Identification

Name
Pregabalin
Accession Number
DB00230  (APRD01198)
Type
Small Molecule
Groups
Approved, Illicit, Investigational
Description

Pregabalin is an anticonvulsant drug used for neuropathic pain, epilepsy and generalized anxiety disorder.[4] It presents antihyperalgesic actions by binding to the α2δ subunit of the voltage-dependent calcium channels without presenting antinociceptive actions.[5] Pregabalin is marketed by Pfizer under the trade name Lyrica and Lyrica Cr (extended release).[13] It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the U.S.[4]

Structure
Thumb
Synonyms
  • (S)-3-(aminomethyl)-5-methylhexanoic acid
  • (S)-3-Isobutyl gaba
  • 3-Isobutyl gaba
  • CI 1008
  • S-(+)-3-isobutylgaba
External IDs
CI-1008
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act PregabalinCapsule150 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule200 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsule300 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule25 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule100 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act PregabalinCapsule75 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule225 mgOralActavis Pharma Company2013-03-06Not applicableCanada
Act PregabalinCapsule50 mgOralActavis Pharma Company2013-03-06Not applicableCanada
LyricaCapsule100 mg/1OralA S Medication Solutions2004-12-302017-06-20Us
LyricaCapsule300 mg/1OralPd Rx Pharmaceuticals, Inc.2004-12-30Not applicableUs00071 1018 68 nlmimage10 5815ac2d
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-pregabalinCapsule100 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule25 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule200 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule75 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule300 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule150 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule50 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-pregabalinCapsule225 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Apo-pregabalinCapsule50 mgOralApotex Corporation2013-06-06Not applicableCanada
Apo-pregabalinCapsule150 mgOralApotex Corporation2013-04-22Not applicableCanada
International/Other Brands
Lyrica (Pfizer) / Lyrica Cr (Pfizer)
Categories
UNII
55JG375S6M
CAS number
148553-50-8
Weight
Average: 159.2261
Monoisotopic: 159.125928793
Chemical Formula
C8H17NO2
InChI Key
AYXYPKUFHZROOJ-ZETCQYMHSA-N
InChI
InChI=1S/C8H17NO2/c1-6(2)3-7(5-9)4-8(10)11/h6-7H,3-5,9H2,1-2H3,(H,10,11)/t7-/m0/s1
IUPAC Name
(3S)-3-(aminomethyl)-5-methylhexanoic acid
SMILES
CC(C)C[[email protected]](CN)CC(O)=O

Pharmacology

Indication

Pregabalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy or spinal cord injury, and postherpetic neuralgia. It is not approved for the management of fibromyalgia or as adjuntive therapy for adult partial onset seizures.[FDA Label]

Structured Indications
Pharmacodynamics

Pregabalin is a structural analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It has been reported that its action presents the function of modulating the release of many excitatory neurotransmitters such as glutamate, norepinephrine, subtance-P and calcitonin gene related peptide.This modulation can cause an inhibitory modulation of overexcited neurons allowing them to get back to a normal state, including te decrease on the hyper excitability caused by tissue damage.[6] The neurotransmitter modulation allows pregabalin to present antiallodynic, anxiolytic and anticonvulsant activity.[7]

Mechanism of action

Pregabalin binds presynaptically to the alpha2-delta subunit of the voltage-gated calcium channels in central nervous system tissues located in the brain and spinal cord.[6] The mechanism of action has not been fully elucidated but studies suggest that pregabalin produces a disruption of calcium channel traficking or a reduction of calcium currents. The inhibition of subunits of voltage-gated calcium channels reduces calcium release which in order inhibits the release of several neurotransmitters [FDA Label] Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. 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]

TargetActionsOrganism
AVoltage-dependent P/Q-type calcium channel subunit alpha-1A
inhibitor
Human
Absorption

Pregabalin has linear and dose-proportional absorption with a steady state achieved at 48-72 hours. Nowadays, there are two different formulations of pregabalin with different pharmacokinetic profiles, this is important due to the fact that the newest formulation has a propety of extended release. Pregabalin, in its both forms, presents a rapid absorption at fasting state. Pregabalin has a Cmax of 3.2mcg/ml, Tmax 0.7 hours and AUC 31.5mcg h/ml, while pregabalin CR (extended release) presents a Cmax 2.0mcg/ml, Tmax 8 hours and AUC 29.4mcg h/ml. Pregabalin is absorbed from the small intestine and proximal colon and its AUC values will depend on the type and quantity of meal calories ingested. [9]

Volume of distribution

Pregabalin does not bind to plasma proteins. The apparent volume of distribution after oral administration is 0.5 L/kg. Pregabalin passage across bloos brain barrier (BBB) is done through the system L. [10]

Protein binding

Pregabalin does not bind to plasma proteins.[FDA Label]

Metabolism

Pregabalin undergoes negligible metabolism in humans.[11]

Route of elimination

Pregabalin presents mainly a renal excretion, it has been reported that 90% of the administered dose is recovered unchanged in the urine. Secondly, it is possible to find N-methylated pregabalin in urine, and this metabolite can account for 0.9% of the dose. Pregabalin (S-enantiomer) did not undergo racemization to the R-enantiomer in pre-clinical studies. [11]

Half life

Mean elimination half-life is 6.3 hours in subjects with normal renal function.[12]

Clearance

Mean renal clearance is estimated to be 67 to 80.9 ml/min in young healthy subjects. Due to its lack of plasma protein binding, it is indicated the presence of renal tubular reabsorption.[FDA Label]

Toxicity

Most common adverse reactions presented in clinical trials are dizziness, somnolence, peripheral edema, nausea, blurred vision, dry mouth and weight gain.[FDA Label]

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

Interactions

Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedioneThe risk or severity of heart failure can be increased when Pregabalin is combined with 2,4-thiazolidinedione.Investigational
7-NitroindazoleThe therapeutic efficacy of 7-Nitroindazole can be decreased when used in combination with Pregabalin.Experimental
AcarboseThe risk or severity of heart failure can be increased when Pregabalin is combined with Acarbose.Approved, Investigational
AcepromazineThe therapeutic efficacy of Acepromazine can be increased when used in combination with Pregabalin.Approved, Vet Approved
AceprometazineThe therapeutic efficacy of Aceprometazine can be increased when used in combination with Pregabalin.Approved
AcetazolamideThe therapeutic efficacy of Acetazolamide can be decreased when used in combination with Pregabalin.Approved, Vet Approved
AcetohexamideThe risk or severity of heart failure can be increased when Pregabalin is combined with Acetohexamide.Approved, Investigational, Withdrawn
AdipiplonThe therapeutic efficacy of Adipiplon can be increased when used in combination with Pregabalin.Investigational
AgomelatineThe therapeutic efficacy of Agomelatine can be increased when used in combination with Pregabalin.Approved, Investigational
AICA ribonucleotideThe risk or severity of heart failure can be increased when Pregabalin is combined with AICA ribonucleotide.Experimental, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Pregabalin is combined with Alaproclate.Experimental
AlbiglutideThe risk or severity of weight gain can be increased when Pregabalin is combined with Albiglutide.Approved
AlfaxaloneThe therapeutic efficacy of Alfaxalone can be increased when used in combination with Pregabalin.Vet Approved
AlfentanilThe therapeutic efficacy of Alfentanil can be increased when used in combination with Pregabalin.Approved, Illicit
AllicinThe risk or severity of heart failure can be increased when Pregabalin is combined with Allicin.Investigational
AllopregnanoloneThe therapeutic efficacy of Allopregnanolone can be increased when used in combination with Pregabalin.Investigational
AlogliptinThe risk or severity of heart failure can be increased when Pregabalin is combined with Alogliptin.Approved
AlphacetylmethadolThe therapeutic efficacy of Alphacetylmethadol can be increased when used in combination with Pregabalin.Experimental, Illicit
AlphaprodineThe therapeutic efficacy of Alphaprodine can be increased when used in combination with Pregabalin.Illicit
AlprazolamThe therapeutic efficacy of Alprazolam can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
AmisulprideThe therapeutic efficacy of Amisulpride can be increased when used in combination with Pregabalin.Approved, Investigational
AmitriptylineThe therapeutic efficacy of Amitriptyline can be increased when used in combination with Pregabalin.Approved
AmobarbitalThe therapeutic efficacy of Amobarbital can be increased when used in combination with Pregabalin.Approved, Illicit
AmoxapineThe therapeutic efficacy of Amoxapine can be increased when used in combination with Pregabalin.Approved
AmperozideThe therapeutic efficacy of Amperozide can be increased when used in combination with Pregabalin.Experimental
Anthranilic acidThe therapeutic efficacy of Anthranilic acid can be decreased when used in combination with Pregabalin.Experimental
AripiprazoleThe therapeutic efficacy of Aripiprazole can be increased when used in combination with Pregabalin.Approved, Investigational
ArticaineThe therapeutic efficacy of Articaine can be increased when used in combination with Pregabalin.Approved
AsenapineThe therapeutic efficacy of Asenapine can be increased when used in combination with Pregabalin.Approved
AzaperoneThe therapeutic efficacy of Azaperone can be increased when used in combination with Pregabalin.Investigational, Vet Approved
AzelastineThe therapeutic efficacy of Azelastine can be increased when used in combination with Pregabalin.Approved
BaclofenThe therapeutic efficacy of Baclofen can be increased when used in combination with Pregabalin.Approved
BalaglitazoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Balaglitazone.Investigational
BarbexacloneThe therapeutic efficacy of Barbexaclone can be decreased when used in combination with Pregabalin.Experimental
BarbitalThe therapeutic efficacy of Barbital can be increased when used in combination with Pregabalin.Illicit
BeclamideThe therapeutic efficacy of Beclamide can be decreased when used in combination with Pregabalin.Experimental
Bempedoic acidThe risk or severity of heart failure can be increased when Pregabalin is combined with Bempedoic acid.Investigational
BenazeprilThe risk or severity of angioedema can be increased when Benazepril is combined with Pregabalin.Approved, Investigational
BenperidolThe therapeutic efficacy of Benperidol can be increased when used in combination with Pregabalin.Approved, Investigational
BenzocaineThe therapeutic efficacy of Benzocaine can be increased when used in combination with Pregabalin.Approved, Investigational
Benzyl alcoholThe therapeutic efficacy of Benzyl alcohol can be increased when used in combination with Pregabalin.Approved
BrexpiprazoleThe therapeutic efficacy of Brexpiprazole can be increased when used in combination with Pregabalin.Approved, Investigational
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved
BrivaracetamThe therapeutic efficacy of Brivaracetam can be decreased when used in combination with Pregabalin.Approved, Investigational
BromazepamThe therapeutic efficacy of Bromazepam can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
BromisovalThe therapeutic efficacy of Bromisoval can be increased when used in combination with Pregabalin.Experimental
BromperidolThe therapeutic efficacy of Bromperidol can be increased when used in combination with Pregabalin.Approved, Investigational
BrompheniramineThe therapeutic efficacy of Brompheniramine can be increased when used in combination with Pregabalin.Approved
BrotizolamThe therapeutic efficacy of Brotizolam can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
BuforminThe risk or severity of heart failure can be increased when Pregabalin is combined with Buformin.Investigational, Withdrawn
BupivacaineThe therapeutic efficacy of Bupivacaine can be increased when used in combination with Pregabalin.Approved, Investigational
BuprenorphinePregabalin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe therapeutic efficacy of Buspirone can be increased when used in combination with Pregabalin.Approved, Investigational
ButabarbitalThe therapeutic efficacy of Butabarbital can be increased when used in combination with Pregabalin.Approved, Illicit
ButacaineThe therapeutic efficacy of Butacaine can be increased when used in combination with Pregabalin.Vet Approved
ButalbitalThe therapeutic efficacy of Butalbital can be increased when used in combination with Pregabalin.Approved, Illicit
ButambenThe therapeutic efficacy of Butamben can be increased when used in combination with Pregabalin.Approved
ButethalThe therapeutic efficacy of Butethal can be increased when used in combination with Pregabalin.Approved, Illicit
ButorphanolThe therapeutic efficacy of Butorphanol can be increased when used in combination with Pregabalin.Approved, Illicit, Vet Approved
CanagliflozinThe risk or severity of heart failure can be increased when Pregabalin is combined with Canagliflozin.Approved
CandoxatrilThe risk or severity of angioedema can be increased when Candoxatril is combined with Pregabalin.Experimental
CanertinibThe therapeutic efficacy of Canertinib can be increased when used in combination with Pregabalin.Investigational
CaptoprilThe risk or severity of angioedema can be increased when Captopril is combined with Pregabalin.Approved
CarbamazepineThe therapeutic efficacy of Carbamazepine can be decreased when used in combination with Pregabalin.Approved, Investigational
CarbinoxamineThe therapeutic efficacy of Carbinoxamine can be increased when used in combination with Pregabalin.Approved
CarbutamideThe risk or severity of heart failure can be increased when Pregabalin is combined with Carbutamide.Experimental
CarfentanilThe therapeutic efficacy of Carfentanil can be increased when used in combination with Pregabalin.Illicit, Investigational, Vet Approved
CarisbamateThe therapeutic efficacy of Carisbamate can be decreased when used in combination with Pregabalin.Investigational
CarisoprodolThe therapeutic efficacy of Carisoprodol can be increased when used in combination with Pregabalin.Approved
CastanospermineThe risk or severity of heart failure can be increased when Pregabalin is combined with Castanospermine.Experimental
CetirizineThe therapeutic efficacy of Cetirizine can be increased when used in combination with Pregabalin.Approved
Chloral hydrateThe therapeutic efficacy of Chloral hydrate can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational, Vet Approved
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
ChlormezanoneThe therapeutic efficacy of Chlormezanone can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
ChloroprocaineThe therapeutic efficacy of Chloroprocaine can be increased when used in combination with Pregabalin.Approved
ChlorphenamineThe therapeutic efficacy of Chlorphenamine can be increased when used in combination with Pregabalin.Approved
ChlorpromazineThe therapeutic efficacy of Chlorpromazine can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
ChlorpropamideThe risk or severity of heart failure can be increased when Pregabalin is combined with Chlorpropamide.Approved, Investigational
ChlorprothixeneThe therapeutic efficacy of Chlorprothixene can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
ChlorzoxazoneThe therapeutic efficacy of Chlorzoxazone can be increased when used in combination with Pregabalin.Approved
CiglitazoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Ciglitazone.Experimental
CilazaprilThe risk or severity of angioedema can be increased when Cilazapril is combined with Pregabalin.Approved
CinchocaineThe therapeutic efficacy of Cinchocaine can be increased when used in combination with Pregabalin.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Pregabalin is combined with Citalopram.Approved
ClemastineThe therapeutic efficacy of Clemastine can be increased when used in combination with Pregabalin.Approved, Investigational
ClidiniumThe therapeutic efficacy of Clidinium can be increased when used in combination with Pregabalin.Approved
ClobazamThe therapeutic efficacy of Clobazam can be decreased when used in combination with Pregabalin.Approved, Illicit
clomethiazoleThe therapeutic efficacy of clomethiazole can be decreased when used in combination with Pregabalin.Investigational
ClomipramineThe therapeutic efficacy of Clomipramine can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Pregabalin.Approved, Illicit
ClonidineThe therapeutic efficacy of Clonidine can be increased when used in combination with Pregabalin.Approved
ClopenthixolThe therapeutic efficacy of Clopenthixol can be increased when used in combination with Pregabalin.Experimental
ClorazepateThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Pregabalin.Approved, Illicit
ClothiapineThe therapeutic efficacy of Clothiapine can be increased when used in combination with Pregabalin.Experimental
ClozapineThe therapeutic efficacy of Clozapine can be increased when used in combination with Pregabalin.Approved
CocaineThe therapeutic efficacy of Cocaine can be increased when used in combination with Pregabalin.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be increased when used in combination with Pregabalin.Approved, Illicit
CyclizineThe therapeutic efficacy of Cyclizine can be increased when used in combination with Pregabalin.Approved
CyclobenzaprineThe therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with Pregabalin.Approved
CyclopropaneThe therapeutic efficacy of Cyclopropane can be increased when used in combination with Pregabalin.Experimental
CyproheptadineThe therapeutic efficacy of Cyproheptadine can be increased when used in combination with Pregabalin.Approved
DantroleneThe therapeutic efficacy of Dantrolene can be increased when used in combination with Pregabalin.Approved, Investigational
DapiprazoleThe therapeutic efficacy of Dapiprazole can be increased when used in combination with Pregabalin.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Dapoxetine.Investigational
DelaprilThe risk or severity of angioedema can be increased when Delapril is combined with Pregabalin.Experimental
DelorazepamThe therapeutic efficacy of Delorazepam can be decreased when used in combination with Pregabalin.Approved, Illicit, Investigational
DeoxyspergualinThe risk or severity of heart failure can be increased when Pregabalin is combined with Deoxyspergualin.Investigational
DeramciclaneThe therapeutic efficacy of Deramciclane can be decreased when used in combination with Pregabalin.Investigational
DesfluraneThe therapeutic efficacy of Desflurane can be increased when used in combination with Pregabalin.Approved
DesipramineThe therapeutic efficacy of Desipramine can be increased when used in combination with Pregabalin.Approved, Investigational
DesloratadineThe therapeutic efficacy of Desloratadine can be increased when used in combination with Pregabalin.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Desvenlafaxine.Approved, Investigational
DetomidineThe therapeutic efficacy of Detomidine can be increased when used in combination with Pregabalin.Vet Approved
DexbrompheniramineThe therapeutic efficacy of Dexbrompheniramine can be increased when used in combination with Pregabalin.Approved
DexmedetomidineThe therapeutic efficacy of Dexmedetomidine can be increased when used in combination with Pregabalin.Approved, Vet Approved
DextromoramideThe therapeutic efficacy of Dextromoramide can be increased when used in combination with Pregabalin.Experimental, Illicit
DextropropoxypheneThe therapeutic efficacy of Dextropropoxyphene can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational, Withdrawn
DezocineThe therapeutic efficacy of Dezocine can be increased when used in combination with Pregabalin.Approved, Investigational
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Pregabalin.Approved, Illicit, Investigational, Vet Approved
Diethyl etherThe therapeutic efficacy of Diethyl ether can be increased when used in combination with Pregabalin.Experimental
DifenoxinThe therapeutic efficacy of Difenoxin can be increased when used in combination with Pregabalin.Approved, Illicit
DihydrocodeineThe therapeutic efficacy of Dihydrocodeine can be increased when used in combination with Pregabalin.Approved, Illicit
DihydroetorphineThe therapeutic efficacy of Dihydroetorphine can be increased when used in combination with Pregabalin.Experimental, Illicit
DihydromorphineThe therapeutic efficacy of Dihydromorphine can be increased when used in combination with Pregabalin.Experimental, Illicit
DimenhydrinateThe therapeutic efficacy of Dimenhydrinate can be increased when used in combination with Pregabalin.Approved
DiphenhydramineThe therapeutic efficacy of Diphenhydramine can be increased when used in combination with Pregabalin.Approved, Investigational
DiphenoxylateThe therapeutic efficacy of Diphenoxylate can be increased when used in combination with Pregabalin.Approved, Illicit
DixyrazineThe therapeutic efficacy of Dixyrazine can be increased when used in combination with Pregabalin.Experimental
DoramectinThe therapeutic efficacy of Doramectin can be decreased when used in combination with Pregabalin.Vet Approved
DoxepinThe therapeutic efficacy of Doxepin can be increased when used in combination with Pregabalin.Approved, Investigational
DoxofyllineThe serum concentration of Doxofylline can be decreased when it is combined with Pregabalin.Approved, Investigational
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Vet Approved
DPDPEThe therapeutic efficacy of DPDPE can be increased when used in combination with Pregabalin.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Vet Approved
DrotebanolThe therapeutic efficacy of Drotebanol can be increased when used in combination with Pregabalin.Experimental, Illicit
DulaglutideThe risk or severity of heart failure can be increased when Pregabalin is combined with Dulaglutide.Approved, Investigational
DuloxetineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Duloxetine.Approved
DyclonineThe therapeutic efficacy of Dyclonine can be increased when used in combination with Pregabalin.Approved
EcgonineThe therapeutic efficacy of Ecgonine can be increased when used in combination with Pregabalin.Experimental, Illicit
EcopipamThe therapeutic efficacy of Ecopipam can be increased when used in combination with Pregabalin.Investigational
EfavirenzThe therapeutic efficacy of Efavirenz can be increased when used in combination with Pregabalin.Approved, Investigational
EltanoloneThe therapeutic efficacy of Eltanolone can be increased when used in combination with Pregabalin.Investigational
EmpagliflozinThe risk or severity of heart failure can be increased when Pregabalin is combined with Empagliflozin.Approved
EnalaprilThe risk or severity of angioedema can be increased when Enalapril is combined with Pregabalin.Approved, Vet Approved
EnalaprilatThe risk or severity of angioedema can be increased when Enalaprilat is combined with Pregabalin.Approved
EnfluraneThe therapeutic efficacy of Enflurane can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
EntacaponeThe therapeutic efficacy of Entacapone can be increased when used in combination with Pregabalin.Approved, Investigational
EperisoneThe therapeutic efficacy of Eperisone can be decreased when used in combination with Pregabalin.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Pregabalin is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Pregabalin.Approved
EstazolamThe therapeutic efficacy of Estazolam can be decreased when used in combination with Pregabalin.Approved, Illicit
EszopicloneThe therapeutic efficacy of Eszopiclone can be increased when used in combination with Pregabalin.Approved, Investigational
EthadioneThe therapeutic efficacy of Ethadione can be decreased when used in combination with Pregabalin.Experimental
EthanolPregabalin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe therapeutic efficacy of Ethchlorvynol can be increased when used in combination with Pregabalin.Approved, Illicit, Withdrawn
EthosuximideThe therapeutic efficacy of Ethosuximide can be decreased when used in combination with Pregabalin.Approved
EthotoinThe therapeutic efficacy of Ethotoin can be decreased when used in combination with Pregabalin.Approved
Ethyl carbamateThe therapeutic efficacy of Ethyl carbamate can be increased when used in combination with Pregabalin.Withdrawn
Ethyl chlorideThe therapeutic efficacy of Ethyl chloride can be increased when used in combination with Pregabalin.Approved, Experimental, Investigational
Ethyl loflazepateThe therapeutic efficacy of Ethyl loflazepate can be increased when used in combination with Pregabalin.Approved, Illicit
EthylmorphineThe therapeutic efficacy of Ethylmorphine can be increased when used in combination with Pregabalin.Approved, Illicit
EtidocaineThe therapeutic efficacy of Etidocaine can be increased when used in combination with Pregabalin.Approved
EtifoxineThe therapeutic efficacy of Etifoxine can be increased when used in combination with Pregabalin.Investigational, Withdrawn
EtiracetamThe therapeutic efficacy of Etiracetam can be decreased when used in combination with Pregabalin.Investigational
EtizolamThe therapeutic efficacy of Etizolam can be increased when used in combination with Pregabalin.Approved
EtomidateThe therapeutic efficacy of Etomidate can be increased when used in combination with Pregabalin.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Pregabalin is combined with Etoperidone.Withdrawn
EtorphineThe therapeutic efficacy of Etorphine can be increased when used in combination with Pregabalin.Illicit, Vet Approved
ExenatideThe risk or severity of heart failure can be increased when Pregabalin is combined with Exenatide.Approved, Investigational
EzogabineThe therapeutic efficacy of Ezogabine can be decreased when used in combination with Pregabalin.Approved, Investigational
FelbamateThe therapeutic efficacy of Felbamate can be decreased when used in combination with Pregabalin.Approved
FencamfamineThe therapeutic efficacy of Fencamfamine can be increased when used in combination with Pregabalin.Approved, Illicit, Withdrawn
FentanylThe therapeutic efficacy of Fentanyl can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe therapeutic efficacy of Fexofenadine can be increased when used in combination with Pregabalin.Approved, Investigational
FlibanserinThe therapeutic efficacy of Flibanserin can be increased when used in combination with Pregabalin.Approved, Investigational
FluanisoneThe therapeutic efficacy of Fluanisone can be increased when used in combination with Pregabalin.Experimental
FludiazepamThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Pregabalin.Approved, Illicit
FlunarizineThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Pregabalin.Approved
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be increased when used in combination with Pregabalin.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe therapeutic efficacy of Flupentixol can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
FluphenazineThe therapeutic efficacy of Fluphenazine can be increased when used in combination with Pregabalin.Approved
FlurazepamThe therapeutic efficacy of Flurazepam can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
FluspirileneThe therapeutic efficacy of Fluspirilene can be increased when used in combination with Pregabalin.Approved, Investigational
Fluticasone propionateThe therapeutic efficacy of Fluticasone propionate can be increased when used in combination with Pregabalin.Approved
FluvoxamineThe therapeutic efficacy of Fluvoxamine can be increased when used in combination with Pregabalin.Approved, Investigational
FosinoprilThe risk or severity of angioedema can be increased when Fosinopril is combined with Pregabalin.Approved
FosphenytoinThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Pregabalin.Approved, Investigational
FospropofolThe therapeutic efficacy of Fospropofol can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
GabapentinThe therapeutic efficacy of Gabapentin can be decreased when used in combination with Pregabalin.Approved, Investigational
Gabapentin EnacarbilThe therapeutic efficacy of Gabapentin Enacarbil can be increased when used in combination with Pregabalin.Approved, Investigational
GaboxadolThe therapeutic efficacy of Gaboxadol can be decreased when used in combination with Pregabalin.Investigational
Gamma Hydroxybutyric AcidThe therapeutic efficacy of Gamma Hydroxybutyric Acid can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
GepironeThe therapeutic efficacy of Gepirone can be increased when used in combination with Pregabalin.Investigational
GlibornurideThe risk or severity of heart failure can be increased when Pregabalin is combined with Glibornuride.Investigational, Withdrawn
GliclazideThe risk or severity of heart failure can be increased when Pregabalin is combined with Gliclazide.Approved
GlimepirideThe risk or severity of heart failure can be increased when Pregabalin is combined with Glimepiride.Approved
GlipizideThe risk or severity of heart failure can be increased when Pregabalin is combined with Glipizide.Approved, Investigational
GliquidoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Gliquidone.Approved, Investigational
GlutethimideThe therapeutic efficacy of Glutethimide can be increased when used in combination with Pregabalin.Approved, Illicit
GlyburideThe risk or severity of heart failure can be increased when Pregabalin is combined with Glyburide.Approved
GuanfacineThe therapeutic efficacy of Guanfacine can be increased when used in combination with Pregabalin.Approved, Investigational
GusperimusThe risk or severity of heart failure can be increased when Pregabalin is combined with Gusperimus.Investigational
HalazepamThe therapeutic efficacy of Halazepam can be increased when used in combination with Pregabalin.Approved, Illicit, Withdrawn
HaloperidolThe therapeutic efficacy of Haloperidol can be increased when used in combination with Pregabalin.Approved
HalothaneThe therapeutic efficacy of Halothane can be increased when used in combination with Pregabalin.Approved, Vet Approved
HeroinThe therapeutic efficacy of Heroin can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
HexobarbitalThe therapeutic efficacy of Hexobarbital can be increased when used in combination with Pregabalin.Approved
HydrocodonePregabalin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe therapeutic efficacy of Hydromorphone can be increased when used in combination with Pregabalin.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved
IfenprodilThe therapeutic efficacy of Ifenprodil can be decreased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
IloperidoneThe therapeutic efficacy of Iloperidone can be increased when used in combination with Pregabalin.Approved
ImidaprilThe risk or severity of angioedema can be increased when Imidapril is combined with Pregabalin.Investigational
ImipramineThe therapeutic efficacy of Imipramine can be increased when used in combination with Pregabalin.Approved
IndalpineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Indalpine.Investigational, Withdrawn
IndiplonThe therapeutic efficacy of Indiplon can be increased when used in combination with Pregabalin.Investigational
Insulin AspartThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Aspart.Approved
Insulin DetemirThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Detemir.Approved
Insulin GlargineThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Glargine.Approved
Insulin GlulisineThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Glulisine.Approved
Insulin HumanThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Human.Approved, Investigational
Insulin LisproThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Lispro.Approved
Insulin PorkThe risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Pork.Approved
IsofluraneThe therapeutic efficacy of Isoflurane can be increased when used in combination with Pregabalin.Approved, Vet Approved
KetamineThe therapeutic efficacy of Ketamine can be increased when used in combination with Pregabalin.Approved, Vet Approved
KetazolamThe therapeutic efficacy of Ketazolam can be increased when used in combination with Pregabalin.Approved
KetobemidoneThe therapeutic efficacy of Ketobemidone can be increased when used in combination with Pregabalin.Approved, Investigational
LacosamideThe therapeutic efficacy of Lacosamide can be decreased when used in combination with Pregabalin.Approved
LamotrigineThe therapeutic efficacy of Lamotrigine can be decreased when used in combination with Pregabalin.Approved, Investigational
LevetiracetamThe therapeutic efficacy of Levetiracetam can be decreased when used in combination with Pregabalin.Approved, Investigational
LevobupivacaineThe therapeutic efficacy of Levobupivacaine can be increased when used in combination with Pregabalin.Approved, Investigational
LevocabastineThe therapeutic efficacy of Levocabastine can be increased when used in combination with Pregabalin.Approved, Investigational
LevocetirizineThe therapeutic efficacy of Levocetirizine can be increased when used in combination with Pregabalin.Approved
LevodopaThe therapeutic efficacy of Levodopa can be increased when used in combination with Pregabalin.Approved
Levomethadyl AcetateThe therapeutic efficacy of Levomethadyl Acetate can be increased when used in combination with Pregabalin.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Pregabalin is combined with Levomilnacipran.Approved, Investigational
LevorphanolThe therapeutic efficacy of Levorphanol can be increased when used in combination with Pregabalin.Approved
LidocaineThe therapeutic efficacy of Lidocaine can be increased when used in combination with Pregabalin.Approved, Vet Approved
LinagliptinThe risk or severity of heart failure can be increased when Pregabalin is combined with Linagliptin.Approved
LiraglutideThe risk or severity of heart failure can be increased when Pregabalin is combined with Liraglutide.Approved
LisinoprilThe risk or severity of angioedema can be increased when Lisinopril is combined with Pregabalin.Approved, Investigational
LithiumThe therapeutic efficacy of Lithium can be increased when used in combination with Pregabalin.Approved
LofentanilThe therapeutic efficacy of Lofentanil can be increased when used in combination with Pregabalin.Illicit
LoprazolamThe therapeutic efficacy of Loprazolam can be increased when used in combination with Pregabalin.Experimental
LoratadineThe therapeutic efficacy of Loratadine can be increased when used in combination with Pregabalin.Approved, Investigational
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Pregabalin.Approved
LormetazepamThe therapeutic efficacy of Lormetazepam can be increased when used in combination with Pregabalin.Approved
LorpiprazoleThe serum concentration of Pregabalin can be increased when it is combined with Lorpiprazole.Approved
LoxapineThe therapeutic efficacy of Loxapine can be increased when used in combination with Pregabalin.Approved
LurasidoneThe therapeutic efficacy of Lurasidone can be increased when used in combination with Pregabalin.Approved, Investigational
Magnesium SulfateThe therapeutic efficacy of Pregabalin can be increased when used in combination with Magnesium Sulfate.Approved, Investigational, Vet Approved
MaprotilineThe therapeutic efficacy of Maprotiline can be increased when used in combination with Pregabalin.Approved, Investigational
MebeverineThe therapeutic efficacy of Mebeverine can be decreased when used in combination with Pregabalin.Approved, Investigational
MebicarThe therapeutic efficacy of Mebicar can be increased when used in combination with Pregabalin.Experimental
MeclizineThe therapeutic efficacy of Meclizine can be increased when used in combination with Pregabalin.Approved
MedazepamThe therapeutic efficacy of Medazepam can be decreased when used in combination with Pregabalin.Experimental
MedetomidineThe therapeutic efficacy of Medetomidine can be increased when used in combination with Pregabalin.Vet Approved
MefloquineThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Mefloquine.Approved, Investigational
MelatoninThe therapeutic efficacy of Melatonin can be increased when used in combination with Pregabalin.Approved, Nutraceutical, Vet Approved
MelperoneThe therapeutic efficacy of Melperone can be increased when used in combination with Pregabalin.Approved, Investigational
MephenytoinThe therapeutic efficacy of Mephenytoin can be decreased when used in combination with Pregabalin.Investigational, Withdrawn
MepivacaineThe therapeutic efficacy of Mepivacaine can be increased when used in combination with Pregabalin.Approved, Vet Approved
MeprobamateThe therapeutic efficacy of Meprobamate can be decreased when used in combination with Pregabalin.Approved, Illicit
MeptazinolThe therapeutic efficacy of Meptazinol can be increased when used in combination with Pregabalin.Experimental
MesoridazineThe therapeutic efficacy of Mesoridazine can be increased when used in combination with Pregabalin.Approved, Investigational
MetaxaloneThe therapeutic efficacy of Metaxalone can be increased when used in combination with Pregabalin.Approved
MetforminThe risk or severity of heart failure can be increased when Pregabalin is combined with Metformin.Approved
MethadoneThe therapeutic efficacy of Methadone can be increased when used in combination with Pregabalin.Approved
Methadyl AcetateThe therapeutic efficacy of Methadyl Acetate can be increased when used in combination with Pregabalin.Approved, Illicit
MethapyrileneThe therapeutic efficacy of Methapyrilene can be increased when used in combination with Pregabalin.Withdrawn
MethaqualoneThe therapeutic efficacy of Methaqualone can be increased when used in combination with Pregabalin.Illicit, Withdrawn
MetharbitalThe therapeutic efficacy of Metharbital can be decreased when used in combination with Pregabalin.Withdrawn
MethocarbamolThe therapeutic efficacy of Methocarbamol can be increased when used in combination with Pregabalin.Approved, Vet Approved
MethohexitalThe therapeutic efficacy of Methohexital can be increased when used in combination with Pregabalin.Approved
MethotrimeprazinePregabalin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved, Investigational
MethoxyfluraneThe therapeutic efficacy of Methoxyflurane can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
MethsuximideThe therapeutic efficacy of Methsuximide can be decreased when used in combination with Pregabalin.Approved
MethylecgonineThe therapeutic efficacy of Methylecgonine can be increased when used in combination with Pregabalin.Experimental
MethylphenobarbitalThe therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Pregabalin.Approved
MetyrosinePregabalin may increase the sedative activities of Metyrosine.Approved
MianserinThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Mianserin.Approved, Investigational
MidazolamThe therapeutic efficacy of Midazolam can be increased when used in combination with Pregabalin.Approved, Illicit
MiglitolThe risk or severity of heart failure can be increased when Pregabalin is combined with Miglitol.Approved
MiglustatThe risk or severity of heart failure can be increased when Pregabalin is combined with Miglustat.Approved
MilnacipranThe risk or severity of adverse effects can be increased when Pregabalin is combined with Milnacipran.Approved, Investigational
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Investigational
MirtazapinePregabalin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitiglinideThe risk or severity of heart failure can be increased when Pregabalin is combined with Mitiglinide.Approved, Investigational
MK-212The therapeutic efficacy of MK-212 can be decreased when used in combination with Pregabalin.Investigational
MoexiprilThe risk or severity of angioedema can be increased when Moexipril is combined with Pregabalin.Approved
MolindoneThe therapeutic efficacy of Molindone can be increased when used in combination with Pregabalin.Approved
MorphineThe therapeutic efficacy of Morphine can be increased when used in combination with Pregabalin.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Investigational
NalbuphineThe therapeutic efficacy of Nalbuphine can be increased when used in combination with Pregabalin.Approved
NateglinideThe risk or severity of heart failure can be increased when Pregabalin is combined with Nateglinide.Approved, Investigational
NefazodoneThe risk or severity of adverse effects can be increased when Pregabalin is combined with Nefazodone.Approved, Withdrawn
NeocitrullamonThe therapeutic efficacy of Neocitrullamon can be decreased when used in combination with Pregabalin.Experimental
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Pregabalin.Approved
Nitrous oxideThe therapeutic efficacy of Nitrous oxide can be increased when used in combination with Pregabalin.Approved, Vet Approved
NorfluraneThe therapeutic efficacy of Norflurane can be increased when used in combination with Pregabalin.Approved, Investigational
NormethadoneThe therapeutic efficacy of Normethadone can be increased when used in combination with Pregabalin.Approved, Illicit
NortriptylineThe therapeutic efficacy of Nortriptyline can be increased when used in combination with Pregabalin.Approved
OlanzapineThe therapeutic efficacy of Olanzapine can be increased when used in combination with Pregabalin.Approved, Investigational
OlopatadineThe therapeutic efficacy of Olopatadine can be increased when used in combination with Pregabalin.Approved
OmapatrilatThe risk or severity of angioedema can be increased when Omapatrilat is combined with Pregabalin.Investigational
OndansetronThe therapeutic efficacy of Ondansetron can be increased when used in combination with Pregabalin.Approved
OpiumThe therapeutic efficacy of Opium can be increased when used in combination with Pregabalin.Approved, Illicit
OrlistatThe serum concentration of Pregabalin can be decreased when it is combined with Orlistat.Approved, Investigational
OrphenadrinePregabalin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe therapeutic efficacy of Osanetant can be increased when used in combination with Pregabalin.Investigational
OxazepamThe therapeutic efficacy of Oxazepam can be increased when used in combination with Pregabalin.Approved
OxcarbazepineThe therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Pregabalin.Approved
OxethazaineThe therapeutic efficacy of Oxethazaine can be increased when used in combination with Pregabalin.Approved, Investigational
OxprenololThe therapeutic efficacy of Oxprenolol can be increased when used in combination with Pregabalin.Approved
OxybuprocaineThe therapeutic efficacy of Oxybuprocaine can be increased when used in combination with Pregabalin.Approved, Investigational
OxycodoneThe therapeutic efficacy of Oxycodone can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
OxymorphoneThe therapeutic efficacy of Oxymorphone can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
PaliperidoneThe therapeutic efficacy of Paliperidone can be increased when used in combination with Pregabalin.Approved
ParaldehydePregabalin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParamethadioneThe therapeutic efficacy of Paramethadione can be decreased when used in combination with Pregabalin.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Paroxetine.Approved, Investigational
PenfluridolThe therapeutic efficacy of Penfluridol can be increased when used in combination with Pregabalin.Experimental
PentazocineThe therapeutic efficacy of Pentazocine can be increased when used in combination with Pregabalin.Approved, Vet Approved
PentobarbitalThe therapeutic efficacy of Pentobarbital can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved
PerazineThe therapeutic efficacy of Perazine can be increased when used in combination with Pregabalin.Approved, Investigational
PerindoprilThe risk or severity of angioedema can be increased when Perindopril is combined with Pregabalin.Approved
PerospironeThe therapeutic efficacy of Perospirone can be increased when used in combination with Pregabalin.Approved
PerphenazineThe therapeutic efficacy of Perphenazine can be increased when used in combination with Pregabalin.Approved
PethidineThe therapeutic efficacy of Pethidine can be increased when used in combination with Pregabalin.Approved
PhenacemideThe therapeutic efficacy of Phenacemide can be decreased when used in combination with Pregabalin.Approved
PhenazocineThe therapeutic efficacy of Phenazocine can be increased when used in combination with Pregabalin.Experimental
PheneturideThe therapeutic efficacy of Pheneturide can be decreased when used in combination with Pregabalin.Experimental
PhenforminThe risk or severity of heart failure can be increased when Pregabalin is combined with Phenformin.Approved, Investigational, Withdrawn
PhenibutThe therapeutic efficacy of Phenibut can be decreased when used in combination with Pregabalin.Experimental
PhenobarbitalThe therapeutic efficacy of Phenobarbital can be decreased when used in combination with Pregabalin.Approved, Investigational
PhenoperidineThe therapeutic efficacy of Phenoperidine can be increased when used in combination with Pregabalin.Experimental
PhenoxyethanolThe therapeutic efficacy of Phenoxyethanol can be increased when used in combination with Pregabalin.Approved
PhensuximideThe therapeutic efficacy of Phensuximide can be decreased when used in combination with Pregabalin.Approved
PhenytoinThe therapeutic efficacy of Phenytoin can be decreased when used in combination with Pregabalin.Approved, Vet Approved
PimozideThe therapeutic efficacy of Pimozide can be increased when used in combination with Pregabalin.Approved
PioglitazoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Pioglitazone.Approved, Investigational
PipamperoneThe therapeutic efficacy of Pipamperone can be increased when used in combination with Pregabalin.Approved, Investigational
PipotiazineThe therapeutic efficacy of Pipotiazine can be increased when used in combination with Pregabalin.Approved, Investigational
PiritramideThe therapeutic efficacy of Piritramide can be increased when used in combination with Pregabalin.Approved, Investigational
PizotifenThe therapeutic efficacy of Pizotifen can be increased when used in combination with Pregabalin.Approved
PomalidomideThe therapeutic efficacy of Pomalidomide can be increased when used in combination with Pregabalin.Approved
PramipexolePregabalin may increase the sedative activities of Pramipexole.Approved, Investigational
PramlintideThe risk or severity of heart failure can be increased when Pregabalin is combined with Pramlintide.Approved, Investigational
PramocaineThe therapeutic efficacy of Pramocaine can be increased when used in combination with Pregabalin.Approved
PrazepamThe therapeutic efficacy of Prazepam can be increased when used in combination with Pregabalin.Approved, Illicit
PrilocaineThe therapeutic efficacy of Prilocaine can be increased when used in combination with Pregabalin.Approved
PrimidoneThe therapeutic efficacy of Primidone can be decreased when used in combination with Pregabalin.Approved, Vet Approved
ProcaineThe therapeutic efficacy of Procaine can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
ProchlorperazineThe therapeutic efficacy of Prochlorperazine can be increased when used in combination with Pregabalin.Approved, Vet Approved
ProgabideThe therapeutic efficacy of Progabide can be decreased when used in combination with Pregabalin.Approved, Investigational
PromazineThe therapeutic efficacy of Promazine can be increased when used in combination with Pregabalin.Approved, Vet Approved
PromethazineThe therapeutic efficacy of Promethazine can be increased when used in combination with Pregabalin.Approved, Investigational
PropanididThe therapeutic efficacy of Propanidid can be increased when used in combination with Pregabalin.Experimental
ProparacaineThe therapeutic efficacy of Proparacaine can be increased when used in combination with Pregabalin.Approved, Vet Approved
PropofolThe therapeutic efficacy of Propofol can be increased when used in combination with Pregabalin.Approved, Investigational, Vet Approved
PropoxycaineThe therapeutic efficacy of Propoxycaine can be increased when used in combination with Pregabalin.Approved
ProtriptylineThe therapeutic efficacy of Protriptyline can be increased when used in combination with Pregabalin.Approved
ProxibarbalThe therapeutic efficacy of Proxibarbal can be increased when used in combination with Pregabalin.Experimental
PSD502The therapeutic efficacy of PSD502 can be increased when used in combination with Pregabalin.Investigational
QuazepamThe therapeutic efficacy of Quazepam can be increased when used in combination with Pregabalin.Approved, Illicit
QuetiapineThe therapeutic efficacy of Quetiapine can be increased when used in combination with Pregabalin.Approved
QuinaprilThe risk or severity of angioedema can be increased when Quinapril is combined with Pregabalin.Approved, Investigational
QuinisocaineThe therapeutic efficacy of Quinisocaine can be increased when used in combination with Pregabalin.Experimental
RacloprideThe therapeutic efficacy of Raclopride can be increased when used in combination with Pregabalin.Investigational
RamelteonThe therapeutic efficacy of Ramelteon can be increased when used in combination with Pregabalin.Approved, Investigational
RamiprilThe risk or severity of angioedema can be increased when Ramipril is combined with Pregabalin.Approved
RemacemideThe therapeutic efficacy of Remacemide can be decreased when used in combination with Pregabalin.Investigational
RemifentanilThe therapeutic efficacy of Remifentanil can be increased when used in combination with Pregabalin.Approved
RemoxiprideThe therapeutic efficacy of Remoxipride can be increased when used in combination with Pregabalin.Approved, Withdrawn
RepaglinideThe risk or severity of heart failure can be increased when Pregabalin is combined with Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of angioedema can be increased when Rescinnamine is combined with Pregabalin.Approved
ReserpineThe therapeutic efficacy of Reserpine can be increased when used in combination with Pregabalin.Approved, Investigational
RiluzoleThe therapeutic efficacy of Riluzole can be decreased when used in combination with Pregabalin.Approved, Investigational
RisperidoneThe therapeutic efficacy of Risperidone can be increased when used in combination with Pregabalin.Approved, Investigational
RitanserinThe therapeutic efficacy of Ritanserin can be increased when used in combination with Pregabalin.Investigational
RomifidineThe therapeutic efficacy of Romifidine can be increased when used in combination with Pregabalin.Vet Approved
RopinirolePregabalin may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe therapeutic efficacy of Ropivacaine can be increased when used in combination with Pregabalin.Approved
RosiglitazoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Rosiglitazone.Approved, Investigational
RotigotinePregabalin may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pregabalin.Approved
SaxagliptinThe risk or severity of heart failure can be increased when Pregabalin is combined with Saxagliptin.Approved
ScopolamineThe therapeutic efficacy of Scopolamine can be increased when used in combination with Pregabalin.Approved, Investigational
SecobarbitalThe therapeutic efficacy of Secobarbital can be increased when used in combination with Pregabalin.Approved, Vet Approved
SepranoloneThe therapeutic efficacy of Sepranolone can be increased when used in combination with Pregabalin.Investigational
SertindoleThe therapeutic efficacy of Sertindole can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Sertraline.Approved
SevofluraneThe therapeutic efficacy of Sevoflurane can be increased when used in combination with Pregabalin.Approved, Vet Approved
SitagliptinThe risk or severity of heart failure can be increased when Pregabalin is combined with Sitagliptin.Approved, Investigational
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved
SotagliflozinThe risk or severity of heart failure can be increased when Pregabalin is combined with Sotagliflozin.Investigational
SpiraprilThe risk or severity of angioedema can be increased when Spirapril is combined with Pregabalin.Approved
StiripentolThe therapeutic efficacy of Stiripentol can be decreased when used in combination with Pregabalin.Approved
SufentanilThe therapeutic efficacy of Sufentanil can be increased when used in combination with Pregabalin.Approved, Investigational
SulodexideThe risk or severity of heart failure can be increased when Pregabalin is combined with Sulodexide.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be increased when used in combination with Pregabalin.Approved, Investigational
SulthiameThe therapeutic efficacy of Sulthiame can be decreased when used in combination with Pregabalin.Experimental
SultoprideThe therapeutic efficacy of Sultopride can be increased when used in combination with Pregabalin.Experimental
SuvorexantPregabalin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved, Investigational
TandospironeThe therapeutic efficacy of Tandospirone can be increased when used in combination with Pregabalin.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved
TasimelteonThe therapeutic efficacy of Tasimelteon can be increased when used in combination with Pregabalin.Approved, Investigational
TemazepamThe therapeutic efficacy of Temazepam can be increased when used in combination with Pregabalin.Approved, Investigational
TemocaprilThe risk or severity of angioedema can be increased when Temocapril is combined with Pregabalin.Experimental, Investigational
TetrabenazineThe therapeutic efficacy of Tetrabenazine can be increased when used in combination with Pregabalin.Approved, Investigational
TetracaineThe therapeutic efficacy of Tetracaine can be increased when used in combination with Pregabalin.Approved, Vet Approved
TetrahydropalmatineThe therapeutic efficacy of Tetrahydropalmatine can be increased when used in combination with Pregabalin.Investigational
TetrodotoxinThe therapeutic efficacy of Tetrodotoxin can be increased when used in combination with Pregabalin.Investigational
ThalidomideThe therapeutic efficacy of Thalidomide can be increased when used in combination with Pregabalin.Approved, Investigational, Withdrawn
ThiamylalThe therapeutic efficacy of Thiamylal can be increased when used in combination with Pregabalin.Approved, Vet Approved
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Pregabalin.Approved, Vet Approved
ThioridazineThe therapeutic efficacy of Thioridazine can be increased when used in combination with Pregabalin.Approved, Withdrawn
ThiothixeneThe therapeutic efficacy of Thiothixene can be increased when used in combination with Pregabalin.Approved
TiagabineThe therapeutic efficacy of Tiagabine can be decreased when used in combination with Pregabalin.Approved, Investigational
TiaprideThe therapeutic efficacy of Tiapride can be increased when used in combination with Pregabalin.Approved, Investigational
TiletamineThe therapeutic efficacy of Tiletamine can be decreased when used in combination with Pregabalin.Vet Approved
TilidineThe therapeutic efficacy of Tilidine can be increased when used in combination with Pregabalin.Experimental
TizanidineThe therapeutic efficacy of Tizanidine can be decreased when used in combination with Pregabalin.Approved, Investigational
TolazamideThe risk or severity of heart failure can be increased when Pregabalin is combined with Tolazamide.Approved, Investigational
TolbutamideThe risk or severity of heart failure can be increased when Pregabalin is combined with Tolbutamide.Approved, Investigational
TolcaponeThe therapeutic efficacy of Tolcapone can be increased when used in combination with Pregabalin.Approved, Withdrawn
TopiramateThe therapeutic efficacy of Topiramate can be decreased when used in combination with Pregabalin.Approved
TramadolThe therapeutic efficacy of Tramadol can be increased when used in combination with Pregabalin.Approved, Investigational
TramiprosateThe therapeutic efficacy of Tramiprosate can be decreased when used in combination with Pregabalin.Investigational
TrandolaprilThe risk or severity of angioedema can be increased when Trandolapril is combined with Pregabalin.Approved
Trans-2-PhenylcyclopropylamineThe therapeutic efficacy of Trans-2-Phenylcyclopropylamine can be increased when used in combination with Pregabalin.Experimental
TranylcypromineThe therapeutic efficacy of Tranylcypromine can be increased when used in combination with Pregabalin.Approved, Investigational
TrazodoneThe therapeutic efficacy of Trazodone can be increased when used in combination with Pregabalin.Approved, Investigational
TriazolamThe therapeutic efficacy of Triazolam can be increased when used in combination with Pregabalin.Approved, Investigational
Tricaine methanesulfonateThe therapeutic efficacy of Tricaine methanesulfonate can be increased when used in combination with Pregabalin.Vet Approved
TrichloroethyleneThe therapeutic efficacy of Trichloroethylene can be increased when used in combination with Pregabalin.Approved
TrifluoperazineThe therapeutic efficacy of Trifluoperazine can be increased when used in combination with Pregabalin.Approved, Investigational
TrifluperidolThe therapeutic efficacy of Trifluperidol can be increased when used in combination with Pregabalin.Experimental
TriflupromazineThe therapeutic efficacy of Triflupromazine can be increased when used in combination with Pregabalin.Approved, Vet Approved
TrimethadioneThe therapeutic efficacy of Trimethadione can be decreased when used in combination with Pregabalin.Approved
TrimipramineThe therapeutic efficacy of Trimipramine can be increased when used in combination with Pregabalin.Approved
TriprolidineThe therapeutic efficacy of Triprolidine can be increased when used in combination with Pregabalin.Approved
TroglitazoneThe risk or severity of heart failure can be increased when Pregabalin is combined with Troglitazone.Investigational, Withdrawn
Valproic AcidThe therapeutic efficacy of Valproic Acid can be decreased when used in combination with Pregabalin.Approved, Investigational
ValpromideThe therapeutic efficacy of Valpromide can be decreased when used in combination with Pregabalin.Experimental
VenlafaxineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Venlafaxine.Approved
VeraliprideThe therapeutic efficacy of Veralipride can be increased when used in combination with Pregabalin.Experimental
VigabatrinThe therapeutic efficacy of Vigabatrin can be decreased when used in combination with Pregabalin.Approved
VildagliptinThe risk or severity of heart failure can be increased when Pregabalin is combined with Vildagliptin.Approved, Investigational
VinpocetineThe therapeutic efficacy of Vinpocetine can be decreased when used in combination with Pregabalin.Investigational
Vinyl etherThe therapeutic efficacy of Vinyl ether can be increased when used in combination with Pregabalin.Experimental
VogliboseThe risk or severity of heart failure can be increased when Pregabalin is combined with Voglibose.Approved, Investigational
VortioxetineThe therapeutic efficacy of Vortioxetine can be increased when used in combination with Pregabalin.Approved, Investigational
XenonThe therapeutic efficacy of Xenon can be increased when used in combination with Pregabalin.Experimental
XylazineThe therapeutic efficacy of Xylazine can be increased when used in combination with Pregabalin.Vet Approved
YohimbineThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Yohimbine.Approved, Investigational, Vet Approved
ZaleplonThe therapeutic efficacy of Zaleplon can be decreased when used in combination with Pregabalin.Approved, Illicit, Investigational
ZiconotideThe therapeutic efficacy of Ziconotide can be increased when used in combination with Pregabalin.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Pregabalin is combined with Zimelidine.Withdrawn
ZiprasidoneThe therapeutic efficacy of Ziprasidone can be increased when used in combination with Pregabalin.Approved
ZofenoprilThe risk or severity of angioedema can be increased when Zofenopril is combined with Pregabalin.Experimental
ZolazepamThe therapeutic efficacy of Zolazepam can be increased when used in combination with Pregabalin.Vet Approved
ZolpidemPregabalin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe therapeutic efficacy of Zonisamide can be decreased when used in combination with Pregabalin.Approved, Investigational
ZopicloneThe therapeutic efficacy of Zopiclone can be increased when used in combination with Pregabalin.Approved
ZotepineThe therapeutic efficacy of Zotepine can be increased when used in combination with Pregabalin.Approved, Investigational
ZuclopenthixolThe therapeutic efficacy of Zuclopenthixol can be increased when used in combination with Pregabalin.Approved, Investigational
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.

References

Synthesis Reference

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

US20030212290
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. Pfizer [Link]
External Links
Human Metabolome Database
HMDB0014375
KEGG Drug
D02716
PubChem Compound
5486971
PubChem Substance
46504934
ChemSpider
4589156
BindingDB
50164279
ChEBI
64356
ChEMBL
CHEMBL1059
Therapeutic Targets Database
DAP001264
PharmGKB
PA164754814
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pregabalin
ATC Codes
N03AX16 — Pregabalin
AHFS Codes
  • 28:12.92 — Miscellaneous Anticonvulsants
FDA label
Download (3.46 MB)
MSDS
Download (106 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentNicotine Dependence1
0CompletedTreatmentPost-Operative Pain1
0RecruitingTreatmentCannabis-use Disorders1
1CompletedNot AvailableHealthy Volunteers10
1CompletedNot AvailableNerve Pain1
1CompletedBasic ScienceHealthy Volunteers8
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
1Unknown StatusTreatmentRefractive Errors1
1, 2CompletedTreatmentEpilepsy, Localization Related1
1, 2CompletedTreatmentPrimary Total Knee Arthroplasty1
1, 2RecruitingTreatmentCoughing1
2CompletedNot AvailableFeeling Anxious1
2CompletedSupportive CareBrain and Central Nervous System Tumors / Seizures1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentCRP1
2CompletedTreatmentCancers / Pain1
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 Pain2
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
2CompletedTreatmentDiabetic Peripheral Neuropathy (DPN) / Pain1
2CompletedTreatmentElective Laparoscopic Cholecystectomy / Sevoflurane Anesthesia1
2CompletedTreatmentEpilepsy, Localization Related1
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2CompletedTreatmentOveractive Bladder1
2CompletedTreatmentPain1
2CompletedTreatmentPain / Postherpetic Neuralgia1
2CompletedTreatmentPostherpetic Neuralgia1
2CompletedTreatmentRestless Legs Syndrome (RLS)1
2RecruitingTreatmentEarache1
2RecruitingTreatmentGulf War Illness1
2RecruitingTreatmentIdiopathic Small Fiber Neuropathy1
2TerminatedPreventionCancer, Breast / Malignant Lymphomas / Pain1
2TerminatedTreatmentFibromyalgia1
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 / Taxane1
2Unknown StatusTreatmentFibromyalgia / Pain, Chronic1
2WithdrawnTreatmentDiabetes Mellitus (DM) / Pain, Neuropathic1
2, 3CompletedBasic ScienceFibromyalgia1
2, 3CompletedPreventionPostoperative pain1
2, 3CompletedTreatmentAcute Agitation / Dementias / Pain1
2, 3CompletedTreatmentDiabetes Mellitus (DM) / Peripheral Neuropathy1
2, 3CompletedTreatmentPancreatitis, Chronic1
2, 3RecruitingPreventionEye Dryness1
2, 3RecruitingPreventionPregabalin on Catheter Related Bladder Discomfort2
3Active Not RecruitingPreventionChronic Post-surgical Pain / Post-mastectomy Pain Syndrome1
3CompletedHealth Services ResearchHysterectomy1
3CompletedPreventionDelirium / Pain1
3CompletedPreventionPain / 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
3CompletedTreatmentEpilepsies1
3CompletedTreatmentEpilepsy, Complex Partial / Epilepsy, Localization Related1
3CompletedTreatmentEpilepsy, Localization Related2
3CompletedTreatmentEpilepsy, Localization Related / Sleep Deprivation1
3CompletedTreatmentEpilepsy, Localization Related / Partial onset seizure Epilepsy1
3CompletedTreatmentFeeling Anxious1
3CompletedTreatmentFibromyalgia13
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
3CompletedTreatmentNeuroses, Anxiety1
3CompletedTreatmentOsteoarthritis (OA)1
3CompletedTreatmentOsteoarthritis (OA) / Postoperative pain1
3CompletedTreatmentPain2
3CompletedTreatmentPain Associated With Fibromyalgia3
3CompletedTreatmentPain, Chronic1
3CompletedTreatmentPain, Neuropathic4
3CompletedTreatmentPainful Diabetic Peripheral Neuropathy (PDPN)1
3CompletedTreatmentNeurocostal neuralgia / Pain / Spinal Cord Diseases / Spinal Cord Injuries (SCI)1
3CompletedTreatmentPost-Herpetic Neuralgia (PHN)1
3CompletedTreatmentPostherpetic Neuralgia2
3CompletedTreatmentPostoperative pain3
3CompletedTreatmentRadicular syndrome1
3CompletedTreatmentRestless Legs Syndrome (RLS)1
3CompletedTreatmentSeizure Disorder, Partial4
3CompletedTreatmentSeizures1
3CompletedTreatmentNeurocostal neuralgia / Spinal Cord Injuries (SCI)1
3CompletedTreatmentNeurocostal neuralgia2
3CompletedTreatmentPartial onset seizure Epilepsy2
3Not Yet RecruitingPreventionHerpetic Neuralgia1
3Not Yet RecruitingTreatmentAlcohol Use Disorder (AUD) / PTSD1
3RecruitingPreventionPersistent Postoperative Pain1
3RecruitingPreventionPhantom Pain1
3RecruitingPreventionPostoperative pain1
3RecruitingTreatmentEpilepsy, Partial Seizures / Epilepsy, Primary Generalized Tonic-Clonic Seizures1
3RecruitingTreatmentFibromyalgia1
3RecruitingTreatmentLiver Cirrhosis / Muscle Cramps1
3RecruitingTreatmentPain of Mononeuropathy1
3RecruitingTreatmentPain, Neuropathic1
3RecruitingTreatmentPeripheral Neuropathic Pain1
3RecruitingTreatmentPostherpetic Neuralgia1
3TerminatedPreventionPain / Spinal Cord Trauma1
3TerminatedSupportive CarePerioperative Pain1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentEpilepsies1
3TerminatedTreatmentEpilepsy, Localization Related1
3TerminatedTreatmentFusion of Spine (Disease)1
3TerminatedTreatmentInfection, Human Immunodeficiency Virus I / Pain, Neuropathic1
3TerminatedTreatmentNeuropathy1
3Unknown StatusPreventionInguinal Hernias / Postoperative pain1
3Unknown StatusTreatmentCancers / Neurocostal neuralgia1
3Unknown StatusTreatmentChronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS)1
3Unknown StatusTreatmentDiabetic Neuropathies1
3Unknown StatusTreatmentPostoperative pain1
3WithdrawnPreventionPain, Chronic1
3WithdrawnTreatmentMigraine Disorders1
3WithdrawnTreatmentRestless Legs Syndrome (RLS)1
4Active Not RecruitingTreatmentAlcoholism1
4Active Not RecruitingTreatmentPain, Acute1
4Active Not RecruitingTreatmentPost Operative Pain1
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 / Partial Seizure Disorder1
4CompletedTreatmentCryptogenic Sensory Polyneuropathy1
4CompletedTreatmentDiabetic Neuropathies1
4CompletedTreatmentDiabetic Neuropathy, Painful3
4CompletedTreatmentDiabetic Peripheral Neuropathic Pain2
4CompletedTreatmentDiabetic Peripheral Neuropathy (DPN)1
4CompletedTreatmentDisk Prolapse / Intervertebral Disk Displacement1
4CompletedTreatmentEpilepsies1
4CompletedTreatmentEpilepsy, Localization Related1
4CompletedTreatmentFailed Back Surgery Syndrome / Intervertebral Disc Herniation / Neuropathy; Radicular, Lumbar, Lumbosacral / Spinal Stenosis1
4CompletedTreatmentFibromyalgia4
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
4CompletedTreatmentPain1
4CompletedTreatmentPain, Chronic1
4CompletedTreatmentPainful Diabetic Neuropathy and Post Herpetic Neuralgia1
4CompletedTreatmentPain / Postoperative1
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 pain3
4CompletedTreatmentSeizures1
4CompletedTreatmentNeurocostal neuralgia / Spinal Cord Injuries (SCI)1
4CompletedTreatmentAdjunct to general anesthesia therapy / Surgery, Laparoscopic1
4CompletedTreatmentTremor, Essential2
4CompletedTreatmentNeurocostal neuralgia1
4Not Yet RecruitingTreatmentPain, Neuropathic1
4RecruitingSupportive CareScoliosis / Spondylolisthesis1
4RecruitingTreatmentArterial Occlusive Diseases / Critical Limb Ischemia (CLI) / Pain / Transient ischemia attacks1
4RecruitingTreatmentEpilepsy, Localization Related1
4RecruitingTreatmentHepatocellular Cancer1
4RecruitingTreatmentLumbar Disc Disease / Lumbar Radiculopathy / Prolapsed Lumbar Disc1
4RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
4RecruitingTreatmentOpiate withdrawal symptoms1
4TerminatedBasic ScienceSubstance-Related Disorders1
4TerminatedTreatmentAbdominal Pain (AP) / Surgical Adhesions1
4TerminatedTreatmentBone Neoplasms / Cancers / 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 StatusPreventionChronic Illnesses / Hyperalgesia / Pain / Pain, Neuropathic1
4Unknown StatusTreatmentFeeling Anxious1
4Unknown StatusTreatmentPain, Neuropathic / Spinal Cord Injuries (SCI)1
4Unknown StatusTreatmentPain, Neuropathic / Tactile Hyperalgesia1
4Unknown StatusTreatmentPolyneuropathies1
4Unknown StatusTreatmentUremic Pruritus2
4WithdrawnDiagnosticLow Back Pain (LBP) / Neurocostal neuralgia1
4WithdrawnTreatmentChronic Pain, Postoperative / Headaches1
4WithdrawnTreatmentDiabetic Polyneuropathy / Postherpetic Neuralgia1
4WithdrawnTreatmentFibromyalgia1
4WithdrawnTreatmentRestless Legs Syndrome (RLS)1
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 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 AvailableCompletedOtherSedation, Conscious1
Not AvailableCompletedPreventionPain2
Not AvailableCompletedPreventionPain, Neuropathic1
Not AvailableCompletedSupportive CarePain1
Not AvailableCompletedSupportive CarePain / Peripheral Neuropathy1
Not AvailableCompletedSupportive CarePostoperative pain1
Not AvailableCompletedTreatmentHepatocellular,Carcinoma / Postoperative pain1
Not AvailableCompletedTreatmentPain2
Not AvailableCompletedTreatmentPostoperative pain1
Not AvailableNot Yet RecruitingPreventionAnterior Cruciate Ligament (ACL) Reconstruction1
Not AvailableNot Yet RecruitingTreatmentFibromyalgia / Hyperbaric Oxygen1
Not AvailableNot Yet RecruitingTreatmentPeripheral Arterial Disease (PAD)1
Not AvailableRecruitingNot AvailablePain, Neuropathic / Postoperative pain1
Not AvailableRecruitingOtherNeuropathy / Pain1
Not AvailableRecruitingSupportive CarePostoperative pain1
Not AvailableRecruitingSupportive CareSpine Surgery1
Not AvailableRecruitingTreatmentOropharyngeal Cancers / Squamous Cell Carcinoma to the Head and Neck1
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 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

Pharmacoeconomics

Manufacturers
Packagers
Dosage forms
FormRouteStrength
CapsuleOral100 mg/1
CapsuleOral100 mg
CapsuleOral150 mg/1
CapsuleOral150 mg
CapsuleOral200 mg
CapsuleOral200 mg/1
CapsuleOral225 mg
CapsuleOral225 mg/1
CapsuleOral25 mg/1
CapsuleOral25 mg
CapsuleOral300 mg
CapsuleOral300 mg/1
CapsuleOral50 mg
CapsuleOral50 mg/1
CapsuleOral75 mg/1
CapsuleOral75 mg
SolutionOral20 mg/mL
Tablet, film coated, extended releaseOral165 mg/1
Tablet, film coated, extended releaseOral330 mg/1
Tablet, film coated, extended releaseOral82.5 mg/1
Prices
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.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5563175No1993-10-082013-10-08Us
CA2327285No2005-06-142019-05-10Canada
CA2297163No2001-11-202018-08-18Canada
US6001876No1998-12-302018-12-30Us
USRE41920No1998-12-302018-12-30Us
US6197819No1998-12-302018-12-30Us
US9144559No2006-11-022026-11-02Us
US8945620No2006-11-022026-11-02Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)186-188ºCNot Available
boiling point (°C)274ºC at 760 mm HgNot Available
water solubilityFreely soluble FDA label
logP-1.35FDA label
pKa4.2 and 10.6 FDA label
Predicted Properties
PropertyValueSource
Water Solubility11.3 mg/mLALOGPS
logP-1.4ALOGPS
logP-1.3ChemAxon
logS-1.2ALOGPS
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
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
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
CarcinogenicityNon-carcinogens0.5678
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
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

Taxonomy

Description
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.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
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
Substituents
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)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1A
Uniprot ID
O00555
Uniprot Name
Voltage-dependent P/Q-type calcium channel subunit alpha-1A
Molecular Weight
282362.39 Da
References
  1. Gazulla J, Tintore M: The P/Q-type voltage-dependent calcium channel: a therapeutic target in spinocerebellar ataxia type 6. Acta Neurol Scand. 2007 May;115(5):356-63. [PubMed:17489948]
  2. Gazulla J, Tintore MA: The P/Q-type voltage-dependent calcium channel as pharmacological target in spinocerebellar ataxia type 6: gabapentin and pregabalin may be of therapeutic benefit. Med Hypotheses. 2007;68(1):131-6. Epub 2006 Aug 8. [PubMed:16899342]
  3. Jacquy J, Lossignol D, Sternon J: [Pregabalin (Lyrica) and neuropathic pain syndromes]. Rev Med Brux. 2006 Sep-Oct;27(5):445-50. [PubMed:17144644]
  4. Taylor CP, Angelotti T, Fauman E: Pharmacology and mechanism of action of pregabalin: the calcium channel alpha2-delta (alpha2-delta) subunit as a target for antiepileptic drug discovery. Epilepsy Res. 2007 Feb;73(2):137-50. Epub 2006 Nov 28. [PubMed:17126531]
  5. Field MJ, Cox PJ, Stott E, Melrose H, Offord J, Su TZ, Bramwell S, Corradini L, England S, Winks J, Kinloch RA, Hendrich J, Dolphin AC, Webb T, Williams D: Identification of the alpha2-delta-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17537-42. Epub 2006 Nov 6. [PubMed:17088553]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other
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
SLC1A1
Uniprot ID
P43005
Uniprot Name
Excitatory amino acid transporter 3
Molecular Weight
57099.835 Da
References
  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]

Drug created on June 13, 2005 07:24 / Updated on February 13, 2018 09:32