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gabapentin
type of chemical entity
Subclass ofGamma-amino acidsπŸ‘ Edit
Get useMedication, substance abuseπŸ‘ Edit
Chemical formulaC₉H₁₇NOβ‚‚πŸ‘ Edit
Canonical SMILESC1CCC(CC1)(CC(=O)O)CNπŸ‘ Edit
Active ingredient inGralise, Neurontin, HorizantπŸ‘ Edit
World Health Organisation international non-proprietary namegabapentinπŸ‘ Edit
Significant drug interactionmorphine, morphine, morphine, morphineπŸ‘ Edit
Pregnancy categoryAustralian pregnancy category B1, US pregnancy category CπŸ‘ Edit
LiverTox likelihood scoreLiverTox toxicity likelihood category CπŸ‘ Edit
ManufacturerPfizerπŸ‘ Edit

Gabapentin, dem sell under de brand name Neurontin among odas, be an anticonvulsant medication dem use to treat neuropathic pain (postherpetic neuralgia) den partial seizures of epilepsy.[1][2] Gabapentin be a central nervous system depressant.[2] Dem dey use am for de treatment of neuropathic pain wey be caused by diabetic neuropathy, postherpetic neuralgia, den central pain.[3] E be moderately effective: about 30–40% of those wey dem dey give gabapentin for diabetic neuropathy anaa postherpetic neuralgia get a meaningful benefit.[4]

Gabapentin dey act by decreasing activity of de Ξ±2Ξ΄-1 protein, wey de CACNA2D1 gene code, dem first know as an auxiliary subunit of voltage-gated calcium channels.[5][6][7] By binding to Ξ±2Ξ΄-1, gabapentin dey reduce de release of excitatory neurotransmitters (primarily glutamate) den as a result, dey reduce excess excitation of neuronal networks insyd de spinal cord den brain. Sleepiness den dizziness be de most common side effects. Serious side effects dey include respiratory depression den allergic reactions.[2] Na dem label gabapentin for an increased risk of suicide.[2]

Na dem first approve gabapentin for use insyd de United Kingdom insyd 1993.[8] Na e be available as a generic medication insyd de United States since 2004.[9] E be de first of chaw oda drugs wey be similar insyd structure den mechanism, dem call gabapentinoids. Insyd 2023, na e be de ninth most commonly prescribed medication insyd de United States, plus more dan 45million prescriptions.[10][11] During de 1990s, na Parke-Davis, a subsidiary of Pfizer, use chaw illegal techniques to encourage physicians insyd de United States to prescribe gabapentin for unapproved uses.[12] Na dem pay out millions of dollars to settle lawsuits wey dey regard dese activities.[13]

References

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  1. ↑ "Neuropathic pain in adults: pharmacological management in non-specialist settings". National Institute for Health and Care Excellence (NICE). 20 November 2013. Retrieved 14 December 2020.
  2. 1 2 3 4 "Neurontin- gabapentin capsule Neurontin- gabapentin tablet, film coated Neurontin- gabapentin solution". DailyMed. 11 April 2019. Retrieved 21 December 2019.
  3. ↑ Attal N, Cruccu G, Baron R, HaanpÀÀ M, Hansson P, Jensen TS, Nurmikko T (September 2010). "EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision". European Journal of Neurology. 17 (9): 1113–1e88. doi:10.1111/j.1468-1331.2010.02999.x. PMID20402746. S2CID14236933.
  4. ↑ Wiffen PJ, Derry S, Bell RF, Rice AS, TΓΆlle TR, Phillips T, Moore RA (June 2017). "Gabapentin for chronic neuropathic pain in adults". The Cochrane Database of Systematic Reviews. 6 (6) CD007938. doi:10.1002/14651858.CD007938.pub4. hdl:10044/1/52908. PMC6452908. PMID28597471.
  5. ↑ Risher WC, Eroglu C (August 2020). "Emerging roles for Ξ±2Ξ΄ subunits in calcium channel function and synaptic connectivity". Current Opinion in Neurobiology. 63: 162–169. doi:10.1016/j.conb.2020.04.007. PMC7483897. PMID32521436.
  6. ↑ Stahl SM, Porreca F, Taylor CP, Cheung R, Thorpe AJ, Clair A (June 2013). "The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities?". Trends in Pharmacological Sciences. 34 (6): 332–339. doi:10.1016/j.tips.2013.04.001. PMID23642658.
  7. ↑ Taylor CP, Harris EW (July 2020). "Analgesia with Gabapentin and Pregabalin May Involve N-Methyl-d-Aspartate Receptors, Neurexins, and Thrombospondins". The Journal of Pharmacology and Experimental Therapeutics. 374 (1): 161–174. doi:10.1124/jpet.120.266056. PMID32321743. S2CID216082872.
  8. ↑ PitkΓ€nen A, Schwartzkroin PA, MoshΓ© SL (2005). Models of Seizures and Epilepsy. Burlington: Elsevier. p.539. ISBN978-0-08-045702-4. Archived from the original on 8 September 2017.
  9. ↑ Reed D (2 March 2012). The Other End of the Stethoscope: The Physician's Perspective on the Health Care Crisis. AuthorHouse. pp.63–. ISBN978-1-4685-4410-7.
  10. ↑ "The Top 300 of 2023". ClinCalc. Archived from the original on 12 August 2025. Retrieved 12 August 2025.
  11. ↑ "Gabapentin Drug Usage Statistics, United States, 2014 - 2023". ClinCalc. Retrieved 17 August 2025.
  12. ↑ Henney JE (August 2006). "Safeguarding patient welfare: who's in charge?". Annals of Internal Medicine. 145 (4): 305–307. doi:10.7326/0003-4819-145-4-200608150-00013. PMID16908923. S2CID39262014.
  13. ↑ Stempel J (2 June 2014). "Pfizer to pay $325 million in Neurontin settlement". Reuters. Retrieved 11 June 2018.

External links

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