psychiatric Publishing Textbook of Psychopharmacology. pp. 767–77. doi:10.1176/appi.books.9781585623860.as38. ISBN 978-1-58562-309-9. 
  9. ^ http://www.clevelandclinicmeded.com/medicalpubs/pharmacy/septoct2005/pregabalin.htm[full citation needed]


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