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Gabapentin

Gabapentin
Gabapentin2DACS.svg
Gabapentin 3D.png
Clinical data
Trade names Neurontin, others
AHFS/Drugs.com Monograph
MedlinePlus a694007
License data
Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
Routes of
administration
By mouth
ATC code N03AX12 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability 27–60% (inversely proportional to dose; a high fat meal also increases bioavailability)
Protein binding Less than 3%
Metabolism Not significantly metabolised
Biological half-life 5 to 7 hours
Excretion Renal
Identifiers
CAS Number 60142-96-3 YesY
PubChem (CID) 3446
IUPHAR/BPS 5483
DrugBank DB00996 YesY
ChemSpider 3328 YesY
UNII 6CW7F3G59X YesY
KEGG D00332 YesY
ChEBI CHEBI:42797 YesY
ChEMBL CHEMBL940 YesY
PDB ligand ID GBN (PDBe, RCSB PDB)
ECHA InfoCard 100.056.415
Chemical and physical data
Formula C9H17NO2
Molar mass 171.237 g/mol
3D model (Jmol) Interactive image
  

Gabapentin (GPN) marketed under the brand name Neurontin among others, is a medication used to treat epilepsy, neuropathic pain, hot flashes, and restless leg syndrome. In epilepsy it may be used for those with partial seizures. It is recommended as one of a number of first line medications for the treatment of neuropathic pain in diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain. A 2014 review of its use for diabetic neuropathy and postherpetic neuralgia found about 14% of people have a meaningful benefit.

Common side effects include sleepiness and dizziness. Serious side effects may include an increased risk of suicide, aggressive behaviour, and drug reaction with eosinophilia and systemic symptoms. It is unclear if it is safe during pregnancy or breastfeeding. Lower doses should be used in people with kidney problems. Gabapentin affects the inhibitory neurotransmitter γ-aminobutyric acid (GABA) but how it works is otherwise unclear.

Gabapentin was first approved for use in 1993. The wholesale price in the developing world is about US$40.50 per month. In the United States it has been available as a generic medication since 2004. As of 2015 the cost for a typical month of medication in the United States is US$100 to US$200. During the 1990s Parke-Davis, a sub-company of Pfizer, used a number of techniques to encourage physicians in the United States to use gabapentin for unapproved uses.



  • AU: B1
  • US: C (Risk not ruled out)
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Wikipedia

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