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Gabapentin
Gabapentin
Neurontin, Gralise, Gabarone, Gabbies
Gabapentin is a depressant substance of the gabapentinoid class and a structural analogue of the neurotransmitter GABAcitation needed. Originally developed in the 1970s to treat epilepsy, it was first approved in the United States in 1993 and is now widely prescribed for neuropathic pain, postherpetic neuralgia, and partial-onset seizures1. Its anxiolytic, sedative, and mildly euphoriant properties have led to recreational usecitation needed, though tolerance is known to develop rapidly.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold~200 mg
Light200-600 mg
Moderate600-900 mg
Strong900-2400 mg
Heavy2400+ mg
Bioavailability
27-80%
Gabapentin exhibits dose-dependent oral bioavailability that decreases at higher amounts owing to saturation of intestinal amino acid transporters. Splitting a total dose into smaller portions taken at 30- to 45-minute intervals can improve absorption relative to a single large dose. Tolerance to the anxiolytic effects typically develops during continuous use and generally resolves within one to two weeks after discontinuation.
Duration
Onset30-120 minutes
Peak2-3 hours
After Effects1-6 hours
Total6-10 hours
Half-life
5-7 hours
Subjective Effects
Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.
Effects vary widely by individual, dose, and context.
Physical
Cognitive
Pharmacology
Pharmacodynamics
Gabapentin primarily acts by binding to the α2δ-1 subunit of voltage-gated calcium channels.citation needed Rather than directly blocking the channel pore, it disrupts the trafficking of calcium channel complexes to the presynaptic membrane, reducing excitatory neurotransmitter release. Gabapentin also competitively inhibits branched-chain aminotransferase (BCAT-1), slowing glutamate synthesis, and modulates glutamate decarboxylase, with neuroimaging studies showing it increases cerebral GABA concentrations by up to 79% from baseline. Despite its structural similarity to GABA, it does not convert to GABA in vivo and does not function as a GABA receptor agonist, though antagonist activity at GABA-B receptor subunits has been separately reported. Secondary targets include KCNQ3 and KCNQ5 potassium channels2 and the adenosine A1 receptor, though the clinical relevance of these interactions remains unclear.
Pharmacokinetics
Gabapentin undergoes virtually no hepatic metabolism, with less than 1% of an administered dose recovered as metabolites.citation needed It is eliminated almost entirely as unchanged drug in the urine, with clearance directly proportional to creatinine clearance.3 Absorption occurs through a saturable amino acid transporter (LAT) in the intestines, resulting in dose-dependent oral bioavailability that decreases substantially at higher doses (approximately 80% at 100 mg per dose down to 27% at 1600 mg per dose).citation needed Gabapentin crosses the blood-brain barrier via the LAT1 transporter,4 achieving cerebrospinal fluid concentrations of approximately 9-14% of plasma levels. Plasma protein binding is minimal (less than 3%).3
Metabolitesnone documented yet
Dangerous
Highest riskThese combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.
DepressantsOpioids
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
1,2-BenzodiazepineAcetazolamideAcetophenazineAgomelatineAlfentanil
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Full Tolerance
Tolerance to anxiolytic and euphoric effects can build rapidly with repeated dosing, sometimes after several days in a row. Reported recreational benefits may fade quickly, with repeat doses producing much smaller returns even during the same session.
Baseline Reset
Tolerance returns to baseline within 7-14 days after cessation of use.
Harm Potential
Addiction & Dependence
Psychological
LowGabapentin is not considered psychologically addictive and demonstrates limited to no rewarding effects in human and animal experiments.citation needed Compulsive drug-seeking behavior and strong cravings are generally not observed, unlike with opioids, alcohol, or benzodiazepines. However, misuse does occur, particularly among individuals with a history of opioid or sedative abuse who may use it to boost opioid effects or manage withdrawal symptoms.
Physical
ModeratePhysical dependence develops with chronic use, with withdrawal symptoms typically emerging 1-2 days after abrupt cessationcitation needed and potentially lasting up to 45 days. Withdrawal symptoms are similar to, though generally less intense than, benzodiazepine withdrawal and include agitation, confusion, disorientation, gastrointestinal complaints, sweating, and less commonly tremor, tachycardia, hypertension, and insomnia. Withdrawal seizures have been reported following chronic use without periodic breaks. Gradual tapering is recommended.5
Toxicity
Cardiovascular
Prolonged gabapentinoid use exceeding one year has been associated with increased risk of cardiovascular events and thrombotic events including deep venous thrombosis and pulmonary thromboembolism; thrombotic risk may emerge as early as three months of use.6
Immunological
Rare cases of drug reaction with eosinophilia and systemic symptoms (DRESS), a potentially fatal multi-organ hypersensitivity reaction, have been reported with gabapentin use.citation needed
Renal
Gabapentin may accumulate in patients with renal impairment, potentially leading to increased toxicity due to diminished clearance rather than direct nephrotoxicity; careful dosing is required in those with kidney problems.citation needed
Reproductive
Sexual dysfunction including loss of libido, anorgasmia, and erectile dysfunction may occur in some patients during gabapentin use.citation needed
Respiratory
Serious breathing suppression may occur when gabapentin is taken by individuals with underlying lung conditions such as COPD, independent of combination with other substances.citation needed
Psychosis Risk
Psychiatric and behavioral adverse effects including hallucinations and psychosis can occur but are rare, primarily affecting pediatric populations and individuals with preexisting psychiatric conditions.citation needed Milder neuropsychiatric symptoms including confusion, depression, mood instability, aggression, agitation, and behavioral disturbances may occur in up to 29% of gabapentin users, though most reactions are mild to moderate and dose-dependent. The FDA has issued warnings regarding increased risk of suicidal thoughts and behaviors;7 some studies suggest approximately 40% increased risk of suicide or suicide attempt compared to other anticonvulsants, particularly in patients with bipolar disorder or epilepsy,citation needed though conflicting data exists with some studies showing reduced suicide rates in certain populations.
Seizure Risk
Gabapentin is an anticonvulsant that reduces seizure activity during use. However, withdrawal seizures may occur in some cases following chronic or semi-chronic use when the drug is discontinued abruptly, particularly in the absence of periodic breaks during repeated consecutive use.citation needed Gradual tapering is recommended to minimize withdrawal seizure risk.
History & Culture
Discovery and Development
Gabapentin was conceived and synthesized at Goedecke AG, a Parke-Davis subsidiary located in Freiburg, Germany.citation needed The compound was designed as a structural analog of gamma-aminobutyric acid (GABA) with enhanced capacity to penetrate the blood-brain…
Legality
By Country
Controlled / restricted3
ThailandRestrictedNotification of the Ministry of Public Health Re: Dangerous Drugs (as amended through No. 36), issued under the Drug Act B.E. 251048495051
Gabapentin is classified in Thailand as a dangerous drug (ยาอันตราย), rather than as an unrestricted over-the-counter medicine. The current Dangerous Drugs notification covers antiepileptic and anticonvulsant drugs other than specially controlled drugs or psychotropic substances, and the Thai FDA's current product record specifically classifies a gabapentin product in that category. Its retail supply is therefore subject to the Drug Act's licensed dangerous-drug sale regime rather than the licence limited to ready-packed drugs that are not dangerous drugs or specially controlled drugs.
United Arab EmiratesRestrictedMOHAP Controlled and Semi-Controlled Medicines List53
Gabapentin is listed as a controlled drug in the United Arab Emirates. Its supply is therefore subject to the Ministry of Health and Prevention's controlled-medicines requirements.
Prescription25
United StatesPrescription onlyGabapentin is a prescription drug in the United States. Its current FDA label states that it is not a controlled substance, and it is not listed in the federal controlled-substance schedules in 21 CFR Part 1308. State controlled-substance scheduling and prescription-monitoring requirements vary by jurisdiction.
By state
Across the 50 states, D.C., and the permanent territories, most jurisdictions treat gabapentin consistently with federal prescription-drug law, while some jurisdictions schedule it as a controlled substance or impose prescription-monitoring requirements beyond the federal baseline.
AlabamaRestrictedAlabama State Board of Health, Controlled Substances List, Schedule V60
Alabama classifies gabapentin as a Schedule V controlled substance. It is therefore subject to the state controlled-substances regime rather than only the ordinary prescription-drug rules that apply federally.
ArkansasRestricted
ConnecticutRestrictedConnecticut requires gabapentin dispensing information to be uploaded to the Connecticut Prescription Monitoring and Reporting System. Gabapentin is not listed in Connecticut's controlled-substance schedules, but the drug-specific reporting requirement creates an additional state control.
DelawareNot scheduledDelaware Uniform Controlled Substances Act, 16 Del. C. §§ 4712, 4714–472265
Delaware’s controlled-substances schedules consist of the substances listed in 16 Del. C. §§ 4714, 4716, 4718, 4720, and 4722. The current Schedule V covers limited narcotic preparations and buprenorphine, not gabapentin; this instrument does not classify gabapentin as a Delaware controlled substance.
District of ColumbiaRestrictedThe District does not list gabapentin in its controlled-substance schedules, but DC Health identifies gabapentin as a drug of concern reported to the Prescription Drug Monitoring Program. Dispensing of a covered substance is reportable to the Program under District law. This creates a District-specific monitoring control beyond ordinary federal prescription-only treatment.
IllinoisRestrictedIllinois Prescription Monitoring Program, current Drugs of Interest list69
Illinois designates gabapentin as a Prescription Monitoring Program drug of interest. Illinois pharmacies and dispensing practitioners must report drugs of interest to the state program, although gabapentin is not placed in an Illinois controlled-substance schedule.
IndianaRestrictedInd. Code §§ 25-26-24-2.5, 25-26-24-3, and 25-26-24-17 (Indiana Scheduled Prescription Electronic Collection and Tracking program)707172
Indiana Code § 25-26-24-2.5 includes gabapentin in the definition of controlled substance for the INSPECT chapter. Under §§ 25-26-24-3 and 25-26-24-17, dispensers must submit controlled-substance prescription data to INSPECT. This chapter-specific inclusion does not place gabapentin in Indiana's controlled-substance schedules or change its prescribing status.
KansasRestricted
KentuckyRestricted902 KAR 55:015 § 5(2)75
Gabapentin is a Schedule V controlled substance in Kentucky. Its designation subjects the drug to Kentucky controlled-substance regulation in addition to its federal prescription-only status.
MassachusettsRestrictedGabapentin is a Schedule VI prescription drug in Massachusetts rather than a Schedule I–V controlled substance. Massachusetts nevertheless designates it as an additional drug for Prescription Monitoring Program reporting, so pharmacies must report its dispensations.
MinnesotaRestricted
MississippiRestricted
MontanaRestricted
New JerseyRestrictedGabapentin remains a prescription drug rather than a New Jersey controlled dangerous substance. Pharmacies filling outpatient gabapentin prescriptions must collect and electronically transmit prescription information to the State's Prescription Monitoring Program daily. This reporting obligation is a state-specific control beyond federal prescription-only treatment.
New MexicoRestrictedNew Mexico does not classify gabapentin as a controlled substance. The Board of Pharmacy designates it as a drug of concern and requires Prescription Monitoring Program reporting in the same manner as controlled-substance dispensing, except for veterinary prescriptions. This creates a state reporting control in addition to ordinary prescription status.
North CarolinaRestrictedGabapentin is not a controlled substance in North Carolina. Dispensers must report gabapentin dispensations to the Controlled Substances Reporting System; the requirement took effect for most dispensers on March 1, 2024 and for veterinary dispensers on March 1, 2025. The reporting rule is a state-specific restriction beyond federal prescription-only treatment.
North DakotaRestrictedN.D. Cent. Code § 19-03.1-13(5)(g)90
North Dakota lists gabapentin as a Schedule V controlled substance in its Uniform Controlled Substances Act. The listing covers material, compounds, mixtures, or preparations containing any quantity of gabapentin, including applicable salts and isomers, unless specifically exempted, excluded, or listed in another schedule.
OhioRestrictedEffective November 15, 2022, Ohio Administrative Code 4729:5-5-08(D) requires a pharmacist to request and review an OARRS report before dispensing an outpatient drug containing gabapentin in specified circumstances, including new therapy or no review within the preceding 12 months. Separately, Ohio Administrative Code 4729:8-2-02 requires submission of dispensing information for all dangerous-drug products containing gabapentin to the State Board of Pharmacy. These are monitoring and review requirements for drugs containing gabapentin; the rules do not themselves create a controlled-substance schedule designation.
OregonRestrictedORS 431A.855(1)(a)(B) and ORS 431A.860(1)93
Oregon’s Prescription Monitoring Program expressly includes prescribed gabapentin dispensed by pharmacies, separately from drugs classified in schedules II through V. A pharmacy must electronically report a prescription drug subject to that program no later than 72 hours after dispensing; this is a reporting requirement, not a state controlled-substance scheduling designation.
TennesseeRestrictedTennessee classifies gabapentin as a Schedule V controlled substance. Accordingly, gabapentin is subject to Tennessee's controlled-substance framework rather than only the federal prescription-drug framework. The state Department of Health states that all gabapentin products have been Schedule V substances since July 1, 2018.
UtahRestricted
VirginiaRestrictedVirginia lists gabapentin [1-(aminomethyl)cyclohexaneacetic acid] as a Schedule V depressant substance. The listing covers material, compounds, mixtures, or preparations containing any quantity of gabapentin unless specifically excepted or listed in another schedule; HB 2557 added the listing effective July 1, 2019.
West VirginiaRestrictedWest Virginia classifies gabapentin as a Schedule V controlled substance. The drug is therefore regulated under the state's controlled-substances framework rather than only under federal prescription-drug law. Gabapentin appears by name in the Schedule V list of other substances.
WisconsinRestrictedWisconsin does not schedule gabapentin as a controlled substance, but the Controlled Substances Board identifies it as a drug with substantial potential for abuse. Gabapentin is consequently a monitored prescription drug for the state PDMP, and dispensers must compile and electronically submit its dispensing data unless an exemption applies. This monitoring regime is a state-specific restriction beyond ordinary federal prescription-only treatment.
WyomingRestricted059-8 Wyo. Code R. § 8-5(b)-(c)105
Wyoming lists gabapentin as a non-controlled substance for which dispensers must report the Chapter 8 information to the Prescription Monitoring Program Clearinghouse. The report is due no later than close of business on the next business day after dispensing; this reporting rule does not place gabapentin in a controlled-substance schedule.
AustriaPrescription onlyBASG Fachinformation for Gabapentin 1A Pharma 300 mg/400 mg Hartkapseln16
Gabapentin 1A Pharma 300 mg and 400 mg hard capsules are authorised medicinal products in Austria. The current BASG product information identifies the 300 mg product as authorisation number 1-27113 and states that both strengths are prescription- and pharmacy-only.
BelgiumPrescription onlyFAGG/AFMPS authorised product information17
Gabapentin is supplied on medical prescription in Belgium. The federal medicines agency's authorised product leaflet states that the medicine is available on prescription.
BrazilPrescription onlyGabapentin is listed as Gabapentina in Lista C1 of ANVISA's current consolidated Portaria SVS/MS no. 344/1998. Lista C1 substances require a Receita de Controle Especial in two copies; dispensing is restricted to pharmacies or drugstores and requires that prescription, with the first copy retained by the dispensing establishment.
Czech RepublicPrescription onlySÚKL Přehled léčiv product record for GABAGAMMA 100MG CPS DUR 100 (SÚKL code 0126157)22
The current SÚKL Přehled léčiv record for GABAGAMMA 100MG CPS DUR 100 identifies GABAPENTIN as its active substance and gives its dispensing code as R, meaning a medicinal product subject to medical prescription. The product holds a valid marketing authorisation, and the prescription requirement applies to that authorised gabapentin medicine.
DenmarkPrescription onlyDanish Medicines Agency prescription-medicines list23
Gabapentin is a prescription medicine in Denmark. The Danish Medicines Agency lists gabapentin among prescription medicines with general reimbursement.
FrancePrescription onlyBase de données publique des médicaments24
Gabapentin is supplied only on prescription in France. The public medicines database records the prescription-only supply condition for authorised gabapentin products.
IrelandPrescription onlyMedicinal Products (Prescription and Control of Supply) Regulations 2003 (S.I. No. 540/2003), regulation 5 and First Schedule; HPRA authorised-medicine record for Neurontin 400 mg hard capsules2829
Gabapentin is subject to prescription control in Ireland. The First Schedule to the Medicinal Products (Prescription and Control of Supply) Regulations 2003 lists gabapentin in Part B, and regulation 5 provides that a medicinal product containing a listed substance may not be supplied except in accordance with a prescription, subject to the stated exceptions. The current HPRA record for authorised Neurontin 400 mg hard capsules identifies gabapentin as the active substance and gives its legal supply status as a product subject to prescription which may be renewed (B).
ItalyPrescription onlyAIFA's current Banca Dati Farmaci record identifies Gabapentin EG 300 mg hard capsules as containing gabapentin and records the supply class RNR, described as medicines subject to medical prescription to be renewed. The listed package is authorised and marketed as a prescription-only medicine in Italy.
JapanPrescription onlyMHLW Notice No. 24 of 2005 under Article 49(1) of the Act on Securing Quality, Efficacy and Safety of Products Including Pharmaceuticals and Medical Devices3435
Gabapentin is a prescription medicine in Japan. Ministry of Health, Labour and Welfare Notice No. 24 of 2005 lists gabapentin among the medicines designated under Article 49(1) of the pharmaceuticals law. PMDA's current approved Gabapen Tablets package insert classifies the product as 処方箋医薬品 and directs that it be used on the prescription of a physician or other practitioner.
NetherlandsPrescription onlyGeneesmiddeleninformatiebank authorised-medicine record36
Gabapentin is a prescription-only medicine in the Netherlands. The official medicines-information database classifies the authorised product with the UR supply status.
New ZealandPrescription onlyMedicines Act 1981; Medsafe medicine information37
Gabapentin is a prescription medicine in New Zealand. Medsafe's current medicine information identifies gabapentin as prescription medicine.
NorwayPrescription onlyLegemiddelsøk medicine register38
Gabapentin is prescription-only in Norway. The official medicine register marks the authorised product as prescription-required and places it in prescription group C.
RussiaPrescription onlyState Register of Medicines record for Gabapentin-LEXVM (ЛП-№(015722)-(РГ-RU))39
Gabapentin is registered in Russia as a prescription medicine. The State Register of Medicines records Gabapentin-LEXVM capsules as dispensed by prescription.
SingaporePrescription onlyHealth Sciences Authority National Drug Formulary product record: ALPENTIN CAPSULE 100MG (SIN16698P)40
Singapore’s Health Sciences Authority National Drug Formulary lists ALPENTIN CAPSULE 100MG with gabapentin 100 mg as its active ingredient and classifies that registered product as a prescription-only medicine. This prescription-only classification applies to the listed registered product and is not a separate controlled-drug classification.
South KoreaPrescription onlyMFDS Integrated Drug Information System product record41
Gabapentin is classified as a prescription drug (전문의약품) in South Korea. The Ministry of Food and Drug Safety's current product record for Ganutin Capsule 300 mg identifies gabapentin as its active ingredient and classifies the product as a prescription drug.
SpainPrescription onlyAEMPS CIMA medicines-register records for Gabapentina Almus products42
AEMPS CIMA's current medicines-register response identifies Gabapentina Almus 300 mg and 400 mg hard capsules and 600 mg and 800 mg film-coated tablets as gabapentin products. Each record gives the dispensing classification ‘Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración’ and marks the product as requiring a prescription (receta: true); all four records are marked as marketed (comerc: true).
SwedenPrescription onlyLäkemedelsverket Läkemedelsfakta43
Gabapentin is a prescription medicine in Sweden. The Swedish Medical Products Agency's medicine record marks authorised gabapentin products as prescription-only.
UkrainePrescription onlyState Register of Medicinal Products of Ukraine52
Gabapentin 400 mg capsules are registered in Ukraine in the State Register of Medicinal Products. The register records their dispensing condition as "за рецептом" (by prescription), so supply is prescription-only.
References
Source Pages
Citations
- NEURONTIN (gabapentin) Prescribing Information. DailyMed, National Library of Medicine (2025). https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=97935fd9-1d4a-43b6-a5d9-de994591187b&type=display1
- Rían W. Manville, & Geoffrey W. Abbott. (October 2018). Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels. Molecular Pharmacology, 94(4), 1155–1163. https://doi.org/10.1124/mol.118.1129531
- Neurontin (gabapentin) Prescribing Information. Pfizer Inc. (n.d.). https://labeling.pfizer.com/showlabeling.aspx?id=63012
- David Dickens, Steven D Webb, Svetlana Antonyuk, Athina Giannoudis, Andrew Owen, Steffen Rädisch, S Samar Hasnain, & Munir Pirmohamed. (June 2013). Transport of gabapentin by LAT1 (SLC7A5). Biochemical Pharmacology, 85(11), 1672–1683. https://doi.org/10.1016/j.bcp.2013.03.0221
- Kien T Tran, Diane Hranicky, Tracey Lark, & Nj Jacob. (June 2005). Gabapentin withdrawal syndrome in the presence of a taper. Bipolar Disorders, 7(3), 302–4. https://doi.org/10.1111/j.1399-5618.2005.00200.x1
- Deep Dutta, Ritin Mohindra, Manoj Kumar, Mainak Banerjee, Meha Sharma, & Satinath Mukhopadhyay. (Apr 2025). Cardiovascular safety of gabapentinoids gabapentin & pregabalin: A systematic review.. Indian J Med Res, 161(4), 363–374. https://doi.org/10.25259/ijmr_1990_202412
- NEURONTIN (gabapentin) Prescribing Information. Pfizer Inc. (2017). https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=798575b9-ddfa-4915-9574-626abbaf025f12
- Gabapentinoids and Risk for Severe Exacerbation in Chronic Obstructive Pulmonary Disease: A Population-Based Cohort Study. Annals of Internal Medicine, 177(Online ahead of print), 144–154 (January 2024). https://doi.org/10.7326/m23-08491
- Gabapentin — Chemistry World Podcast. Chemistry World (Royal Society of Chemistry) (n.d.). https://www.chemistryworld.com/podcasts/gabapentin/1017577.article1
- Peckham AM, Evoy KE, Ochs L, & Covvey JR. (2018). Gabapentin for Off-Label Use: Evidence-Based or Cause for Concern?. Substance Abuse: Research and Treatment. https://doi.org/10.1177/117822181880131112
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Recent changes8 human edits · latest
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26 August 2026
Lyrea · Changed a word in Dosage & Duration › Routes 1 › Bioavailability
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Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
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