You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameRifampicin
Accession NumberDB01045  (APRD00207, EXPT02777)
TypeSmall Molecule
GroupsApproved
Description

A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)

Structure
Thumb
Synonyms
SynonymLanguageCode
3-(((4-Methyl-1-piperazinyl)imino)methyl)rifamycin svNot AvailableNot Available
RFPNot AvailableNot Available
RifampicinaNot AvailableNot Available
RifampicinumNot AvailableNot Available
RifampinNot AvailableUSAN
Salts
Name/CAS Structure Properties
Rifampicin sodium
Thumb Not applicable DBSALT001014
Brand names
NameCompany
RifadinNot Available
RifadineNot Available
RifaldinNot Available
RifoldinNot Available
RimactanNot Available
RimactaneNot Available
RofactNot Available
TubocinNot Available
Brand mixtures
Brand NameIngredients
AfracinRifampin + Isoniazid
IsonaRifIsoniazid + Rifampicin
RifamateRifampin + Isoniazid
RifaterIsoniazid + Pyrazinaamide + Rifampin
Categories
CAS number13292-46-1
WeightAverage: 822.9402
Monoisotopic: 822.40512334
Chemical FormulaC43H58N4O12
InChI KeyJQXXHWHPUNPDRT-WLSIYKJHSA-N
InChI
InChI=1S/C43H58N4O12/c1-21-12-11-13-22(2)42(55)45-33-28(20-44-47-17-15-46(9)16-18-47)37(52)30-31(38(33)53)36(51)26(6)40-32(30)41(54)43(8,59-40)57-19-14-29(56-10)23(3)39(58-27(7)48)25(5)35(50)24(4)34(21)49/h11-14,19-21,23-25,29,34-35,39,49-53H,15-18H2,1-10H3,(H,45,55)/b12-11+,19-14+,22-13-,44-20+/t21-,23+,24+,25+,29-,34-,35+,39+,43-/m0/s1
IUPAC Name
(7S,11S,12R,13S,14R,15R,16R,17S,18S)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(E)-N-(4-methylpiperazin-1-yl)carboximidoyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1^{4,7}.0^{5,28}]triaconta-1,3,5(28),9,19,21,25(29),26-octaen-13-yl acetate
SMILES
CO[C@H]1\C=C\O[C@@]2(C)OC3=C(C2=O)C2=C(O)C(\C=N\N4CCN(C)CC4)=C(NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C(O)=C2C(O)=C3C
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassNaphthofurans
SubclassNot Available
Direct parentNaphthofurans
Alternative parentsNaphthols and Derivatives; Benzofurans; Hydroquinones; Ortho Cresols; Toluenes; Alkyl Aryl Ethers; Diazinanes; Piperazines; Hydrazones; Polyols; Ketones; Secondary Carboxylic Acid Amides; Secondary Alcohols; Tertiary Amines; Aldimines; Carboxylic Acid Esters; Enols; Enolates; Carboxylic Acids; Polyamines; Acetals
Substituents1-naphthol; acene; naphthalene; benzofuran; o-cresol; hydroquinone; alkyl aryl ether; toluene; phenol derivative; benzene; piperazine; 1,4-diazinane; hydrazone; ketone; secondary alcohol; secondary carboxylic acid amide; tertiary amine; aldimine; carboxylic acid ester; polyol; carboxamide group; enol; ether; acetal; carboxylic acid; polyamine; carboxylic acid derivative; enolate; carbonyl group; organonitrogen compound; alcohol; imine; amine
Classification descriptionThis compound belongs to the naphthofurans. These are compounds containing a furan ring fused to a naphthalene moeity.
Pharmacology
IndicationFor the treatment of Tuberculosis and Tuberculosis-related mycobacterial infections.
PharmacodynamicsRifampin is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency.
Mechanism of actionRifampin acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
AbsorptionWell absorbed from gastrointestinal tract.
Volume of distributionNot Available
Protein binding89%
Metabolism

Primarily hepatic, rapidly deacetylated.

Route of eliminationLess than 30% of the dose is excreted in the urine as rifampin or metabolites.
Half life3.35 (+/- 0.66) hours
Clearance
  • 0.19 +/- 0.06 L/hr/kg [300 mg IV]
  • 0.14 +/- 0.03 L/hr/kg [600 mg IV]
ToxicityLD50=1570 mg/kg (rat), chronic exposure may cause nausea and vomiting and unconsciousness
Affected organisms
  • Mycobacteria
  • Various gram-negative and gram-positive eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.5553
Blood Brain Barrier - 0.974
Caco-2 permeable - 0.7123
P-glycoprotein substrate Substrate 0.9308
P-glycoprotein inhibitor I Inhibitor 0.8564
P-glycoprotein inhibitor II Non-inhibitor 0.6049
Renal organic cation transporter Non-inhibitor 0.8178
CYP450 2C9 substrate Non-substrate 0.8508
CYP450 2D6 substrate Non-substrate 0.9115
CYP450 3A4 substrate Substrate 0.7296
CYP450 1A2 substrate Non-inhibitor 0.9045
CYP450 2C9 substrate Non-inhibitor 0.907
CYP450 2D6 substrate Non-inhibitor 0.9231
CYP450 2C19 substrate Non-inhibitor 0.9025
CYP450 3A4 substrate Non-inhibitor 0.8432
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9099
Ames test Non AMES toxic 0.5803
Carcinogenicity Non-carcinogens 0.8493
Biodegradation Not ready biodegradable 0.9962
Rat acute toxicity 2.6875 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.908
hERG inhibition (predictor II) Non-inhibitor 0.5486
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
  • Lannett holdings inc
  • Sandoz inc
  • Versapharm inc
  • Actavis totowa llc
  • Akorn strides llc
  • Bedford laboratories div ben venue laboratories inc
Packagers
Dosage forms
FormRouteStrength
CapsuleOral
Prices
Unit descriptionCostUnit
Rifadin iv 600 mg vial140.9USDvial
Rifampin iv 600 mg vial136.3USDvial
Rifampin crystals6.72USDg
Rifampin powder3.98USDg
Rifadin 300 mg capsule3.09USDcapsule
Rifadin 150 mg capsule2.57USDcapsule
Rifampin 300 mg capsule2.37USDcapsule
Rimactane 300 mg capsule2.35USDcapsule
Rifampin 150 mg capsule2.27USDcapsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point183 °CNot Available
water solubility1400 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.7Not Available
pKa1.7SANGSTER (2004)
Predicted Properties
PropertyValueSource
Water Solubility0.0413ALOGPS
logP3.85ALOGPS
logP2.77ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)6.9ChemAxon
pKa (Strongest Basic)7.53ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count6ChemAxon
Polar Surface Area220.15 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity225.58 m3·mol-1ChemAxon
Polarizability86.46 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Klaus Jurgen, Joachim Seydel, “Combination preparations containing rifampicin and thioacetazon.” U.S. Patent US5104875, issued August, 1973.

US5104875
General Reference
  1. Baysarowich J, Koteva K, Hughes DW, Ejim L, Griffiths E, Zhang K, Junop M, Wright GD: Rifamycin antibiotic resistance by ADP-ribosylation: Structure and diversity of Arr. Proc Natl Acad Sci U S A. 2008 Mar 25;105(12):4886-91. Epub 2008 Mar 18. Pubmed
External Links
ResourceLink
KEGG DrugD00211
KEGG CompoundC06688
ChEBI28077
ChEMBLCHEMBL374478
Therapeutic Targets DatabaseDNC000965
PharmGKBPA451250
IUPHAR2765
Guide to Pharmacology2765
Drug Product Database393444
RxListhttp://www.rxlist.com/cgi/generic2/rifampin.htm
Drugs.comhttp://www.drugs.com/cdi/rifampin.html
WikipediaRifampin
ATC CodesJ04AB02
AHFS Codes
  • 08:16.04
PDB Entries
FDA labelshow(43.3 KB)
MSDSshow(86.7 KB)
Interactions
Drug Interactions
Drug
AbirateroneStrong CYP3A4 inducers may decrease levels of abiraterone. Monitor concomitant therapy closely.
AcenocoumarolRifampin may decrease the anticoagulant effect of acenocoumarol by increasing its metabolism.
AcetohexamideRifampin may decrease the effect of sulfonylurea, acetohexamide.
AlfentanilRifampin reduces levels and efficacy of alfentanil
AminophyllineRifampin decreases the effect of theophylline
AmiodaroneRifampin decreases the effect of amiodarone
AmitriptylineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, amitriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if rifampin is initiated, discontinued or dose changed.
AmoxapineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, amoxapine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amoxapine if rifampin is initiated, discontinued or dose changed.
AmprenavirIn presence of rifampin anticipate decrease of amprenavir efficiency
AnisindioneRifampin may decrease the anticoagulant effect of anisindione.
AprepitantThe CYP3A4 inducer, rifampin, may decrease the effect of aprepitant.
ArtemetherOral administration of rifampin, a strong CYP3A4 inducer, with Coartem Tablets resulted in significant decreases in exposure to artemether, dihydroartemisinin (DHA, metabolite of artemether) and lumefantrine by 89%, 85% and 68%, respectively, when compared to exposure values after Coartem Tablets alone. Concomitant use of strong inducers of CYP3A4 such as rifampin, carbamazepine, phenytoin and St. John’s wort is contraindicated with Coartem Tablets.
AtazanavirRifampin reduces levels and efficacy of atazanavir
AtorvastatinRifampin may decrease the effect of atorvastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of atorvastatin if rifampin is initiated, discontinued or dose changed.
AtovaquoneRifampin may decrease the effect of atovaquone.
BedaquilineStrong CYP3A4 inducers may decrease exposure of bedaquiline. Co-administration should be avoided.
BendamustineCYP1A2 metabolism may result in increased levels of active metabolites, decreases levels of bendamustine.
BetamethasoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, betamethasone.
BisoprololRifampin may decrease the serum concentration of bisprolol by increasing its metabolism.
BoceprevirStrong CYP3A4 inducers will decrease levels of boceprevir. Concomitant therapy is contraindicated.
BosutinibStrong CYP3A4 inducers may decrease levels of bosutinib. Monitor concomitant therapy closely.
BromazepamRifampin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifampin is initiated, discontinued or dose changed.
BupropionRifampin reduces bupropion levels
BuspironeRifampin decreases the effect of buspirone
CabazitaxelConcomitant therapy with a strong CYP3A inducer may decrease concentrations of cabazitaxel. Avoid concomitant therapy.
CanagliflozinNonselective inducers of UGT enzymes may decrease levels of canagliflozin, thus decreasing efficacy. Consider increase the dose to 300 mg once daily.
CaspofunginDecreased levels/effects of caspofungin
CelecoxibRifampin, a strong CYP2C9 inducer, may decrease the serum levels of celecoxib by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects if rifampin is initiated, discontinued or dose changed.
CerivastatinRifampin may decrease the effect of cerivastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of cerivastatin if rifampin is initiated, discontinued or dose changed.
ChloramphenicolRifampin decreases the effect of chloramphenicol
ChlorpropamideRifampin may decrease the effect of sulfonylurea, chlorpropamide.
ClarithromycinThe rifamycin, rifampin, may decrease the effect of the macrolide, clarithromycin.
ClomipramineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, clomipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of clomipramine if rifampin is initiated, discontinued or dose changed.
ClozapineRifampin decreases the effect of clozapine
Cortisone acetateThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, cortisone acetate.
CrizotinibStrong CYP3A4 inducers may decrease levels of crizotinib. Monitor concomitant therapy closely.
CrizotinibStrong CYP3A4 inducers may decrease levels of crizotinib. Monitor concomitant therapy closely.
CyclosporineThe rifamycin decreases the effect of cyclosporine
Dabigatran etexilateP-Glycoprotein inducers such as rifampin may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
DabrafenibStrong CYP3A4 inducers may decrease levels of dabrafenib. Consider alternate therapy.
DapsoneDecreased levels of dapsone
DasatinibRifampin may decrease the serum level and efficacy of dasatinib.
DelavirdineRifampin decreases the effect of delavirdine
DesipramineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, desipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of desipramine if rifampin is initiated, discontinued or dose changed.
DexamethasoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, dexamethasone.
DiazepamRifampin may decrease the effect of the benzodiazepine, diazepam.
DiclofenacRifampin, a CYP2C9 inducer, may increase the metabolism of diclofenac.
DicoumarolRifampin may decrease the anticoagulant effect of dicumarol.
DiltiazemRifampin decreases levels of diltiazem
DisopyramideRifampin decreases the effect of disopyramide
DoxepinThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, doxepin, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of doxepin if rifampin is initiated, discontinued or dose changed.
DoxycyclineThe rifamycin decreases the effect of doxycycline
DyphyllineRifampin decreases the effect of theophylline
EnalaprilRifampin, a strong CYP3A4 inducer, may increase the metabolism of enalapril. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of enalapril if rifampin is initiated, discontinued or dose changed.
ErlotinibDecreased levels/effect of erlotinib
ErythromycinThe rifamycin, rifampin, may decrease the effect of the macrolide, erythromycin.
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
EthotoinRifampin decreases the effect of the hydantoin
EtoricoxibRifampin reduces levels and efficacy of etoricoxib
FentanylRifampin may decrease the serum level and therapeutic effect of fentanyl.
FluconazoleRifampin may decrease the effect of fluconazole.
FludrocortisoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, fludrocortisone.
FluvastatinRifampin may decrease the effect of fluvastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of fluvastatin if rifampin is initiated, discontinued or dose changed.
FosamprenavirRifampin may decrease the effectiveness of fosamprenavir.
FosphenytoinRifampin may decrease the effect of fosphenytoin.
GadoxetateSubstrates of OATP1B1 and OATP1B3 may limit uptake of gadoxetate disodium into heptatocytes. This may alter the intensity of the signal.
GefitinibRifampin reduces levels and efficacy of gefitinib
GliclazideRifampin may decrease the effect of sulfonylurea, gliclazide.
GlimepirideRifampin may decrease the effect of sulfonylurea, glimepiride.
GlipizideRifampin may decrease the effect of sulfonylurea, glipizide.
GlisoxepideRifampin may decrease the effect of sulfonylurea, glisoxepide.
GlyburideRifampin may decrease the effect of sulfonylurea, glibenclamide.
GlycodiazineRifampin may decrease the effect of sulfonylurea, glycodiazine.
HaloperidolThe rifamycin decreases the effect of haloperidol
HydrocortisoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, hydrocortisone.
ImatinibRifampin decreases levels of imatinib
ImipramineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, imipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of imipramine if rifampin is initiated, discontinued or dose changed.
IndinavirRifampin decreases the effect of indinavir
ItraconazoleRifampin may decrease the effect of itraconazole.
IvacaftorStrong CYP3A4 inducers may decrease levels of ivacaftor. Monitor concomitant therapy closely.
JosamycinThe rifamycin, rifampin, may decrease the effect of the macrolide, josamycin.
KetoconazoleRifampin may decrease the effect of ketoconazole.
LamotrigineRifampin decreases levels of lamotrigine
LeflunomideRifampin increases the effect of leflunomide
LinagliptinCYP3A4 and p-glycoprotein inducers may decreases levels of linagliptin. Monitor concomitant therapy closely.
LosartanRifampin decreases the effect of losartan
LovastatinRifampin may decrease the effect of lovastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of lovastatin if rifampin is initiated, discontinued or dose changed.
MefloquineRifampin lowers mefloquine levels
MephenytoinRifampin decreases the effect of the hydantoin
MestranolThis product may cause a slight decrease of contraceptive effect
MethadoneThe rifamycin decreases the effect of methadone
MethylprednisoloneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.
MetoprololRifampin may decrease the serum concentration of metoprolol by increasing its metabolism.
MexiletineRifampin decreases the effect of mexiletine
MidazolamRifampin may increase the metabolism of midazolam. Monitor for changes in the therapeutic and adverse effects of midazolam if rifampin is initiated, discontinued or dose changed.
MirabegronStrong CYP3A4 inducers may decrease levels of mirabegron. Monitor concomitant therapy closely.
MorphineRifampin decreases the effect of morphine/codeine
Mycophenolate mofetilRifampin may decrease the serum concentration of mycophenolate. Concomitant therapy should be avoided.
NelfinavirRifampin decreases the effect of nelfinavir
NifedipineRifampin decreases the effect of the calcium channel blocker, nifedipine.
NorethindroneThis product may cause a slight decrease of contraceptive effect
NortriptylineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, nortriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nortriptyline if rifampin is initiated, discontinued or dose changed.
OspemifeneRifampin, a strong CYP3A4 / moderate CYP2C9 / moderate CYP2C19 inducer, decreases the systemic exposure of ospemifene by 58%. Therefore, co-administration of ospemifene with drugs such as rifampin which induce CYP3A4, CYP2C9 and/or CYP2C19 activity would be expected to decrease the systemic exposure of ospemifene, which may decrease the clinical effect.
OxtriphyllineRifampin may decrease the effect and toxicity of oxtriphylline.
ParamethasoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, paramethasone.
PazopanibConcomitant therapy with a CYP3A4 inducer may decrease exposure of pazopanib.
PhenytoinRifampin may decrease the therapeutic and adverse effects of phenytoin.
PitavastatinRifampin significantly increased pitavastatin exposure. In patients taking rifampin, a dose of LIVALO 2 mg once daily should not be exceeded.
PitavastatinRifampin significantly increased pitavastatin exposure. In patients taking rifampin, a dose of LIVALO 2 mg once daily should not be exceeded.
PomalidomideStrong CYP3A4 inducers may decrease levels of pomalidomide. Concomitant therapy should be avoided.
PonatinibStrong CYP3A4 inducers may decrease levels of ponatinib. Monitor concomitant therapy closely.
PonatinibStrong CYP3A4 inducers may decrease levels of ponatinib. Monitor concomitant therapy closely.
PraziquantelSignificant decrease in praziquantel level
PrednisoloneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisolone.
PrednisoneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisone.
PropafenoneRifampin decreases the effect of propafenone
PropranololRifampin may decrease the serum concentration of propranolol by increasing its metabolism.
ProtriptylineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, protriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of protriptyline if rifampin is initiated, discontinued or dose changed.
QuinidineRifampin decreases the effect of quinidine
Quinidine barbiturateRifampin decreases the effect of quinidine
RamelteonRifampin reduces the levels/effect of ramelteon
RegorafenibStrong CYP3A4 inducers may decrease levels of regorafenib.
RepaglinideRifampin decreases the effect of repaglinide
RilpivirineStrong inducers of CYP3A4 decrease the exposure of rilpivirine thus decreasing efficacy.
RitonavirRifampin decreases the effect of ritonavir
RoflumilastAffects CYP3A4 metabolism, decreases level or effect of roflumilast. Also decreases the level or effect of roflumilast by affecting CYP1A2 metabolism.
RosiglitazoneRifampin reduces levels and efficacy of rosiglitazone
RuxolitinibStrong CYP3A4 inducers may decrease levels of ruxolitinib. Closely monitor patient.
SaquinavirRifampin decreases the effect of saquinavir
SaxagliptinRifampin is a strong inducer of CYP3A4 which decreases exposure of saxagliptin. The exposure of the active metabolite, 5-hydroxy saxagliptin, also increases.
SimvastatinRifampin may decrease the effect of simvastatin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of simvastatin if rifampin is initiated, discontinued or dose changed.
SirolimusThe rifamycin decreases the effect of sirolimus
SunitinibPossible decrease in sunitinib levels
TacrolimusRifampin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Rifampin therapy is initiated, discontinued or altered.
TadalafilRifampin may reduce Tadalafil plasma concentrations and efficacy.
TamoxifenThe rifamycin decreases the effect of anti-estrogen
TelaprevirStrong CYP3A4 inducers will decrease levels of telaprevir. Concomitant therapy is contraindicated.
TelithromycinRifampin may decrease the plasma concentration of Telithromycin. Concomitant therapy should be avoided.
TemsirolimusRifampin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
TerbinafineRifampin may increase the metabolism and clearance of Terbinafine. Co-administration may result in Terbinafine treatment failure.
TheophyllineRifampin decreases the effect of theophylline
TipranavirRifampin may decrease the plasma concentration of Tipranavir. Concomitant use is not recommended.
TocainideRifampin lowers tocainide levels/effects
TofacitinibRifampin (and other potent CYP3A4 inducers), when used in combination with tofacitinib, may decrease tofacitinib toxicity.
TolazamideRifampin may decrease the effect of sulfonylurea, tolazamide.
TolbutamideRifampin may decrease the effect of sulfonylurea, tolbutamide.
TolvaptanRifampin is a CYP3A4 inducer and will decrease serum concentrations of tolvaptan and ultimately, its clinical effects.
ToremifeneThe rifamycin decreases the effect of anti-estrogen
TramadolRifampin may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
TrazodoneThe CYP3A4 inducer, Rifampin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifampin is initiated, discontinued or dose changed.
TretinoinThe strong CYP2C8 inducer, Rifampin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rifampin is initiated, discontinued or dose changed.
TriamcinoloneThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, triamcinolone.
TriazolamRifampin may decrease the effect of the benzodiazepine, triazolam.
TrimethoprimRifampin decreases the effect of trimethoprim
TrimipramineThe rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, trimipramine, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of trimipramine if rifampin is initiated, discontinued or dose changed.
UlipristalConcomitant therapy with strong CYP3A4 inducers may decrease plasma concentrations of ulipristal and ultimately its effectiveness. Avoid combination therapy.
Valproic AcidRifampin may reduce the serum concentration of Valproic acid by increasing Valproic acid metabolism. Valproic acid dose adjustments may be required during concomitant therapy. Monitor Valproic acid serum concentrations, efficacy and toxicity if Rifampin is initiated, discontinued or dose changed.
VandetanibDecreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
VemurafenibStrong CYP3A4 inducers may decrease levels of vemurafenib. Monitor concomitant therapy closely.
VerapamilRifampin, a CYP3A4 inducer, may decrease the serum concentration of Verapamil by increasing its metabolism (particularly in the intestinal mucosa) and decreasing its absorption. Monitor for changes in the therapeutic/adverse effects of Verapamil if Rifampin is initiated, discontinued or dose changed.
VoriconazoleRifampin may decrease the serum concentration of voriconazole likely by increasing its metabolism via CYP3A enzymes. Voriconazole may increase the serum concentration of rifampin likely by inhibiting its metabolism via CYP3A. Concomitant therapy is contraindicated.
WarfarinRifampin may decrease the anticoagulant effect of warfarin by increasing its metabolism.
ZaleplonRifampin decreases the effect of zaleplon
ZidovudineRifampin may decrease the serum concentration of zidovudine by increasing its metabolism. Monitor for changes in the serum concentration and therapeutic and adverse effects of zidovudine if rifampin is initiated, discontinued or dose changed.
Food Interactions
  • Avoid alcohol.
  • Take on empty stomach: 1 hour before or 2 hours after meals.
  • Take with a full glass of water.

Targets

1. DNA-directed RNA polymerase subunit beta

Kind: protein

Organism: Escherichia coli (strain K12)

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
DNA-directed RNA polymerase subunit beta P0A8V2 Details

References:

  1. Villain-Guillot P, Bastide L, Gualtieri M, Leonetti JP: Progress in targeting bacterial transcription. Drug Discov Today. 2007 Mar;12(5-6):200-8. Epub 2007 Feb 5. Pubmed
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. Pubmed
  3. Tupin A, Gualtieri M, Roquet-Baneres F, Morichaud Z, Brodolin K, Leonetti JP: Resistance to rifampicin: at the crossroads between ecological, genomic and medical concerns. Int J Antimicrob Agents. 2010 Jun;35(6):519-23. Epub 2010 Feb 24. Pubmed
  4. Campbell EA, Korzheva N, Mustaev A, Murakami K, Nair S, Goldfarb A, Darst SA: Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. Pubmed
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. Pubmed

2. DNA-directed RNA polymerase subunit beta'

Kind: protein

Organism: Escherichia coli (strain K12)

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
DNA-directed RNA polymerase subunit beta' P0A8T7 Details

References:

  1. Villain-Guillot P, Bastide L, Gualtieri M, Leonetti JP: Progress in targeting bacterial transcription. Drug Discov Today. 2007 Mar;12(5-6):200-8. Epub 2007 Feb 5. Pubmed
  2. White RJ, Lancini GC, Silvestri LG: Mechanism of action of rifampin on Mycobacterium smegmatis. J Bacteriol. 1971 Nov;108(2):737-41. Pubmed
  3. Tupin A, Gualtieri M, Roquet-Baneres F, Morichaud Z, Brodolin K, Leonetti JP: Resistance to rifampicin: at the crossroads between ecological, genomic and medical concerns. Int J Antimicrob Agents. 2010 Jun;35(6):519-23. Epub 2010 Feb 24. Pubmed
  4. Campbell EA, Korzheva N, Mustaev A, Murakami K, Nair S, Goldfarb A, Darst SA: Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. Pubmed
  5. Wehrli W: Rifampin: mechanisms of action and resistance. Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11. Pubmed

3. Nuclear receptor subfamily 1 group I member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
Nuclear receptor subfamily 1 group I member 2 O75469 Details

References:

  1. Chen J, Raymond K: Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann Clin Microbiol Antimicrob. 2006 Feb 15;5:3. Pubmed
  2. Cheng J, Ma X, Krausz KW, Idle JR, Gonzalez FJ: Rifampicin-activated human pregnane X receptor and CYP3A4 induction enhance acetaminophen-induced toxicity. Drug Metab Dispos. 2009 Aug;37(8):1611-21. Epub 2009 May 21. Pubmed

Enzymes

1. 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. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. Pubmed
  3. 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. 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

3. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor 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. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. Pubmed
  3. 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 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. 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

5. 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. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD: Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007 Oct;35(10):1853-9. Epub 2007 Jul 16. Pubmed
  3. 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

6. UDP-glucuronosyltransferase 1-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-1 P22309 Details

References:

  1. Ellis E, Wagner M, Lammert F, Nemeth A, Gumhold J, Strassburg CP, Kylander C, Katsika D, Trauner M, Einarsson C, Marschall HU: Successful treatment of severe unconjugated hyperbilirubinemia via induction of UGT1A1 by rifampicin. J Hepatol. 2006 Jan;44(1):243-5. Epub 2005 Oct 27. Pubmed
  2. Jemnitz K, Lengyel G, Vereczkey L: In vitro induction of bilirubin conjugation in primary rat hepatocyte culture. Biochem Biophys Res Commun. 2002 Feb 15;291(1):29-33. Pubmed

7. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 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

8. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate 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

9. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: 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

10. Cytochrome P450 3A43

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A43 Q9HB55 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 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

12. 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. Epub 2009 Nov 24. Pubmed

13. 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

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. Pubmed
  2. 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
  3. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, Kroemer HK: The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest. 1999 Jul;104(2):147-53. Pubmed
  4. Fardel O, Lecureur V, Loyer P, Guillouzo A: Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells. Biochem Pharmacol. 1995 May 11;49(9):1255-60. Pubmed
  5. Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G: Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26. Pubmed
  6. Kuypers DR, Verleden G, Naesens M, Vanrenterghem Y: Drug interaction between mycophenolate mofetil and rifampin: possible induction of uridine diphosphate-glucuronosyltransferase. Clin Pharmacol Ther. 2005 Jul;78(1):81-8. Pubmed
  7. Gurley BJ, Barone GW, Williams DK, Carrier J, Breen P, Yates CR, Song PF, Hubbard MA, Tong Y, Cheboyina S: Effect of milk thistle (Silybum marianum) and black cohosh (Cimicifuga racemosa) supplementation on digoxin pharmacokinetics in humans. Drug Metab Dispos. 2006 Jan;34(1):69-74. Epub 2005 Oct 12. Pubmed
  8. Chen J, Raymond K: Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann Clin Microbiol Antimicrob. 2006 Feb 15;5:3. Pubmed
  9. Lamba J, Strom S, Venkataramanan R, Thummel KE, Lin YS, Liu W, Cheng C, Lamba V, Watkins PB, Schuetz E: MDR1 genotype is associated with hepatic cytochrome P450 3A4 basal and induction phenotype. Clin Pharmacol Ther. 2006 Apr;79(4):325-38. Epub 2006 Feb 20. Pubmed
  10. Huang R, Murry DJ, Kolwankar D, Hall SD, Foster DR: Vincristine transcriptional regulation of efflux drug transporters in carcinoma cell lines. Biochem Pharmacol. 2006 Jun 14;71(12):1695-704. Epub 2006 Apr 18. Pubmed

2. Solute carrier organic anion transporter family member 1B3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B3 Q9NPD5 Details

References:

  1. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. Pubmed
  2. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. Pubmed
  3. Cui Y, Konig J, Keppler D: Vectorial transport by double-transfected cells expressing the human uptake transporter SLC21A8 and the apical export pump ABCC2. Mol Pharmacol. 2001 Nov;60(5):934-43. Pubmed

3. Multidrug resistance-associated protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

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

References:

  1. Courtois A, Payen L, Vernhet L, de Vries EG, Guillouzo A, Fardel O: Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells. Cancer Lett. 1999 May 3;139(1):97-104. Pubmed

4. Solute carrier organic anion transporter family member 2B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 2B1 O94956 Details

References:

  1. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. Pubmed

5. Bile salt export pump

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Bile salt export pump O95342 Details

References:

  1. Byrne JA, Strautnieks SS, Mieli-Vergani G, Higgins CF, Linton KJ, Thompson RJ: The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology. 2002 Nov;123(5):1649-58. Pubmed
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. Pubmed
  3. Noe J, Hagenbuch B, Meier PJ, St-Pierre MV: Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. Hepatology. 2001 May;33(5):1223-31. Pubmed
  4. Stieger B, Fattinger K, Madon J, Kullak-Ublick GA, Meier PJ: Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver. Gastroenterology. 2000 Feb;118(2):422-30. Pubmed

6. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

References:

  1. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. Pubmed
  2. Fattinger K, Cattori V, Hagenbuch B, Meier PJ, Stieger B: Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2. Hepatology. 2000 Jul;32(1):82-6. Pubmed
  3. Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y: Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res. 2002 Feb;19(2):147-53. Pubmed
  4. van Montfoort JE, Stieger B, Meijer DK, Weinmann HJ, Meier PJ, Fattinger KE: Hepatic uptake of the magnetic resonance imaging contrast agent gadoxetate by the organic anion transporting polypeptide Oatp1. J Pharmacol Exp Ther. 1999 Jul;290(1):153-7. Pubmed

7. Solute carrier family 22 member 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 7 Q9Y694 Details

References:

  1. Sekine T, Cha SH, Tsuda M, Apiwattanakul N, Nakajima N, Kanai Y, Endou H: Identification of multispecific organic anion transporter 2 expressed predominantly in the liver. FEBS Lett. 1998 Jun 12;429(2):179-82. Pubmed

8. Solute carrier organic anion transporter family member 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 Details

References:

  1. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. Pubmed
  2. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K: Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72. Pubmed
  3. Tirona RG, Leake BF, Wolkoff AW, Kim RB: Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. J Pharmacol Exp Ther. 2003 Jan;304(1):223-8. Pubmed
  4. Sharma P, Holmes VE, Elsby R, Lambert C, Surry D: Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions. Xenobiotica. 2010 Jan;40(1):24-37. Pubmed

9. Multidrug resistance-associated protein 5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Multidrug resistance-associated protein 5 O15440 Details

References:

  1. 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

10. 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. Kauffmann HM, Pfannschmidt S, Zoller H, Benz A, Vorderstemann B, Webster JI, Schrenk D: Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46. Pubmed
  2. Fromm MF, Kauffmann HM, Fritz P, Burk O, Kroemer HK, Warzok RW, Eichelbaum M, Siegmund W, Schrenk D: The effect of rifampin treatment on intestinal expression of human MRP transporters. Am J Pathol. 2000 Nov;157(5):1575-80. Pubmed

11. 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. Teng S, Jekerle V, Piquette-Miller M: Induction of ABCC3 (MRP3) by pregnane X receptor activators. Drug Metab Dispos. 2003 Nov;31(11):1296-9. Pubmed

Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on January 17, 2014 14:51