GABAPENTIN

USDailyMed:Gabapentin AU:B1 PrototypicalGabapentinoidAnticonvulsantGABA analogue N02BF01(WHO) AU:S4(Prescription only)BR:Class C1(Other controlled substances)CA:℞-onlyUK:Class CUS:Schedule V controlled substance(Select States)SE: Rx-onlyIn general: Prescription only SE: Rx-onlyIn general: Prescription only 2-[1-(Aminomethyl)cyclohexyl]acetic acid 60142-96-3 3446 5483 DB00996 3328 6CW7F3G59X D00332 CHEBI:42797 ChEMBL940 GBN (PDBe,RCSB PDB) DTXSID0020074 Interactive image 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)Key:UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin, sold under the brand nameNeurontinamong others, is ananticonvulsantmedication used to treatneuropathic pain(postherpetic neuralgia) andpartial seizuresofepilepsy.Gabapentin is acentra‍‍‍‍‍‍​​​‍​​​​​​l nervous system(CNS)depressantand derivative of the inhibitory neurotransmitter,GABA.It is used for the treatment of neuropathic pain caused bydiabetic neuropathy,postherpetic neuralgia, andcentral pain.It is moderately effective: about 30–40% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a meaningful benefit. Gabapentin binds toα2δsubunits to modulatecalcium channelfunction andneurotransmitterrelease, weakly affectsglutamate, and does not act on GABA receptors.Sleepiness anddizzinessare the most commonside effects. Serious side effects includerespiratory depressionandallergic reactions.On December 16, 2008, the FDA issued gabapentin a class warning for an increased risk of suicide.Approximately two years after this pronouncement, a pharmacoepidemiologic study was conducted that showed there was no outstanding difference in suicide attempt rates between pre- and post- gabapentin prescription groups. Gabapentin was first approved for use in the United Kingdom in 1993.It has been available as ageneric medicationin the United States since 2004.It is the first of several other drugs that are similar in structure and mechanism, calledgabapentinoids. In 2023, it was the ninth most commonly prescribed medication in the United States, with more than 45million prescriptions.During the 1990s,Parke-Davis, a subsidiary ofPfizer, used several illegal techniques to encourage physicians in the United States to prescribe gabapentin forunapproveduses.They have paid out millions of dollars to settle lawsuits regarding these activities.