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Identification
NamePhenobarbital
Accession NumberDB01174  (APRD00184)
TypeSmall Molecule
GroupsApproved
Description

A barbituric acid derivative that acts as a nonselective central nervous system depressant. It promotes binding to inhibitory gamma-aminobutyric acid subtype receptors, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. [PubChem]

Structure
Thumb
Synonyms
5-ethyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Ethyl-5-phenyl-pyrimidine-2,4,6-trione
5-Ethyl-5-phenylbarbituric acid
5-ethyl-5-phenylpyrimidine-2,4,6(1H,3H,5H)-trione
5-Phenyl-5-ethylbarbituric acid
Luminal
Phenobarbital
Phenobarbitol
Phenobarbitone
Phenobarbituric Acid
Phenylaethylbarbitursaeure
Phenylethylbarbiturate
Phenylethylbarbituric Acid
Phenylethylbarbitursaeure
PHENYLETHYLMALONYLUREA
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Barbilixir Elx 4mg/mlelixir4 mgoralD.C. Labs Limited1983-12-312005-07-19Canada
Phenobarbtablet15 mgoralPendopharm Division Of De Pharmascience Inc1957-12-31Not applicableCanada
Phenobarbtablet100 mgoralPendopharm Division Of De Pharmascience Inc1957-12-31Not applicableCanada
Phenobarbtablet60 mgoralPendopharm Division Of De Pharmascience Inc1957-12-31Not applicableCanada
Phenobarbtablet30 mgoralPendopharm Division Of De Pharmascience Inc1957-12-31Not applicableCanada
Phenobarb Elixirelixir5 mgoralPendopharm Division Of De Pharmascience Inc1965-12-31Not applicableCanada
Phenobarbitaltablet60 mg/1oralMc Kesson Contract Packaging2011-11-142016-04-05Us
Phenobarbitaltablet32.4 mg/1oralContract Pharmacy Services Pa2003-02-012016-04-05Us
Phenobarbitaltablet16.2 mg/1oralCardinal Health2002-03-012016-04-05Us
Phenobarbitaltablet16.2 mg/1oralE5 Pharma, Llc2016-01-072016-04-05Us
Phenobarbitaltablet97.2 mg/1oralECI Pharmaceuticals, LLC2014-11-242016-04-05Us
Phenobarbitaltablet97.2 mg/1oralQualitest Pharmaceuticals2001-12-012016-04-23Us
Phenobarbitaltablet30 mg/1oralC.O. Truxton, Inc.2012-03-012016-04-23Us
Phenobarbitaltablet30 mg/1oralMc Kesson Contract Packaging2011-10-242016-04-05Us
Phenobarbitaltablet32.4 mg/1oralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2007-07-172016-04-05Us
Phenobarbitaltablet100 mg/1oralWest Ward Pharmaceuticals Corp2012-03-012016-04-23Us
Phenobarbitaltablet64.8 mg/1oralECI Pharmaceuticals, LLC2014-11-242016-04-05Us
Phenobarbitaltablet64.8 mg/1oralQualitest Pharmaceuticals2001-12-012016-04-23Us
Phenobarbitaltablet60 mg/1oralWest Ward Pharmaceuticals Corp2012-03-012016-04-23Us
Phenobarbitaltablet32.4 mg/1oralECI Pharmaceuticals, LLC2014-11-242016-04-05Us
Phenobarbitaltablet32.4 mg/1oralQualitest Pharmaceuticals2003-02-012016-04-23Us
Phenobarbitaltablet15 mg/1oralMc Kesson Contract Packaging2012-02-202016-04-05Us
Phenobarbitaltablet16.2 mg/1oralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2007-09-052016-04-05Us
Phenobarbitaltablet16.2 mg/1oralECI Pharmaceuticals, LLC2014-11-242016-04-05Us
Phenobarbitaltablet16.2 mg/1oralQualitest Pharmaceuticals2002-03-012016-04-23Us
Phenobarbitaltablet97.2 mg/1oralAmerican Health Packaging2015-03-312016-04-05Us
Phenobarbitaltablet16.2 mg/1oralbryant ranch prepack2002-03-012016-04-05Us
Phenobarbitaltablet30 mg/1oralWest Ward Pharmaceuticals Corp2012-03-012016-04-23Us
Phenobarbitaltablet64.8 mg/1oralAmerican Health Packaging2015-03-312016-04-05Us
Phenobarbitaltablet15 mg/1oralbryant ranch prepack2000-01-012016-04-05Us
Phenobarbitaltablet15 mg/1oralWest Ward Pharmaceuticals Corp2012-03-012016-04-23Us
Phenobarbitalelixir20 mg/5mLoralAtlantic Biologicals Corps1997-01-012016-04-05Us
Phenobarbitalelixir20 mg/5mLoralQualitest Pharmaceuticals1997-01-012016-04-23Us
Phenobarbitaltablet32.4 mg/1oralAmerican Health Packaging2014-08-292016-04-05Us
Phenobarbitaltablet64.8 mg/1oralDIRECT RX2014-01-012016-04-05Us
Phenobarbitaltablet97.2 mg/1oralE5 Pharma, Llc2016-01-072016-04-05Us
Phenobarbitalliquid20 mg/5mLoralPACK Pharmaceuticals, LLC2011-07-082016-04-05Us
Phenobarbitaltablet100 mg/1oralC.O. Truxton, Inc.2012-03-012016-04-23Us
Phenobarbitaltablet32.4 mg/1oralAphena Pharma Solutions Tennessee, Inc.2003-02-012016-04-05Us
Phenobarbitaltablet32.4 mg/1oralPd Rx Pharmaceuticals, Inc.2003-02-012016-04-05Us
Phenobarbitaltablet64.8 mg/1oralE5 Pharma, Llc2016-01-072016-04-05Us
Phenobarbitaltablet15 mg/1oralC.O. Truxton, Inc.2012-03-012016-04-23Us
Phenobarbitaltablet64.8 mg/1oralContract Pharmacy Services Pa2001-12-012016-04-05Us
Phenobarbitaltablet32.4 mg/1oralCardinal Health2003-02-012016-04-05Us
Phenobarbitaltablet32.4 mg/1oralE5 Pharma, Llc2016-01-072016-04-05Us
Phenobarbitaltablet60 mg/1oralC.O. Truxton, Inc.2012-03-012016-04-23Us
Phenobarbital 100mg Tabtablet100 mgoralValeant Canada Lp Valeant Canada S.E.C.1975-12-312009-07-02Canada
Phenobarbital Sodiuminjection130 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.1971-01-012016-04-23Us
Phenobarbital Sodiuminjection65 mg/mLintramuscular; intravenousWest Ward Pharmaceutical Corp.1971-01-012016-04-23Us
Phenobarbital Sodium Injection 120mg/mlsolution120 mgintramuscular; intravenousHospira Healthcare Corporation1981-12-312012-08-03Canada
Phenobarbital Sodium Injection 30mg/mlsolution30 mgintramuscular; intravenous; subcutaneousHospira Healthcare Corporation1981-12-312012-08-03Canada
Phenobarbital Sodium Injection, USPsolution30 mgintramuscular; intravenousSandoz Canada Incorporated2008-02-29Not applicableCanada
Phenobarbital Sodium Injection, USPsolution120 mgintramuscular; intravenousSandoz Canada Incorporated2008-02-29Not applicableCanada
Phenobarbital Tab 15mgtablet15 mgoralErfa Canada 2012 Inc1951-12-312005-08-12Canada
Phenobarbital Tab 15mgtablet15 mgoralValeant Canada Lp Valeant Canada S.E.C.1962-12-312009-07-02Canada
Phenobarbital Tab 30mgtablet30 mgoralValeant Canada Lp Valeant Canada S.E.C.1962-12-312009-07-02Canada
Phenobarbital Tab 30mgtablet30 mgoralErfa Canada 2012 Inc1951-12-312005-08-12Canada
Phenobarbital Tab 60mgtablet60 mgoralErfa Canada 2012 Inc1951-12-312005-08-12Canada
Phenobarbital Tab 60mgtablet60 mgoralValeant Canada Lp Valeant Canada S.E.C.1974-12-312009-07-02Canada
Phenobarbital Tablet 100mgtablet100 mgoralD.C. Labs Limited1951-12-312003-07-11Canada
Phenobarbital Tablet 15mgtablet15 mgoralD.C. Labs Limited1951-12-312003-07-11Canada
Phenobarbital Tablet 30mgtablet30 mgoralD.C. Labs Limited1951-12-312005-07-19Canada
Phenobarbital Tablet 60mgtablet60 mgoralD.C. Labs Limited1951-12-312005-07-19Canada
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
LuminalNot Available
Brand mixtures
NameLabellerIngredients
B-donnaWinder Laboratories, LLC
Belladonna Alkaloids With PhenobartbitalLiberty Pharmaceuticals, Inc.
DiclophenPro Doc Limitee
Dilantin W Phenobarbital 15mgParke Davis Division, Warner Lambert Canada Inc.
Dilantin W Phenobarbital 30mg CapParke Davis Division, Warner Lambert Canada Inc.
DonnatalKAISER FOUNDATION HOSPITALS
Donnatal ElixirAyerst Laboratories
Donnatal ExtentabsPBM Pharmaceuticals, Inc
Donnatal Extentabs SrtWyeth Ayerst Canada Inc.
Donnatal TabWyeth Ayerst Canada Inc.
Me-PB-hyosMethod Pharmaceuticals, Llc
Phenaphen No 2 CapAyerst Laboratories
Phenaphen No 3 CapAyerst Laboratories
Phenaphen No 4 CapAyerst Laboratories
Phenaphen No.2 CapWyeth Ayerst Canada Inc.
Phenaphen No.3 CapWyeth Ayerst Canada Inc.
Phenaphen No.4 CapWyeth Ayerst Canada Inc.
PhenohytroWinder Laboratories, LLC
QuadrapaxRebel Distributors Corp
Re-PB Hyos ElixirKAISER FOUNDATION HOSPITALS
Se-donna Pb HyosSeton Pharmaceuticals
Salts
Name/CASStructureProperties
Phenobarbital sodium
ThumbNot applicableDBSALT001491
Categories
UNIIYQE403BP4D
CAS number50-06-6
WeightAverage: 232.2353
Monoisotopic: 232.08479226
Chemical FormulaC12H12N2O3
InChI KeyInChIKey=DDBREPKUVSBGFI-UHFFFAOYSA-N
InChI
InChI=1S/C12H12N2O3/c1-2-12(8-6-4-3-5-7-8)9(15)13-11(17)14-10(12)16/h3-7H,2H2,1H3,(H2,13,14,15,16,17)
IUPAC Name
5-ethyl-5-phenyl-1,3-diazinane-2,4,6-trione
SMILES
CCC1(C(=O)NC(=O)NC1=O)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as barbituric acid derivatives. These are compounds containing a perhydropyrimidine ring substituted at C-2, -4 and -6 by oxo groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentBarbituric acid derivatives
Alternative Parents
Substituents
  • Barbiturate
  • Ureide
  • Benzenoid
  • 1,3-diazinane
  • Monocyclic benzene moiety
  • Urea
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of all types of seizures except absence seizures.
PharmacodynamicsPhenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal).
Mechanism of actionPhenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal.
Related Articles
AbsorptionAbsorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach.
Volume of distributionNot Available
Protein binding20 to 45%
Metabolism

Hepatic (mostly via CYP2C19).

SubstrateEnzymesProduct
Phenobarbital
p-HydroxyphenobarbitalDetails
p-Hydroxyphenobarbital
Not Available
Phenobarbital O-sulfateDetails
p-Hydroxyphenobarbital
Not Available
Phenobarbital O-glucuronideDetails
Route of eliminationNot Available
Half life53 to 118 hours (mean 79 hours)
ClearanceNot Available
ToxicityCNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur.
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 Absorption+0.9935
Blood Brain Barrier+0.9736
Caco-2 permeable-0.5561
P-glycoprotein substrateSubstrate0.5157
P-glycoprotein inhibitor INon-inhibitor0.6472
P-glycoprotein inhibitor IINon-inhibitor0.9869
Renal organic cation transporterNon-inhibitor0.9235
CYP450 2C9 substrateNon-substrate0.6962
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7702
CYP450 1A2 substrateNon-inhibitor0.84
CYP450 2C9 inhibitorNon-inhibitor0.9023
CYP450 2D6 inhibitorNon-inhibitor0.9593
CYP450 2C19 inhibitorNon-inhibitor0.8664
CYP450 3A4 inhibitorNon-inhibitor0.9236
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9164
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.7469
BiodegradationNot ready biodegradable0.9894
Rat acute toxicity3.1244 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.99
hERG inhibition (predictor II)Non-inhibitor0.9354
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Elixiroral4 mg
Tabletoral
Tablet (extended-release)oral
Tablet, film coated, extended releaseoral
Capsuleoral
Tabletoral100 mg
Tabletoral15 mg
Tabletoral30 mg
Tabletoral60 mg
Elixiroral5 mg
Elixiroral20 mg/5mL
Liquidoral20 mg/5mL
Tabletoral100 mg/1
Tabletoral15 mg/1
Tabletoral16.2 mg/1
Tabletoral30 mg/1
Tabletoral32.4 mg/1
Tabletoral60 mg/1
Tabletoral64.8 mg/1
Tabletoral97.2 mg/1
Injectionintramuscular; intravenous130 mg/mL
Injectionintramuscular; intravenous65 mg/mL
Solutionintramuscular; intravenous; subcutaneous30 mg
Solutionintramuscular; intravenous120 mg
Solutionintramuscular; intravenous30 mg
Elixiroral
Prices
Unit descriptionCostUnit
Phenobarbital 130 mg/ml vial4.32USD ml
Phenobarbital 65 mg/ml vial1.63USD ml
Phenobarbital sodium powder0.36USD g
Pms-Phenobarbital 100 mg Tablet0.15USD tablet
Phenobarbital powder0.13USD g
Pms-Phenobarbital 60 mg Tablet0.11USD tablet
Phenobarbital 97.2 mg tablet0.1USD tablet
Phenobarbital 64.8 mg tablet0.09USD tablet
Pms-Phenobarbital 5 mg/ml Elixir0.09USD ml
Phenobarbital 16.2 mg tablet0.08USD tablet
Phenobarbital 30 mg tablet0.08USD tablet
Phenobarbital 32.4 mg tablet0.08USD tablet
Pms-Phenobarbital 30 mg Tablet0.08USD tablet
Phenobarbital 100 mg tablet0.07USD tablet
Pms-Phenobarbital 15 mg Tablet0.07USD tablet
PHENobarbital 20 mg/5ml Elixir0.06USD ml
Phenobarbital 60 mg tablet0.03USD tablet
Phenobarbital 15 mg tablet0.02USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point174 °CPhysProp
water solubility1110 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.47HANSCH,C ET AL. (1995)
pKa7.3BUDAVARI,S ET AL. (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.276 mg/mLALOGPS
logP1.4ALOGPS
logP1.41ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)8.14ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity59.75 m3·mol-1ChemAxon
Polarizability22.61 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.44 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-ozn0000000-193bf296d3e5d1705628View in MoNA
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
References
Synthesis Reference

Tong Sun, Shawn Watson, Rajesh Manchanda, “PHENOBARBITAL SALTS; METHODS OF MAKING; AND METHODS OF USE THEREOF.” U.S. Patent US20100035904, issued February 11, 2010.

US20100035904
General References
  1. Kwan P, Brodie MJ: Phenobarbital for the treatment of epilepsy in the 21st century: a critical review. Epilepsia. 2004 Sep;45(9):1141-9. [PubMed:15329080 ]
  2. Taylor S, Tudur Smith C, Williamson PR, Marson AG: Phenobarbitone versus phenytoin monotherapy for partial onset seizures and generalized onset tonic-clonic seizures. Cochrane Database Syst Rev. 2001;(4):CD002217. [PubMed:11687150 ]
  3. Tudur Smith C, Marson AG, Williamson PR: Carbamazepine versus phenobarbitone monotherapy for epilepsy. Cochrane Database Syst Rev. 2003;(1):CD001904. [PubMed:12535420 ]
  4. Kalviainen R, Eriksson K, Parviainen I: Refractory generalised convulsive status epilepticus : a guide to treatment. CNS Drugs. 2005;19(9):759-68. [PubMed:16142991 ]
  5. Booth D, Evans DJ: Anticonvulsants for neonates with seizures. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD004218. [PubMed:15495087 ]
External Links
ATC CodesN03AA02
AHFS Codes
  • 28:24.04
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (53 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Phenobarbital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Phenobarbital.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Phenobarbital.
AlbendazoleThe serum concentration of the active metabolites of Albendazole can be reduced when Albendazole is used in combination with Phenobarbital resulting in a loss in efficacy.
AldesleukinPhenobarbital may increase the hypotensive activities of Aldesleukin.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Phenobarbital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Phenobarbital.
AmphetamineThe serum concentration of Phenobarbital can be decreased when it is combined with Amphetamine.
AmrinoneThe metabolism of Amrinone can be increased when combined with Phenobarbital.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Phenobarbital.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Phenobarbital.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Phenobarbital.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Phenobarbital resulting in a loss in efficacy.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Phenobarbital.
AzelastinePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Phenobarbital.
BazedoxifeneThe serum concentration of Bazedoxifene can be decreased when it is combined with Phenobarbital.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Phenobarbital.
BendamustineThe serum concentration of Bendamustine can be decreased when it is combined with Phenobarbital.
BepridilThe metabolism of Bepridil can be increased when combined with Phenobarbital.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Phenobarbital.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Phenobarbital.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Phenobarbital.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Phenobarbital.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Phenobarbital.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
BuprenorphinePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Phenobarbital.
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Phenobarbital.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Phenobarbital.
CathinoneThe serum concentration of Phenobarbital can be decreased when it is combined with Cathinone.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Phenobarbital.
ChloramphenicolThe metabolism of Phenobarbital can be decreased when combined with Chloramphenicol.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Phenobarbital.
CholestyramineThe serum concentration of Phenobarbital can be decreased when it is combined with Cholestyramine.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Phenobarbital.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Phenobarbital.
CobicistatThe serum concentration of Cobicistat can be decreased when it is combined with Phenobarbital.
CosyntropinCosyntropin may increase the hepatotoxic activities of Phenobarbital.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Phenobarbital.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Phenobarbital.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Phenobarbital.
DabrafenibThe serum concentration of Phenobarbital can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Phenobarbital.
DapsoneThe risk or severity of adverse effects can be increased when Dapsone is combined with Phenobarbital.
DarunavirThe serum concentration of Phenobarbital can be decreased when it is combined with Darunavir.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Phenobarbital.
DeferasiroxThe serum concentration of Deferasirox can be decreased when it is combined with Phenobarbital.
DexamethasoneThe serum concentration of Dexamethasone can be decreased when it is combined with Phenobarbital.
DexmethylphenidateThe serum concentration of Phenobarbital can be increased when it is combined with Dexmethylphenidate.
DextroamphetamineThe serum concentration of Phenobarbital can be decreased when it is combined with Dextroamphetamine.
DiclofenacThe serum concentration of Diclofenac can be decreased when it is combined with Phenobarbital.
DicoumarolThe metabolism of Dicoumarol can be increased when combined with Phenobarbital.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Phenobarbital.
DisopyramideThe serum concentration of Disopyramide can be decreased when it is combined with Phenobarbital.
DolutegravirThe serum concentration of Dolutegravir can be decreased when it is combined with Phenobarbital.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Phenobarbital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Phenobarbital.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Phenobarbital.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Phenobarbital.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Phenobarbital.
ElvitegravirThe serum concentration of Elvitegravir can be decreased when it is combined with Phenobarbital.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Phenobarbital.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Phenobarbital.
Eslicarbazepine acetateThe serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Phenobarbital.
EthanolPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Phenobarbital.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Phenobarbital.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Phenobarbital.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Phenobarbital.
FelbamateThe serum concentration of Felbamate can be decreased when it is combined with Phenobarbital.
FelodipineThe metabolism of Felodipine can be increased when combined with Phenobarbital.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Phenobarbital.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Phenobarbital.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Phenobarbital.
FlunarizineThe metabolism of Flunarizine can be increased when combined with Phenobarbital.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Phenobarbital.
FluvoxamineThe metabolism of Fluvoxamine can be increased when combined with Phenobarbital.
Folic AcidThe serum concentration of Phenobarbital can be decreased when it is combined with Folic Acid.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
GabapentinThe metabolism of Gabapentin can be increased when combined with Phenobarbital.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Phenobarbital.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Phenobarbital.
GuanfacineThe serum concentration of Guanfacine can be decreased when it is combined with Phenobarbital.
HydrocodonePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Phenobarbital.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Phenobarbital.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Phenobarbital.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Phenobarbital.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Phenobarbital resulting in a loss in efficacy.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be reduced when Isavuconazonium is used in combination with Phenobarbital resulting in a loss in efficacy.
IsradipineThe metabolism of Isradipine can be increased when combined with Phenobarbital.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Phenobarbital.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Phenobarbital.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Phenobarbital.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Phenobarbital.
LacosamideThe serum concentration of Lacosamide can be decreased when it is combined with Phenobarbital.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Phenobarbital.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Phenobarbital.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Phenobarbital.
LercanidipineThe metabolism of Lercanidipine can be increased when combined with Phenobarbital.
LeucovorinThe serum concentration of Phenobarbital can be decreased when it is combined with Leucovorin.
LevomefolateThe serum concentration of Phenobarbital can be decreased when it is combined with Levomefolate.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Phenobarbital.
LisdexamfetamineThe serum concentration of Phenobarbital can be decreased when it is combined with Lisdexamfetamine.
LopinavirThe serum concentration of Lopinavir can be decreased when it is combined with Phenobarbital.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Phenobarbital.
LuliconazoleThe serum concentration of Phenobarbital can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Phenobarbital can be decreased when it is combined with Lumacaftor.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Phenobarbital.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Phenobarbital.
MACITENTANThe serum concentration of MACITENTAN can be decreased when it is combined with Phenobarbital.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Phenobarbital.
MefloquineThe therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mefloquine.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Phenobarbital.
MethamphetamineThe serum concentration of Phenobarbital can be decreased when it is combined with Methamphetamine.
MethotrimeprazinePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe serum concentration of Phenobarbital can be increased when it is combined with Methylphenidate.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Phenobarbital.
MetronidazoleThe serum concentration of Metronidazole can be decreased when it is combined with Phenobarbital.
MetyrosinePhenobarbital may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Phenobarbital.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Phenobarbital.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Phenobarbital.
NicardipineThe metabolism of Nicardipine can be increased when combined with Phenobarbital.
NicotineThe metabolism of Nicotine can be increased when combined with Phenobarbital.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Phenobarbital.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Phenobarbital.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Phenobarbital.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Phenobarbital.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Phenobarbital.
NitrendipineThe metabolism of Nitrendipine can be increased when combined with Phenobarbital.
Nitric OxideThe risk or severity of adverse effects can be increased when Nitric Oxide is combined with Phenobarbital.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Phenobarbital.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Phenobarbital.
OrlistatThe serum concentration of Phenobarbital can be decreased when it is combined with Orlistat.
OrphenadrinePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxcarbazepineThe serum concentration of the active metabolites of Oxcarbazepine can be reduced when Oxcarbazepine is used in combination with Phenobarbital resulting in a loss in efficacy.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Phenobarbital.
PaliperidoneThe serum concentration of Paliperidone can be decreased when it is combined with Phenobarbital.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Phenobarbital.
ParaldehydePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Phenobarbital.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Phenobarbital.
PerhexilineThe metabolism of Perhexiline can be increased when combined with Phenobarbital.
PethidinePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PhendimetrazineThe serum concentration of Phenobarbital can be decreased when it is combined with Phendimetrazine.
PhentermineThe serum concentration of Phenobarbital can be decreased when it is combined with Phentermine.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
PirfenidoneThe serum concentration of Pirfenidone can be decreased when it is combined with Phenobarbital.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Phenobarbital.
PramipexolePhenobarbital may increase the sedative activities of Pramipexole.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Phenobarbital.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Phenobarbital.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Phenobarbital.
PrenylamineThe metabolism of Prenylamine can be increased when combined with Phenobarbital.
PrilocaineThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Prilocaine.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Phenobarbital.
PropacetamolThe metabolism of Propacetamol can be increased when combined with Phenobarbital.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Phenobarbital.
PyridoxineThe metabolism of Phenobarbital can be increased when combined with Pyridoxine.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Phenobarbital.
QuinidinePhenobarbital may increase the hepatotoxic activities of Quinidine.
QuinineThe serum concentration of Phenobarbital can be increased when it is combined with Quinine.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Phenobarbital.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Phenobarbital.
RifabutinThe metabolism of Phenobarbital can be increased when combined with Rifabutin.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Phenobarbital.
RisedronateThe metabolism of Risedronate can be increased when combined with Phenobarbital.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Phenobarbital.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Phenobarbital.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Phenobarbital.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Phenobarbital.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Phenobarbital.
RotigotinePhenobarbital may increase the sedative activities of Rotigotine.
RufinamideThe serum concentration of Phenobarbital can be increased when it is combined with Rufinamide.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Phenobarbital.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Phenobarbital.
SildenafilThe metabolism of Sildenafil can be increased when combined with Phenobarbital.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Phenobarbital.
Sodium NitriteThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Sodium Nitrite.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Phenobarbital.
SomatostatinThe risk or severity of adverse effects can be increased when Somatostatin is combined with Phenobarbital.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Phenobarbital.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Phenobarbital.
StiripentolThe serum concentration of Stiripentol can be decreased when it is combined with Phenobarbital.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Phenobarbital.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Phenobarbital.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Phenobarbital.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Phenobarbital.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Phenobarbital.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Phenobarbital.
ThalidomidePhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Phenobarbital resulting in a loss in efficacy.
TipranavirThe serum concentration of Tipranavir can be decreased when it is combined with Phenobarbital.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Phenobarbital.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Phenobarbital.
TorasemideThe metabolism of Torasemide can be increased when combined with Phenobarbital.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Phenobarbital.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Phenobarbital.
TreprostinilThe serum concentration of Treprostinil can be decreased when it is combined with Phenobarbital.
TrichlormethiazidePhenobarbital may increase the orthostatic hypotensive activities of Trichlormethiazide.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Phenobarbital.
Valproic AcidThe serum concentration of Phenobarbital can be increased when it is combined with Valproic Acid.
ValsartanPhenobarbital may increase the hypotensive activities of Valsartan.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Phenobarbital.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Phenobarbital.
VerapamilThe metabolism of Verapamil can be increased when combined with Phenobarbital.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Phenobarbital.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Phenobarbital.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Phenobarbital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Phenobarbital.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Phenobarbital.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Phenobarbital.
ZolpidemPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZonisamideThe serum concentration of Zonisamide can be decreased when it is combined with Phenobarbital.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Phenobarbital.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
  • Take on an empty stomach for quicker absorption

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. [PubMed:14579514 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  3. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  4. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
  5. Macdonald RL, McLean MJ: Anticonvulsant drugs: mechanisms of action. Adv Neurol. 1986;44:713-36. [PubMed:2871724 ]
  6. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  7. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ligand-gated ion channel activity
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions.
Gene Name:
CHRNA4
Uniprot ID:
P43681
Molecular Weight:
69956.47 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Toxic substance binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
Gene Name:
CHRNA7
Uniprot ID:
P36544
Molecular Weight:
56448.925 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ionotropic glutamate receptor activity
Specific Function:
Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and t...
Gene Name:
GRIA2
Uniprot ID:
P42262
Molecular Weight:
98820.32 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
  3. Jin LJ, Schlesinger F, Song YP, Dengler R, Krampfl K: The interaction of the neuroprotective compounds riluzole and phenobarbital with AMPA-type glutamate receptors: a patch-clamp study. Pharmacology. 2010;85(1):54-62. doi: 10.1159/000268641. Epub 2009 Dec 23. [PubMed:20051697 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Kainate selective glutamate receptor activity
Specific Function:
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inacti...
Gene Name:
GRIK2
Uniprot ID:
Q13002
Molecular Weight:
102582.475 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated cation channel activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors (By similarity).
Components:
NameUniProt IDDetails
Glutamate receptor ionotropic, NMDA 1Q05586 Details
Glutamate receptor ionotropic, NMDA 2AQ12879 Details
Glutamate receptor ionotropic, NMDA 2BQ13224 Details
Glutamate receptor ionotropic, NMDA 2CQ14957 Details
Glutamate receptor ionotropic, NMDA 2DO15399 Details
Glutamate receptor ionotropic, NMDA 3AQ8TCU5 Details
Glutamate receptor ionotropic, NMDA 3BO60391 Details
References
  1. Daniell LC: Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles. Pharmacology. 1994 Nov;49(5):296-307. [PubMed:7862741 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Madan A, Graham RA, Carroll KM, Mudra DR, Burton LA, Krueger LA, Downey AD, Czerwinski M, Forster J, Ribadeneira MD, Gan LS, LeCluyse EL, Zech K, Robertson P Jr, Koch P, Antonian L, Wagner G, Yu L, Parkinson A: Effects of prototypical microsomal enzyme inducers on cytochrome P450 expression in cultured human hepatocytes. Drug Metab Dispos. 2003 Apr;31(4):421-31. [PubMed:12642468 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Kawalek JC, Howard KD, Farrell DE, Derr J, Cope CV, Jackson JD, Myers MJ: Effect of oral administration of low doses of pentobarbital on the induction of cytochrome P450 isoforms and cytochrome P450-mediated reactions in immature Beagles. Am J Vet Res. 2003 Sep;64(9):1167-75. [PubMed:13677397 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Kawalek JC, Howard KD, Farrell DE, Derr J, Cope CV, Jackson JD, Myers MJ: Effect of oral administration of low doses of pentobarbital on the induction of cytochrome P450 isoforms and cytochrome P450-mediated reactions in immature Beagles. Am J Vet Res. 2003 Sep;64(9):1167-75. [PubMed:13677397 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. von Bahr C, Steiner E, Koike Y, Gabrielsson J: Time course of enzyme induction in humans: effect of pentobarbital on nortriptyline metabolism. Clin Pharmacol Ther. 1998 Jul;64(1):18-26. [PubMed:9695715 ]
  3. Venkatakrishnan K, von Moltke LL, Greenblatt DJ: Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): implications for interactions with enzyme-inducing drugs. J Clin Pharmacol. 1999 Jun;39(6):567-77. [PubMed:10354960 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Sakuma T, Ohtake M, Katsurayama Y, Jarukamjorn K, Nemoto N: Induction of CYP1A2 by phenobarbital in the livers of aryl hydrocarbon-responsive and -nonresponsive mice. Drug Metab Dispos. 1999 Mar;27(3):379-84. [PubMed:10064569 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Kawalek JC, Howard KD, Farrell DE, Derr J, Cope CV, Jackson JD, Myers MJ: Effect of oral administration of low doses of pentobarbital on the induction of cytochrome P450 isoforms and cytochrome P450-mediated reactions in immature Beagles. Am J Vet Res. 2003 Sep;64(9):1167-75. [PubMed:13677397 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Leukotriene-b4 20-monooxygenase activity
Specific Function:
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 20-hydroxyeicosatetraenoic acid (20-HETE).
Gene Name:
CYP4A11
Uniprot ID:
Q02928
Molecular Weight:
59347.31 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP4B1
Uniprot ID:
P13584
Molecular Weight:
58990.64 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764 ]
  2. Luna-Tortos C, Fedrowitz M, Loscher W: Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008 Dec;55(8):1364-75. doi: 10.1016/j.neuropharm.2008.08.032. Epub 2008 Sep 11. [PubMed:18824002 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Kiuchi Y, Suzuki H, Hirohashi T, Tyson CA, Sugiyama Y: cDNA cloning and inducible expression of human multidrug resistance associated protein 3 (MRP3). FEBS Lett. 1998 Aug 14;433(1-2):149-52. [PubMed:9738950 ]
  2. Cherrington NJ, Slitt AL, Maher JM, Zhang XX, Zhang J, Huang W, Wan YJ, Moore DD, Klaassen CD: Induction of multidrug resistance protein 3 (mrp3) in vivo is independent of constitutive androstane receptor. Drug Metab Dispos. 2003 Nov;31(11):1315-9. [PubMed:14570762 ]
  3. Slitt AL, Cherrington NJ, Maher JM, Klaassen CD: Induction of multidrug resistance protein 3 in rat liver is associated with altered vectorial excretion of acetaminophen metabolites. Drug Metab Dispos. 2003 Sep;31(9):1176-86. [PubMed:12920174 ]
  4. Ogawa K, Suzuki H, Hirohashi T, Ishikawa T, Meier PJ, Hirose K, Akizawa T, Yoshioka M, Sugiyama Y: Characterization of inducible nature of MRP3 in rat liver. Am J Physiol Gastrointest Liver Physiol. 2000 Mar;278(3):G438-46. [PubMed:10712264 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Molecular Weight:
146405.83 Da
References
  1. Kast HR, Goodwin B, Tarr PT, Jones SA, Anisfeld AM, Stoltz CM, Tontonoz P, Kliewer S, Willson TM, Edwards PA: Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. J Biol Chem. 2002 Jan 25;277(4):2908-15. Epub 2001 Nov 12. [PubMed:11706036 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Kiuchi Y, Suzuki H, Hirohashi T, Tyson CA, Sugiyama Y: cDNA cloning and inducible expression of human multidrug resistance associated protein 3 (MRP3). FEBS Lett. 1998 Aug 14;433(1-2):149-52. [PubMed:9738950 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
May mediate the release of newly synthesized prostaglandins from cells, the transepithelial transport of prostaglandins, and the clearance of prostaglandins from the circulation. Transports PGD2, as well as PGE1, PGE2 and PGF2A.
Gene Name:
SLCO2A1
Uniprot ID:
Q92959
Molecular Weight:
70043.33 Da
References
  1. Hagenbuch N, Reichel C, Stieger B, Cattori V, Fattinger KE, Landmann L, Meier PJ, Kullak-Ublick GA: Effect of phenobarbital on the expression of bile salt and organic anion transporters of rat liver. J Hepatol. 2001 Jun;34(6):881-7. [PubMed:11451172 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Courtois A, Payen L, Le Ferrec E, Scheffer GL, Trinquart Y, Guillouzo A, Fardel O: Differential regulation of multidrug resistance-associated protein 2 (MRP2) and cytochromes P450 2B1/2 and 3A1/2 in phenobarbital-treated hepatocytes. Biochem Pharmacol. 2002 Jan 15;63(2):333-41. [PubMed:11841808 ]
  2. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161 ]
  3. Kast HR, Goodwin B, Tarr PT, Jones SA, Anisfeld AM, Stoltz CM, Tontonoz P, Kliewer S, Willson TM, Edwards PA: Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. J Biol Chem. 2002 Jan 25;277(4):2908-15. Epub 2001 Nov 12. [PubMed:11706036 ]
  4. Kauffmann HM, Schrenk D: Sequence analysis and functional characterization of the 5'-flanking region of the rat multidrug resistance protein 2 (mrp2) gene. Biochem Biophys Res Commun. 1998 Apr 17;245(2):325-31. [PubMed:9571149 ]
  5. Johnson DR, Habeebu SS, Klaassen CD: Increase in bile flow and biliary excretion of glutathione-derived sulfhydryls in rats by drug-metabolizing enzyme inducers is mediated by multidrug resistance protein 2. Toxicol Sci. 2002 Mar;66(1):16-26. [PubMed:11861969 ]
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Drug created on June 13, 2005 07:24 / Updated on November 30, 2015 14:23