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Identification
NameIbuprofen
Accession NumberDB01050  (APRD00372)
Typesmall molecule
Groupsapproved
Description

Ibuprofen, a propionic acid derivative, is a prototypical nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties.

Structure
Thumb
Synonyms
SynonymLanguageCode
(+-)-2-(P-Isobutylphenyl)propionic acidNot AvailableNot Available
(+-)-alpha-Methyl-4-(2-methylpropyl)benzeneacetic acidNot AvailableNot Available
(+-)-IbuprofenNot AvailableNot Available
(+-)-P-Isobutylhydratropic acidNot AvailableNot Available
(4-Isobutylphenyl)-alpha-methylacetic acidNot AvailableNot Available
(RS)-ibuprofenNot AvailableNot Available
2-(4-Isobutylphenyl)propanoic acidNot AvailableNot Available
4-Isobutylhydratropic acidNot AvailableNot Available
AdranNot AvailableNot Available
AdvilNot AvailableNot Available
alpha-(4-Isobutylphenyl)propionic acidNot AvailableNot Available
alpha-(P-Isobutylphenyl)propionic acidNot AvailableNot Available
AmibufenNot AvailableNot Available
AncoNot AvailableNot Available
AnflagenNot AvailableNot Available
ApsifenNot AvailableNot Available
BlutonNot AvailableNot Available
BrufenNot AvailableNot Available
BrufortNot AvailableNot Available
BuburoneNot AvailableNot Available
ButyleninNot AvailableNot Available
DolginNot AvailableNot Available
DolgiridNot AvailableNot Available
DolgitNot AvailableNot Available
Dolo-dolgitNot AvailableNot Available
EbufacNot AvailableNot Available
EpobronNot AvailableNot Available
FemadonNot AvailableNot Available
HaltranNot AvailableNot Available
Ibu-attritinNot AvailableNot Available
IbumetinNot AvailableNot Available
IbuprocinNot AvailableNot Available
IbuprofenNot AvailableNot Available
IbuprophenNot AvailableNot Available
IbutidNot AvailableNot Available
InabrinNot AvailableNot Available
InovenNot AvailableNot Available
LamidonNot AvailableNot Available
LebrufenNot AvailableNot Available
LiptanNot AvailableNot Available
MediprenNot AvailableNot Available
MotrinNot AvailableNot Available
MynosedinNot AvailableNot Available
NobfenNot AvailableNot Available
NobgenNot AvailableNot Available
NuprinNot AvailableNot Available
NurofenNot AvailableNot Available
P-Isobutylhydratropic AcidNot AvailableNot Available
Para-Isobutylhydratropic AcidNot AvailableNot Available
PediaprofenNot AvailableNot Available
RoideninNot AvailableNot Available
RufenNot AvailableNot Available
SeclodinNot AvailableNot Available
SusprenNot AvailableNot Available
TabalonNot AvailableNot Available
TrendarNot AvailableNot Available
UremNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
Act-3Healthcare Logistics
ActiprofenSterling Health
AdexDexxon
AdranNot Available
AdvilWyeth
Advil Liqui-GelsWyeth
AktrenBayer
Alges-XAxapharm
AlgoflexChinoin
AlgofrenIntermed
AliviumBristol-Myers Squibb
ArtofenTeva
BetagesicAdcock Ingram Pharmaceuticals
BetaprofenBe-Tabs Pharmaceuticals
BlutonNot Available
BonifenKrka
BrufenAbbott
BuburoneTowa Yakuhin
BugesicNot Available
BuprovilNot Available
BuranaOrion
ButyleninNot Available
CaldolorCumberland
CalprofenMcNeil
Cap-ProfenPERRIGO
Children's AdvilPfizer
Children's ElixsurePfizer
Children's IbuprofenPfizer
Children's MotrinJohnson & Johnson
DalsyAbbott
DismenolMerz
DiverinNot Available
DolgiridNot Available
DolgitDolorgiet
DolofortNot Available
DolorazNot Available
DolorminNot Available
DorivalNot Available
EbufacNot Available
EmuProfenNot Available
EpobronNot Available
EspidifenNot Available
EveNot Available
FemadonNot Available
FenbidNot Available
FenpaedNot Available
FinalflexNot Available
GalprofenNot Available
HaltranNot Available
Herron BlueNot Available
i-profen Not Available
IbalginNot Available
IBUNot Available
Ibu-AttritinNot Available
IBU-RatiopharmNot Available
Ibu-VivimedNot Available
IbuflamNot Available
IbugelNot Available
IbugesicNot Available
IbuHEXALNot Available
IbuleveNot Available
IbumNot Available
IbumaxNot Available
IbumetinNot Available
IbumidolNot Available
IbupainNot Available
IbuprocinNot Available
IbupromNot Available
IbuprosynNot Available
IbuproxNot Available
IbustarNot Available
IbutidNot Available
IbuxNot Available
IbuxinNot Available
InabrinNot Available
InovenNot Available
IprenNot Available
Junior Strength AdvilNot Available
Junior Strength IbuprofenNot Available
Junior Strength MotrinNot Available
KratalginNot Available
LamidonNot Available
LebrufenNot Available
LiptanNot Available
LotemNot Available
MedicolNot Available
MediprenNot Available
Midol IBNot Available
MotrinNot Available
MynosedinNot Available
MypaidNot Available
MyprodolNot Available
NarfenNot Available
Naron Ace Not Available
NeobrufenNot Available
NeoProfenOvation
NobfenNot Available
NobgenNot Available
NorvectanNot Available
NuprinNot Available
NureflexNot Available
NurofenNot Available
OrbifenNot Available
PanafenNot Available
PediaprofenNot Available
PerifarNot Available
ProfinNot Available
RanfenNot Available
RapidolNot Available
RatiodolorNot Available
RimafenNot Available
RoideninNot Available
RufenNot Available
SalvarinaNot Available
SeclodinNot Available
SolpaflexNot Available
Speedpain NANONot Available
SpidifenZambon
SusprenNot Available
TabalonNot Available
TefinNot Available
TrendarNot Available
UnafenNot Available
UpfenNot Available
UremNot Available
Brand mixtures
Brand NameIngredients
Advil Cold & Sinusibuprofen + pseudoephedrine HCl
Advil Cold & Sinus Daytimeibuprofen + pseudoephedrine HCl
Advil Cold and Sinus Nighttimeibuprofen + pseudoephedrine HCll + chlorpheniramine maleate
Advil Cold and Sinus Plusibuprofen + pseudoephedrine HCl + chlorpheniramine maleate
Advil Flu & Body Acheibuprofen + pseudoephedrine HCl
Children's Advil Coldibuprofen + pseudoephedrine HCl
Dristan Sinus Capletsibuprofen + pseudoephedrine HCl
IBUDONEHydrocodone + Ibuprofen
Motrin Children's Coldibuprofen + pseudoephedrine HCl
Motrin Sinus Headacheibuprofen + pseudoephedrine HCl
NorcoHydrocodone + Ibuprofen
NORCOHydrocodone + Ibuprofen
REPREXAINHydrocodone + Ibuprofen
REZIRAHydrocodone + Ibuprofen
Robax Platinummethocarbamol + ibuprofen
Sudafed Sinus Advanceibuprofen + pseudoephedrine HCl
TUSSICAPSHydrocodone + Ibuprofen
Vicoprofenibuprofen + hydrocodone bitartrate
Categories
CAS number15687-27-1
WeightAverage: 206.2808
Monoisotopic: 206.13067982
Chemical FormulaC13H18O2
InChI KeyHEFNNWSXXWATRW-UHFFFAOYSA-N
InChI
InChI=1S/C13H18O2/c1-9(2)8-11-4-6-12(7-5-11)10(3)13(14)15/h4-7,9-10H,8H2,1-3H3,(H,14,15)
IUPAC Name
2-[4-(2-methylpropyl)phenyl]propanoic acid
SMILES
CC(C)CC1=CC=C(C=C1)C(C)C(O)=O
Mass Specshow(11.4 KB)
Taxonomy
KingdomOrganic Compounds
SuperclassPhenylpropanoids and Polyketides
ClassPhenylpropanoic Acids
SubclassNot Available
Direct parentPhenylpropanoic Acids
Alternative parentsAromatic Monoterpenes; Phenylacetic Acid Derivatives; Monocyclic Monoterpenes; Enolates; Carboxylic Acids; Polyamines
Substituentsbenzene; polyamine; enolate; carboxylic acid; carboxylic acid derivative
Classification descriptionThis compound belongs to the phenylpropanoic acids. These are compounds whose structure contain a benzene ring conjugated to a propanoic acid.
Pharmacology
IndicationFor symptomatic treatment of rheumatoid arthritis, juvenile rheumatoid arthritis and osteoarthritis. May be used to treat mild to moderate pain and for the management of dysmenorrhea. May be used to reduce fever. Has been used with some success for treating ankylosing spondylitis, gout and psoriatic arthritis. May reduce pain, fever and inflammation of pericarditis. May be used IV with opiates to relieve moderate to severe pain. Ibuprofen lysine may be used IV to treat patent ductus arteriosus (PDA) in premature neonates.
PharmacodynamicsIbuprofen is a nonsteroidal anti-inflammatory agent (NSAIA) or nonsteroidal anti-inflammatory drug (NSAID), with analgesic and antipyretic properties. Ibuprofen has pharmacologic actions similar to those of other prototypical NSAIAs, which are thought to act through inhibition of prostaglandin synthesis.
Mechanism of actionThe exact mechanism of action of ibuprofen is unknown. Ibuprofen is a non-selective inhibitor of cyclooxygenase, an enzyme invovled in prostaglandin synthesis via the arachidonic acid pathway. Its pharmacological effects are believed to be due to inhibition cylooxygenase-2 (COX-2) which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer is believed to be the more pharmacologically active enantiomer.
Absorption~ 80% absorbed from GI tract

Time to reach peak plasma concentration = 47 minutes (suspension), 62 minutes (chewable tablets), 120 minutes (conventional tablets)

Volume of distributionNot Available
Protein binding90-99% to whole human plasma and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.
Metabolism

R-enanatiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo. Metablized by oxidation to 2 inactive metabolites: (+)-2[4´-(2-hydroxy-2-methylpropyl)phenyl]propionic acid and (+)-2-[4´-(2-carboxypropyl)phenyl]propionic acid. Very small amounts of 1-hydroxyibuprofen and 3-hydroxyibuprofen have been recovered from urine. Cytochrome P450 2C9 is the major catalyst in the formation of oxidative metabolites. Oxidative metabolites may be conjugated to glucuronide prior to excretion.

SubstrateEnzymesProduct
Ibuprofen
Ibuprofen glucuronideDetails
Ibuprofen
2-HydroxyibuprofenDetails
Ibuprofen
3-HydroxyibuprofenDetails
Ibuprofen
Not Available
1-hydroxyibuprofenDetails
3-Hydroxyibuprofen
Carboxy-ibuprofenDetails
Route of eliminationIbuprofen is rapidly metabolized and eliminated in the urine.
Half life2-4 hours
ClearanceNot Available
Toxicity

Side effects: May cause peripheral edema and fluid retention. Use caution in patients with congestive heart failure or severe uncontrolled hypertension. May cause dyspepsia, heartburn, nausea, vomiting, anorexia, diarrhea, constipation, stomatitis, flatulence, bloating, epigastric pain, and abdominal pain. Peptic ulcer and GI bleeding have been reported. May also cause dizziness, headache and nervousness. Acute renal failure accompanied by acute tubular necrosis has been reported.

Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).

LD50=1255mg/kg(orally in mice)

Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.9927
Blood Brain Barrier + 0.9619
Caco-2 permeable + 0.8866
P-glycoprotein substrate Non-substrate 0.759
P-glycoprotein inhibitor I Non-inhibitor 0.9705
P-glycoprotein inhibitor II Non-inhibitor 0.9323
Renal organic cation transporter Non-inhibitor 0.9323
CYP450 2C9 substrate Non-substrate 0.7594
CYP450 2D6 substrate Non-substrate 0.9116
CYP450 3A4 substrate Non-substrate 0.6877
CYP450 1A2 substrate Non-inhibitor 0.9045
CYP450 2C9 substrate Non-inhibitor 0.9305
CYP450 2D6 substrate Non-inhibitor 0.9231
CYP450 2C19 substrate Non-inhibitor 0.9881
CYP450 3A4 substrate Non-inhibitor 0.9655
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9691
Ames test Non AMES toxic 0.9894
Carcinogenicity Carcinogens 0.5553
Biodegradation Ready biodegradable 0.5142
Rat acute toxicity 2.3092 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9719
hERG inhibition (predictor II) Non-inhibitor 0.9734
Pharmacoeconomics
Manufacturers
  • Wyeth consumer healthcare
  • Banner pharmacaps inc
  • Contract pharmacal corp
  • Dr reddys laboratories ltd
  • Marksans pharma ltd
  • Bayer healthcare llc
  • Cumberland pharmaceuticals inc
  • Mcneil consumer healthcare
  • Perrigo co
  • Tris pharma inc
  • Mcneil consumer products co div mcneilab inc
  • Alterna tchp llc
  • L perrigo co
  • Abbott laboratories pharmaceutical products div
  • Actavis mid atlantic llc
  • Perrigo r and d co
  • Mcneil consumer healthcare div mcneil ppc inc
  • Mcneil pediatrics
  • Lederle laboratories div american cyanamid co
  • Basf corp
  • Pliva inc
  • Advent pharmaceuticals inc
  • Amneal pharmaceuticals ny llc
  • Dr reddys laboratories louisiana llc
  • Dr reddys laboratories inc
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Leiner health products inc
  • Lnk international inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Mylan laboratories inc
  • Northstar healthcare holdings ltd
  • Ohm corp
  • Ohm laboratories inc
  • Par pharmaceutical inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Shasun usa inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Alra laboratories inc
  • Bristol myers products inc
  • Lundbeck inc
Packagers
Dosage forms
FormRouteStrength
CapsuleOral200 mg
ConcentrateIntravenous100 mg/ml
SuspensionOral100 mg/5 ml
SuspensionOral40 mg/ml
TabletOral200 mg
TabletOral400 mg
TabletOral600 mg
TabletOral800 mg
Tablet, chewableOral100 mg
Tablet, chewableOral50 mg
Tablet, film coatedOral100 mg
Tablet, film coatedOral200 mg
Tablet, film coatedOral400 mg
Tablet, film coatedOral600 mg
Tablet, film coatedOral800 mg
Prices
Unit descriptionCostUnit
Neoprofen 20 mg/2 ml vial304.5USDml
Caldolor 400 mg/4 ml vial2.21USDml
Caldolor 800 mg/8 ml vial1.58USDml
Nuprin arthritis patch1.11USDpatch
Ibuprofen powder1.04USDg
Nuprin muscle & joint patch1.03USDpatch
Profen II 45-800 mg 12 Hour tablet0.69USDtablet
Motrin 800 mg tablet0.59USDtablet
Advil allergy sinus caplet0.5USDcaplet
Ibu-drops 40 mg/ml suspension drops0.42USDml
Motrin 600 mg tablet0.4USDtablet
Ibuprofen 800 mg tablet0.36USDtablet
Ibuprofen 400 mg tablet0.35USDtablet
Infant's motrin 50 mg/1.25 ml0.34USDml
Childs ibuprofen susp drp0.33USDml
Ibuprofen 600 mg tablet0.33USDtablet
Wal-profen cold & sinus cplt0.3USDcaplet
Infant ibuprofen susp drop0.29USDml
Motrin 400 mg tablet0.29USDtablet
CVS Pharmacy infant ibuprofen susp drop0.25USDml
Infants medi-profen susp0.23USDml
Advil cold & sinus caplet0.22USDcaplet
Advil pm caplet0.22USDcaplet
Soba profen cold-sinus tablet0.22USDtablet
Midol caplet0.21USDcaplet
Advil migraine 200 mg capsule0.2USDcapsule
Ibuprofen cold-sinus caplet0.2USDcaplet
Motrin 100 mg caplet0.2USDcaplet
Motrin pm caplet0.2USDcaplet
Advil 200 mg liqui-gel capsule0.19USDcapsule
Soba profen ib caplet0.19USDcaplet
Motrin 100 mg tablet chew0.18USDtablet
Pub infants profenib drops0.18USDml
Sm ibuprofen ib 100 mg tablet0.18USDtablet
Eck ibuprofen jr caplet0.17USDcaplet
Ibuprofen pm caplet0.17USDcaplet
Advil 200 mg caplet0.15USDcapsule
Advil 200 mg gel caplet0.15USDcaplet
Advil 200 mg tablet0.15USDtablet
Ibuprofen 100 mg tablet chew0.15USDtablet
Motrin ib 200 mg caplet0.15USDcaplet
Apo-Ibuprofen 600 mg Tablet0.14USDtablet
CVS Pharmacy ibuprofen jr str 100 mg tablet0.14USDtablet
Nu-Ibuprofen 600 mg Tablet0.14USDtablet
Motrin ib 200 mg tablet0.13USDtablet
Motrin ib 200 mg gelcap0.12USDcapsule
Nuprin 200 mg caplet0.12USDcaplet
Wal-profen 200 mg caplet0.12USDcaplet
Wal-profen 200 mg tablet0.12USDtablet
Eql ibuprofen 200 mg tablet0.1USDtablet
Nuprin 200 mg tablet0.1USDtablet
Apo-Ibuprofen 400 mg Tablet0.08USDtablet
Ibuprofen ib 200 mg tablet0.08USDtablet
Novo-Profen 400 mg Tablet0.08USDtablet
Apo-Ibuprofen 300 mg Tablet0.07USDtablet
Medi-profen 200 mg tablet0.07USDtablet
Ibuprofen 100 mg/5ml Suspension0.06USDml
Ibuprofen 200 mg caplet0.06USDcaplet
Child ibuprofen susp0.05USDml
Children's medi-profen susp0.05USDml
Children's motrin cold suspension0.05USDml
CVS Pharmacy ibuprofen 200 mg tablet0.05USDtablet
Ibuprofen cold suspension0.05USDml
I-prin 200 mg tablet0.05USDtablet
Novo-Profen 600 mg Tablet0.05USDtablet
Children's motrin cold0.04USDml
Pv ibuprofen 200 mg caplet0.04USDcaplet
Soba children's profenib susp0.04USDml
Ibuprofen 200 mg tablet0.03USDtablet
CVS Pharmacy ibuprofen 200 mg caplet0.02USDcaplet
Pv ibuprofen 200 mg tablet0.02USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States67272862001-11-272021-11-27
United States52157551993-06-012010-06-01
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point75-77.5U.S. Patent 3,228,831 U.S. Patent 3,385,886
water solubility21 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP3.97AVDEEF,A (1997)
logS-3.99ADME Research, USCD
Caco2 permeability-4.28ADME Research, USCD
pKa4.91SANGSTER (1994)
Predicted Properties
PropertyValueSource
water solubility6.84e-02 g/lALOGPS
logP3.5ALOGPS
logP3.84ChemAxon
logS-3.5ALOGPS
pKa (strongest acidic)4.85ChemAxon
physiological charge-1ChemAxon
hydrogen acceptor count2ChemAxon
hydrogen donor count1ChemAxon
polar surface area37.3ChemAxon
rotatable bond count4ChemAxon
refractivity60.73ChemAxon
polarizability23.76ChemAxon
number of rings1ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleYesChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraGC-MSMS/MS1D NMR2D NMR
References
Synthesis Reference

http://en.wikipedia.org/wiki/Ibuprofen#Synthesis

General Reference
  1. Zawada ET Jr: Renal consequences of nonsteroidal antiinflammatory drugs. Postgrad Med. 1982 May;71(5):223-30. Pubmed
  2. Townsend KP, Pratico D: Novel therapeutic opportunities for Alzheimer’s disease: focus on nonsteroidal anti-inflammatory drugs. FASEB J. 2005 Oct;19(12):1592-601. Pubmed
  3. Chen H, Jacobs E, Schwarzschild MA, McCullough ML, Calle EE, Thun MJ, Ascherio A: Nonsteroidal antiinflammatory drug use and the risk for Parkinson’s disease. Ann Neurol. 2005 Dec;58(6):963-7. Pubmed
  4. Geisslinger G, Dietzel K, Bezler H, Nuernberg B, Brune K: Therapeutically relevant differences in the pharmacokinetical and pharmaceutical behavior of ibuprofen lysinate as compared to ibuprofen acid. Int J Clin Pharmacol Ther Toxicol. 1989 Jul;27(7):324-8. Pubmed
  5. Bergner T, Przybilla B: Photosensitization caused by ibuprofen. J Am Acad Dermatol. 1992 Jan;26(1):114-6. Pubmed
  6. Dill J, Patel AR, Yang XL, Bachoo R, Powell CM, Li S: A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons. J Neurosci. 2010 Jan 20;30(3):963-72. doi: 10.1523/JNEUROSCI.5045-09.2010. Pubmed
External Links
ResourceLink
KEGG DrugD00126
KEGG CompoundC01588
PubChem Compound3672
PubChem Substance46507255
ChemSpider3544
ChEBI5855
ChEMBLCHEMBL521
Therapeutic Targets DatabaseDAP000780
PharmGKBPA449957
IUPHAR2713
Guide to Pharmacology2713
HETIBP
Drug Product Database636525
RxListhttp://www.rxlist.com/cgi/generic/ibup.htm
Drugs.comhttp://www.drugs.com/ibuprofen.html
WikipediaIbuprofen
ATC CodesC01EB16G02CC01M01AE01M01AE14M02AA13
AHFS Codes
  • 28:08.04.92
PDB EntriesNot Available
FDA labelshow(1.77 MB)
MSDSshow(73.5 KB)
Interactions
Drug Interactions
Drug
AcebutololRisk of inhibition of renal prostaglandins
AcenocoumarolThe NSAID, ibuprofen, may increase the anticoagulant effect of acenocoumarol.
Acetylsalicylic acidConcomitant therapy of the NSAID, ketoprofen, and acetylsalicylic acid may result in additive adverse/toxic effects (e.g. GI bleeding). The NSAID may also limit the cardioprotective effect of acetylsalicylic acid. Occasional concomitant use may not cause clinically significant problems, but regular, frequent concomitant therapy is not recommended.
AlendronateIncreased risk of gastric toxicity
AnisindioneThe NSAID, ibuprofen, may increase the anticoagulant effect of anisindione.
AtenololRisk of inhibition of renal prostaglandins
Azilsartan medoxomilIncreases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
BetaxololNonsteroidal Anti-Inflammatory Agents such as ibuprofen may diminish the antihypertensive effect of Beta-Blockers such as betaxolol. Monitor for increases in blood pressure if a nonsteroidal anti-inflammatory agent (NSAID) is initiated/dose increased, or decreases in blood pressure if a NSAID is discontinued/dose decreased; this is particularly important if NSAID treatment is for extended periods of time. Ophthalmic beta-blockers are likely of little concern.
BevantololRisk of inhibition of renal prostaglandins
BisoprololRisk of inhibition of renal prostaglandins
BumetanideThe NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, bumetanide.
CarteololRisk of inhibition of renal prostaglandins
CarvedilolRisk of inhibition of renal prostaglandins
ColesevelamBile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
CyclosporineMonitor for nephrotoxicity
DicoumarolThe NSAID, ibuprofen, may increase the anticoagulant effect of dicumarol.
EltrombopagIncreases levels of Ibuprofen via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
EsmololRisk of inhibition of renal prostaglandins
Ethacrynic acidThe NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, ethacrynic acid.
FurosemideThe NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, furosemide.
Ginkgo bilobaAdditive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
HomoharringtonineAvoid combination with ibuprofen and other nonsteroidal anti-inflammatory drugs (NSAIDs) due to the potential enhancement of homoharringtonine associated bleeding-related adverse effects. Specifically it is suggested to avoid this combination in patients with a platelet count of less than 50,000/uL.
LabetalolRisk of inhibition of renal prostaglandins
LithiumThe NSAID, ibuprofen, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
MethotrexateThe NSAID, ibuprofen, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
MetoprololRisk of inhibition of renal prostaglandins
NadololRisk of inhibition of renal prostaglandins
OxprenololRisk of inhibition of renal prostaglandins
PenbutololRisk of inhibition of renal prostaglandins
PindololRisk of inhibition of renal prostaglandins
PractololRisk of inhibition of renal prostaglandins
PralatrexateNSAIDs increase the risk of toxicity due to impairment of renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects or adjust dose of pralatrexate.
PrasugrelCoadministration with NSAIDS used chronically may increase the risk of bleeding.
PropranololRisk of inhibition of renal prostaglandins
SotalolRisk of inhibition of renal prostaglandins
TamoxifenIbuprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Ibuprofen is initiated, discontinued or dose changed.
TolbutamideIbuprofen, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Ibuprofen is initiated, discontinued or dose changed.
TorasemideThe NSAID, ibuprofen, may decrease the diuretic and antihypertensive effect of the loop diuretic, torasemide.
TrandolaprilThe NSAID, Ibuprofen, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Ibuprofen is initiated, discontinued or dose changed.
TreprostinilThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ibuprofen. Monitor for increased bleeding during concomitant thearpy.
TriflusalThe metabolite of triflusal, 2-hydroxy-4-trifluoro-methyl-benzoic acid (HTB), impairs the serum protein binding of ibuprofen to the same extent as acetylsalisylic acid. Thus, the free fraction of glisentide may be increased. A dosage reduction may be required if used in combination.
TrimethoprimThe strong CYP2C9 inhibitor, Ibuprofen, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Ibuprofen is initiated, discontinued or dose changed.
VilazodoneIncreased risk of bleeding with concomitant use of non-steroidal anti-inflammatory drugs with vilazodone.
VoriconazoleIbuprofen, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole if ibuprofen is initiated, discontinued or dose changed.
WarfarinIbuprofen, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. The antiplatelet effect of ibuprofen may also increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if ibuprofen is initiated, discontinued or dose changed.
Food Interactions
  • Avoid alcohol
  • Food delays the time to reach peak plasma concentrations by 30-60 minutes and reduces peak plasma concentrations by 30-50%. Extent of absorption is unaffected.
  • Take with food to reduce gastric irritation.

Targets

1. Prostaglandin G/H synthase 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Prostaglandin G/H synthase 2 P35354 Details

References:

  1. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. Pubmed
  2. Ouellet M, Falgueyret JP, Percival MD: Detergents profoundly affect inhibitor potencies against both cyclo-oxygenase isoforms. Biochem J. 2004 Feb 1;377(Pt 3):675-84. Pubmed
  3. Gallego-Sandin S, Novalbos J, Rosado A, Gisbert JP, Galvez-Mugica MA, Garcia AG, Pajares JM, Abad-Santos F: Effect of ibuprofen on cyclooxygenase and nitric oxide synthase of gastric mucosa: correlation with endoscopic lesions and adverse reactions. Dig Dis Sci. 2004 Sep;49(9):1538-44. Pubmed
  4. Murphey LJ, Williams MK, Sanchez SC, Byrne LM, Csiki I, Oates JA, Johnson DH, Morrow JD: Quantification of the major urinary metabolite of PGE2 by a liquid chromatographic/mass spectrometric assay: determination of cyclooxygenase-specific PGE2 synthesis in healthy humans and those with lung cancer. Anal Biochem. 2004 Nov 15;334(2):266-75. Pubmed
  5. Sanchez-Fidalgo S, Martin-Lacave I, Illanes M, Motilva V: Angiogenesis, cell proliferation and apoptosis in gastric ulcer healing. Effect of a selective cox-2 inhibitor. Eur J Pharmacol. 2004 Nov 28;505(1-3):187-94. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Prostaglandin G/H synthase 1

Kind: protein

Organism: Human

Pharmacological action: yes

Components

Name UniProt ID Details
Prostaglandin G/H synthase 1 P23219 Details

References:

  1. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. Pubmed
  2. Patrignani P: Aspirin insensitive eicosanoid biosynthesis in cardiovascular disease. Thromb Res. 2003 Jun 15;110(5-6):281-6. Pubmed
  3. Gupta K, Kaub CJ, Carey KN, Casillas EG, Selinsky BS, Loll PJ: Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors. Bioorg Med Chem Lett. 2004 Feb 9;14(3):667-71. Pubmed
  4. Martic M, Tatic I, Markovic S, Kujundzic N, Kostrun S: Synthesis, biological activity and molecular modeling studies of novel COX-1 inhibitors. Eur J Med Chem. 2004 Feb;39(2):141-51. Pubmed
  5. Hillarp A: [Acetylsalicylic acid resistance—clinical diagnosis with unclear mechanism] Lakartidningen. 2004 Nov 4;101(45):3504-6, 3508-9. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  8. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  9. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  10. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  11. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  12. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  13. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  14. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  15. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  16. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed
  17. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed

3. Apoptosis regulator Bcl-2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: modulator

Components

Name UniProt ID Details
Apoptosis regulator Bcl-2 P10415 Details

References:

  1. Palayoor ST, J-Aryankalayil M, Makinde AY, Cerna D, Falduto MT, Magnuson SR, Coleman CN: Gene expression profile of coronary artery cells treated with nonsteroidal anti-inflammatory drugs reveals off-target effects. J Cardiovasc Pharmacol. 2012 Jun;59(6):487-99. doi: 10.1097/FJC.0b013e31824ba6b5. Pubmed

4. Thrombomodulin

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: modulator

Components

Name UniProt ID Details
Thrombomodulin P07204 Details

References:

  1. Palayoor ST, J-Aryankalayil M, Makinde AY, Cerna D, Falduto MT, Magnuson SR, Coleman CN: Gene expression profile of coronary artery cells treated with nonsteroidal anti-inflammatory drugs reveals off-target effects. J Cardiovasc Pharmacol. 2012 Jun;59(6):487-99. doi: 10.1097/FJC.0b013e31824ba6b5. Pubmed

5. Tissue-type plasminogen activator

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: negative modulator

Components

Name UniProt ID Details
Tissue-type plasminogen activator P00750 Details

References:

  1. Palayoor ST, J-Aryankalayil M, Makinde AY, Cerna D, Falduto MT, Magnuson SR, Coleman CN: Gene expression profile of coronary artery cells treated with nonsteroidal anti-inflammatory drugs reveals off-target effects. J Cardiovasc Pharmacol. 2012 Jun;59(6):487-99. doi: 10.1097/FJC.0b013e31824ba6b5. Pubmed

6. Fatty acid-binding protein, intestinal

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Fatty acid-binding protein, intestinal P12104 Details

References:

  1. Velkov T, Chuang S, Wielens J, Sakellaris H, Charman WN, Porter CJ, Scanlon MJ: The interaction of lipophilic drugs with intestinal fatty acid-binding protein. J Biol Chem. 2005 May 6;280(18):17769-76. Epub 2005 Feb 18. Pubmed

7. Peroxisome proliferator-activated receptor gamma

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: activator

Components

Name UniProt ID Details
Peroxisome proliferator-activated receptor gamma P37231 Details

References:

  1. Dill J, Patel AR, Yang XL, Bachoo R, Powell CM, Li S: A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons. J Neurosci. 2010 Jan 20;30(3):963-72. doi: 10.1523/JNEUROSCI.5045-09.2010. Pubmed

8. Cystic fibrosis transmembrane conductance regulator

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cystic fibrosis transmembrane conductance regulator P13569 Details

References:

  1. Devor DC, Schultz BD: Ibuprofen inhibits cystic fibrosis transmembrane conductance regulator-mediated Cl- secretion. J Clin Invest. 1998 Aug 15;102(4):679-87. Pubmed

Enzymes

1. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Mo SL, Zhou ZW, Yang LP, Wei MQ, Zhou SF: New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126. Pubmed
  2. 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
  3. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  4. 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. Carlile DJ, Hakooz N, Bayliss MK, Houston JB: Microsomal prediction of in vivo clearance of CYP2C9 substrates in humans. Br J Clin Pharmacol. 1999 Jun;47(6):625-35. Pubmed

2. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  2. Yu L, Shi D, Ma L, Zhou Q, Zeng S: Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. Biopharm Drug Dispos. 2013 Jul;34(5):278-87. doi: 10.1002/bdd.1842. Epub 2013 Jun 3. Pubmed

3. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

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

4. UDP-glucuronosyltransferase 1-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-1 P22309 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

5. UDP-glucuronosyltransferase 1-3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-3 P35503 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

6. UDP-glucuronosyltransferase 1-9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-9 O60656 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

7. UDP-glucuronosyltransferase 2B4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 2B4 P06133 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

8. UDP-glucuronosyltransferase 2B7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 2B7 P16662 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

9. Prostaglandin G/H synthase 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Prostaglandin G/H synthase 1 P23219 Details

References:

  1. Palayoor ST, J-Aryankalayil M, Makinde AY, Cerna D, Falduto MT, Magnuson SR, Coleman CN: Gene expression profile of coronary artery cells treated with nonsteroidal anti-inflammatory drugs reveals off-target effects. J Cardiovasc Pharmacol. 2012 Jun;59(6):487-99. doi: 10.1097/FJC.0b013e31824ba6b5. Pubmed

10. Prostaglandin G/H synthase 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Prostaglandin G/H synthase 2 P35354 Details

References:

  1. Palayoor ST, J-Aryankalayil M, Makinde AY, Cerna D, Falduto MT, Magnuson SR, Coleman CN: Gene expression profile of coronary artery cells treated with nonsteroidal anti-inflammatory drugs reveals off-target effects. J Cardiovasc Pharmacol. 2012 Jun;59(6):487-99. doi: 10.1097/FJC.0b013e31824ba6b5. Pubmed

Carriers

1. Serum albumin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. Yamasaki K, Rahman MH, Tsutsumi Y, Maruyama T, Ahmed S, Kragh-Hansen U, Otagiri M: Circular dichroism simulation shows a site-II-to-site-I displacement of human serum albumin-bound diclofenac by ibuprofen. AAPS PharmSciTech. 2000 May 14;1(2):E12. Pubmed
  2. Galantini L, Leggio C, Konarev PV, Pavel NV: Human serum albumin binding ibuprofen: a 3D description of the unfolding pathway in urea. Biophys Chem. 2010 Apr;147(3):111-22. doi: 10.1016/j.bpc.2010.01.002. Epub 2010 Jan 18. Pubmed

Transporters

1. Solute carrier organic anion transporter family member 2B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

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

References:

  1. Satoh H, Yamashita F, Tsujimoto M, Murakami H, Koyabu N, Ohtani H, Sawada Y: Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos. 2005 Apr;33(4):518-23. Epub 2005 Jan 7. Pubmed

2. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. Pubmed

3. Multidrug resistance-associated protein 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 4 O15439 Details

References:

  1. Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. Pubmed

4. 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. Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. Pubmed

5. 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. 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

6. Solute carrier family 22 member 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

References:

  1. Mulato AS, Ho ES, Cihlar T: Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1. J Pharmacol Exp Ther. 2000 Oct;295(1):10-5. Pubmed
  2. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
  3. Uwai Y, Saito H, Inui K: Interaction between methotrexate and nonsteroidal anti-inflammatory drugs in organic anion transporter. Eur J Pharmacol. 2000 Dec 1;409(1):31-6. Pubmed
  4. Apiwattanakul N, Sekine T, Chairoungdua A, Kanai Y, Nakajima N, Sophasan S, Endou H: Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. Mol Pharmacol. 1999 May;55(5):847-54. Pubmed

7. Solute carrier family 22 member 8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

References:

  1. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. Pubmed
  2. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
  3. Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. Pubmed

8. Solute carrier family 22 member 11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
  2. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. Pubmed

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