User:Mr. Ibrahem/Gabapentin

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Mr. Ibrahem/Gabapentin
Clinical data
Trade namesNeurontin, others[1]
Other namesCI-945; GOE-3450; DM-1796 (Gralise)
AHFS/Drugs.comMonograph
MedlinePlusa694007
License data
Pregnancy
category
Dependence
liability		Low
Addiction
liability		Low
Routes of
administration		By mouth
Drug classGabapentinoid
Legal status
Legal status
Pharmacokinetic data
Bioavailability27–60% (inversely proportional to dose; a high fat meal also increases bioavailability)[3][4]
Protein bindingLess than 3%[3][4]
MetabolismNot significantly metabolized[3][4]
Elimination half-life5 to 7 hours[3][4]
ExcretionKidney[3][4]
Identifiers
  • 1-(Aminomethyl)cyclohexaneacetic acid
Chemical and physical data
FormulaC9H17NO2
Molar mass171.240 g·mol−1
3D model (JSmol)
  • O=C(O)CC1(CN)CCCCC1
  • InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12) checkY
  • Key:UGJMXCAKCUNAIE-UHFFFAOYSA-N checkY
  (verify)

Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication used to treat partial seizures, neuropathic pain, hot flashes, and restless legs syndrome.[5][6] It is recommended as one of a number of first-line medications for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central neuropathic pain.[8] About 15% of people with diabetic neuropathy or postherpetic neuralgia have a measurable benefit.[9] Gabapentin is taken by mouth.[5]

Common side effects include sleepiness and dizziness.[5] Serious side effects include an increased risk of suicide, aggressive behavior, and drug reactions.[5] It is unclear if it is safe during pregnancy or breastfeeding.[10] Lower doses are recommended in those low kidney function.[5] Gabapentin is a gabapentinoid.[11] It has a molecular structure similar to that of the neurotransmitter γ-aminobutyric acid (GABA) and acts by inhibiting certain calcium channels.[12][11][13]

Gabapentin was first approved for use in 1993.[14][15] It has been available as a generic medication in the United States since 2004.[5] The wholesale price in the developing world as of 2015 was about US$10.80 per month;[16] in the United States, it was US$100 to US$200.[17] In 2017, it was the eleventh most commonly prescribed medication in the United States, with more than 46 million prescriptions.[18][19] During the 1990s, Parke-Davis, a subsidiary of Pfizer, began using a number of illegal techniques to encourage physicians in the United States to use gabapentin for unapproved uses.[20] They have paid out millions of dollars to settle lawsuits regarding these activities.[21]

References[edit]

  1. ^ Drugs.com international listings for Gabapentin Archived 16 February 2016 at the Wayback Machine Page accessed 9 February 2016
  2. ^ a b "Gabapentin Use During Pregnancy". Drugs.com. 2 December 2019. Archived from the original on 29 August 2017. Retrieved 21 December 2019.
  3. ^ a b c d e "Neurontin, Gralise (gabapentin) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 16 December 2014. Retrieved 6 April 2014.
  4. ^ a b c d e Goa KL, Sorkin EM (September 1993). "Gabapentin. A review of its pharmacological properties and clinical potential in epilepsy". Drugs. 46 (3): 409–427. doi:10.2165/00003495-199346030-00007. PMID 7693432.
  5. ^ a b c d e f g h "Gabapentin". The American Society of Health-System Pharmacists. Archived from the original on 19 August 2017. Retrieved 23 Oct 2015.
  6. ^ a b Wijemanne S, Jankovic J (June 2015). "Restless legs syndrome: clinical presentation diagnosis and treatment". Sleep Medicine. 16 (6): 678–90. doi:10.1016/j.sleep.2015.03.002. PMID 25979181.
  7. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 18 August 2020. Retrieved 2 September 2020.
  8. ^ Attal N, Cruccu G, Baron R, Haanpää 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–e88. doi:10.1111/j.1468-1331.2010.02999.x. PMID 20402746.
  9. ^ Wiffen PJ, Derry S, Bell RF, Rice AS, Tölle TR, Phillips T, Moore RA (June 2017). "Gabapentin for chronic neuropathic pain in adults". The Cochrane Database of Systematic Reviews. 6: CD007938. doi:10.1002/14651858.CD007938.pub4. hdl:10044/1/52908. PMC 6452908. PMID 28597471.
  10. ^ "Gabapentin Pregnancy and Breastfeeding Warnings". Archived from the original on 29 August 2017. Retrieved 13 March 2016.
  11. ^ a b Calandre EP, Rico-Villademoros F, Slim M (November 2016). "2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". Expert Review of Neurotherapeutics. 16 (11): 1263–1277. doi:10.1080/14737175.2016.1202764. PMID 27345098.
  12. ^ Sneader, Walter (2005). Drug Discovery: A History. John Wiley & Sons. pp. 219–220. ISBN 978-0-470-01552-0. Archived from the original on 8 September 2017. Retrieved 31 August 2017.
  13. ^ Uchitel OD, Di Guilmi MN, Urbano FJ, Gonzalez-Inchauspe C (2010). "Acute modulation of calcium currents and synaptic transmission by gabapentinoids". Channels. 4 (6): 490–6. doi:10.4161/chan.4.6.12864. PMID 21150315.
  14. ^ Pitkänen, Asla; Schwartzkroin, Philip A.; Moshé, Solomon L. (2005). Models of Seizures and Epilepsy. Burlington: Elsevier. p. 539. ISBN 978-0-08-045702-4. Archived from the original on 8 September 2017.
  15. ^ "Neurontin- gabapentin capsule Neurontin- gabapentin tablet, film coated Neurontin- gabapentin solution". DailyMed. 11 April 2019. Archived from the original on 7 July 2020. Retrieved 21 December 2019.
  16. ^ "Gabapentin". International Drug Price Indicator Guide. Archived from the original on 12 June 2018. Retrieved 13 March 2016.
  17. ^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 327. ISBN 978-1-284-05756-0.
  18. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  19. ^ "Gabapentin - Drug Usage Statistics". ClinCalc. 23 December 2019. Archived from the original on 11 April 2020. Retrieved 11 April 2020.
  20. ^ Henney JE (August 2006). "Safeguarding patient welfare: who's in charge?". Annals of Internal Medicine. 145 (4): 305–7. doi:10.7326/0003-4819-145-4-200608150-00013. PMID 16908923.
  21. ^ Stempel, Jonathan (2 June 2014). "Pfizer to pay $325 million in Neurontin settlement". Reuters. Archived from the original on 12 June 2018. Retrieved 11 June 2018.
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