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Pregabalin
3-Isobutyl GABA
Lyrica, Nervalin, Pregab
Pregabalin is a depressant and anxiolytic substance of the gabapentinoid class, structurally related to GABA.1 First synthesized in 1989 and was approved under the trade name Lyrica in 2004,2 it is commonly prescribed for neuropathic pain345, anxiety67, epilepsy8, and fibromyalgia.9 Compared to the related compound gabapentin, pregabalin offers greater bioavailability and potency.10 It is also used recreationally for its reported euphoric, anxiolytic, and pro-social properties.11
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold~25 mg
Light25-150 mg
Moderate150-300 mg
Strong300-600 mg
Heavy600+ mg
Bioavailability
≥90%
Peak plasma serum is greatly reduced and time to max plasma serum is greatly increased by consumption of food12 which reduces the experienced effects, but total bioavailability is not affected.
Duration
Onset30-120 minutes
Come Up1-2 hours
Peak2-4 hours
Offset3-6 hours
After Effects6-24 hours
Total6-12 hours
Half-life
6.3 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
The physical effects of pregabalin can be broken down into several components which progressively intensify proportional to dosage.
Cognitive
Pregabalin's headspace is comparable to a more clear-headed alcohol or benzodiazepine intoxication, although it can take a more dissociative turn at very high dosages.
Visual
Pharmacology
Pharmacodynamics
Pregabalin acts by binding to the α2δ subunit of presynaptic voltage-gated calcium channels in the central nervous system, with similar affinity for both the α2δ-1 and α2δ-2 subtypes.13 Despite being a structural analogue of GABA, pregabalin does not bind directly to GABA-A, GABA-B, or benzodiazepine receptors and does not alter brain GABA concentrations.14 Through its α2δ binding, pregabalin reduces the release of several excitatory neurotransmitters including glutamate, substance P, norepinephrine, acetylcholine, and calcitonin gene-related peptide.citation needed It also reduces the normal trafficking of calcium channels to the cell membrane and blocks thrombospondin-mediated formation of new excitatory synapses in animal models.
Pharmacokinetics
Pregabalin has high oral bioavailability (≥90%) with linear pharmacokinetics, reaching peak plasma concentrations within 1.5 hours.15 It undergoes negligible metabolism, with approximately 98% excreted unchanged in the urine via renal elimination.citation needed Its elimination half-life is approximately 6.3 hours, and steady state is achieved within 24 to 48 hours of repeated dosing.16
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.
GHB/GBLNBOMe compoundsOpioids
Unsafe
AvoidThere is considerable risk of physical harm when taking these combinations, they should be avoided where possible.
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.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Full Tolerance
Tolerance to the euphoric and depressant effects develops relatively quickly with repeated recreational use, often within several uses. At medical doses for conditions such as generalized anxiety disorder, long-term trials have demonstrated continued effectiveness without significant tolerance development. However, in recreational settings where higher doses are used, tolerance builds rapidly, sometimes leading users to escalate to doses exceeding 1 gram daily.
Baseline Reset
Tolerance returns to baseline within 7 to 14 days after cessation of use.
Harm Potential
Addiction & Dependence
Psychological
ModerateInitially assessed as having low abuse potential, recreational use has prompted re-evaluation.citation needed Euphoric effects can lead to escalating doses above therapeutic ranges, particularly in individuals with current or past substance use disorders. At standard therapeutic doses the risk of addiction is low, but increases with higher doses and prolonged use.
Physical
ModeratePhysical dependence can develop with chronic use, though the FDA determined the dependence profile is quantitatively less severe than benzodiazepines.citation needed Withdrawal symptoms after abrupt discontinuation include anxiety, insomnia, sweating, muscle spasms, gastrointestinal disturbances, palpitations, and flu-like symptoms. Even short-term users have reported withdrawal effects. Gradual tapering over at least one week is recommended.
Toxicity
Respiratory
Respiratory depression can occur, particularly when combined with opioids or other CNS depressants, or in individuals with pre-existing lung conditions; the effect is less pronounced than with opioids or benzodiazepines when pregabalin is used alone.citation needed
Cardiovascular
Prolonged use beyond one year has been associated with increased risk of thrombotic events including deep venous thrombosis and pulmonary embolism; heart failure risk does not appear elevated.citation needed
Renal
Kidney damage is listed among serious side effects; patients with pre-existing renal impairment may accumulate the drug and develop myoclonus due to reduced clearance.citation needed
Musculoskeletal
Elevated creatine kinase levels occur commonly; rhabdomyolysis and myositis have been reported rarely, primarily with prolonged high-dose use.citation needed
Hematologic
Thrombocytopenia occurs infrequently and neutropenia rarely; these effects are generally identified through routine monitoring rather than clinical symptoms.citation needed
Psychosis Risk
Psychotic side effects including hallucinations and confusion occur in a minority of users even at therapeutic doses19and pregabalin is strongly associated with delirium in patients older than 60.20 Sleep deprivation strongly potentiates this risk, and individuals genetically predisposed to schizophrenia may be more susceptible. Hallucinations are reported in 0.1-1% of users.21
Seizure Risk
Paradoxically, despite being an anticonvulsant, pregabalin may induce or increase seizure risk at recreational doses exceeding 600mg. There is little evidence of concern at medical doses. The drug may aggravate myoclonus and myoclonic seizures in susceptible populations.22 Risk factors include low sodium, sleep deprivation, and intensive physical activity.
History & Culture
Discovery and Synthesis
Pregabalin emerged from research conducted at Northwestern University in Evanston, Illinois. In 1988, medicinal chemist Richard Silverman enlisted the help of Dr. Ryszard Andruszkiewicz, a visiting scholar from the Technical University of Gdańsk, to synthesize a series of 3-alkyl-GABA and…
Legality
International
Pregabalin does not appear in the current schedules to the 1961 Single Convention, the 1971 Convention on Psychotropic Substances, or Tables I and II of the 1988 Convention. It is not internationally scheduled under those three conventions.
By Country
Illegal1
United StatesIllegalClassified under Schedule V of the Controlled Substances Act, indicating low potential for abuse relative to Schedule IV substances such as benzodiazepines. Illegal to sell without a DEA license and illegal to possess without a valid prescription.83
By state
Across the 50 states, D.C., and the permanent territories, most jurisdictions treat Pregabalin consistently with federal control; listed entries record independently verified differences in state classification or coverage.
AlaskaNot scheduled
DelawareNot scheduled
VermontNot scheduled18 V.S.A. § 4215a88
Vermont's statutory Schedule V list does not name pregabalin. The list consists of limited-quantity narcotic preparations, so pregabalin has no Vermont Schedule V designation under that statute. This state classification does not alter federal Schedule V control.
Controlled / restricted8
BelgiumRestrictedRoyal Decree of 6 September 2017 regulating narcotic and psychotropic substances, as amended by the Royal Decree of 15 March 2026303132
Since 19 July 2026, pregabalin has been listed in Annexe IVB to Belgium's Royal Decree of 6 September 2017 regulating narcotic and psychotropic substances. The listing subjects pregabalin to the decree's controlled-substance regime, and a pharmacist may supply a medicine containing it to the public only on a lawfully obtained, signed and dated medical prescription.
RussiaRestrictedMinistry of Health Order No. 459н of 1 September 2023, Section II, as amended by Order No. 653н of 28 October 20255657
Pregabalin is expressly listed in Section II of Russia's list of medicinal products subject to quantitative accounting (предметно-количественный учет, ПКУ). Section II covers pharmaceutical substances and medicinal products included in the potent and poisonous substances lists under Government Resolution No. 964 for Criminal Code Article 234 purposes; its scope is medical-use pharmaceutical substances and medicinal products, not every product generally. Order No. 653н took effect on 1 March 2026 and amends Section II by inserting prasterone after the retained pregabalin entry, so pregabalin remains on the operative list.
ThailandRestrictedNotification of the Ministry of Public Health Re: Dangerous Drugs, item 27 (signed 26 May 1978; current Thai FDA consolidation through amendment No. 36)6970717273
The Thai FDA's current Dangerous Drugs consolidation retains item 27, signed 26 May 1978, for antiepileptic or anticonvulsant drugs except those separately declared specially controlled drugs or psychotropic substances. The FDA's registered-drug database identifies pregabalin products, and an FDA-hosted approved pregabalin product document describes anticonvulsant effects and an epilepsy indication. The current FDA specially controlled-drugs consolidation does not list pregabalin, and the FDA's controlled-psychotropic-substances table, updated 25 July 2025, does not list pregabalin; pregabalin medicinal products within item 27's therapeutic scope are therefore dangerous drugs, rather than prescription-only or psychotropic substances. This classification does not establish a rule for unregistered products.
United KingdomRestrictedMisuse of Drugs Act 1971, Class C; Misuse of Drugs Regulations 2001 and Misuse of Drugs Regulations (Northern Ireland) 2002, Schedule 3787980
Pregabalin has been a Class C controlled drug under the Misuse of Drugs Act 1971 since 1 April 2019. It is listed in Schedule 3 to the Misuse of Drugs Regulations 2001 in Great Britain and in Schedule 3 to the Misuse of Drugs Regulations (Northern Ireland) 2002. Possession, production, supply, and prescribing are subject to the applicable controlled-drugs regime and its statutory exemptions.
Prescription21
AustriaPrescription onlyAustria's current Rezeptpflichtverordnung lists PREGABALIN as RP in Anlage A, Humanarzneimittel, Teil 2. The schedule defines RP as rezeptpflichtig (prescription-only) and states that Part 2 covers chemically defined active ingredients and, unless expressly stated otherwise, their salts, esters, and salts of esters. Pregabalin has no exception marker in that entry, so the prescription classification applies at the substance level rather than only to a particular product. RIS identifies the consolidated regulation as last amended by BGBl. II Nr. 282/2025, promulgated on 10 December 2025; that amendment does not alter the pregabalin entry.
BrazilPrescription onlyANVISA Portaria SVS/MS No. 344/199833
Pregabalin is listed in Lista C1 of substances subject to special control in Brazil. Its supply is subject to the special-control prescription regime administered by ANVISA.
ChilePrescription onlyResolución Inscríbase N° 11516 (Registro Sanitario ISP F-14400/24)37
Chile’s current ISP sanitary registration for Lyrica capsules identifies pregabalin as the active ingredient and sets its sale condition as Receta Simple. Pregabalin is therefore supplied on a medical prescription rather than as an unrestricted product. The registration is in force and lists its next renewal date as 24 December 2029.
ColombiaPrescription onlyINVIMA Resolution No. 2024048209 (23 October 2024), granting Registro Sanitario INVIMA 2024M-0021636 for LEGABIN CR 165 mg3839
INVIMA Resolution No. 2024048209 grants a five-year sanitary registration to LEGABIN CR 165 mg, an extended-release tablet containing 165 mg of pregabalin, with the sale condition "Con formula facultativa." Article 7 makes the resolution effective upon its finality, and INVIMA's current CUM register lists Registro Sanitario INVIMA 2024M-0021636 as vigente through 7 November 2029. The prescription condition applies to the authorised LEGABIN product; the resolution does not itself schedule pregabalin as a controlled substance or set a rule for every pregabalin product.
Czech RepublicPrescription onlySÚKL medicinal-product register: KARTESADA 150 MG CPS DUR 100 (code 0237178)40
Pregabalin is a prescription-only medicine in the Czech Republic. The State Institute for Drug Control (SÚKL) register identifies pregabalin as the active substance in the authorised KARTESADA product and classifies its dispensing as Rx. It is supplied on a medical prescription.
DenmarkPrescription onlyPregabalin is prescription-only in Denmark. The Danish Medicines Agency lists Lyrica, a pregabalin medicine, in delivery group B; the Prescription Order places group B among prescription-only medicines and permits further dispensing under the same prescription only in instalments or when the prescriber specifies the number and intervals.
FrancePrescription onlyBase de données publique des médicaments — LYRICA 25 mg, gélule (CIS 67928173)45
The current valid French government medicines-database record for LYRICA 25 mg identifies its active substance as prégabaline and lists it in Liste I. Its prescription and dispensing conditions are a six-month prescription limit and a prescription on an ordonnance sécurisée. These product-level dispensing conditions apply to the valid LYRICA authorisation, rather than the withdrawn PREGABALINE ALTER authorisation, and do not establish controls on every pregabalin product outside the listed medicine record.
IrelandPrescription onlyThe Health Products Regulatory Authority (HPRA) record identifies pregabalin as the active substance in Lyrica 150 mg orodispersible tablets and classifies that authorised product as subject to prescription which may not be renewed (A). The record also states that it is supplied through pharmacies only and is subject to medical prescription; it shows the licence as authorised and issued on 23 April 2025. This product-specific regulator classification does not constitute a substance-wide Irish Statute Book schedule entry; the published First Schedule to the Medicinal Products (Prescription and Control of Supply) Regulations 2003 does not name pregabalin.
JapanPrescription onlyPMDA package-insert database49
Pregabalin is a prescription medicine in Japan. The PMDA package-insert database labels authorised pregabalin products as prescription medicines.
NetherlandsPrescription onlyGeneesmiddeleninformatiebank authorised-medicine record50
Pregabalin is a prescription-only medicine in the Netherlands. The official medicines-information bank records authorised pregabalin products with the UR supply classification.
New ZealandPrescription onlyMedicines Regulations 1984, Schedule 1 (Prescription medicines)51
Medsafe's official Classification Database, updated 20 July 2026, returns the exact active ingredient "Pregabalin" as "Prescription" with no conditions. Medsafe says the database is compiled from Schedule 1 of the Medicines Regulations 1984 and directs users to the latest amendment and subsequent New Zealand Gazette notices for the accurate legislative record. Its Schedule 1 scope statement says that, unless specifically stated otherwise, a reference covers preparations and admixtures containing a listed substance and its salts and esters, and applies to non-injection and non-eye preparations only above 10 milligrams per litre or kilogram. The classification applies at substance level and is independent of the Australian Pregabalin-AFT product leaflet.
PortugalPrescription onlyPregabalin is a prescription-only medicine in Portugal. Lyrica's European Commission marketing authorisation is valid throughout the European Union, and its approved conditions of supply classify it as a medicinal product subject to medical prescription.
SingaporePrescription onlyNational Drug Formulary product record58
Pregabalin is a prescription-only medicine in Singapore. The National Drug Formulary classifies registered pregabalin products as prescription-only medicines and records no exemption for supply without prescription.
South AfricaPrescription onlyMedicines and Related Substances Act scheduling; SAHPRA-approved product information59
Pregabalin is a Schedule 5 medicine in South Africa. SAHPRA-approved pregabalin product information gives the medicine the S5 scheduling status.
South KoreaPrescription onlyMFDS Integrated Drug Information System authorised-medicines record for GABANEURO CR Tablet 150 mg60
Pregabalin is classified as a prescription drug (전문의약품) in South Korea. The Ministry of Food and Drug Safety's Integrated Drug Information System records GABANEURO CR Tablet 150 mg as a pregabalin product and marks it as a prescription drug.
SpainPrescription onlyArticle 19, Royal Legislative Decree 1/2015 (consolidated Medicines Act), and AEMPS CIMA marketing-authorisation records for pregabalin products616263
Spain's consolidated medicines law requires AEMPS to set the prescription category in each medicine's authorisation. AEMPS's current CIMA search for pregabalin returns 182 product records; all returned records are classified as medicines subject to medical prescription and carry receta: true. This dispensing classification applies to authorised pregabalin medicines; it does not schedule pregabalin itself as a narcotic or psychotropic substance.
UkrainePrescription onlyRules for Issuing Prescriptions and Procedure for Dispensing Medicines from Pharmacies (MOH Order No. 360)7677
Pregabalin is a prescription-only medicine in Ukraine. The State Register of Medicines records the registered Pregabalin-Teva product's conditions of supply as by prescription. Ministry of Health Order No. 360 requires pharmacies to dispense medicines whose instructions require a prescription on presentation of an electronic or paper prescription.
References
Source Pages
Citations
- National Center for Biotechnology Information. (n.d.). PubChem compound summary for CID 5486971, pregabalin. PubChem. Retrieved September 5, 2026. (n.d.). https://pubchem.ncbi.nlm.nih.gov/compound/Pregabalin#section=ATC-Code1
- Saba Hadidi, Farshad Shiri, & Mohammadsaleh Norouzibazaz. (2020). Pregabalin. https://doi.org/10.1016/j.molstruc.2020.1280481
- Charles E. Argoff. (2011). Review of Current Guidelines on the Care of Postherpetic Neuralgia. https://doi.org/10.3810/pgm.2011.09.24691
- Chen Tong, Zuo Zhengyao, Li Mei, Su Dongpo, Han Qian, & Mu Fengqun. (2021). Pregabalin and Gabapentin in Patients with Spinal Cord Injury-Related Neuropathic Pain: A Network Meta-Analysis. https://doi.org/10.1007/s40122-021-00302-81
- Bragg S, Marrison ST, & Haley S. (2024). Diabetic Peripheral Neuropathy: Prevention and Treatment.. https://pubmed.ncbi.nlm.nih.gov/385742121
- Frampton JE. (2014). Pregabalin: a review of its use in adults with generalized anxiety disorder.. https://pubmed.ncbi.nlm.nih.gov/251498631
- Gabapentin and pregabalin in bipolar disorder, anxiety states, and insomnia: Systematic review, meta-analysis, and rationale. Molecular Psychiatry, 27(3), 1339–1349 (March 2022). https://doi.org/10.1038/s41380-021-01386-61
- Jacqueline French, Patrick Kwan, Toufic Fakhoury, Verne Pitman, Sarah DuBrava, Lloyd Knapp, & Lorraine Yurkewicz. (2014). Pregabalin monotherapy in patients with partial-onset seizures. https://doi.org/10.1212/wnl.00000000000001191
- Ali Bidari, Ehsan Moazen-Zadeh, Banafsheh Ghavidel-Parsa, Shahrzad Rahmani, Sajjad Hosseini, & Amir Hassankhani. (2019). Comparing duloxetine and pregabalin for treatment of pain and depression in women with fibromyalgia: an open-label randomized clinical trial. https://doi.org/10.1007/s40199-019-00257-41
- Gabapentinoids: pharmacokinetics, pharmacodynamics and considerations for clinical practice. (n.d.). https://pmc.ncbi.nlm.nih.gov/articles/PMC7265598/1
Further Reading
Bobes et al. 2012 - Pregabalin for discontinuation of long-term benzodiazepine use
Case series - Pregabalin dependence and withdrawal
High-dose pregabalin abuse case report
MHRA Drug Safety Update - Severe respiratory depression- Misuse and abuse qualitative study in Jordan
Pregabalin – pharmacology & half-life- Pregabalin poisoning and recreational use review
Systematic review of pregabalin abuse potential
TalkToFrank - Recreational effects and harm
Article Status
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Recent changes8 human edits · latest
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5 September 2026
Contributor · Updated the article: Update Pregabalin (proposed by Contributor, approved by Contributor)
4 September 2026
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Lyrea · Added a source: Torrent Pharmaceuticals Limited. (2026, March). Pregabalin capsule [Package insert]. U.S. National Library of Medicine.
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