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Identification
NameDiclofenac
Accession NumberDB00586  (APRD00527)
TypeSmall Molecule
GroupsApproved
Description

A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
[2-(2,6-Dichloroanilino)phenyl]acetic acidNot AvailableNot Available
2-((2,6-Dichlorophenyl)amino)benzeneacetic acidNot AvailableNot Available
DiclofenacNot AvailableNot Available
Diclofenac AcidNot AvailableNot Available
DiclofenacoNot AvailableNot Available
DiclofenacumNot AvailableNot Available
ISV-205Not AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cataflamtablet, sugar coated50 mgoralNovartis Pharmaceuticals Corporation1993-11-24Not AvailableUs
Voltarensolution1 mg/mLophthalmicNovartis Pharmaceutical Corporation1991-03-28Not AvailableUs
Diclofenac Sodiumgel30 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2013-05-06Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralSandoz Inc1996-03-08Not AvailableUs
Solarazegel30 mg/gtopicalPharma Derm, A Division Of Fougera Pharmaceuticals Inc.2000-10-16Not AvailableUs
Zipsorcapsule, liquid filled25 mgoralDepomed, Inc.2009-06-16Not AvailableUs
Cambiapowder, for solution50 mgoralDepomed, Inc.2010-04-20Not AvailableUs
Pennsaidliquid16.05 mg/mLtopicalSTAT Rx USA LLC2010-04-05Not AvailableUs
Voltarengel10 mg/gtopicalSTAT Rx USA LLC2007-10-17Not AvailableUs
Flectorpatch180 mgtopicalRebel Distributors Corp2008-11-17Not AvailableUs
Voltarengel10 mg/gtopicalRebel Distributors Corp2007-10-17Not AvailableUs
Pennsaidliquid16.05 mg/mLtopicalMallinckrodt, Inc2010-04-05Not AvailableUs
Pennsaidsolution20 mg/gtopicalMallinckrodt, Inc2012-04-27Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralRx Change Co.2014-11-26Not AvailableUs
Flectorpatch180 mg/14gtopicalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-11Not AvailableUs
Voltarengel10 mg/gtopicalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-11Not AvailableUs
Zipsorcapsule, liquid filled25 mgoralLake Erie Medical DBA Quality Care Products2010-12-22Not AvailableUs
Pennsaidliquid16.05 mg/mLtopicalLake Erie Medical DBA Quality Care Products LLC2010-04-05Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralLake Erie Medical DBA Quality Care Products LLC1996-03-08Not AvailableUs
Zorvolexcapsule18 mgoralIroko Pharmaceuticals LLC2013-10-31Not AvailableUs
Zorvolexcapsule35 mgoralIroko Pharmaceuticals LLC2013-10-31Not AvailableUs
Flectorpatch180 mgtopicalRebel Distributors Corp2008-01-14Not AvailableUs
Flectorpatch180 mgtopicalSTAT Rx USA LLC2008-06-08Not AvailableUs
Voltarengel10 mg/gtopicalSTAT Rx USA LLC2007-10-17Not AvailableUs
Zipsorcapsule, liquid filled25 mgoralPd Rx Pharmaceuticals, Inc.2010-04-30Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPd Rx Pharmaceuticals, Inc.1996-03-08Not AvailableUs
Cambiapowder, for solution1 mg/mgoralNautilus Neurosciences, Inc.2010-04-20Not AvailableUs
Pennsaidliquid16.05 mg/mLtopicalUnit Dose Services2010-04-05Not AvailableUs
Flectorpatch180 mgtopicalUnit Dose Services2008-01-14Not AvailableUs
Voltarengel10 mg/gtopicalUnit Dose Services2007-10-17Not AvailableUs
Voltarengel10 mg/gtopicalREMEDYREPACK INC.2014-06-16Not AvailableUs
Flectorpatch180 mgtopicalH.J. Harkins Company, Inc.2008-01-14Not AvailableUs
Voltarengel10 mg/gtopicalPhysicians Total Care, Inc.2008-11-21Not AvailableUs
Voltarengel10 mg/gtopicalClinical Solutions Wholesale2007-10-17Not AvailableUs
Flectorpatch180 mgtopicalKing Pharmaceuticals, Inc.2008-01-14Not AvailableUs
Flectorpatch180 mgtopicalREMEDYREPACK INC.2014-09-11Not AvailableUs
Voltarengel10 mg/gtopicalDIRECT RX2014-01-01Not AvailableUs
Voltarengel10 mg/gtopicalEndo Pharmaceuticals, Inc.2007-10-17Not AvailableUs
Flectorpatch180 mgtopicalbryant ranch prepack2008-01-14Not AvailableUs
Voltarengel10 mg/gtopicalbryant ranch prepack2007-10-17Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralbryant ranch prepack1996-03-08Not AvailableUs
Zipsorcapsule, liquid filled25 mgoralXanodyne Pharmaceuticals, Inc.2010-04-302015-02-28Us
Voltarengel10 mg/gtopicalKeltman Pharmaceuticals Inc.2011-01-27Not AvailableUs
Voltarengel10 mg/gtopicalPreferred Pharmaceuticals, Inc.2014-10-08Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPreferred Pharmaceuticals, Inc.2014-07-17Not AvailableUs
Pennsaidsolution20 mg/gtopicalHorizon Pharma Inc.2015-01-01Not AvailableUs
Cambiapowder for solution50 mgoralTribute Pharmaceuticals Canada IncNot AvailableNot AvailableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Diclofenac Potassiumtablet, film coated50 mgoralTeva Pharmaceuticals USA Inc1998-08-11Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralTEVA Pharmaceuticals USA Inc.2000-02-28Not AvailableUs
Diclofenac Sodiumgel30 mg/gtopicalGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2013-11-21Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralActavis Elizabeth LLC1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralActavis Elizabeth LLC1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralActavis Elizabeth LLC2002-01-09Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralMylan Pharmaceuticals Inc.2002-02-15Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralMylan Pharmaceuticals Inc.2012-08-13Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralMylan Pharmaceuticals Inc.2010-05-18Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralMylan Pharmaceuticals Inc.2010-05-18Not AvailableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalPaddock Laboratories, LLC2014-11-24Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralWatson Laboratories, Inc.2002-11-06Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralSandoz Inc1995-09-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralSandoz Inc1995-09-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralSandoz Inc1995-11-30Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralSandoz Inc1998-11-20Not AvailableUs
Diclofenac Potassiumtablet50 mgoralApotheca, Inc2007-08-20Not AvailableUs
Diclofenac Sodiumsolution/ drops3.5 mg/mLophthalmicPACK Pharmaceuticals, LLC2008-06-20Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralPACK Pharmaceuticals, LLC2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPACK Pharmaceuticals, LLC2010-12-31Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralPACK Pharmaceuticals, LLC2010-12-31Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralStat Rx USA2004-03-18Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralStat Rx USA1995-09-28Not AvailableUs
Diclofenacsolution/ drops1 mg/mLophthalmicAkorn, Inc.2008-05-01Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralRebel Distributors Corp1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralRebel Distributors Corp1996-03-26Not AvailableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicRebel Distributors Corp2007-12-28Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralRebel Distributors Corp2010-01-21Not AvailableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicBausch & Lomb Incorporated2007-12-28Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralAidarex Pharmaceuticals LLC1998-08-11Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralLake Erie Medical DBA Quality Care Products LLC1998-08-11Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralLake Erie Medical DBA Quality Care Products LLC2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralLake Erie Medical DBA Quality Care Products LLC2010-12-31Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralLake Erie Medical DBA Quality Care Products LLC2002-01-09Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralRebel Distributors Corp2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralAv Kare, Inc.1998-11-13Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralAv Kare, Inc.1998-11-13Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralSTAT Rx USA LLC2010-03-05Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralSTAT Rx USA LLC2010-03-05Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPd Rx Pharmaceuticals, Inc.2010-01-27Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPd Rx Pharmaceuticals, Inc.1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralAphena Pharma Solutions Tennessee, Inc.1998-11-13Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralREMEDYREPACK INC.2011-06-02Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralREMEDYREPACK INC.2012-03-02Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralREMEDYREPACK INC.2012-03-27Not AvailableUs
Diclofenac Sodiumtablet, extended release100 mgoralREMEDYREPACK INC.2012-03-28Not AvailableUs
Diclofenac Potassiumtablet50 mgoralREMEDYREPACK INC.2012-03-30Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-05Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralUnit Dose Services1995-09-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralUnit Dose Services2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralMylan Institutional Inc.2010-06-04Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralMylan Institutional Inc.2010-06-04Not AvailableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalTaro Pharmaceuticals U.S.A., Inc.2014-11-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralH.J. Harkins Company, Inc.2008-08-19Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralH.J. Harkins Company, Inc.2010-01-21Not AvailableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicH.J. Harkins Company, Inc.2007-12-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPhysicians Total Care, Inc.1995-11-16Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralPhysicians Total Care, Inc.1997-02-10Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralPhysicians Total Care, Inc.2004-05-21Not AvailableUs
Diclofenac Sodiumtablet, extended release100 mgoralPhysicians Total Care, Inc.2004-03-02Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralPhysicians Total Care, Inc.2008-10-15Not AvailableUs
Flectorpatch180 mgtopicalPhysicians Total Care, Inc.2008-11-17Not AvailableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicPhysicians Total Care, Inc.2011-07-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralCardinal Health1995-11-30Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralPd Rx Pharmaceuticals, Inc.1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPd Rx Pharmaceuticals, Inc.1995-09-28Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralPd Rx Pharmaceuticals, Inc.1998-11-20Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralClinical Solutions Wholesale2010-12-31Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralClinical Solutions Wholesale2010-12-31Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralClinical Solutions Wholesale1998-11-20Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralApotex Corp2006-03-20Not AvailableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalApotex Corp.2014-05-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralSt Marys Medical Park Pharmacy2014-04-21Not AvailableUs
Diclofenac Sodiumsolution1 mg/mLophthalmicSandoz Inc2008-02-14Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralDIRECT RX2014-01-01Not AvailableUs
Flectorpatch180 mgtopicalDIRECT RX2014-01-01Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralDIRECT RX2014-01-01Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralProficient Rx LP2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralProficient Rx LP1996-03-08Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralbryant ranch prepack1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, extended release100 mgoralbryant ranch prepack2004-03-02Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralbryant ranch prepack2010-01-21Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-07-01Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralDispensing Solutions, Inc.1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralDispensing Solutions, Inc.2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralAphena Pharma Solutions Tennessee, Inc.1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralAphena Pharma Solutions Tennessee, Inc.1996-03-26Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralBlue Point Laboratories2014-02-24Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralBlue Point Laboratories2014-02-24Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralBlue Point Laboratories2014-02-24Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralAmerican Health Packaging2009-04-02Not AvailableUs
Diclofenac Potassiumtablet, film coated50 mgoralCarilion Materials Management1998-08-11Not AvailableUs
Diclofenac Sodiumtablet, delayed release25 mgoralCarilion Materials Management1995-09-28Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralKeltman Pharmaceuticals Inc.2009-07-01Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPreferred Pharmaceuticals, Inc.2010-12-31Not AvailableUs
Diclofenac Sodiumtablet, delayed release50 mgoralPreferred Pharmaceuticals, Inc.2010-05-18Not AvailableUs
Diclofenac Sodiumtablet, delayed release75 mgoralPreferred Pharmaceuticals, Inc.2008-08-19Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPreferred Pharmaceuticals, Inc.2014-06-02Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPreferred Pharmaceuticals, Inc.2014-02-03Not AvailableUs
Diclofenac Sodiumtablet, film coated, extended release100 mgoralPreferred Pharmaceuticals, Inc.2012-06-04Not AvailableUs
Over the Counter ProductsNot Available
International Brands
NameCompany
AclonacNot Available
AllvoranNot Available
DylojectHospira
EcofenacNot Available
EffektonNot Available
Nu-DicloNot Available
PrimofenacNot Available
ProphenatinNot Available
RhumalganNot Available
Voltaren EmulgelNot Available
VoltarolNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Diclofenac potassium
ThumbNot applicableDBSALT000864
Diclofenac sodium
15307-79-6
Thumb
  • InChI Key: KPHWPUGNDIVLNH-UHFFFAOYSA-M
  • Monoisotopic Mass: 316.998628658
  • Average Mass: 318.13
DBSALT000466
Categories
CAS number15307-86-5
WeightAverage: 296.149
Monoisotopic: 295.016684015
Chemical FormulaC14H11Cl2NO2
InChI KeyDCOPUUMXTXDBNB-UHFFFAOYSA-N
InChI
InChI=1S/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19)
IUPAC Name
2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
SMILES
OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetic acid derivatives. These are compounds containing a phenylacetic acid moiety, which consists of a phenyl group substituted at the second position by an acetic acid.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetic acid derivatives
Direct ParentPhenylacetic acid derivatives
Alternative Parents
Substituents
  • Phenylacetate
  • Substituted aniline
  • 1,3-dichlorobenzene
  • Halobenzene
  • Chlorobenzene
  • Aniline
  • Aryl halide
  • Aryl chloride
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
PharmacodynamicsDiclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis
Mechanism of actionThe antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.
AbsorptionCompletely absorbed from the gastrointestinal tract.
Volume of distribution
  • 1.3 L/kg
Protein bindingMore than 99%
Metabolism

Hepatic

SubstrateEnzymesProduct
Diclofenac
4'-HydroxydiclofenacDetails
Diclofenac
Diclofenac acyl glucuronideDetails
Diclofenac
3'-HydroxydiclofenacDetails
Diclofenac
5-HydroxydiclofenacDetails
4'-Hydroxydiclofenac
Not Available
4',5-DihydroxydiclofenacDetails
5-Hydroxydiclofenac
Not Available
4',5-DihydroxydiclofenacDetails
Route of eliminationDiclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites.
Half life2 hours
Clearance
  • oral cl=622 mL/min [healthy]
  • renal cl <1 mL/min [healthy]
ToxicitySymptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD50=390mg/kg (orally in mice)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Diclofenac Action PathwayDrug actionSMP00093
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9548
Blood Brain Barrier+0.9541
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.7976
P-glycoprotein inhibitor INon-inhibitor0.8254
P-glycoprotein inhibitor IINon-inhibitor0.9548
Renal organic cation transporterNon-inhibitor0.9086
CYP450 2C9 substrateNon-substrate0.7779
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6724
CYP450 1A2 substrateInhibitor0.5923
CYP450 2C9 substrateInhibitor0.6786
CYP450 2D6 substrateNon-inhibitor0.848
CYP450 2C19 substrateNon-inhibitor0.8947
CYP450 3A4 substrateNon-inhibitor0.8647
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6607
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.6706
BiodegradationNot ready biodegradable0.9719
Rat acute toxicity3.6447 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9514
hERG inhibition (predictor II)Non-inhibitor0.868
Pharmacoeconomics
Manufacturers
  • Institut biochemique sa
  • Xanodyne pharmaceutics inc
  • Nautilus neurosciences inc
  • Novartis pharmaceuticals corp
  • Apotex inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Nycomed us inc
  • Novartis consumer health inc
  • Akorn inc
  • Alcon inc
  • Apotex inc richmond hill
  • Bausch and lomb inc
  • Falcon pharmaceuticals ltd
  • Nexus pharmaceuticals inc
  • Mallinckrodt inc
  • Actavis elizabeth llc
  • Alphapharm party ltd
  • Carlsbad technology inc
  • Nostrum laboratories inc
  • Pliva inc
  • Roxane laboratories inc
  • Teva pharmaceuticals usa
  • Unique pharmaceutical laboratories
  • Biovail laboratories inc
  • Dexcel ltd
Packagers
Dosage forms
FormRouteStrength
Capsuleoral18 mg
Capsuleoral35 mg
Capsule, liquid filledoral25 mg
Geltopical10 mg/g
Geltopical30 mg/g
Liquidtopical16.05 mg/mL
Patchtopical180 mg
Patchtopical180 mg/14g
Powder for solutionoral50 mg
Powder, for solutionoral1 mg/mg
Powder, for solutionoral50 mg
Solutionophthalmic1 mg/mL
Solutiontopical16.05 mg/mL
Solutiontopical20 mg/g
Solution/ dropsophthalmic1 mg/mL
Solution/ dropsophthalmic3.5 mg/mL
Tabletoral50 mg
Tablet, delayed releaseoral25 mg
Tablet, delayed releaseoral50 mg
Tablet, delayed releaseoral75 mg
Tablet, extended releaseoral100 mg
Tablet, film coatedoral50 mg
Tablet, film coated, extended releaseoral100 mg
Tablet, sugar coatedoral50 mg
Prices
Unit descriptionCostUnit
Voltaren Ophtha 0.1 % Solution2.73USD ml
Voltaren 100 mg Suppository1.88USD suppository
Voltaren Sr 100 mg Sustained-Release Tablet1.86USD tablet
Voltaren 50 mg Suppository1.4USD suppository
Voltaren Sr 75 mg Sustained-Release Tablet1.31USD tablet
Voltaren 50 mg Enteric-Coated Tablet0.93USD tablet
Pms-Diclofenac 100 mg Suppository0.88USD suppository
Sandoz Diclofenac 100 mg Suppository0.88USD suppository
Novo-Difenac Sr 100 mg Sustained-Release Tablet0.8USD tablet
Pms-Diclofenac-Sr 100 mg Sustained-Release Tablet0.8USD tablet
Sandoz Diclofenac Sr 100 mg Sustained-Release Tablet0.8USD tablet
Pms-Diclofenac 50 mg Suppository0.65USD suppository
Sandoz Diclofenac 50 mg Suppository0.65USD suppository
Novo-Difenac Sr 75 mg Sustained-Release Tablet0.6USD tablet
Pms-Diclofenac-Sr 75 mg Sustained-Release Tablet0.6USD tablet
Sandoz Diclofenac Sr 75 mg Sustained-Release Tablet0.6USD tablet
Apo-Diclo 50 mg Enteric-Coated Tablet0.4USD tablet
Novo-Difenac 50 mg Enteric-Coated Tablet0.4USD tablet
Pms-Diclofenac 50 mg Enteric-Coated Tablet0.4USD tablet
Sandoz Diclofenac 50 mg Enteric-Coated Tablet0.4USD tablet
Apo-Diclo 25 mg Enteric-Coated Tablet0.2USD tablet
Novo-Difenac 25 mg Enteric-Coated Tablet0.2USD tablet
Nu-Diclo 25 mg Enteric-Coated Tablet0.2USD tablet
Pms-Diclofenac 25 mg Enteric-Coated Tablet0.2USD tablet
Sandoz Diclofenac 25 mg Enteric-Coated Tablet0.2USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States56076901994-04-132014-04-13
United States76628582009-02-242029-02-24
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point283-285 °CNot Available
water solubility2.37 mg/L (at 25 °C)FINI,A ET AL. (1986)
logP4.51AVDEEF,A (1997)
pKa4.15SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.00447 mg/mLALOGPS
logP4.98ALOGPS
logP4.26ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)4ChemAxon
pKa (Strongest Basic)-2.1ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area49.33 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity75.46 m3·mol-1ChemAxon
Polarizability27.93 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraMS
References
Synthesis Reference

Takuzo Kamishita, “Gel preparations for topical application of diclofenac sodium.” U.S. Patent US4670254, issued October, 1983.

US4670254
General Reference
  1. Kearney PM, Baigent C, Godwin J, Halls H, Emberson JR, Patrono C: Do selective cyclo-oxygenase-2 inhibitors and traditional non-steroidal anti-inflammatory drugs increase the risk of atherothrombosis? Meta-analysis of randomised trials. BMJ. 2006 Jun 3;332(7553):1302-8. Pubmed
  2. Solomon DH, Avorn J, Sturmer T, Glynn RJ, Mogun H, Schneeweiss S: Cardiovascular outcomes in new users of coxibs and nonsteroidal antiinflammatory drugs: high-risk subgroups and time course of risk. Arthritis Rheum. 2006 May;54(5):1378-89. Pubmed
  3. FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med. 2001 Aug 9;345(6):433-42. Pubmed
  4. Graham DJ: COX-2 inhibitors, other NSAIDs, and cardiovascular risk: the seduction of common sense. JAMA. 2006 Oct 4;296(13):1653-6. Epub 2006 Sep 12. Pubmed
  5. Brater DC: Renal effects of cyclooxygyenase-2-selective inhibitors. J Pain Symptom Manage. 2002 Apr;23(4 Suppl):S15-20; discussion S21-3. Pubmed
  6. Sigma Aldrich Link
  7. Gan TJ: Diclofenac: an update on its mechanism of action and safety profile. Curr Med Res Opin. 2010 Jul;26(7):1715-31. Pubmed
External Links
ATC CodesD11AX18M01AB05M02AA15S01BC03
AHFS Codes
  • 28:08.04.08
  • 28:08.04.92
PDB EntriesNot Available
FDA labelDownload (37.5 KB)
MSDSDownload (73.6 KB)
Interactions
Drug Interactions
Drug
AlendronateIncreased risk of gastric toxicity
AnisindioneThe NSAID, diclofenac, may increase the anticoagulant effect of anisindione.
Azilsartan medoxomilIncreases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
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, diclofenac, may increase the anticoagulant effect of dicumarol.
DifluprednateNSAIDs may slow healing.
EltrombopagEltrombopag increases levels of Diclofenac via metabolism decrease. UDP-glucuronosyltransferase inhibition.
Ginkgo bilobaAdditive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
LithiumThe NSAID, diclofenac, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
MethotrexateThe NSAID, diclofenac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
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.
RifampicinRifampin, a CYP2C9 inducer, may increase the metabolism of diclofenac.
TacrineThe metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Diclofenac, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Diclofenac is initiated, discontinued or if the dose is changed.
TelmisartanConcomitant use of Telmisartan and Diclofenac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
TimololThe NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol.
TizanidineDiclofenac may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
TrandolaprilThe NSAID, Diclofenac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Diclofenac is initiated, discontinued or dose changed.
TreprostinilThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
VilazodoneIncreased risk of bleeding with concomitant use of NSAIDs with vilazodone.
VoriconazoleVoriconazole, a strong CYP2C9 inhibitor, may increase the serum concentration of diclofenac by decreasing its metabolism. Renal impairment may increase the risk of diclofenac adverse effects. Monitor for changes in therapeutic and adverse effects of diclofenac if voriconazole is initiated, discontinued or dose changed.
WarfarinThe antiplatelet effects of oral diclofenac may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce 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. Kirchheiner J, Meineke I, Steinbach N, Meisel C, Roots I, Brockmoller J: Pharmacokinetics of diclofenac and inhibition of cyclooxygenases 1 and 2: no relationship to the CYP2C9 genetic polymorphism in humans. Br J Clin Pharmacol. 2003 Jan;55(1):51-61. Pubmed
  2. Blomme EA, Chinn KS, Hardy MM, Casler JJ, Kim SH, Opsahl AC, Hall WA, Trajkovic D, Khan KN, Tripp CS: Selective cyclooxygenase-2 inhibition does not affect the healing of cutaneous full-thickness incisional wounds in SKH-1 mice. Br J Dermatol. 2003 Feb;148(2):211-23. Pubmed
  3. Beubler E: [Pharmacology of cyclooxygenase 2 inhibition] Wien Med Wochenschr. 2003;153(5-6):95-9. Pubmed
  4. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. Pubmed
  5. Rowlinson SW, Kiefer JR, Prusakiewicz JJ, Pawlitz JL, Kozak KR, Kalgutkar AS, Stallings WC, Kurumbail RG, Marnett LJ: A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385. J Biol Chem. 2003 Nov 14;278(46):45763-9. Epub 2003 Aug 18. Pubmed

2. Prostaglandin G/H synthase 1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

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

References:

  1. Calkin AC, Sudhir K, Honisett S, Williams MR, Dawood T, Komesaroff PA: Rapid potentiation of endothelium-dependent vasodilation by estradiol in postmenopausal women is mediated via cyclooxygenase 2. J Clin Endocrinol Metab. 2002 Nov;87(11):5072-5. Pubmed
  2. Kirchheiner J, Meineke I, Steinbach N, Meisel C, Roots I, Brockmoller J: Pharmacokinetics of diclofenac and inhibition of cyclooxygenases 1 and 2: no relationship to the CYP2C9 genetic polymorphism in humans. Br J Clin Pharmacol. 2003 Jan;55(1):51-61. Pubmed
  3. Kampfer H, Brautigam L, Geisslinger G, Pfeilschifter J, Frank S: Cyclooxygenase-1-coupled prostaglandin biosynthesis constitutes an essential prerequisite for skin repair. J Invest Dermatol. 2003 May;120(5):880-90. Pubmed
  4. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. Pubmed
  5. Hinz B, Rau T, Auge D, Werner U, Ramer R, Rietbrock S, Brune K: Aceclofenac spares cyclooxygenase 1 as a result of limited but sustained biotransformation to diclofenac. Clin Pharmacol Ther. 2003 Sep;74(3):222-35. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

3. Arachidonate 5-lipoxygenase

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Arachidonate 5-lipoxygenase P09917 Details

References:

  1. Charlier C, Michaux C: Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) as a new strategy to provide safer non-steroidal anti-inflammatory drugs. Eur J Med Chem. 2003 Jul-Aug;38(7-8):645-59. Pubmed
  2. Kudo C, Kori M, Matsuzaki K, Yamai K, Nakajima A, Shibuya A, Niwa H, Kamisaki Y, Wada K: Diclofenac inhibits proliferation and differentiation of neural stem cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. Pubmed
  3. Whittle BJ: Cyclooxygenase and nitric oxide systems in the gut as therapeutic targets for safer anti-inflammatory drugs. Curr Opin Pharmacol. 2004 Dec;4(6):538-45. Pubmed

4. Sodium channel protein type 4 subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Sodium channel protein type 4 subunit alpha P35499 Details

References:

  1. Yang YC, Kuo CC: An inactivation stabilizer of the Na+ channel acts as an opportunistic pore blocker modulated by external Na+. J Gen Physiol. 2005 May;125(5):465-81. Epub 2005 Apr 11. Pubmed
  2. Voilley N: Acid-sensing ion channels (ASICs): new targets for the analgesic effects of non-steroid anti-inflammatory drugs (NSAIDs). Curr Drug Targets Inflamm Allergy. 2004 Mar;3(1):71-9. Pubmed
  3. Jones NG, Slater R, Cadiou H, McNaughton P, McMahon SB: Acid-induced pain and its modulation in humans. J Neurosci. 2004 Dec 1;24(48):10974-9. Pubmed

5. Acid-sensing ion channel 1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Acid-sensing ion channel 1 P78348 Details

References:

  1. Voilley N, de Weille J, Mamet J, Lazdunski M: Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors. J Neurosci. 2001 Oct 15;21(20):8026-33. Pubmed

6. Potassium voltage-gated channel subfamily KQT member 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: other

Components

Name UniProt ID Details
Potassium voltage-gated channel subfamily KQT member 2 O43526 Details

References:

  1. Peretz A, Degani N, Nachman R, Uziyel Y, Gibor G, Shabat D, Attali B: Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties. Mol Pharmacol. 2005 Apr;67(4):1053-66. Epub 2004 Dec 14. Pubmed
  2. Xiong Q, Gao Z, Wang W, Li M: Activation of Kv7 (KCNQ) voltage-gated potassium channels by synthetic compounds. Trends Pharmacol Sci. 2008 Feb;29(2):99-107. Epub 2008 Jan 18. Pubmed

7. Potassium voltage-gated channel subfamily KQT member 3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: other

Components

Name UniProt ID Details
Potassium voltage-gated channel subfamily KQT member 3 O43525 Details

References:

  1. Xiong Q, Gao Z, Wang W, Li M: Activation of Kv7 (KCNQ) voltage-gated potassium channels by synthetic compounds. Trends Pharmacol Sci. 2008 Feb;29(2):99-107. Epub 2008 Jan 18. Pubmed
  2. Peretz A, Degani N, Nachman R, Uziyel Y, Gibor G, Shabat D, Attali B: Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties. Mol Pharmacol. 2005 Apr;67(4):1053-66. Epub 2004 Dec 14. Pubmed

8. Phospholipase A2, membrane associated

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Phospholipase A2, membrane associated P14555 Details

References:

  1. Madanick RD, O’Loughlin CJ, Barkin JS: Diclofenac reduces the incidence of acute pancreatitis after endoscopic retrograde cholangiopancreatography. Dig Dis Sci. 2005 May;50(5):879-81. Pubmed
  2. Singh N, Jabeen T, Sharma S, Somvanshi RK, Dey S, Srinivasan A, Singh TP: Specific binding of non-steroidal anti-inflammatory drugs (NSAIDs) to phospholipase A2: structure of the complex formed between phospholipase A2 and diclofenac at 2.7 A resolution. Acta Crystallogr D Biol Crystallogr. 2006 Apr;62(Pt 4):410-6. Epub 2006 Mar 18. Pubmed
  3. Makela A, Kuusi T, Schroder T: Inhibition of serum phospholipase-A2 in acute pancreatitis by pharmacological agents in vitro. Scand J Clin Lab Invest. 1997 Aug;57(5):401-7. 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. Obach RS, Reed-Hagen AE: Measurement of Michaelis constants for cytochrome P450-mediated biotransformation reactions using a substrate depletion approach. Drug Metab Dispos. 2002 Jul;30(7):831-7. Pubmed
  6. Leemann T, Transon C, Dayer P: Cytochrome P450TB (CYP2C): a major monooxygenase catalyzing diclofenac 4’-hydroxylation in human liver. Life Sci. 1993;52(1):29-34. Pubmed

2. 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

3. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

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

4. 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

5. 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

6. 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

7. Prostaglandin G/H synthase 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Prostaglandin G/H synthase 1 P23219 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. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 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 2C18

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C18 P33260 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

12. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

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

Carriers

1. Transthyretin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Transthyretin P02766 Details

References:

  1. Miller SR, Sekijima Y, Kelly JW: Native state stabilization by NSAIDs inhibits transthyretin amyloidogenesis from the most common familial disease variants. Lab Invest. 2004 May;84(5):545-52. Pubmed
  2. Almeida MR, Macedo B, Cardoso I, Alves I, Valencia G, Arsequell G, Planas A, Saraiva MJ: Selective binding to transthyretin and tetramer stabilization in serum from patients with familial amyloidotic polyneuropathy by an iodinated diflunisal derivative. Biochem J. 2004 Jul 15;381(Pt 2):351-6. Pubmed

2. 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

Transporters

1. 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

2. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Wang E, Lew K, Barecki M, Casciano CN, Clement RP, Johnson WW: Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. Chem Res Toxicol. 2001 Dec;14(12):1596-603. 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. 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. 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. Kuze K, Graves P, Leahy A, Wilson P, Stuhlmann H, You G: Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells. J Biol Chem. 1999 Jan 15;274(3):1519-24. Pubmed
  3. 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

5. 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

6. Solute carrier organic anion transporter family member 1C1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1C1 Q9NYB5 Details

References:

  1. Westholm DE, Stenehjem DD, Rumbley JN, Drewes LR, Anderson GW: Competitive inhibition of organic anion transporting polypeptide 1c1-mediated thyroxine transport by the fenamate class of nonsteroidal antiinflammatory drugs. Endocrinology. 2009 Feb;150(2):1025-32. Epub 2008 Oct 9. Pubmed
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed

7. 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. 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 17:11