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Identification
Namegabapentin enacarbil
Accession NumberDB08872
TypeSmall Molecule
GroupsApproved
DescriptionGabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Structure
Thumb
Synonyms
Gabapentina enacarbilo
Gabapentine enacarbil
Gabapentinum enacarbilum
Horizant
XP 13512
XP-13512
XP13512
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Horizanttablet, extended release600 mg/1oralXeno Port Inc.2013-05-01Not applicableUs
Horizanttablet, extended release300 mg/1oralXeno Port Inc.2013-05-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII75OCL1SPBQ
CAS number478296-72-9
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationFor the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
PharmacodynamicsSince gabapentin enacarbil is a prodrug of gabapentin, it's physiological effects are the same as gabapentin. Concerning PHN, gabapentin prevents allodynia and hyperalgesia.
Mechanism of actionAlthough the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Related Articles
AbsorptionGabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
Volume of distribution

The volume of distribution is 76L.

Protein bindingGabapentin plasma protein binding is less than 3%.
Metabolism

Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.

Route of eliminationGabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
Half lifeThe elimination half-life of gabapentin is 5.1 to 6.0 hours.
Clearance

Renal clearance of gabapentin is 5 to 7 L/hr.

ToxicityMost common adverse reactions are headache, dizziness, and somnolence.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, extended releaseoral300 mg/1
Tablet, extended releaseoral600 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6818787 No2002-11-062022-11-06Us
US8026279 No2006-11-102026-11-10Us
US8048917 No2002-11-062022-11-06Us
US8114909 No2006-04-112026-04-11Us
US8686034 No2005-01-242025-01-24Us
US8795725 No2009-06-102029-06-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting pointMelting onset of about 64°C.From FDA label.
water solubilitySolubility of 0.5 mg/mL in water From FDA label.
pKapKa 5.0From The Merck Index.
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
References
Synthesis Reference

1. Cundy KC, Branch R, Chernov-Rogan T, Dias T, Estrada T, Hold K, Koller K, Liu X, Mann A, Panuwat M, Raillard SP, Upadhyay S, Wu QQ, Xiang JN, Yan H, Zerangue N, Zhou CX, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. Epub 2004 May 14.

General References
  1. Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. [PubMed:15146029 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (347 KB)
MSDSDownload (30.7 KB)
Interactions
Drug Interactions
Drug
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with gabapentin enacarbil.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with gabapentin enacarbil.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with gabapentin enacarbil.
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with gabapentin enacarbil.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with gabapentin enacarbil.
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with gabapentin enacarbil.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with gabapentin enacarbil.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with gabapentin enacarbil.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with gabapentin enacarbil.
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with gabapentin enacarbil.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with gabapentin enacarbil.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with gabapentin enacarbil.
AmoxapineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with gabapentin enacarbil.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with gabapentin enacarbil.
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with gabapentin enacarbil.
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with gabapentin enacarbil.
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with gabapentin enacarbil.
Azelastinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with gabapentin enacarbil.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with gabapentin enacarbil.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with gabapentin enacarbil.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with gabapentin enacarbil.
BrexpiprazoleThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
BrimonidineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with gabapentin enacarbil.
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with gabapentin enacarbil.
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with gabapentin enacarbil.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with gabapentin enacarbil.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with gabapentin enacarbil.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with gabapentin enacarbil.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with gabapentin enacarbil.
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with gabapentin enacarbil.
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with gabapentin enacarbil.
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with gabapentin enacarbil.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with gabapentin enacarbil.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with gabapentin enacarbil.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with gabapentin enacarbil.
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with gabapentin enacarbil.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with gabapentin enacarbil.
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with gabapentin enacarbil.
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with gabapentin enacarbil.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with gabapentin enacarbil.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with gabapentin enacarbil.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with gabapentin enacarbil.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with gabapentin enacarbil.
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with gabapentin enacarbil.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with gabapentin enacarbil.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with gabapentin enacarbil.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with gabapentin enacarbil.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with gabapentin enacarbil.
CitalopramThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with gabapentin enacarbil.
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with gabapentin enacarbil.
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with gabapentin enacarbil.
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with gabapentin enacarbil.
ClomipramineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with gabapentin enacarbil.
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with gabapentin enacarbil.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with gabapentin enacarbil.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with gabapentin enacarbil.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with gabapentin enacarbil.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with gabapentin enacarbil.
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with gabapentin enacarbil.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with gabapentin enacarbil.
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with gabapentin enacarbil.
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with gabapentin enacarbil.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with gabapentin enacarbil.
DapoxetineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Dapoxetine.
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with gabapentin enacarbil.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with gabapentin enacarbil.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with gabapentin enacarbil.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with gabapentin enacarbil.
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with gabapentin enacarbil.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with gabapentin enacarbil.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with gabapentin enacarbil.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with gabapentin enacarbil.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with gabapentin enacarbil.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with gabapentin enacarbil.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with gabapentin enacarbil.
DifenoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with gabapentin enacarbil.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with gabapentin enacarbil.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with gabapentin enacarbil.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with gabapentin enacarbil.
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with gabapentin enacarbil.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with gabapentin enacarbil.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with gabapentin enacarbil.
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with gabapentin enacarbil.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with gabapentin enacarbil.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
DoxylamineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with gabapentin enacarbil.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with gabapentin enacarbil.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with gabapentin enacarbil.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with gabapentin enacarbil.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with gabapentin enacarbil.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with gabapentin enacarbil.
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with gabapentin enacarbil.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with gabapentin enacarbil.
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with gabapentin enacarbil.
EscitalopramThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with gabapentin enacarbil.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with gabapentin enacarbil.
Ethanolgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with gabapentin enacarbil.
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with gabapentin enacarbil.
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with gabapentin enacarbil.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with gabapentin enacarbil.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with gabapentin enacarbil.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with gabapentin enacarbil.
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with gabapentin enacarbil.
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with gabapentin enacarbil.
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with gabapentin enacarbil.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with gabapentin enacarbil.
EtoperidoneThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with gabapentin enacarbil.
EzogabineThe risk or severity of adverse effects can be increased when Ezogabine is combined with gabapentin enacarbil.
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with gabapentin enacarbil.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with gabapentin enacarbil.
FenfluramineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with gabapentin enacarbil.
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with gabapentin enacarbil.
FlibanserinThe risk or severity of adverse effects can be increased when Flibanserin is combined with gabapentin enacarbil.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with gabapentin enacarbil.
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with gabapentin enacarbil.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with gabapentin enacarbil.
FluoxetineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with gabapentin enacarbil.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with gabapentin enacarbil.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with gabapentin enacarbil.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with gabapentin enacarbil.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with gabapentin enacarbil.
FluvoxamineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with gabapentin enacarbil.
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with gabapentin enacarbil.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with gabapentin enacarbil.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with gabapentin enacarbil.
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with gabapentin enacarbil.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with gabapentin enacarbil.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with gabapentin enacarbil.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with gabapentin enacarbil.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with gabapentin enacarbil.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with gabapentin enacarbil.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with gabapentin enacarbil.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with gabapentin enacarbil.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
HydroxyzineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Iloperidone is combined with gabapentin enacarbil.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with gabapentin enacarbil.
IndalpineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with gabapentin enacarbil.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with gabapentin enacarbil.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with gabapentin enacarbil.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with gabapentin enacarbil.
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with gabapentin enacarbil.
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with gabapentin enacarbil.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with gabapentin enacarbil.
LevocabastineThe risk or severity of adverse effects can be increased when Levocabastine is combined with gabapentin enacarbil.
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with gabapentin enacarbil.
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with gabapentin enacarbil.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with gabapentin enacarbil.
LevomilnacipranThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with gabapentin enacarbil.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with gabapentin enacarbil.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with gabapentin enacarbil.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with gabapentin enacarbil.
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with gabapentin enacarbil.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with gabapentin enacarbil.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with gabapentin enacarbil.
Lu AA21004The risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with gabapentin enacarbil.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Magnesium SulfateThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with gabapentin enacarbil.
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with gabapentin enacarbil.
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with gabapentin enacarbil.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with gabapentin enacarbil.
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with gabapentin enacarbil.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with gabapentin enacarbil.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with gabapentin enacarbil.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with gabapentin enacarbil.
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with gabapentin enacarbil.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with gabapentin enacarbil.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with gabapentin enacarbil.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with gabapentin enacarbil.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with gabapentin enacarbil.
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with gabapentin enacarbil.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with gabapentin enacarbil.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with gabapentin enacarbil.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with gabapentin enacarbil.
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with gabapentin enacarbil.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with gabapentin enacarbil.
Metyrosinegabapentin enacarbil may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with gabapentin enacarbil.
MilnacipranThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Mirtazapinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with gabapentin enacarbil.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with gabapentin enacarbil.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with gabapentin enacarbil.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
NabiloneThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with gabapentin enacarbil.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with gabapentin enacarbil.
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with gabapentin enacarbil.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with gabapentin enacarbil.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with gabapentin enacarbil.
OlanzapineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with gabapentin enacarbil.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with gabapentin enacarbil.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with gabapentin enacarbil.
Orphenadrinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with gabapentin enacarbil.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with gabapentin enacarbil.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with gabapentin enacarbil.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with gabapentin enacarbil.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with gabapentin enacarbil.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with gabapentin enacarbil.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with gabapentin enacarbil.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with gabapentin enacarbil.
Paraldehydegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with gabapentin enacarbil.
ParoxetineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with gabapentin enacarbil.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with gabapentin enacarbil.
PerampanelThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with gabapentin enacarbil.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with gabapentin enacarbil.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with gabapentin enacarbil.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with gabapentin enacarbil.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with gabapentin enacarbil.
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with gabapentin enacarbil.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with gabapentin enacarbil.
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with gabapentin enacarbil.
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with gabapentin enacarbil.
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with gabapentin enacarbil.
PomalidomideThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Pomalidomide.
Pramipexolegabapentin enacarbil may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with gabapentin enacarbil.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with gabapentin enacarbil.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with gabapentin enacarbil.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with gabapentin enacarbil.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with gabapentin enacarbil.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with gabapentin enacarbil.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with gabapentin enacarbil.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with gabapentin enacarbil.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with gabapentin enacarbil.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with gabapentin enacarbil.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with gabapentin enacarbil.
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with gabapentin enacarbil.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with gabapentin enacarbil.
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with gabapentin enacarbil.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with gabapentin enacarbil.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with gabapentin enacarbil.
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with gabapentin enacarbil.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with gabapentin enacarbil.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with gabapentin enacarbil.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with gabapentin enacarbil.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with gabapentin enacarbil.
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with gabapentin enacarbil.
Ropinirolegabapentin enacarbil may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with gabapentin enacarbil.
Rotigotinegabapentin enacarbil may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with gabapentin enacarbil.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with gabapentin enacarbil.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with gabapentin enacarbil.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with gabapentin enacarbil.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with gabapentin enacarbil.
SertralineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with gabapentin enacarbil.
Sodium oxybateThe risk or severity of adverse effects can be increased when Sodium oxybate is combined with gabapentin enacarbil.
StiripentolThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with gabapentin enacarbil.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with gabapentin enacarbil.
SuvorexantThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with gabapentin enacarbil.
TasimelteonThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with gabapentin enacarbil.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with gabapentin enacarbil.
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with gabapentin enacarbil.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with gabapentin enacarbil.
Thalidomidegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with gabapentin enacarbil.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with gabapentin enacarbil.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with gabapentin enacarbil.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with gabapentin enacarbil.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with gabapentin enacarbil.
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with gabapentin enacarbil.
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with gabapentin enacarbil.
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with gabapentin enacarbil.
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with gabapentin enacarbil.
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with gabapentin enacarbil.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with gabapentin enacarbil.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with gabapentin enacarbil.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with gabapentin enacarbil.
TrazodoneThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with gabapentin enacarbil.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with gabapentin enacarbil.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with gabapentin enacarbil.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with gabapentin enacarbil.
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with gabapentin enacarbil.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with gabapentin enacarbil.
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with gabapentin enacarbil.
VilazodoneThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with gabapentin enacarbil.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with gabapentin enacarbil.
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with gabapentin enacarbil.
ZimelidineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with gabapentin enacarbil.
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with gabapentin enacarbil.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with gabapentin enacarbil.
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with gabapentin enacarbil.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with gabapentin enacarbil.
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with gabapentin enacarbil.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with gabapentin enacarbil.
Food Interactions
  • No food effects.

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Symporter activity
Specific Function:
Acts as an electrogenic sodium (Na(+)) and chloride (Cl-)-dependent sodium-coupled solute transporter, including transport of monocarboxylates (short-chain fatty acids including L-lactate, D-lactate, pyruvate, acetate, propionate, valerate and butyrate), lactate, mocarboxylate drugs (nicotinate, benzoate, salicylate and 5-aminosalicylate) and ketone bodies (beta-D-hydroxybutyrate, acetoacetate ...
Gene Name:
SLC5A8
Uniprot ID:
Q8N695
Molecular Weight:
66577.005 Da
References
  1. Cundy KC, Branch R, Chernov-Rogan T, Dias T, Estrada T, Hold K, Koller K, Liu X, Mann A, Panuwat M, Raillard SP, Upadhyay S, Wu QQ, Xiang JN, Yan H, Zerangue N, Zhou CX, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. Epub 2004 May 14. [PubMed:15146028 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Sodium-dependent multivitamin transmembrane transporter activity
Specific Function:
Transports pantothenate, biotin and lipoate in the presence of sodium.
Gene Name:
SLC5A6
Uniprot ID:
Q9Y289
Molecular Weight:
68641.27 Da
References
  1. Cundy KC, Branch R, Chernov-Rogan T, Dias T, Estrada T, Hold K, Koller K, Liu X, Mann A, Panuwat M, Raillard SP, Upadhyay S, Wu QQ, Xiang JN, Yan H, Zerangue N, Zhou CX, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. Epub 2004 May 14. [PubMed:15146028 ]
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Drug created on May 02, 2013 15:20 / Updated on September 26, 2016 02:14