Global InformationGabapentin information
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| Trade names | Neurontin, others[1] |
| Other names | CI-945; GOE-3450; DM-1796 (Gralise) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a694007 |
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| Dependence liability | Physical: High[3] Psychological: Moderate |
| Addiction liability | Low[4] |
| Routes of administration | By mouth |
| Drug class | Gabapentinoid |
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| Pharmacokinetic data | |
| Bioavailability | 27–60% (inversely proportional to dose; a high fat meal also increases bioavailability)[8][9] |
| Protein binding | Less than 3%[8][9] |
| Metabolism | Not significantly metabolized[8][9] |
| Elimination half-life | 5 to 7 hours[8][9] |
| Excretion | Kidney[8][9] |
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| ECHA InfoCard | 100.056.415 |
| Chemical and physical data | |
| Formula | C9H17NO2 |
| Molar mass | 171.240 g·mol−1 |
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Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat partial seizures and neuropathic pain.[7][10] It is commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain.[11] It is moderately effective: about 30–40% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a meaningful benefit.[12]
Sleepiness and dizziness are the most common side effects. Serious side effects include an increased risk of suicide, respiratory depression, and allergic reactions.[7] Lower doses are recommended in those with kidney disease.[7] Gabapentin acts by decreasing activity of a subset of calcium channels.[13][14][15]
Gabapentin was first approved for use in 1993.[16] It has been available as a generic medication in the United States since 2004.[17] In 2021, it was the tenth most commonly prescribed medication in the United States, with more than 47 million prescriptions.[18][19] During the 1990s, Parke-Davis, a subsidiary of Pfizer, used a number of illegal techniques to encourage physicians in the United States to prescribe gabapentin for unapproved uses.[20] They have paid out millions of dollars to settle lawsuits regarding these activities.[21]
- ^ Cite error: The named reference
Drugs.comwas invoked but never defined (see the help page). - ^ "Gabapentin Use During Pregnancy". Drugs.com. 2 December 2019. Retrieved 21 December 2019.
- ^ Tran KT, Hranicky D, Lark T, Jacob NJ (June 2005). "Gabapentin withdrawal syndrome in the presence of a taper". Bipolar Disorders. 7 (3): 302–4. doi:10.1111/j.1399-5618.2005.00200.x. PMID 15898970.
- ^ Schifano F (June 2014). "Misuse and abuse of pregabalin and gabapentin: cause for concern?". CNS Drugs. 28 (6): 491–496. doi:10.1007/s40263-014-0164-4. PMID 24760436.
- ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
- ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
- ^ a b c d Cite error: The named reference
Neurontin labelwas invoked but never defined (see the help page). - ^ 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.
- ^ 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. S2CID 265753780.
- ^ Cite error: The named reference
NICEwas invoked but never defined (see the help page). - ^ Attal N, Cruccu G, Baron R, Haanpää M, Hansson P, Jensen TS, et al. (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. PMID 20402746. S2CID 14236933.
- ^ Cite error: The named reference
Wiffen2017was invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid32521436was invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid23642658was invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid32321743was invoked but never defined (see the help page). - ^ Pitkänen A, Schwartzkroin PA, Moshé SL (2005). Models of Seizures and Epilepsy. Burlington: Elsevier. p. 539. ISBN 978-0-08-045702-4. Archived from the original on 8 September 2017.
- ^ Cite error: The named reference
Reed2012was invoked but never defined (see the help page). - ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Gabapentin – Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ 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. PMID 16908923. S2CID 39262014.
- ^ Stempel J (2 June 2014). "Pfizer to pay $325 million in Neurontin settlement". Reuters. Retrieved 11 June 2018.