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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
SynonymLanguageCode
5-ethyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrioneNot AvailableNot Available
5-Ethyl-5-phenyl-pyrimidine-2,4,6-trioneNot AvailableNot Available
5-Ethyl-5-phenylbarbituric acidNot AvailableNot Available
5-ethyl-5-phenylpyrimidine-2,4,6(1H,3H,5H)-trioneNot AvailableNot Available
5-Phenyl-5-ethylbarbituric acidNot AvailableNot Available
LuminalNot AvailableNot Available
PhenobarbitalNot AvailableNot Available
PhenobarbitolNot AvailableNot Available
PhenobarbitoneNot AvailableNot Available
Phenobarbituric AcidNot AvailableNot Available
PhenylaethylbarbitursaeureNot AvailableNot Available
PhenylethylbarbiturateNot AvailableNot Available
Phenylethylbarbituric AcidNot AvailableNot Available
PhenylethylbarbitursaeureNot AvailableNot Available
PHENYLETHYLMALONYLUREANot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
LuminalNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number50-06-6
WeightAverage: 232.2353
Monoisotopic: 232.08479226
Chemical FormulaC12H12N2O3
InChI KeyDDBREPKUVSBGFI-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.
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 substrateNon-inhibitor0.9023
CYP450 2D6 substrateNon-inhibitor0.9593
CYP450 2C19 substrateNon-inhibitor0.8664
CYP450 3A4 substrateNon-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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage formsNot Available
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)
SpectraMS1D NMR
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 Reference
  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
  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
  3. Tudur Smith C, Marson AG, Williamson PR: Carbamazepine versus phenobarbitone monotherapy for epilepsy. Cochrane Database Syst Rev. 2003;(1):CD001904. Pubmed
  4. Kalviainen R, Eriksson K, Parviainen I: Refractory generalised convulsive status epilepticus : a guide to treatment. CNS Drugs. 2005;19(9):759-68. Pubmed
  5. Booth D, Evans DJ: Anticonvulsants for neonates with seizures. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD004218. Pubmed
External Links
ATC CodesN03AA02
AHFS Codes
  • 28:24.04
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (53 KB)
Interactions
Drug Interactions
Drug
AcetaminophenBarbiturates may increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage.
AfatinibP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Afatinib.
AlbendazoleMay decrease serum concentrations of the active metabolite(s) of Albendazole.
AmlodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
AmphetamineAmphetamines may decrease the serum concentration of PHENobarbital.
AmrinoneBarbiturates may increase the metabolism of Calcium Channel Blockers.
ApixabanCYP3A4 Inducers (Strong) may decrease the serum concentration of Apixaban.
ApremilastCYP3A4 Inducers (Strong) may decrease the serum concentration of Apremilast.
AripiprazoleCYP3A4 Inducers may decrease the serum concentration of ARIPiprazole.
ArtemetherCYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite(s) of Artemether. Specifically, dihydroartemisinin concentrations may be reduced. CYP3A4 Inducers (Strong) may decrease the serum concentration of Artemether.
AxitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Axitinib.
bazedoxifenePHENobarbital may decrease the serum concentration of Bazedoxifene. This may lead to loss of efficacy or, if bazedoxifene is combined with estrogen therapy, an increased risk of endometrial hyperplasia.
BedaquilineCYP3A4 Inducers (Strong) may decrease the serum concentration of Bedaquiline.
BendamustineCYP1A2 Inducers (Strong) may decrease the serum concentration of Bendamustine. Concentrations of active metabolites may be increased.
BepridilBarbiturates may increase the metabolism of Calcium Channel Blockers.
BoceprevirPHENobarbital may decrease the serum concentration of Boceprevir.
BortezomibCYP3A4 Inducers (Strong) may decrease the serum concentration of Bortezomib.
BosutinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Bosutinib.
Brentuximab vedotinCYP3A4 Inducers (Strong) may decrease the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be decreased.
BuprenorphineCNS Depressants may enhance the CNS depressant effect of Buprenorphine.
CabozantinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Cabozantinib.
CanagliflozinPHENobarbital may decrease the serum concentration of Canagliflozin.
CathinoneMay decrease the serum concentration of PHENobarbital.
ChloramphenicolBarbiturates may increase the metabolism of Chloramphenicol. Chloramphenicol may decrease the metabolism of Barbiturates.
CholestyramineCholestyramine Resin may decrease the serum concentration of PHENobarbital.
ClarithromycinCYP3A4 Inducers (Strong) may increase serum concentrations of the active metabolite(s) of Clarithromycin. Clarithromycin may increase the serum concentration of CYP3A4 Inducers (Strong). CYP3A4 Inducers (Strong) may decrease the serum concentration of Clarithromycin.
ClozapineCYP3A4 Inducers (Strong) may decrease the serum concentration of CloZAPine.
CosyntropinMay enhance the hepatotoxic effect of PHENobarbital.
CrizotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Crizotinib.
Dabigatran etexilateP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Dabigatran Etexilate.
DabrafenibMay decrease the serum concentration of CYP2C19 Substrates.
DarunavirMay decrease the serum concentration of PHENobarbital.
DasatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
DeferasiroxPHENobarbital may decrease the serum concentration of Deferasirox.
DexmethylphenidateMay increase the serum concentration of PHENobarbital.
DextroamphetamineAmphetamines may decrease the serum concentration of PHENobarbital.
DisopyramideMay decrease the serum concentration of Disopyramide.
DolutegravirPHENobarbital may decrease the serum concentration of Dolutegravir.
DoxycyclineBarbiturates may decrease the serum concentration of Doxycycline.
DoxylamineMay enhance the CNS depressant effect of CNS Depressants.
DronabinolCYP3A4 Inducers (Strong) may decrease the serum concentration of Dronabinol.
DronedaroneCYP3A4 Inducers (Strong) may decrease the serum concentration of Dronedarone.
DroperidolMay enhance the CNS depressant effect of CNS Depressants.
EliglustatCYP3A4 Inducers (Strong) may decrease the serum concentration of Eliglustat.
EnzalutamideCYP2C8 Inducers (Strong) may decrease the serum concentration of Enzalutamide.
ErlotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Erlotinib.
EtoposideBarbiturates may decrease the serum concentration of Etoposide.
EtravirinePHENobarbital may decrease the serum concentration of Etravirine.
EverolimusCYP3A4 Inducers (Strong) may decrease the serum concentration of Everolimus.
ExemestaneCYP3A4 Inducers (Strong) may decrease the serum concentration of Exemestane.
FelbamateFelbamate may increase the serum concentration of PHENobarbital. PHENobarbital may decrease the serum concentration of Felbamate.
FelodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
FentanylCYP3A4 Inducers (Strong) may decrease the serum concentration of FentaNYL.
FlunarizineBarbiturates may increase the metabolism of Calcium Channel Blockers.
Folic AcidFolic Acid may decrease the serum concentration of PHENobarbital.
FosphenytoinMay enhance the CNS depressant effect of PHENobarbital. Fosphenytoin may increase the serum concentration of PHENobarbital. PHENobarbital may decrease the serum concentration of Fosphenytoin.
GabapentinBarbiturates may increase the metabolism of Calcium Channel Blockers.
GefitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Gefitinib.
GriseofulvinBarbiturates may decrease the serum concentration of Griseofulvin.
GuanfacineCYP3A4 Inducers (Strong) may decrease the serum concentration of GuanFACINE.
HydrocodoneCNS Depressants may enhance the CNS depressant effect of Hydrocodone.
HydroxyzineMay enhance the CNS depressant effect of Barbiturates.
ImatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Imatinib.
IrinotecanCYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite(s) of Irinotecan. Specifically, serum concentrations of SN-38 may be reduced. CYP3A4 Inducers (Strong) may decrease the serum concentration of Irinotecan.
IsradipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
ItraconazoleCYP3A4 Inducers (Strong) may decrease the serum concentration of Itraconazole.
IvacaftorCYP3A4 Inducers (Strong) may decrease the serum concentration of Ivacaftor.
IxabepiloneCYP3A4 Inducers (Strong) may decrease the serum concentration of Ixabepilone.
LacosamidePHENobarbital may decrease the serum concentration of Lacosamide.
LamotrigineBarbiturates may increase the metabolism of Calcium Channel Blockers.
LapatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Lapatinib.
LedipasvirP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Ledipasvir.
LercanidipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
LinagliptinCYP3A4 Inducers (Strong) may decrease the serum concentration of Linagliptin.
LisdexamfetamineAmphetamines may decrease the serum concentration of PHENobarbital.
LopinavirPHENobarbital may decrease the serum concentration of Lopinavir.
LULICONAZOLEMay increase the serum concentration of CYP2C19 Substrates.
LumefantrineCYP3A4 Inducers (Strong) may decrease the serum concentration of Lumefantrine.
LurasidoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Lurasidone.
MACITENTANCYP3A4 Inducers (Strong) may decrease the serum concentration of Macitentan.
Magnesium SulfateBarbiturates may increase the metabolism of Calcium Channel Blockers.
MaravirocCYP3A4 Inducers (Strong) may decrease the serum concentration of Maraviroc.
MefloquineMefloquine may diminish the therapeutic effect of Anticonvulsants. Mefloquine may decrease the serum concentration of Anticonvulsants.
MethadoneMay decrease the serum concentration of Methadone.
MethamphetamineAmphetamines may decrease the serum concentration of PHENobarbital.
MethotrimeprazineCNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants.
MethylphenidateMethylphenidate may increase the serum concentration of PHENobarbital.
MethylprednisoloneCYP3A4 Inducers (Strong) may decrease the serum concentration of MethylPREDNISolone.
MetyrosineCNS Depressants may enhance the sedative effect of Metyrosine.
MianserinMay enhance the CNS depressant effect of Barbiturates. Mianserin may diminish the therapeutic effect of Barbiturates. Barbiturates may decrease the serum concentration of Mianserin.
MifepristoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Mifepristone.
NabiloneMay enhance the CNS depressant effect of CNS Depressants.
NicardipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NifedipineCYP3A4 Inducers (Strong) may decrease the serum concentration of NIFEdipine.
NilotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Nilotinib.
NimodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NisoldipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NitrendipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
Nitric OxideMay enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia.
OrlistatOrlistat may decrease the serum concentration of Anticonvulsants. Exceptions: Fosphenytoin; PENTobarbital; Thiopental.
OrphenadrineCNS Depressants may enhance the CNS depressant effect of Orphenadrine.
OxcarbazepineMay decrease serum concentrations of the active metabolite(s) of OXcarbazepine. Specifically, concentrations of the major active 10-monohydroxy metabolite may be reduced. OXcarbazepine may increase the serum concentration of PHENobarbital.
PaliperidoneInducers of CYP3A4 and P-glycoprotein may decrease the serum concentration of Paliperidone.
PanobinostatCYP3A4 Inducers (Strong) may decrease the serum concentration of Panobinostat.
PazopanibCYP3A4 Inducers (Strong) may decrease the serum concentration of PAZOPanib.
PerampanelCYP3A4 Inducers (Strong) may decrease the serum concentration of Perampanel.
PerhexilineBarbiturates may increase the metabolism of Calcium Channel Blockers.
PhendimetrazineAmphetamines may decrease the serum concentration of PHENobarbital.
PhentermineAmphetamines may decrease the serum concentration of PHENobarbital.
PhenytoinPhenytoin may enhance the CNS depressant effect of PHENobarbital. PHENobarbital may decrease the serum concentration of Phenytoin. Phenytoin may increase the serum concentration of PHENobarbital.
PirfenidoneCYP1A2 Inducers (Strong) may decrease the serum concentration of Pirfenidone.
PomalidomideCYP1A2 Inducers (Strong) may decrease the serum concentration of Pomalidomide.
PonatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
PramipexoleCNS Depressants may enhance the sedative effect of Pramipexole.
PraziquantelCYP3A4 Inducers (Strong) may decrease the serum concentration of Praziquantel.
PrednisoneCYP3A4 Inducers (Strong) may decrease the serum concentration of PredniSONE.
PrenylamineBarbiturates may increase the metabolism of Calcium Channel Blockers.
PrilocaineMethemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia.
PrimidoneMay enhance the adverse/toxic effect of Barbiturates. Primidone is converted to phenobarbital, and thus becomes additive with existing barbiturate therapy.
PropafenoneBarbiturates may decrease the serum concentration of Propafenone.
PyridoxineMay increase the metabolism of Barbiturates. Apparent in high pyridoxine doses (eg, 200 mg/day)
QuetiapineCYP3A4 Inducers (Strong) may decrease the serum concentration of QUEtiapine.
QuinidineMay enhance the hepatotoxic effect of QuiNIDine. PHENobarbital may decrease the serum concentration of QuiNIDine.
QuinineMay decrease the serum concentration of QuiNINE. QuiNINE may increase the serum concentration of PHENobarbital.
RanolazineCYP3A4 Inducers (Strong) may decrease the serum concentration of Ranolazine.
RegorafenibCYP3A4 Inducers (Strong) may decrease the serum concentration of Regorafenib.
RilpivirinePHENobarbital may decrease the serum concentration of Rilpivirine.
RisedronateBarbiturates may increase the metabolism of Calcium Channel Blockers.
RivaroxabanCYP3A4 Inducers (Strong) may decrease the serum concentration of Rivaroxaban.
RoflumilastCYP3A4 Inducers (Strong) may decrease the serum concentration of Roflumilast.
RomidepsinCYP3A4 Inducers (Strong) may decrease the serum concentration of RomiDEPsin.
RotigotineCNS Depressants may enhance the sedative effect of Rotigotine.
RufinamidePHENobarbital may decrease the serum concentration of Rufinamide. Rufinamide may increase the serum concentration of PHENobarbital.
SaxagliptinCYP3A4 Inducers may decrease the serum concentration of Saxagliptin.
SimeprevirCYP3A4 Inducers (Strong) may decrease the serum concentration of Simeprevir.
SofosbuvirP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Sofosbuvir.
SorafenibCYP3A4 Inducers (Strong) may decrease the serum concentration of SORAfenib.
SunitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of SUNItinib.
SuvorexantCYP3A4 Inducers (Strong) may decrease the serum concentration of Suvorexant.
TadalafilCYP3A4 Inducers (Strong) may decrease the serum concentration of Tadalafil.
TapentadolMay enhance the CNS depressant effect of CNS Depressants.
TelaprevirPHENobarbital may decrease the serum concentration of Telaprevir.
TeniposideBarbiturates may decrease the serum concentration of Teniposide.
ThalidomideCNS Depressants may enhance the CNS depressant effect of Thalidomide.
TicagrelorCYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inducers (Strong) may decrease the serum concentration of Ticagrelor.
TipranavirMay decrease the serum concentration of Tipranavir. Tipranavir may decrease the serum concentration of PHENobarbital.
TofacitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Tofacitinib.
TolvaptanCYP3A4 Inducers (Strong) may decrease the serum concentration of Tolvaptan.
ToremifeneCYP3A4 Inducers (Strong) may decrease the serum concentration of Toremifene.
TrabectedinCYP3A4 Inducers (Strong) may decrease the serum concentration of Trabectedin.
TreprostinilCYP2C8 Inducers (Strong) may decrease the serum concentration of Treprostinil.
UlipristalCYP3A4 Inducers (Strong) may decrease the serum concentration of Ulipristal.
VandetanibCYP3A4 Inducers (Strong) may decrease the serum concentration of Vandetanib.
VemurafenibCYP3A4 Inducers (Strong) may decrease the serum concentration of Vemurafenib.
VerapamilBarbiturates may increase the metabolism of Calcium Channel Blockers.
VilazodoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Vilazodone.
VorapaxarCYP3A4 Inducers (Strong) may decrease the serum concentration of Vorapaxar.
VoriconazoleBarbiturates may decrease the serum concentration of Voriconazole.
ZolpidemCNS Depressants may enhance the CNS depressant effect of Zolpidem.
ZonisamideMay decrease the serum concentration of Zonisamide.
ZuclopenthixolCYP3A4 Inducers (Strong) may decrease the serum concentration of Zuclopenthixol.
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

1. Gamma-aminobutyric acid receptor subunit alpha-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-1 P14867 Details

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
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed
  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
  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
  5. Macdonald RL, McLean MJ: Anticonvulsant drugs: mechanisms of action. Adv Neurol. 1986;44:713-36. Pubmed
  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
  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

2. Neuronal acetylcholine receptor subunit alpha-4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Neuronal acetylcholine receptor subunit alpha-4 P43681 Details

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
  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
  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

3. Neuronal acetylcholine receptor subunit alpha-7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Neuronal acetylcholine receptor subunit alpha-7 P36544 Details

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
  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
  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

4. Glutamate receptor 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor 2 P42262 Details

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
  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
  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

5. Glutamate receptor ionotropic, kainate 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor ionotropic, kainate 2 Q13002 Details

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
  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

6. NMDA receptor

Kind: protein group

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor ionotropic, NMDA 1 Q05586 Details
Glutamate receptor ionotropic, NMDA 2A Q12879 Details
Glutamate receptor ionotropic, NMDA 2B Q13224 Details
Glutamate receptor ionotropic, NMDA 2C Q14957 Details
Glutamate receptor ionotropic, NMDA 2D O15399 Details
Glutamate receptor ionotropic, NMDA 3A Q8TCU5 Details
Glutamate receptor ionotropic, NMDA 3B O60391 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

Enzymes

1. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed
  3. 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

2. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

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
  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. Epub 2009 Nov 24. Pubmed
  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

3. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed
  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

5. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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. Epub 2009 Nov 24. Pubmed
  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
  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

6. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

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. Epub 2009 Nov 24. Pubmed
  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

7. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

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. Epub 2009 Nov 24. Pubmed
  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

8. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

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. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

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. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 4A11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 4A11 Q02928 Details

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. Epub 2009 Nov 24. Pubmed

11. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

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

12. Cytochrome P450 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 1B1 Q16678 Details

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

13. Cytochrome P450 2C18

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C18 P33260 Details

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

14. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

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

15. Cytochrome P450 4B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 4B1 P13584 Details

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

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

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
  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. Epub 2008 Sep 11. Pubmed

2. Canalicular multispecific organic anion transporter 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 2 O15438 Details

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
  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
  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
  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

3. Bile salt export pump

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Bile salt export pump O95342 Details

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

4. Multidrug resistance-associated protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Multidrug resistance-associated protein 1 P33527 Details

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

5. Solute carrier organic anion transporter family member 2A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 2A1 Q92959 Details

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

6. Canalicular multispecific organic anion transporter 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 1 Q92887 Details

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
  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
  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
  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
  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

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13