Accession Number
DB00230  (APRD01198)
Small Molecule
Approved, Investigational

Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.13 It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.20 Although as per the FDA Label the mechanism of action has not been definitively defined, there is evidence that pregabalin exerts its effects by binding to the α2δ subunit of voltage-dependent calcium channels.2022 Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).2122 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 PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
Act PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
Act PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
Act PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
Act PregabalinCapsuleOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsuleOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
Act PregabalinCapsuleOralActavis Pharma Company2013-03-062019-07-09Canada
LyricaCapsule150 mg/1OralA S Medication Solutions2004-12-30Not applicableUs54569 870720180907 15195 dr4c8i
LyricaCapsule100 mg/1OralParke-Davis Div of Pfizer Inc2004-12-30Not applicableUs0071 101520180814 13942 ciilta
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ach-pregabalinCapsuleOralAccord Healthcare IncNot applicableNot applicableCanada
Ag-pregabalinCapsuleOralAngita Pharma Inc.2018-09-28Not applicableCanada
Ag-pregabalinCapsuleOralAngita Pharma Inc.2018-09-28Not applicableCanada
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  • 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 indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury, and as adjunctive therapy for the treatment of partial-onset seizures in patients 1 month of age and older.22

Associated Conditions

Although the structure of pregabalin is similar to gamma-aminobutyric acid (GABA), it does not bind to GABA receptors.620 Instead, it binds the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system.620 Pregabalin does not modulate dopamine receptors, serotonin receptors, opiate receptors, sodium channels or cyclooxygenase activity.20

Mechanism of action

Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.22

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 including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide.6 In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action.15

Although pregabalin is a structural derivative of the 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
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After oral dosing administered in the fasted state, pregabalin absorption is rapid, and extensive.8 Pregabalin oral bioavailability is reported to be ≥90% regardless of the dose.8 Cmax is attained within 1.5 hours after single or multiple doses, and steady state is attained within 24-48 hours with repeated administration.822 Both Cmax and AUC appear to be dose proportional.8

Food decreases the rate of pregabalin absorption and as a result, lowers the Cmax by an estimated 25-30% and increases the Tmax to approximately 3 hours.22 However, the effect of food does not appear to impact the total absorption of pregabalin in a way that is clinically relevant. As a result, pregabalin can be administered with or without food.22

Volume of distribution

After oral administration of pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg.22

Although pregabalin is not very lipophilic, it is able to cross the blood brain barrier(BBB).16 System L transporters facilitate the transport of large amino acids across the BBB and it has been confirmed that pregabalin is a substrate.2216 This information suggests that system L transporters are responsible for pregabalin uptake into the BBB.16

In rat models, pregabalin has been shown to cross the placenta.22

Protein binding

Pregabalin is not plasma protein bound.822


Less than 2% of pregabalin is metabolized and it is excreted virtually unchanged in the urine.822

Route of elimination

Pregabalin is almost exclusively eliminated in the urine.1718

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 6.3 hours.22


In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min.22 Given pregabalin's lack of plasma protein binding, this clearance rate suggests that renal tubular reabsorption is involved.22


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.

The most common symptoms of pregabalin toxicity (dose range includes 800 mg/day and single doses up to 11,500 mg) include somnolence, confusion, restlessness, agitation, depression, affective disorder and seizures.23

Since there is no antidote for pregabalin overdose, patients should receive general supportive care. If appropriate, gastric lavage or emesis may help eliminate unabsorbed pregabalin (healthcare providers should take standard precautions to maintain the airway).23

Pregabalin pharmacokinetic properties suggest that extra-corporeal elimination methods including haemodialysis, may be useful in situations of severe toxicity.19 However, there are cases where patients have presented with very high serum levels of pregabalin and have been successfully managed with supportive care alone.19

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


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
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.
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-methoxy-N,N-dimethyltryptamineThe therapeutic efficacy of 5-methoxy-N,N-dimethyltryptamine can be increased when used in combination with Pregabalin.
6-O-benzylguaninePregabalin may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-DeazaguaninePregabalin may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-NitroindazoleThe therapeutic efficacy of 7-Nitroindazole can be increased when used in combination with Pregabalin.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe therapeutic efficacy of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be increased when used in combination with Pregabalin.
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Food Interactions
  • Avoid alcohol. Alcohol may increase CNS effects.
  • Take with or without food. Food alters drug absorption, but not to a clinically significant extent.


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. 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]
  17. Stump P: [Pregabalin--profile of efficacy and tolerability in neuropathic pain]. Drugs Today (Barc). 2009 Oct;45 Suppl C:19-27. [PubMed:20087482]
  18. Lee DW, Lee HJ, Kim HJ, Chang SH, Park DJ: Two cases of pregabalin neurotoxicity in chronic kidney disease patients. NDT Plus. 2011 Apr;4(2):138. doi: 10.1093/ndtplus/sfq219. [PubMed:25984138]
  19. Wood DM, Berry DJ, Glover G, Eastwood J, Dargan PI: Significant pregabalin toxicity managed with supportive care alone. J Med Toxicol. 2010 Dec;6(4):435-7. doi: 10.1007/s13181-010-0052-3. [PubMed:20373065]
  20. Cross AL, Sherman Al: Pregabalin . [PubMed:29261857]
  21. Pfizer [Link]
  22. FDA Label Pregabalin [Link]
  23. Pfizer Medical Information - Lyrica [Link]
External Links
Human Metabolome Database
PubChem Compound
PubChem Substance
Therapeutic Targets Database
RxList Drug Page Drug Page
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 Volunteers11
1CompletedNot AvailablePain, Nerve1
1CompletedBasic ScienceHealthy Volunteers9
1CompletedOtherHealthy Volunteers1
1CompletedScreeningHealthy Volunteers1
1CompletedTreatmentDiabetic Neuropathies / Idiopathic Distal Sensory Polyneuropathy / Painful Small-Fiber Neuropathy / Postherpetic Neuralgia1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentPain, Acute1
1CompletedTreatmentPeripheral Neuropathy Pain1
1CompletedTreatmentPeripheral Nueropathy Pain1
1CompletedTreatmentUncomplicated Singleton Pregnancies1
1RecruitingTreatmentPain, Neuropathic1
1RecruitingTreatmentPostoperative pain1
1Unknown StatusTreatmentRefractive Errors1
1, 2CompletedTreatmentEpilepsy, Localization Related1
1, 2CompletedTreatmentPrimary Total Knee Arthroplasty1
1, 2RecruitingTreatmentCoughing1
2CompletedNot AvailableAnxiety1
2CompletedSupportive CareBrain and Central Nervous System Tumors / Seizures1
2CompletedSupportive CarePain / Peripheral neuropathy1
2CompletedSupportive CarePostoperative pain1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentAlcohol Use Disorder (AUD)1
2CompletedTreatmentDental Anxiety1
2CompletedTreatmentDental Pain1
2CompletedTreatmentDiabetes Mellitus / Diabetic Neuropathies / Pain, Chronic1
2CompletedTreatmentDiabetic Neuropathic Pain1
2CompletedTreatmentDiabetic Neuropathies2
2CompletedTreatmentDiabetic Neuropathy, Painful2
2CompletedTreatmentDiabetic Neuropathy, Painful; Diabetic Neuropathies1
2CompletedTreatmentDiabetic Peripheral Neuropathic Pain (DPN)2
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Pain1
2CompletedTreatmentElective Laparoscopic Cholecystectomy / Sevoflurane Anesthesia1
2CompletedTreatmentEpilepsy, Localization Related1
2CompletedTreatmentIdiopathic Small Fiber Neuropathy1
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2CompletedTreatmentMalignancies / Pain1
2CompletedTreatmentPain, Neuropathic1
2CompletedTreatmentPain / Postherpetic Neuralgia1
2CompletedTreatmentPostherpetic Neuralgia1
2CompletedTreatmentRestless Legs Syndrome (RLS)1
2CompletedTreatmentSedation, Conscious1
2CompletedTreatmentUrinary Bladder, Overactive1
2Not Yet RecruitingTreatmentAlcohol Use Disorder (AUD)1
2Not Yet RecruitingTreatmentOpiate withdrawal symptoms1
2Not Yet RecruitingTreatmentPostoperative pain1
2TerminatedPreventionBreast Cancer / Malignant Lymphomas / Pain1
2TerminatedTreatmentGulf War Illness1
2TerminatedTreatmentHerpes Zoster / Postherpetic Neuralgia1
2TerminatedTreatmentOrofacial Pain / Pain, Neuropathic1
2TerminatedTreatmentPain, Chronic1
2TerminatedTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
2TerminatedTreatmentPostherpetic Neuralgia1
2TerminatedTreatmentVulvar Vestibulitis / Vulvodynia1
2Unknown StatusTreatmentBreast Cancer / Drug-Related Side Effects and Adverse Reactions / Pain / Taxane1
2Unknown StatusTreatmentFibromyalgia / Pain, Chronic1
2WithdrawnTreatmentDiabetes / Pain, Neuropathic1
2WithdrawnTreatmentPainful Diabetic Neuropathy (PDN)1
2, 3CompletedBasic ScienceFibromyalgia1
2, 3CompletedPreventionDry Eye1
2, 3CompletedPreventionPostoperative pain1
2, 3CompletedPreventionPregabalin on Catheter Related Bladder Discomfort1
2, 3CompletedTreatmentAgitation / Dementias / Pain1
2, 3CompletedTreatmentDiabetes Mellitus / Peripheral neuropathy1
2, 3CompletedTreatmentPancreatitis, Chronic1
2, 3CompletedTreatmentPost Operative Pain1
2, 3Not Yet RecruitingTreatmentAddictions / Kidney Stones / Opioids Use / Postoperative pain1
2, 3WithdrawnPreventionPregabalin on Catheter Related Bladder Discomfort1
3Active Not RecruitingTreatmentAnaesthesia therapy / Anesthesia Morbidity / Calcium Nephrolithiasis / Pain, Acute / Perioperative/Postoperative Complications / Postoperative pain / Urolithiasis / Urologic Diseases1
3CompletedHealth Services ResearchHysterectomy1
3CompletedPreventionChronic Post-surgical Pain / Post-mastectomy Pain Syndrome1
3CompletedPreventionDelirium / Pain1
3CompletedPreventionPain / Pain, Neuropathic / Polyneuropathies1
3CompletedPreventionPost Operative Pain1
3CompletedSupportive CareBreast Cancer / Hot Flushes1
3CompletedSupportive CareIntervertebral Disc Herniation1
3CompletedTreatmentBreast Cancer Surgery / Post Operative Pain1
3CompletedTreatmentDiabetic Neuropathies1
3CompletedTreatmentDiabetic Neuropathies / Neuralgia1
3CompletedTreatmentDiabetic Neuropathy, Painful7
3CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
3CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Pain, Nerve1
3CompletedTreatmentDisseminated Sclerosis / Pain, Neuropathic1
3CompletedTreatmentEpilepsy, Complex Partial / Epilepsy, Localization Related1
3CompletedTreatmentEpilepsy, Localization Related2
3CompletedTreatmentEpilepsy, Localization Related / Partial-Onset Seizures1
3CompletedTreatmentEpilepsy, Localization Related / Sleep Deprivation1
3CompletedTreatmentEpilepsy, Partial Seizures1
3CompletedTreatmentEpilepsy, Partial Seizures / Epilepsy, Primary Generalized Tonic-Clonic Seizures1
3CompletedTreatmentFibromyalgia / Sleep disorders and disturbances1
3CompletedTreatmentGeneralized Anxiety Disorder (GAD)2
3CompletedTreatmentGeneralized Tonic Clonic Seizures / Grand mal Generalized tonic-clonic seizure1
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Peripheral neuropathy2
3CompletedTreatmentIdiopathic Restless Legs Syndrome1
3CompletedTreatmentInguinal Hernias / Postoperative pain1
3CompletedTreatmentLiver Cirrhosis / Muscle Cramps1
3CompletedTreatmentNeuralgia / Pain / Spinal Cord Diseases / Spinal Cord Injuries (SCI)1
3CompletedTreatmentNeuralgia / Spinal Cord Injuries (SCI)1
3CompletedTreatmentNeuroses, Anxiety1
3CompletedTreatmentOsteoarthritis (OA)1
3CompletedTreatmentOsteoarthritis (OA) / Postoperative pain1
3CompletedTreatmentPain Associated With Fibromyalgia3
3CompletedTreatmentPain of Mononeuropathy1
3CompletedTreatmentPain, Chronic1
3CompletedTreatmentPain, Neuropathic4
3CompletedTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
3CompletedTreatmentPartial-Onset Seizures3
3CompletedTreatmentPeripheral Neuropathic Pain1
3CompletedTreatmentPilon Fracture1
3CompletedTreatmentPost-Herpetic Neuralgia (PHN)1
3CompletedTreatmentPostherpetic Neuralgia2
3CompletedTreatmentPostoperative pain3
3CompletedTreatmentRadicular syndrome1
3CompletedTreatmentRestless Legs Syndrome (RLS)1
3CompletedTreatmentSeizure Disorder, Partial4
3Not Yet RecruitingPreventionHerpetic Neuralgia1
3RecruitingPreventionPersistent Postoperative Pain1
3RecruitingPreventionPostoperative pain1
3RecruitingSupportive CareBreast Cancer Patient1
3RecruitingTreatmentAlcohol Use Disorder (AUD) / Post Traumatic Stress Disorder (PTSD)1
3RecruitingTreatmentEpidermolysis Bullosa / Itching / Pain, Neuropathic1
3RecruitingTreatmentPostherpetic Neuralgia1
3TerminatedPreventionPain / Spinal Cord Trauma1
3TerminatedSupportive CarePerioperative Pain1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenia1
3TerminatedTreatmentEpilepsy, Localization Related1
3TerminatedTreatmentFusion of Spine (Disease)1
3TerminatedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection / Pain, Neuropathic1
3Unknown StatusPreventionInguinal Hernias / Postoperative pain1
3Unknown StatusTreatmentChronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS)1
3Unknown StatusTreatmentDiabetic Neuropathies1
3Unknown StatusTreatmentMalignancies / Neuralgia1
3Unknown StatusTreatmentPostoperative pain1
3WithdrawnPreventionPain, Chronic1
3WithdrawnPreventionPhantom Pain1
3WithdrawnTreatmentMigraine Disorders1
3WithdrawnTreatmentRestless Legs Syndrome (RLS)1
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
4CompletedTreatmentAlcohol Dependence1
4CompletedTreatmentAnxiety-comorbidity to Schizophrenia / Schizophrenia1
4CompletedTreatmentBack Pain Lower Back / Pain, Neuropathic1
4CompletedTreatmentCentral Neuropathic Pain1
4CompletedTreatmentCervical Spondylotic Myelopathy / Cervical Spondylotic Radiculopathy / Spondylosis, Cervical1
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 / Stenosis, Spinal1
4CompletedTreatmentGeneralized Anxiety Disorder (GAD)1
4CompletedTreatmentIschemia Reperfusion Injury1
4CompletedTreatmentLaparoscopic Cholecystectomy / Postoperative pain1
4CompletedTreatmentLiving Donors1
4CompletedTreatmentLumbar Spinal Fusions1
4CompletedTreatmentNeuralgia / Spinal Cord Injuries (SCI)1
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
4CompletedTreatmentObsessive Compulsive Disorder (OCD)1
4CompletedTreatmentOpiate withdrawal symptoms1
4CompletedTreatmentOpioids Use / Postoperative pain1
4CompletedTreatmentPain, Acute1
4CompletedTreatmentPain, Chronic1
4CompletedTreatmentPainful Diabetic Neuropathy and Post Herpetic Neuralgia1
4CompletedTreatmentPain / Postoperative1
4CompletedTreatmentPost Operative Pain2
4CompletedTreatmentPost-Herpetic Neuralgia (PHN)1
4CompletedTreatmentPost-thoracotomy Pain1
4CompletedTreatmentPostherpetic Neuralgia ( PHN )1
4CompletedTreatmentPostoperative Pain Management1
4CompletedTreatmentPostoperative Pain Management / Total Knee Arthroplasty (TKA)1
4CompletedTreatmentPostoperative pain4
4CompletedTreatmentAdjunct to general anesthesia therapy / Surgery, Laparoscopic1
4CompletedTreatmentTremor, Essential2
4Enrolling by InvitationTreatmentHead and Neck Carcinoma / Postoperative pain1
4Enrolling by InvitationTreatmentNonspecific Pain Post Traumatic Injury1
4RecruitingBasic ScienceChronic Migraine / Fibromyalgia / Pain, Chronic1
4RecruitingPreventionOsteoarthritis of the Knee1
4RecruitingSupportive CareScoliosis / Spondylolisthesis1
4RecruitingTreatmentCentral pain syndrome / Spinal Cord Injuries (SCI)1
4RecruitingTreatmentEpilepsy, Localization Related1
4RecruitingTreatmentHepatocellular Cancer1
4RecruitingTreatmentHerpes Zoster1
4RecruitingTreatmentOpioids Use1
4RecruitingTreatmentPain, Neuropathic1
4RecruitingTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
4RecruitingTreatmentPost-Dural Puncture Headache1
4TerminatedBasic ScienceSubstance-Related Disorders1
4TerminatedTreatmentAbdominal Pain / Surgical Adhesions1
4TerminatedTreatmentAnxiety / Epilepsies1
4TerminatedTreatmentArterial Occlusive Diseases / Critical Limb Ischemia (CLI) / Ischaemia / Pain1
4TerminatedTreatmentBone Neoplasms / Malignancies / Pain, Intractable1
4TerminatedTreatmentChemotherapy Induced Peripheral Neuropathy (CIPN) / Chemotherapy-induced Peripheral Neuropathy (CIPN)1
4TerminatedTreatmentChronic Low Back Pain With a Neuropathic Component1
4TerminatedTreatmentEpilepsy, Complex Partial1
4TerminatedTreatmentMalignant Neoplasm of Pancreas / Visceral Pain1
4TerminatedTreatmentPartial-Onset Seizures1
4TerminatedTreatmentPostherpetic Neuralgia1
4TerminatedTreatmentPostoperative pain1
4TerminatedTreatmentUterine Artery Embolization / Uterine Leiomyomas1
4Unknown StatusBasic ScienceDiabetes Mellitus / Painful Distal Symmetric Sensorimotor Polyneuropathy1
4Unknown StatusPreventionHyperalgesia / Illness, Chronic / Pain / Pain, Neuropathic1
4Unknown StatusTreatmentAnxiety1
4Unknown StatusTreatmentPain, Neuropathic / Spinal Cord Injuries (SCI)1
4Unknown StatusTreatmentPain, Neuropathic / Tactile Hyperalgesia1
4Unknown StatusTreatmentPolyneuropathies1
4Unknown StatusTreatmentUremic Pruritus2
4WithdrawnDiagnosticBack Pain Lower Back / Neuralgia1
4WithdrawnTreatmentChronic Pain, Postoperative / Headache1
4WithdrawnTreatmentDiabetic Polyneuropathy / Postherpetic Neuralgia1
4WithdrawnTreatmentRestless Legs Syndrome (RLS)1
Not AvailableActive Not RecruitingNot AvailablePeripheral Neuropathic Pain1
Not AvailableActive Not RecruitingPreventionPain, Cancer / Pain, Neuropathic / Persistent Post-surgical Pain1
Not AvailableActive Not RecruitingSupportive CarePain / Peripheral neuropathy1
Not AvailableAvailableNot AvailableAcute and Chronic Pain Following Modified Radical Mastectomy1
Not AvailableCompletedNot AvailableBlock1
Not AvailableCompletedNot AvailableEpilepsies2
Not AvailableCompletedNot AvailableEpilepsies / Fibromyalgia / Pain, Neuropathic / Post-market Surveillance1
Not AvailableCompletedNot AvailableEpilepsies / Neuralgia1
Not AvailableCompletedNot AvailableNeuralgia1
Not AvailableCompletedNot AvailablePain Associated With Fibromyalgia1
Not AvailableCompletedNot AvailablePain, Neuropathic2
Not AvailableCompletedOtherNeuropathies / Pain1
Not AvailableCompletedOtherPostoperative Pain After Knee Arthroscopy1
Not AvailableCompletedOtherSedation, Conscious1
Not AvailableCompletedPreventionAnterior Cruciate Ligament (ACL) Reconstruction1
Not AvailableCompletedPreventionPain2
Not AvailableCompletedPreventionPain, Neuropathic1
Not AvailableCompletedSupportive CarePain1
Not AvailableCompletedSupportive CarePostoperative pain2
Not AvailableCompletedTreatmentFibromyalgia, Primary1
Not AvailableCompletedTreatmentHealthy Volunteers1
Not AvailableCompletedTreatmentHepatocellular,Carcinoma / Postoperative pain1
Not AvailableCompletedTreatmentOropharyngeal Cancers / Squamous Cell Carcinoma to the Head and Neck1
Not AvailableCompletedTreatmentPain2
Not AvailableCompletedTreatmentPancreatitis, Chronic1
Not AvailableCompletedTreatmentPost-Mastectomy Chronic Pain Syndrome1
Not AvailableCompletedTreatmentPostoperative pain2
Not AvailableCompletedTreatmentLumbar epidural anesthesia therapy / Shivering1
Not AvailableEnrolling by InvitationTreatmentChronic Post-thoracotomy Pain1
Not AvailableNot Yet RecruitingTreatmentFibromyalgia / Hyperbaric Oxygen1
Not AvailableNot Yet RecruitingTreatmentOsteoarthritis (OA)1
Not AvailableNot Yet RecruitingTreatmentPeripheral Arterial Disease (PAD)1
Not AvailableRecruitingNot AvailableChemotherapy Induced Peripheral Neuropathy (CIPN) / Chemotherapy-induced Peripheral Neuropathy (CIPN)1
Not AvailableRecruitingNot AvailablePain, Neuropathic / Postoperative pain1
Not AvailableRecruitingBasic ScienceFibromyalgia1
Not AvailableRecruitingOtherPost Operative Nausea and Vomiting (PONV) / Postoperative Complications1
Not AvailableRecruitingSupportive CareSpine Surgery1
Not AvailableRecruitingTreatmentEmotional Trauma / Fibromyalgia1
Not AvailableRecruitingTreatmentFibromyalgia1
Not AvailableRecruitingTreatmentPain, Neuropathic1
Not AvailableSuspendedTreatmentSmall Fibre Neuropathy / Small-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 CarePain1
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 AvailableWithdrawnPreventionPain1
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
CapsuleOral150 mg/1
CapsuleOral200 mg/1
CapsuleOral225 mg/1
CapsuleOral25 mg/1
CapsuleOral300 mg/1
CapsuleOral50 mg/1
CapsuleOral75 mg/1
Tablet, film coated, extended releaseOral165 mg/1
Tablet, film coated, extended releaseOral330 mg/1
Tablet, film coated, extended releaseOral82.5 mg/1
SolutionOral20 mg/1mL
CapsuleOral100 mg
CapsuleOral150 mg
CapsuleOral200 mg
CapsuleOral225 mg
CapsuleOral25 mg
CapsuleOral300 mg
CapsuleOral50 mg
CapsuleOral75 mg
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)176 - 178ºC
boiling point (°C)144 - 147 ºC
water solubilityFreely soluble
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 04, 2020 15:41

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