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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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rifadincapsule300 mgoralSanofi Aventis U.S. Llc1971-05-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifadin Ivinjection, powder, lyophilized, for solution600 mg/10mLintravenousSanofi Aventis U.S. Llc1989-05-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifadincapsule300 mgoralSanofi Aventis Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Rifadincapsule150 mgoralSanofi Aventis Canada IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rifadincapsule150 mgoralSanofi Aventis U.S. Llc1981-07-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousPfizer Laboratories Div Pfizer Inc2011-05-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousPfizer Laboratories Div Pfizer Inc2011-05-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralEon Labs, Inc.1997-05-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralEon Labs, Inc.1998-01-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralLannett Company, Inc.2008-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralLannett Company, Inc.2008-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoral; oralMajor Pharmaceuticals2009-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousAkorn, Inc.2012-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralRebel Distributors Corp1997-05-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousHeritage Pharmaceuticals Inc.2014-08-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule, coated300 mgoralREMEDYREPACK INC.2013-10-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralRebel Distributors Corp2008-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralREMEDYREPACK INC.2011-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralREMEDYREPACK INC.2011-06-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralREMEDYREPACK INC.2011-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralMylan Institutional Inc.2012-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule, coated300 mgoralH.J. Harkins Company, Inc.2001-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule, coated300 mgoralState of Florida DOH Central Pharmacy2009-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralPhysicians Total Care, Inc.2008-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralPhysicians Total Care, Inc.2008-04-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralCardinal Health2011-05-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule, coated300 mgoralCardinal Health2001-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousBedford Laboratories2002-02-182015-07-31Us 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralVersa Pharm Incorporated2001-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralVersa Pharm Incorporated2001-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mgintravenousFresenius Kabi USA, LLC2014-08-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralbryant ranch prepack1997-05-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2006-11-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampininjection, powder, lyophilized, for solution600 mg/10mLintravenousMylan Institutional LLC2008-05-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralAmerican Health Packaging2009-09-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralAmerican Health Packaging2009-09-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule, coated300 mgoralCarilion Materials Management2001-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule150 mgoralLupin Pharmaceuticals, Inc.2013-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Rifampincapsule300 mgoralLupin Pharmaceuticals, Inc.2013-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
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
Salts
Name/CASStructureProperties
Rifampicin sodium
ThumbNot applicableDBSALT001014
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,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(1E)-[(4-methylpiperazin-1-yl)imino]methyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1⁴,⁷.0⁵,²⁸]triaconta-1(29),2,4,9,19,21,25,27-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
Taxonomy
ClassificationNot classified
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
  • Mycobacterium tuberculosis
  • Various gram-negative and gram-positive eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.5553
Blood Brain Barrier-0.974
Caco-2 permeable-0.7123
P-glycoprotein substrateSubstrate0.9308
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IINon-inhibitor0.6049
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8508
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7296
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 substrateNon-inhibitor0.907
CYP450 2D6 substrateNon-inhibitor0.9231
CYP450 2C19 substrateNon-inhibitor0.9025
CYP450 3A4 substrateNon-inhibitor0.8432
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9099
Ames testNon AMES toxic0.5803
CarcinogenicityNon-carcinogens0.8493
BiodegradationNot ready biodegradable0.9962
Rat acute toxicity2.6875 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.908
hERG inhibition (predictor II)Non-inhibitor0.5486
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral150 mg
Capsuleoral300 mg
Capsuleoral; oral300 mg
Capsule, coatedoral300 mg
Injection, powder, lyophilized, for solutionintravenous600 mg
Injection, powder, lyophilized, for solutionintravenous600 mg/10mL
Prices
Unit descriptionCostUnit
Rifadin iv 600 mg vial140.9USD vial
Rifampin iv 600 mg vial136.3USD vial
Rifampin crystals6.72USD g
Rifampin powder3.98USD g
Rifadin 300 mg capsule3.09USD capsule
Rifadin 150 mg capsule2.57USD capsule
Rifampin 300 mg capsule2.37USD capsule
Rimactane 300 mg capsule2.35USD capsule
Rifampin 150 mg capsule2.27USD capsule
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 Solubility0.0413 mg/mLALOGPS
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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
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
ATC CodesJ04AB02
AHFS Codes
  • 08:16.04
PDB Entries
FDA labelDownload (43.3 KB)
MSDSDownload (86.7 KB)
Interactions
Drug Interactions
Drug
AfatinibP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Afatinib.
AlfentanilRifamycin Derivatives may decrease the serum concentration of Alfentanil.
AmiodaroneRifampin may decrease serum concentrations of the active metabolite(s) of Amiodarone. Specifically, desethylamiodarone concentrations may decrease. Rifampin may decrease the serum concentration of Amiodarone.
AmlodipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
AmrinoneRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
ApixabanCYP3A4 Inducers (Strong) may decrease the serum concentration of Apixaban.
ApremilastCYP3A4 Inducers (Strong) may decrease the serum concentration of Apremilast.
AprepitantRifampin may decrease the serum concentration of Aprepitant.
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.
AtazanavirRifampin may decrease the serum concentration of Atazanavir.
AtovaquoneRifamycin Derivatives may decrease the serum concentration of Atovaquone.
AxitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Axitinib.
bazedoxifeneRifampin 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.
BepridilRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
BoceprevirRifampin may decrease the serum concentration of Boceprevir.
BortezomibCYP3A4 Inducers (Strong) may decrease the serum concentration of Bortezomib.
BosentanRifampin may decrease the serum concentration of Bosentan. Following the initial several weeks of concurrent rifampin, this effect is most likely. Rifampin may increase the serum concentration of Bosentan. This effect is most likely to be observed within the initial few weeks of concurrent therapy (and may be greatest immediately following initiation of the combination).
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.
BuspironeRifamycin Derivatives may decrease the serum concentration of BusPIRone.
ButabarbitalRifamycin Derivatives may increase the metabolism of Barbiturates.
ButethalRifamycin Derivatives may increase the metabolism of Barbiturates.
CabozantinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Cabozantinib.
CanagliflozinRifampin may decrease the serum concentration of Canagliflozin.
CaspofunginRifampin may decrease the serum concentration of Caspofungin.
ChloramphenicolRifampin may increase the metabolism of Chloramphenicol.
CitalopramRifampin may decrease the serum concentration of Citalopram.
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.
ClopidogrelRifamycin Derivatives may enhance the adverse/toxic effect of Clopidogrel. Specifically,clopidogrel antiplatelet effects may be enhanced.
ClozapineCYP3A4 Inducers (Strong) may decrease the serum concentration of CloZAPine.
CrizotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Crizotinib.
Dabigatran etexilateP-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Dabigatran Etexilate.
DarunavirRifampin may decrease the serum concentration of Darunavir.
DasatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
DeferasiroxRifampin may decrease the serum concentration of Deferasirox.
DelavirdineRifamycin Derivatives may increase the metabolism of Delavirdine. Delavirdine may increase the serum concentration of Rifamycin Derivatives. Specifically, Rifabutin serum concentration may be increased.
DiltiazemRifampin may decrease the serum concentration of Diltiazem.
DisopyramideRifampin may decrease the serum concentration of Disopyramide.
DolutegravirRifampin may decrease the serum concentration of Dolutegravir.
DoxycyclineRifampin may decrease the serum concentration of Doxycycline.
DronabinolCYP3A4 Inducers (Strong) may decrease the serum concentration of Dronabinol.
DronedaroneCYP3A4 Inducers (Strong) may decrease the serum concentration of Dronedarone.
EfavirenzRifampin may decrease the serum concentration of Efavirenz.
EliglustatCYP3A4 Inducers (Strong) may decrease the serum concentration of Eliglustat.
EltrombopagMay increase the serum concentration of OATP1B1/SLCO1B1 Substrates.
EnzalutamideCYP2C8 Inducers (Strong) may decrease the serum concentration of Enzalutamide.
ErlotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Erlotinib.
EsomeprazoleRifampin may decrease the serum concentration of Esomeprazole.
EtravirineRifamycin Derivatives 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.
FelodipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
FentanylCYP3A4 Inducers (Strong) may decrease the serum concentration of FentaNYL.
FexofenadineRifampin may decrease the serum concentration of Fexofenadine. Rifampin may increase the serum concentration of Fexofenadine.
FlunarizineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
FosamprenavirRifampin may decrease the serum concentration of Fosamprenavir. Specifically, concentrations of amprenavir (active metabolite) may be decreased.
FosaprepitantRifampin may decrease the serum concentration of Fosaprepitant. More specifically, rifampin may decrease concentrations of the active metabolite aprepitant.
FosphenytoinRifampin may decrease the serum concentration of Fosphenytoin.
GabapentinRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
GefitinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Gefitinib.
GuanfacineCYP3A4 Inducers (Strong) may decrease the serum concentration of GuanFACINE.
HeptabarbitalRifamycin Derivatives may increase the metabolism of Barbiturates.
HexobarbitalRifamycin Derivatives may increase the metabolism of Barbiturates.
HydrocodoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Hydrocodone.
ImatinibRifamycin Derivatives may decrease the serum concentration of Imatinib.
IndinavirRifampin may decrease the serum concentration of Indinavir.
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.
IsoniazidRifamycin Derivatives may enhance the hepatotoxic effect of Isoniazid. Even so, this is a frequently employed combination regimen.
IsradipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms 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.
LamotrigineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms 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.
LeflunomideRifampin may increase serum concentrations of the active metabolite(s) of Leflunomide.
LercanidipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
LinagliptinCYP3A4 Inducers (Strong) may decrease the serum concentration of Linagliptin.
LopinavirRifampin may enhance the adverse/toxic effect of Lopinavir. Specifically, the risk of hepatocellular toxicity may be increased. Rifampin may decrease the serum concentration of Lopinavir.
LosartanRifampin may decrease the serum concentration of Losartan.
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 SulfateRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
MaravirocCYP3A4 Inducers (Strong) may decrease the serum concentration of Maraviroc.
MethadoneRifamycin Derivatives may decrease the serum concentration of Methadone.
MethohexitalRifamycin Derivatives may increase the metabolism of Barbiturates.
MethylprednisoloneCYP3A4 Inducers (Strong) may decrease the serum concentration of MethylPREDNISolone.
MifepristoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Mifepristone.
MirabegronRifampin may decrease the serum concentration of Mirabegron.
NelfinavirRifampin may decrease the serum concentration of Nelfinavir.
NevirapineRifampin may decrease the serum concentration of Nevirapine.
NicardipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
NifedipineCYP3A4 Inducers (Strong) may decrease the serum concentration of NIFEdipine.
NilotinibCYP3A4 Inducers (Strong) may decrease the serum concentration of Nilotinib.
NimodipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
NisoldipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
NitrazepamRifampin may decrease the serum concentration of Nitrazepam.
NitrendipineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
OmeprazoleRifampin may decrease the serum concentration of Omeprazole.
OxycodoneRifampin may decrease the serum concentration of OxyCODONE.
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.
PentobarbitalRifamycin Derivatives may increase the metabolism of Barbiturates.
PerampanelCYP3A4 Inducers (Strong) may decrease the serum concentration of Perampanel.
PerhexilineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
PhenytoinRifampin may decrease the serum concentration of Phenytoin.
PirfenidoneCYP1A2 Inducers (Strong) may decrease the serum concentration of Pirfenidone.
PitavastatinRifamycin Derivatives may increase the serum concentration of Pitavastatin.
PomalidomideCYP1A2 Inducers (Strong) may decrease the serum concentration of Pomalidomide.
PonatinibCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
PrasugrelRifampin may diminish the antiplatelet effect of Prasugrel.
PraziquantelCYP3A4 Inducers (Strong) may decrease the serum concentration of Praziquantel.
PrednisoneCYP3A4 Inducers (Strong) may decrease the serum concentration of PredniSONE.
PrenylamineRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
PrimidoneRifamycin Derivatives may increase the metabolism of Barbiturates.
PropafenoneRifamycin Derivatives may decrease the serum concentration of Propafenone.
PropofolRifampin may enhance the hypotensive effect of Propofol.
PyrazinamideMay enhance the hepatotoxic effect of Rifampin. Severe (even fatal) liver injury has been reported in patients receiving these 2 drugs as a 2-month treatment regimen for latent TB infection.
QuetiapineCYP3A4 Inducers (Strong) may decrease the serum concentration of QUEtiapine.
QuinidineRifamycin Derivatives may decrease the serum concentration of QuiNIDine.
QuinineRifampin may decrease the serum concentration of QuiNINE.
RaltegravirRifampin may decrease the serum concentration of Raltegravir.
RamelteonRifamycin Derivatives may increase the metabolism of Ramelteon.
RanolazineRifampin may decrease the serum concentration of Ranolazine.
RegorafenibCYP3A4 Inducers (Strong) may decrease the serum concentration of Regorafenib.
RepaglinideRifampin may decrease the serum concentration of Repaglinide.
RilpivirineRifamycin Derivatives may decrease the serum concentration of Rilpivirine.
RisedronateRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
RitonavirRifampin may decrease the serum concentration of Ritonavir.
RivaroxabanCYP3A4 Inducers (Strong) may decrease the serum concentration of Rivaroxaban.
RoflumilastRifampin may decrease the serum concentration of Roflumilast.
RomidepsinRifampin may increase the serum concentration of RomiDEPsin.
SaquinavirRifampin may enhance the adverse/toxic effect of Saquinavir. Specifically, the risk of hepatocellular toxicity may be increased. Rifampin may decrease the serum concentration of Saquinavir.
SaxagliptinCYP3A4 Inducers may decrease the serum concentration of Saxagliptin.
SecobarbitalRifamycin Derivatives may increase the metabolism of Barbiturates.
SimeprevirCYP3A4 Inducers (Strong) may decrease the serum concentration of Simeprevir.
SirolimusRifampin may increase the metabolism of Sirolimus.
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.
TamoxifenRifamycin Derivatives may increase the metabolism of Tamoxifen.
TelaprevirRifampin may decrease the serum concentration of Telaprevir.
TemsirolimusRifamycin Derivatives may decrease the serum concentration of Temsirolimus. Rifamycins will likely cause an even greater decrease in the concentration of the active metabolite sirolimus.
TeriflunomideMay increase the serum concentration of OATP1B1/SLCO1B1 Substrates.
TicagrelorCYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inducers (Strong) may decrease the serum concentration of Ticagrelor.
TipranavirRifampin may decrease the serum concentration of Tipranavir.
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.
VerapamilRifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers.
VilazodoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Vilazodone.
VorapaxarCYP3A4 Inducers (Strong) may decrease the serum concentration of Vorapaxar.
VoriconazoleMay increase the serum concentration of Rifamycin Derivatives. Rifamycin Derivatives may decrease the serum concentration of Voriconazole.
ZaleplonRifamycin Derivatives may increase the metabolism of Zaleplon.
ZidovudineRifamycin Derivatives may decrease the serum concentration of Zidovudine.
ZolpidemRifamycin Derivatives may decrease the serum concentration of Zolpidem.
ZuclopenthixolCYP3A4 Inducers (Strong) may decrease the serum concentration of Zuclopenthixol.
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

4. Solute carrier organic anion transporter family member 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 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. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

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

6. Solute carrier organic anion transporter family member 1B3

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

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

7. Lanosterol 14-alpha demethylase

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Lanosterol 14-alpha demethylase Q16850 Details

References:

  1. Ekins S, Mankowski DC, Hoover DJ, Lawton MP, Treadway JL, Harwood HJ Jr: Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. Drug Metab Dispos. 2007 Mar;35(3):493-500. Epub 2006 Dec 28. Pubmed

8. Serum albumin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. Baneres-Roquet F, Gualtieri M, Villain-Guillot P, Pugniere M, Leonetti JP: Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions. Antimicrob Agents Chemother. 2009 Apr;53(4):1528-31. doi: 10.1128/AAC.00971-08. Epub 2009 Jan 21. Pubmed

9. Solute carrier organic anion transporter family member 2B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

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

References:

  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. Pubmed

Enzymes

1. 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

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. 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

5. 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

6. 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

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

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Drug created on June 13, 2005 07:24 / Updated on January 17, 2014 14:51