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Accession Number
DB00230  (APRD01198)
Small Molecule
Approved, Illicit, Investigational

Pregabalin is an anticonvulsant drug used for neuropathic pain, epilepsy and generalized anxiety disorder.4 Although as per the FDA Label the mechanism of action has not been definitively defined, there is evidence that pregabalin achieves antihyperalgesic activity by binding to the α2δ subunit of the voltage-dependent calcium channels 5. Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).16Label It may have dependence liability if misused but the risk appears to be highest in patients with current or past substance use disorders 4.

  • (S)-3-Isobutyl GABA
  • 3-Isobutyl GABA
  • Pregabalin
  • Pregabalina
External IDs
CI 1008 / CI-1008 / PD-144723 / YNP-1807
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act PregabalinCapsule225 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule200 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsule150 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule100 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsule75 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule50 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule300 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule25 mgOralActavis Pharma Company2013-03-06Not applicableCanada
LyricaCapsule50 mg/1OralA-S Medication Solutions2004-12-302016-02-29Us50090 123020180907 15195 1l6w2zk
LyricaCapsule50 mg/1OralU.S. Pharmaceuticals2004-12-30Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-pregabalinCapsule200 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule25 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule150 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule100 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule300 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule75 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule225 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule50 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ag-pregabalinCapsule75 mgOralAngita Pharma Inc.2018-09-28Not applicableCanada
Ag-pregabalinCapsule50 mgOralAngita Pharma Inc.2018-09-28Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

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CAS number
Average: 159.2261
Monoisotopic: 159.125928793
Chemical Formula
InChI Key
(3S)-3-(aminomethyl)-5-methylhexanoic acid



Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, and as adjunctive therapy for adult patients with partial onset seizures Label.

Associated Conditions

Pregabalin is structurally analogous to the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). The molecule exerts it's effect on voltage gated calcium channels by binding presynaptically to the alpha-2-delta subunit. Since voltage gated calcium channels are widely distributed throughout the central nervous system, pregabalin is able to modulate the release of several excitatory neurotransmitters such as glutamate, substance-P, norepinephrine and calcitonin gene related peptide. This results in inhibition of overexcited neurons, which ultimately returns them to a normal state of function 6. As a result, Pregabalin has anticonvulsant, analgesic, anxiolytic and sleep modulating effects. 13

Mechanism of action

Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that the presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models Label. By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters 6. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn which contributes to the blunting of excitatory neurotransmitter release 15. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors 8.

AVoltage-dependent calcium channel subunit alpha-2/delta-1Not AvailableHumans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

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Absorption of pregabalin is rapid and extensive reflecting it's relatively quick onset of efficacy. Maximal plasma concentration occurs ~1 hour after administration and steady state occurs within 24-48 hours. 8

Volume of distribution

The apparent volume of distribution after oral administration is 0.5 L/kg. It is also likely that pregabalin crosses the blood brain barrier based on evidence from several animal models. Label

Protein binding

Pregabalin is not plasma protein bound 8


In humans, less than 2% of pregabalin is metabolized and it is excreted virtually unchanged in the urine 8.

Route of elimination

Pregabalin is mainly renally excreted with 98% of the drug eliminated unchanged in the urine, while less than 0.1% of the drug is eliminated through the fecal route. Further, based on preclinical studies, pregabalin does not appear to undergo racemization to the R enantiomer in the body 11.

Half life

The elimination half life of pregabalin is roughly 6 hours Label.


In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min. This renal clearance rate along with the drug's lack of plasma protein binding suggests that renal tubular reabsorption is involved.Label


In a systematic review that included 38 randomized controlled trials, there were 20 identified adverse effects that were significantly associated with pregabalin, most of which involve the central nervous system and cognition. The identified adverse effects include vertigo, dizziness, balance disorder, incoordination, ataxia, blurred vision, diplopia, amblyopia, somnolence, confusional state, tremor, disturbance in attention, abnormal thinking, asthenia, fatigue, euphoria, edema, peripheral edema, dry mouth, and constipation 14.

Affected organisms
  • Humans and other mammals
Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Pregabalin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Pregabalin.
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Pregabalin is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylthioamphetamineThe therapeutic efficacy of 2,5-Dimethoxy-4-ethylthioamphetamine can be increased when used in combination with Pregabalin.
3-isobutyl-1-methyl-7H-xanthinePregabalin may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Pregabalin.
4-Bromo-2,5-dimethoxyamphetamineThe therapeutic efficacy of 4-Bromo-2,5-dimethoxyamphetamine can be increased when used in combination with Pregabalin.
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be increased when used in combination with Pregabalin.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Pregabalin.
5-methoxy-N,N-dimethyltryptamineThe therapeutic efficacy of 5-methoxy-N,N-dimethyltryptamine can be increased when used in combination with Pregabalin.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity

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Food Interactions
  • Avoid alcohol (may increase CNS effects).
  • When taken with food, Cmax decreases, while Tmax is prolonged. Despite these observations, the total absorption of pregabalin is not effected to a clinically relevant degree. Pregabalin can be taken with or without food.


Synthesis Reference

Mark Burk, "Asymmetric synthesis of pregabalin." U.S. Patent US20030212290, issued November 13, 2003.

General References
  1. Authors unspecified: Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist. 2005 Jul 28;70(144):43633-5. [PubMed:16050051]
  2. Su TZ, Feng MR, Weber ML: Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther. 2005 Jun;313(3):1406-15. Epub 2005 Mar 15. [PubMed:15769862]
  3. Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, Cui M, Hoffman D, Donevan S: Pregabalin is a potent and selective ligand for alpha(2)delta-1 and alpha(2)delta-2 calcium channel subunits. Eur J Pharmacol. 2011 Sep 30;667(1-3):80-90. doi: 10.1016/j.ejphar.2011.05.054. Epub 2011 Jun 1. [PubMed:21651903]
  4. Bonnet U, Scherbaum N: How addictive are gabapentin and pregabalin? A systematic review. Eur Neuropsychopharmacol. 2017 Oct 5. pii: S0924-977X(17)30897-0. doi: 10.1016/j.euroneuro.2017.08.430. [PubMed:28988943]
  5. Field MJ, Oles RJ, Lewis AS, McCleary S, Hughes J, Singh L: Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents. Br J Pharmacol. 1997 Aug;121(8):1513-22. [PubMed:9283683]
  6. Rajappa GC, Vig S, Bevanaguddaiah Y, Anadaswamy TC: Efficacy of Pregabalin as Premedication for Post-Operative Analgesia in Vaginal Hysterectomy. Anesth Pain Med. 2016 May 14;6(3):e34591. doi: 10.5812/aapm.34591. eCollection 2016 Jun. [PubMed:27642577]
  7. Bender G, Florian JA Jr, Bramwell S, Field MJ, Tan KK, Marshall S, DeJongh J, Bies RR, Danhof M: Pharmacokinetic-pharmacodynamic analysis of the static allodynia response to pregabalin and sildenafil in a rat model of neuropathic pain. J Pharmacol Exp Ther. 2010 Aug;334(2):599-608. doi: 10.1124/jpet.110.166074. Epub 2010 May 5. [PubMed:20444880]
  8. Ben-Menachem E: Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8. [PubMed:15315511]
  9. Prompila N, Eiamart W, Jumroen Y, Sayankuldilok N, Chariyavilaskul P, Ketchat W, Wittayalertpanya S: Pharmacokinetics and bioequivalence of a pregabalin 150-mg capsule in healthy Thai subjects. Int J Clin Pharmacol Ther. 2017 Oct;55(10):811-817. doi: 10.5414/CP202954. [PubMed:28513426]
  10. Hong T, Han S, Lee J, Jeon S, Yim DS: Comparison of oral absorption models for pregabalin: usefulness of transit compartment model. Drug Des Devel Ther. 2016 Dec 7;10:3995-4003. eCollection 2016. [PubMed:27994441]
  11. Rodriguez J, Castaneda G, Munoz L: Direct determination of pregabalin in human urine by nonaqueous CE-TOF-MS. Electrophoresis. 2013 May;34(9-10):1429-36. doi: 10.1002/elps.201200564. Epub 2013 Apr 16. [PubMed:23463484]
  12. Randinitis EJ, Posvar EL, Alvey CW, Sedman AJ, Cook JA, Bockbrader HN: Pharmacokinetics of pregabalin in subjects with various degrees of renal function. J Clin Pharmacol. 2003 Mar;43(3):277-83. [PubMed:12638396]
  13. Gajraj NM: Pregabalin: its pharmacology and use in pain management. Anesth Analg. 2007 Dec;105(6):1805-15. doi: 10.1213/01.ane.0000287643.13410.5e. [PubMed:18042886]
  14. Zaccara G, Gangemi P, Perucca P, Specchio L: The adverse event profile of pregabalin: a systematic review and meta-analysis of randomized controlled trials. Epilepsia. 2011 Apr;52(4):826-36. doi: 10.1111/j.1528-1167.2010.02966.x. Epub 2011 Feb 14. [PubMed:21320112]
  15. Toth C: Pregabalin: latest safety evidence and clinical implications for the management of neuropathic pain. Ther Adv Drug Saf. 2014 Feb;5(1):38-56. doi: 10.1177/2042098613505614. [PubMed:25083261]
  16. Pfizer [Link]
External Links
Human Metabolome Database
PubChem Compound
PubChem Substance
Therapeutic Targets Database
ATC Codes
N03AX16 — Pregabalin
AHFS Codes
  • 28:12.92 — Miscellaneous Anticonvulsants
FDA label
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Clinical Trials

Clinical Trials
0CompletedTreatmentNicotine Dependence1
0CompletedTreatmentPost-Operative Pain1
0Not Yet RecruitingTreatmentFracture; Rib, Multiple1
0RecruitingTreatmentCannabis-use Disorders1
1CompletedNot AvailableHealthy Volunteers9
1CompletedNot AvailableNerve Pain1
1CompletedBasic ScienceHealthy Volunteers8
1CompletedOtherHealthy Volunteers1
1CompletedScreeningHealthy Volunteers1
1CompletedTreatmentDiabetic Neuropathies / Idiopathic Distal Sensory Polyneuropathy / Painful Small-Fiber Neuropathy / Postherpetic Neuralgia1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentPain, Acute1
1CompletedTreatmentPeripheral Neuropathy Pain1
1CompletedTreatmentPeripheral Nueropathy Pain1
1Not Yet RecruitingTreatmentHealthy Volunteers1
1RecruitingTreatmentPain, Neuropathic1
1Unknown StatusTreatmentRefractive Errors1
1, 2CompletedTreatmentEpilepsy, Localization Related1
1, 2CompletedTreatmentPrimary Total Knee Arthroplasty1
1, 2RecruitingTreatmentCoughing1
2Active Not RecruitingSupportive CarePostoperative pain1
2Active Not RecruitingTreatmentSedation, Conscious1
2CompletedNot AvailableFeeling Anxious1
2CompletedSupportive CareBrain and Central Nervous System Tumors / Seizures1
2CompletedSupportive CarePain NOS / Peripheral Neuropathy1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentDental Anxiety1
2CompletedTreatmentDiabetes Mellitus (DM) / Diabetic Neuropathies / Pain, Chronic1
2CompletedTreatmentDiabetic Neuropathic Pain1
2CompletedTreatmentDiabetic Neuropathies1
2CompletedTreatmentDiabetic Neuropathy, Painful2
2CompletedTreatmentDiabetic Neuropathy, Painful; Diabetic Neuropathies1
2CompletedTreatmentDiabetic Peripheral Neuropathic Pain (DPN)2
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Pain NOS1
2CompletedTreatmentElective Laparoscopic Cholecystectomy / Sevoflurane Anesthesia1
2CompletedTreatmentEpilepsy, Localization Related1
2CompletedTreatmentIdiopathic Small Fiber Neuropathy1
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2CompletedTreatmentMalignancies / Pain NOS1
2CompletedTreatmentPain NOS1
2CompletedTreatmentPain NOS / Postherpetic Neuralgia1
2CompletedTreatmentPain, Neuropathic1
2CompletedTreatmentPostherpetic Neuralgia1
2CompletedTreatmentRestless Legs Syndrome (RLS)1
2CompletedTreatmentUrinary Bladder, Overactive1
2RecruitingTreatmentAlcohol Use Disorder (AUD)1
2RecruitingTreatmentGulf War Illness1
2TerminatedPreventionCancer, Breast / Malignant Lymphomas / Pain NOS1
2TerminatedTreatmentHerpes Zoster / Postherpetic Neuralgia1
2TerminatedTreatmentOrofacial Pain / Pain, Neuropathic1
2TerminatedTreatmentPain, Chronic1
2TerminatedTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
2TerminatedTreatmentPostherpetic Neuralgia1
2TerminatedTreatmentVulvar Vestibulitis / Vulvodynia1
2TerminatedTreatmentNeurocostal neuralgia1
2Unknown StatusTreatmentCancer, Breast / Drug-Related Side Effects and Adverse Reactions / Pain NOS / Taxane1
2Unknown StatusTreatmentFibromyalgia / Pain, Chronic1
2WithdrawnTreatmentDiabetes Mellitus (DM) / Pain, Neuropathic1
2, 3Active Not RecruitingPreventionPregabalin on Catheter Related Bladder Discomfort2
2, 3CompletedBasic ScienceFibromyalgia1
2, 3CompletedPreventionEye Dryness1
2, 3CompletedPreventionPostoperative pain1
2, 3CompletedTreatmentAcute Agitation / Dementias / Pain NOS1
2, 3CompletedTreatmentDiabetes Mellitus (DM) / Peripheral Neuropathy1
2, 3CompletedTreatmentPancreatitis, Chronic1
3Active Not RecruitingTreatmentEpilepsy, Partial Seizures / Epilepsy, Primary Generalized Tonic-Clonic Seizures1
3CompletedHealth Services ResearchHysterectomy1
3CompletedPreventionChronic Post-surgical Pain / Post-mastectomy Pain Syndrome1
3CompletedPreventionDelirium / Pain NOS1
3CompletedPreventionPain NOS / Pain, Neuropathic / Polyneuropathies1
3CompletedPreventionPost-Operative Pain1
3CompletedSupportive CareCancer, Breast / Menopausal Hot Flushes1
3CompletedSupportive CareIntervertebral Disc Herniation1
3CompletedTreatmentBreast Cancer Surgery / Post Operative Pain1
3CompletedTreatmentDiabetic Neuropathies1
3CompletedTreatmentDiabetic Neuropathies / Neurocostal neuralgia1
3CompletedTreatmentDiabetic Neuropathy, Painful7
3CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
3CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Nerve Pain1
3CompletedTreatmentDisseminated Sclerosis / Pain, Neuropathic1
3CompletedTreatmentEpilepsy, Complex Partial / Epilepsy, Localization Related1
3CompletedTreatmentEpilepsy, Localization Related2
3CompletedTreatmentEpilepsy, Localization Related / Sleep Deprivation1
3CompletedTreatmentEpilepsy, Localization Related / Partial onset seizure Epilepsy1
3CompletedTreatmentFeeling Anxious1
3CompletedTreatmentFibromyalgia / Sleep disorders and disturbances1
3CompletedTreatmentGeneralized Anxiety Disorder (GAD)2
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral Neuropathy2
3CompletedTreatmentIdiopathic Restless Legs Syndrome1
3CompletedTreatmentInguinal Hernias / Postoperative pain1
3CompletedTreatmentLiver Cirrhosis / Muscle Cramps1
3CompletedTreatmentNeuroses, Anxiety1
3CompletedTreatmentOsteoarthritis (OA)1
3CompletedTreatmentOsteoarthritis (OA) / Postoperative pain1
3CompletedTreatmentPain Associated With Fibromyalgia3
3CompletedTreatmentPain NOS2
3CompletedTreatmentNeurocostal neuralgia / Pain NOS / Spinal Cord Diseases / Spinal Cord Injuries (SCI)1
3CompletedTreatmentPain of Mononeuropathy1
3CompletedTreatmentPain, Chronic1
3CompletedTreatmentPain, Neuropathic4
3CompletedTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
3CompletedTreatmentPeripheral Neuropathic Pain1
3CompletedTreatmentPost-Herpetic Neuralgia (PHN)1
3CompletedTreatmentPostherpetic Neuralgia2
3CompletedTreatmentPostoperative pain3
3CompletedTreatmentRadicular syndrome1
3CompletedTreatmentRestless Legs Syndrome (RLS)1
3CompletedTreatmentSeizure Disorder, Partial4
3CompletedTreatmentNeurocostal neuralgia / Spinal Cord Injuries (SCI)1
3CompletedTreatmentNeurocostal neuralgia2
3CompletedTreatmentPartial onset seizure Epilepsy2
3Not Yet RecruitingPreventionHerpetic Neuralgia1
3Not Yet RecruitingTreatmentAnaesthesia therapy / Anesthesia Morbidity / Calcium Nephrolithiasis / Pain, Acute / Perioperative/Postoperative Complications / Postoperative pain / Urolithiasis / Urologic Diseases1
3RecruitingPreventionPersistent Postoperative Pain1
3RecruitingPreventionPostoperative pain1
3RecruitingSupportive CareBreast Cancer Patient1
3RecruitingTreatmentAlcohol Use Disorder (AUD) / Post Traumatic Stress Disorder (PTSD)1
3RecruitingTreatmentPostherpetic Neuralgia1
3TerminatedPreventionPain NOS / Spinal Cord Trauma1
3TerminatedSupportive CarePerioperative Pain1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentEpilepsy, Localization Related1
3TerminatedTreatmentFusion of Spine (Disease)1
3TerminatedTreatmentInfection, Human Immunodeficiency Virus I / Pain, Neuropathic1
3Unknown StatusPreventionInguinal Hernias / Postoperative pain1
3Unknown StatusTreatmentChronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS)1
3Unknown StatusTreatmentDiabetic Neuropathies1
3Unknown StatusTreatmentMalignancies / Neurocostal neuralgia1
3Unknown StatusTreatmentPostoperative pain1
3WithdrawnPreventionPain, Chronic1
3WithdrawnPreventionPhantom Pain1
3WithdrawnTreatmentMigraine Disorders1
3WithdrawnTreatmentRestless Legs Syndrome (RLS)1
4Active Not RecruitingTreatmentAlcohol Dependence1
4Active Not RecruitingTreatmentLumbar Disc Disease / Lumbar Radiculopathy / Prolapsed Lumbar Disc1
4CompletedNot AvailableHealthy Lactating Women1
4CompletedNot AvailableHealthy Volunteers2
4CompletedNot AvailableIrritable Bowel Syndrome (IBS)1
4CompletedNot AvailablePain, Neuropathic2
4CompletedNot AvailablePostoperative pain1
4CompletedDiagnosticAnxiety Disorders1
4CompletedOtherHealthy Volunteers1
4CompletedTreatmentAnxiety-comorbidity to Schizophrenia / Schizophrenic Disorders1
4CompletedTreatmentCentral Neuropathic Pain1
4CompletedTreatmentCervical Spondylosis / Cervical Spondylotic Myelopathy / Cervical Spondylotic Radiculopathy1
4CompletedTreatmentChemotherapy Induced Neuropathic Pain / Diabetic Peripheral Neuropathic Pain (DPN) / HIV-related Neuropathic Pain (HIV) / Postherpetic Neuralgia ( PHN )1
4CompletedTreatmentComplex Partial Seizure Disorder / Epilepsies / Epilepsy, Localization Related / Seizure Disorder, Partial1
4CompletedTreatmentCryptogenic Sensory Polyneuropathy1
4CompletedTreatmentDiabetic Neuropathies1
4CompletedTreatmentDiabetic Neuropathy, Painful3
4CompletedTreatmentDiabetic Peripheral Neuropathic Pain (DPN)2
4CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
4CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Fibromyalgia / Seizure Disorder, Partial1
4CompletedTreatmentDisk Prolapse / Intervertebral Disk Displacement1
4CompletedTreatmentEffect of Laryngoscopy and Tracheal Intubation1
4CompletedTreatmentEpilepsy, Localization Related1
4CompletedTreatmentFailed Back Surgery Syndrome / Intervertebral Disc Herniation / Neuropathy; Radicular, Lumbar, Lumbosacral / Spinal Stenosis1
4CompletedTreatmentGeneralized Anxiety Disorder (GAD)1
4CompletedTreatmentLaparoscopic Cholecystectomy / Postoperative pain1
4CompletedTreatmentLiving Donors1
4CompletedTreatmentLumbar Spinal Fusions1
4CompletedTreatmentNeurogenic Intermittent Claudication / Spinal Stenosis of Lumbar Region1
4CompletedTreatmentNeurologic Claudication in Patients With Lumbar Spinal Stenosis1
4CompletedTreatmentNon-diabetic Painful Peripheral Polyneuropathy / Peripheral Nerve Injury (PNI) / Postherpetic Neuralgia ( PHN )1
4CompletedTreatmentOpioids Use / Postoperative pain1
4CompletedTreatmentPain NOS1
4CompletedTreatmentPain NOS / Postoperative1
4CompletedTreatmentPain, Acute1
4CompletedTreatmentPain, Chronic1
4CompletedTreatmentPainful Diabetic Neuropathy and Post Herpetic Neuralgia1
4CompletedTreatmentPost Operative Pain1
4CompletedTreatmentPost-Herpetic Neuralgia (PHN)1
4CompletedTreatmentPost-Operative Pain1
4CompletedTreatmentPost-thoracotomy Pain1
4CompletedTreatmentPostherpetic Neuralgia ( PHN )1
4CompletedTreatmentPostoperative Pain Management1
4CompletedTreatmentPostoperative Pain Management / Total Knee Arthroplasty (TKA)1
4CompletedTreatmentPostoperative pain4
4CompletedTreatmentNeurocostal neuralgia / Spinal Cord Injuries (SCI)1
4CompletedTreatmentAdjunct to general anesthesia therapy / Surgery, Laparoscopic1
4CompletedTreatmentTremor, Essential2
4CompletedTreatmentNeurocostal neuralgia1
4Enrolling by InvitationTreatmentHead and Neck Carcinoma / Postoperative pain1
4Enrolling by InvitationTreatmentNonspecific Pain Post Traumatic Injury1
4Not Yet RecruitingPreventionKnee Osteoarthritis (Knee OA)1
4RecruitingSupportive CareScoliosis / Spondylolisthesis1
4RecruitingTreatmentCentral pain syndrome / Spinal Cord Injuries (SCI)1
4RecruitingTreatmentEpilepsy, Localization Related1
4RecruitingTreatmentHepatocellular Cancer1
4RecruitingTreatmentHerpes Zoster1
4RecruitingTreatmentObsessive Compulsive Disorder (OCD)1
4RecruitingTreatmentOpiate withdrawal symptoms1
4RecruitingTreatmentPain, Neuropathic1
4TerminatedBasic ScienceSubstance-Related Disorders1
4TerminatedTreatmentAbdominal Pain (AP) / Surgical Adhesions1
4TerminatedTreatmentArterial Occlusive Diseases / Critical Limb Ischemia (CLI) / Pain NOS / Transient ischemia attacks1
4TerminatedTreatmentBone Neoplasms / Malignancies / Pain, Intractable1
4TerminatedTreatmentChemotherapy-induced Peripheral Neuropathy (CIPN)1
4TerminatedTreatmentChronic Low Back Pain With a Neuropathic Component1
4TerminatedTreatmentEpilepsies / Feeling Anxious1
4TerminatedTreatmentEpilepsy, Complex Partial1
4TerminatedTreatmentMalignant Neoplasm of Pancreas / Visceral Pain1
4TerminatedTreatmentPostherpetic Neuralgia1
4TerminatedTreatmentPostoperative pain1
4TerminatedTreatmentUterine Artery Embolization / Uterine Leiomyomas1
4TerminatedTreatmentPartial onset seizure Epilepsy1
4Unknown StatusBasic ScienceDiabetes Mellitus (DM) / Painful Distal Symmetric Sensorimotor Polyneuropathy1
4Unknown StatusPreventionHyperalgesia / Illness, Chronic / Pain NOS / Pain, Neuropathic1
4Unknown StatusTreatmentFeeling Anxious1
4Unknown StatusTreatmentPain, Neuropathic / Spinal Cord Injuries (SCI)1
4Unknown StatusTreatmentPain, Neuropathic / Tactile Hyperalgesia1
4Unknown StatusTreatmentPolyneuropathies1
4Unknown StatusTreatmentUremic Pruritus2
4WithdrawnDiagnosticBack Pain Lower Back / Neurocostal neuralgia1
4WithdrawnTreatmentChronic Pain, Postoperative / Headaches1
4WithdrawnTreatmentDiabetic Polyneuropathy / Postherpetic Neuralgia1
4WithdrawnTreatmentRestless Legs Syndrome (RLS)1
Not AvailableActive Not RecruitingPreventionPain, Cancer / Pain, Neuropathic / Persistent Post-surgical Pain1
Not AvailableActive Not RecruitingSupportive CarePain NOS / Peripheral Neuropathy1
Not AvailableAvailableNot AvailableAcute and Chronic Pain Following Modified Radical Mastectomy1
Not AvailableCompletedNot AvailableBlock1
Not AvailableCompletedNot AvailableEpilepsies1
Not AvailableCompletedNot AvailableEpilepsies / Fibromyalgia / Pain, Neuropathic / Post-market Surveillance1
Not AvailableCompletedNot AvailableEpilepsies / Neurocostal neuralgia1
Not AvailableCompletedNot AvailablePain Associated With Fibromyalgia1
Not AvailableCompletedNot AvailablePain, Neuropathic2
Not AvailableCompletedNot AvailableNeurocostal neuralgia1
Not AvailableCompletedOtherNeuropathy / Pain NOS1
Not AvailableCompletedOtherSedation, Conscious1
Not AvailableCompletedPreventionAnterior Cruciate Ligament (ACL) Reconstruction1
Not AvailableCompletedPreventionPain NOS2
Not AvailableCompletedPreventionPain, Neuropathic1
Not AvailableCompletedSupportive CarePain NOS1
Not AvailableCompletedSupportive CarePostoperative pain2
Not AvailableCompletedTreatmentHepatocellular,Carcinoma / Postoperative pain1
Not AvailableCompletedTreatmentPain NOS2
Not AvailableCompletedTreatmentPostoperative pain1
Not AvailableCompletedTreatmentLumbar epidural anesthesia therapy / Shivering1
Not AvailableEnrolling by InvitationTreatmentChronic Post-thoracotomy Pain1
Not AvailableNot Yet RecruitingOtherPostoperative Pain After Knee Arthroscopy1
Not AvailableNot Yet RecruitingTreatmentFibromyalgia / Hyperbaric Oxygen1
Not AvailableNot Yet RecruitingTreatmentPeripheral Arterial Disease (PAD)1
Not AvailableRecruitingNot AvailablePain, Neuropathic / Postoperative pain1
Not AvailableRecruitingBasic ScienceFibromyalgia1
Not AvailableRecruitingSupportive CareSpine Surgery1
Not AvailableRecruitingTreatmentFibromyalgia1
Not AvailableRecruitingTreatmentFibromyalgia, Primary1
Not AvailableRecruitingTreatmentOropharyngeal Cancers / Squamous Cell Carcinoma to the Head and Neck1
Not AvailableRecruitingTreatmentPain, Neuropathic1
Not AvailableSuspendedTreatmentSmall-Fiber Neuropathy1
Not AvailableTerminatedNot AvailableSpinal Cord Injuries (SCI)1
Not AvailableTerminatedTreatmentChronic Pain, Postoperative1
Not AvailableTerminatedTreatmentCocaine Abuse / Cocaine-Related Disorders1
Not AvailableTerminatedTreatmentComplex Regional Pain Syndromes (CRPS)1
Not AvailableTerminatedTreatmentPostoperative pain1
Not AvailableUnknown StatusSupportive CareNasal Septum Deviation1
Not AvailableUnknown StatusSupportive CarePain NOS1
Not AvailableUnknown StatusSupportive CarePostoperative pain1
Not AvailableUnknown StatusTreatmentFibromyalgia1
Not AvailableUnknown StatusTreatmentMultimodal Analgesia / Postoperative Pain Control1
Not AvailableUnknown StatusTreatmentTo Assess the Beneficial Preemptive and Preventive Effects of PGL on the Immediate and Late (1- and 3 Months) Postoperative Analgesia Requirements1
Not AvailableWithdrawnPreventionPain NOS1
Not AvailableWithdrawnTreatmentAnalgesia, Postoperative / CSOM - Chronic Suppurative Otitis Media1


  • Cp pharmaceuticals cv
  • Pfizer inc
  • A-S Medication Solutions LLC
  • Bryant Ranch Prepack
  • Cardinal Health
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Goedecke GmbH
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pfizer Inc.
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Shasun Chemicals & Drugs Ltd.
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • US Pharmaceutical Group
Dosage forms
CapsuleOral100 mg/1
CapsuleOral100 mg
CapsuleOral150 mg
CapsuleOral150 mg/1
CapsuleOral200 mg/1
CapsuleOral200 mg
CapsuleOral225 mg
CapsuleOral225 mg/1
CapsuleOral25 mg/1
CapsuleOral25 mg
CapsuleOral300 mg/1
CapsuleOral300 mg
CapsuleOral50 mg
CapsuleOral50 mg/1
CapsuleOral75 mg
CapsuleOral75 mg/1
SolutionOral20 mg/1mL
Tablet, film coated, extended releaseOral165 mg/1
Tablet, film coated, extended releaseOral330 mg/1
Tablet, film coated, extended releaseOral82.5 mg/1
PowderNot applicable1 kg/1kg
Unit descriptionCostUnit
Lyrica 100 mg capsule2.88USD capsule
Lyrica 150 mg capsule2.88USD capsule
Lyrica 50 mg capsule2.88USD capsule
Lyrica 75 mg capsule2.88USD capsule
Lyrica 200 mg capsule2.75USD capsule
Lyrica 225 mg capsule2.75USD capsule
Lyrica 25 mg capsule2.75USD capsule
Lyrica 300 mg capsule2.75USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more


Experimental Properties
melting point (°C)186-188ºC
boiling point (°C)274ºC at 760 mm Hg
water solubilityFreely soluble FDA label
logP-1.35FDA label
pKapKa1 = 4.2, pKa2 = 10.6FDA label
Predicted Properties
Water Solubility11.3 mg/mLALOGPS
pKa (Strongest Acidic)4.8ChemAxon
pKa (Strongest Basic)10.23ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area63.32 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity43.68 m3·mol-1ChemAxon
Polarizability18.08 Å3ChemAxon
Number of Rings0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Human Intestinal Absorption+0.9727
Blood Brain Barrier+0.9382
Caco-2 permeable-0.6531
P-glycoprotein substrateNon-substrate0.683
P-glycoprotein inhibitor INon-inhibitor0.965
P-glycoprotein inhibitor IINon-inhibitor0.9424
Renal organic cation transporterNon-inhibitor0.9245
CYP450 2C9 substrateNon-substrate0.8758
CYP450 2D6 substrateNon-substrate0.7926
CYP450 3A4 substrateNon-substrate0.6914
CYP450 1A2 substrateNon-inhibitor0.9385
CYP450 2C9 inhibitorNon-inhibitor0.9425
CYP450 2D6 inhibitorNon-inhibitor0.9539
CYP450 2C19 inhibitorNon-inhibitor0.9629
CYP450 3A4 inhibitorNon-inhibitor0.9352
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9784
Ames testNon AMES toxic0.938
BiodegradationReady biodegradable0.8201
Rat acute toxicity1.7046 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9868
hERG inhibition (predictor II)Non-inhibitor0.8909
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0900000000-555454e7e8e11dab591d
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0900000000-1a52554257d7f4b1c62e
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0900000000-d48cd6eeef012787cc04
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0900000000-4b11df5208caa2e97dd2
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-0900000000-605dc241ffd3a07a9220
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01ox-0900000000-fb081cde39dde2ce89f8
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-3d95bb5278c7866658a0
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-96cebf4a3610cbf02059
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-8900000000-385584fca9e88b90a95b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-9800000000-a1c6718b087b06101b8d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9200000000-5f291c943a1d1ae214ad
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9100000000-5283d02d98611a8c2c38
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9000000000-8797f8d2776fcdb4b6d5
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-9000000000-a9ddfcf2032ffc9f53ad


This compound belongs to the class of organic compounds known as gamma amino acids and derivatives. These are amino acids having a (-NH2) group attached to the gamma carbon atom.
Organic compounds
Super Class
Organic acids and derivatives
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Gamma amino acids and derivatives
Alternative Parents
Medium-chain fatty acids / Branched fatty acids / Amino fatty acids / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organic oxides / Monoalkylamines / Hydrocarbon derivatives
show 1 more
Gamma amino acid or derivatives / Medium-chain fatty acid / Amino fatty acid / Branched fatty acid / Fatty acyl / Fatty acid / Amino acid / Carboxylic acid / Monocarboxylic acid or derivatives / Amine
show 11 more
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
gamma-amino acid (CHEBI:64356)


Pharmacological action
General Function
Voltage-gated calcium channel activity
Specific Function
The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Plays an important role in excitation-...
Gene Name
Uniprot ID
Uniprot Name
Voltage-dependent calcium channel subunit alpha-2/delta-1
Molecular Weight
124566.93 Da
  1. Verma V, Singh N, Singh Jaggi A: Pregabalin in neuropathic pain: evidences and possible mechanisms. Curr Neuropharmacol. 2014 Jan;12(1):44-56. doi: 10.2174/1570159X1201140117162802. [PubMed:24533015]


Pharmacological action
General Function
Sodium:dicarboxylate symporter activity
Specific Function
Transports L-glutamate, L- and D-aspartate and L-cystein (PubMed:21123949). Essential for terminating the postsynaptic action of glutamate by rapidly removing released glutamate from the synaptic c...
Gene Name
Uniprot ID
Uniprot Name
Excitatory amino acid transporter 3
Molecular Weight
57099.835 Da
  1. Ryu JH, Lee PB, Kim JH, Do SH, Kim CS: Effects of pregabalin on the activity of glutamate transporter type 3. Br J Anaesth. 2012 Aug;109(2):234-9. doi: 10.1093/bja/aes120. Epub 2012 Apr 16. [PubMed:22511482]
Pharmacological action
General Function
Peptide antigen binding
Specific Function
Sodium-independent, high-affinity transport of large neutral amino acids such as phenylalanine, tyrosine, leucine, arginine and tryptophan, when associated with SLC3A2/4F2hc. Involved in cellular a...
Gene Name
Uniprot ID
Uniprot Name
Large neutral amino acids transporter small subunit 1
Molecular Weight
55009.62 Da
  1. Takahashi Y, Nishimura T, Higuchi K, Noguchi S, Tega Y, Kurosawa T, Deguchi Y, Tomi M: Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line. Pharm Res. 2018 Oct 29;35(12):246. doi: 10.1007/s11095-018-2532-0. [PubMed:30374619]

Drug created on June 13, 2005 07:24 / Updated on June 19, 2019 12:33