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Identification
NameDiclofenac
Accession NumberDB00586  (APRD00527)
TypeSmall Molecule
GroupsApproved, Vet Approved
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
[2-(2,6-Dichloroanilino)phenyl]acetic acid
2-((2,6-Dichlorophenyl)amino)benzeneacetic acid
Diclofenac
Diclofenac Acid
Diclofenaco
Diclofenacum
ISV-205
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-diclofenactablet (enteric-coated)50 mgoralAvanstra Inc2011-08-182014-08-21Canada
Ava-diclofenactablet (enteric-coated)25 mgoralAvanstra Inc2011-08-182014-08-21Canada
Ava-diclofenac SRtablet (extended-release)100 mgoralAvanstra Inc2011-09-272014-08-21Canada
Ava-diclofenac SRtablet (extended-release)75 mgoralAvanstra Inc2011-08-182014-08-21Canada
Cambiapowder for solution50 mgoralTribute Pharmaceuticals Canada Inc2012-06-02Not applicableCanada
Cambiapowder, for solution50 mg/1oralDepomed, Inc.2010-04-20Not applicableUs
Cambiapowder, for solution50 mg/1oralDepomed, Inc.2016-03-10Not applicableUs
Cambiapowder, for solution1 mg/mgoralNautilus Neurosciences, Inc.2010-04-20Not applicableUs
Cataflamtablet, sugar coated50 mg/1oralNovartis Pharmaceuticals Corporation1993-11-24Not applicableUs
Diclofenac ECtablet (enteric-coated)50 mgoralSanis Health Inc2010-06-15Not applicableCanada
Diclofenac Ect 25mgtablet (enteric-coated)25 mgoralPro Doc Limitee1990-12-312010-07-13Canada
Diclofenac Ect 50mgtablet (enteric-coated)50 mgoralPro Doc Limitee1990-12-31Not applicableCanada
Diclofenac Ktablet50 mgoralSanis Health Inc2010-06-15Not applicableCanada
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralbryant ranch prepack1996-03-08Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralRx Change Co.2014-11-26Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralSandoz Inc1996-03-08Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralLake Erie Medical DBA Quality Care Products LLC1996-03-08Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPreferred Pharmaceuticals, Inc.2014-07-17Not applicableUs
Diclofenac Sodiumgel30 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2013-05-06Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-08Not applicableUs
Diclofenac Sodiumgel30 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2016-02-23Not applicableUs
Diclofenac SRtablet (extended-release)75 mgoralSanis Health Inc2010-06-152016-03-02Canada
Diclofenac Topical Solutionsolution1.5 %topicalSterimax Inc2015-11-23Not applicableCanada
Diclofenac-SRtablet (extended-release)100 mgoralPro Doc Limitee1997-01-15Not applicableCanada
Diclofenac-SRtablet (extended-release)75 mgoralPro Doc Limitee1997-08-06Not applicableCanada
Diclotecsuppository100 mgrectalTechnilab Pharma Inc.1998-06-292004-08-03Canada
Diclotecsuppository50 mgrectalTechnilab Pharma Inc.1998-06-292004-08-03Canada
Dom-diclofenactablet50 mgoralDominion Pharmacal1998-12-17Not applicableCanada
Dom-diclofenactablet25 mgoralDominion Pharmacal1997-12-17Not applicableCanada
Dom-diclofenac-SRtablet (extended-release)100 mgoralDominion Pharmacal1998-03-202003-07-18Canada
Dom-diclofenac-SRtablet (extended-release)75 mgoralDominion Pharmacal1998-03-20Not applicableCanada
Dylojectinjection, solution37.5 mg/mLintravenousHospira, Inc.2015-04-01Not applicableUs
Flectorpatch180 mg/1topicalH.J. Harkins Company, Inc.2008-01-14Not applicableUs
Flectorpatch180 mg/14gtopicalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-11Not applicableUs
Flectorpatch180 mg/1topicalSTAT Rx USA LLC2008-06-08Not applicableUs
Flectorpatch180 mg/1topicalRebel Distributors Corp2008-01-14Not applicableUs
Flectorpatch180 mg/1topicalbryant ranch prepack2008-01-14Not applicableUs
Flectorpatch180 mg/1topicalUnit Dose Services2008-01-14Not applicableUs
Flectorpatch180 mg/1topicalRebel Distributors Corp2008-11-17Not applicableUs
Flectorpatch180 mg/1topicalREMEDYREPACK INC.2014-09-112016-04-05Us
Flectorpatch180 mg/1topicalPfizer, Inc.2008-01-14Not applicableUs
Ntp-diclofenac Potassiumtablet50 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-diclofenac Sodiumtablet (enteric-coated)50 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-diclofenac Sodium SRtablet (extended-release)75 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-diclo Enteric Coated Tab 25mgtablet (enteric-coated)25 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Nu-diclo Enteric Coated Tab 50mgtablet (enteric-coated)50 mgoralNu Pharm Inc1990-12-312012-09-04Canada
Nu-diclo Rapidetablet50 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-diclo SR - Srt 100mgtablet (extended-release)100 mgoralNu Pharm Inc1998-03-162012-09-04Canada
Nu-diclo SR - Srt 75mgtablet (extended-release)75 mgoralNu Pharm Inc1998-03-162012-09-04Canada
Pennsaidsolution20 mg/gtopicalMallinckrodt, Inc2012-04-27Not applicableUs
Pennsaidliquid16.05 mg/mLtopicalMallinckrodt, Inc2010-04-05Not applicableUs
Pennsaidsolution20 mg/gtopicalHorizon Pharma Inc.2015-01-01Not applicableUs
Pennsaidliquid16.05 mg/mLtopicalUnit Dose Services2010-04-05Not applicableUs
Pennsaidliquid16.05 mg/mLtopicalLake Erie Medical DBA Quality Care Products LLC2010-04-05Not applicableUs
Pennsaidsolution1.5 %topicalPaladin Labs Inc2003-04-01Not applicableCanada
Pennsaidliquid16.05 mg/mLtopicalSTAT Rx USA LLC2010-04-05Not applicableUs
Penta-diclofenac - 25mgtablet (enteric-coated)25 mgoralPentapharm Ltd.1997-06-062004-07-30Canada
Penta-diclofenac - 50mgtablet (enteric-coated)50 mgoralPentapharm Ltd.1997-06-252004-07-30Canada
PMS-diclofenacsolution1.5 %topicalPharmascience Inc2014-12-02Not applicableCanada
PMS-diclofenactablet50 mgoralPharmascience Inc1997-11-28Not applicableCanada
PMS-diclofenactablet25 mgoralPharmascience Inc1997-11-28Not applicableCanada
PMS-diclofenactablet (delayed-release)50 mgoralPharmascience Inc2008-05-12Not applicableCanada
PMS-diclofenacsuppository100 mgrectalPharmascience Inc1998-08-07Not applicableCanada
PMS-diclofenactablet (delayed-release)25 mgoralPharmascience Inc2008-05-12Not applicableCanada
PMS-diclofenacsuppository50 mgrectalPharmascience Inc1998-08-07Not applicableCanada
PMS-diclofenac Ktablet50 mgoralPharmascience Inc1999-03-04Not applicableCanada
PMS-diclofenac-SRtablet (extended-release)100 mgoralPharmascience Inc1997-11-28Not applicableCanada
PMS-diclofenac-SRtablet (extended-release)75 mgoralPharmascience Inc1997-11-28Not applicableCanada
Pro-diclo Rapide - 50tablet50 mgoralPro Doc Limitee2008-07-07Not applicableCanada
Rho-diclofenactablet (enteric-coated)50 mgoralRhoxalpharma IncNot applicableNot applicableCanada
Rho-diclofenactablet (enteric-coated)25 mgoralRhoxalpharma IncNot applicableNot applicableCanada
Riva-diclofenac 100mg SR Tabletstablet (extended-release)100 mgoralLaboratoire Riva Inc1999-08-272003-07-28Canada
Riva-diclofenac 50mg Tabletstablet (enteric-coated)50 mgoralLaboratoire Riva Inc1999-08-272003-07-28Canada
Riva-diclofenac 75mg SR Tabletstablet (extended-release)75 mgoralLaboratoire Riva Inc1999-08-272003-07-28Canada
Riva-diclofenac-K 50mg Tabletstablet50 mgoralLaboratoire Riva Inc1999-08-302003-07-28Canada
Sandoz Diclofenacsuppository100 mgrectalSandoz Canada Incorporated2000-01-212010-08-05Canada
Sandoz Diclofenacsuppository50 mgrectalSandoz Canada Incorporated2000-01-212010-08-05Canada
Sandoz Diclofenac Ophthasolution0.1 %ophthalmicSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz-diclofenactablet (delayed-release)25 mgoralSandoz Canada Incorporated2006-02-02Not applicableCanada
Sandoz-diclofenacsuppository100 mgrectalSandoz Canada Incorporated2008-10-01Not applicableCanada
Sandoz-diclofenacsuppository50 mgrectalSandoz Canada Incorporated2008-10-01Not applicableCanada
Sandoz-diclofenactablet (delayed-release)50 mgoralSandoz Canada Incorporated2006-02-02Not applicableCanada
Sandoz-diclofenac Rapidetablet50 mgoralSandoz Canada Incorporated2006-02-02Not applicableCanada
Sandoz-diclofenac SRtablet (extended-release)100 mgoralSandoz Canada Incorporated2006-02-02Not applicableCanada
Sandoz-diclofenac SRtablet (extended-release)75 mgoralSandoz Canada Incorporated2006-02-02Not applicableCanada
Solarazegel30 mg/gtopicalPharma Derm, A Division Of Fougera Pharmaceuticals Inc.2000-10-16Not applicableUs
Taro-diclofenacsolution1.5 %topicalTaro Pharmaceuticals Inc2014-03-31Not applicableCanada
Taro-diclofenac Tab 25mgtablet25 mgoralTaro Pharmaceuticals Inc1993-12-312000-08-31Canada
Taro-diclofenac Tab 50mgtablet50 mgoralTaro Pharmaceuticals Inc1993-12-312000-08-31Canada
Teva-diclofenacsuppository100 mgrectalTeva Canada Limited1996-03-15Not applicableCanada
Teva-diclofenacsuppository50 mgrectalTeva Canada Limited1996-12-31Not applicableCanada
Teva-diclofenac ECtablet (enteric-coated)50 mgoralTeva Canada Limited1989-12-31Not applicableCanada
Teva-diclofenac ECtablet (enteric-coated)25 mgoralTeva Canada Limited1989-12-31Not applicableCanada
Teva-diclofenac SRtablet (extended-release)75 mgoralTeva Canada Limited1995-12-31Not applicableCanada
Teva-diclofenac SRtablet (extended-release)100 mgoralTeva Canada Limited1993-12-31Not applicableCanada
Teva-diclofenac-Ktablet50 mgoralTeva Canada Limited1999-01-13Not applicableCanada
Vofenal 0.1%liquid0.1 %ophthalmicAlcon Canada Inc1998-08-282000-06-30Canada
Voltarengel10 mg/gtopicalSTAT Rx USA LLC2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-11Not applicableUs
Voltarengel10 mg/gtopicalPhysicians Total Care, Inc.2008-11-21Not applicableUs
Voltarengel10 mg/gtopicalREMEDYREPACK INC.2014-06-16Not applicableUs
Voltarengel10 mg/gtopicalbryant ranch prepack2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalUnit Dose Services2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalEndo Pharmaceuticals Inc.2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalProficient Rx LP2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalRebel Distributors Corp2007-10-17Not applicableUs
Voltarengel10 mg/gtopicalDIRECT RX2015-01-01Not applicableUs
Voltarengel10 mg/gtopicalPreferred Pharmaceuticals, Inc.2014-10-08Not applicableUs
Voltarengel10 mg/gtopicalSTAT Rx USA LLC2007-10-17Not applicableUs
Voltarensolution1 mg/mLophthalmicNovartis Pharmaceutical Corporation1991-03-28Not applicableUs
Voltarengel10 mg/gtopicalKeltman Pharmaceuticals Inc.2011-01-27Not applicableUs
Voltarengel10 mg/gtopicalClinical Solutions Wholesale2007-10-17Not applicableUs
Voltaren Ophthasolution0.1 %ophthalmicAlcon Canada Inc1991-12-31Not applicableCanada
Voltaren Rapide Tablets 50mgtablet50 mgoralNovartis Pharmaceuticals Canada Inc1993-12-31Not applicableCanada
Voltaren SR 75 Tabtablet (extended-release)75 mgoralNovartis Pharmaceuticals Canada Inc1989-12-31Not applicableCanada
Voltaren SR Tab 100mgtablet (extended-release)100 mgoralNovartis Pharmaceuticals Canada Inc1985-12-31Not applicableCanada
Voltaren Sup 100mgsuppository100 mgrectalNovartis Pharmaceuticals Canada Inc1985-12-31Not applicableCanada
Voltaren Sup 50mgsuppository50 mgrectalNovartis Pharmaceuticals Canada Inc1985-12-31Not applicableCanada
Voltaren Tab 25mgtablet (delayed-release)25 mgoralNovartis Pharmaceuticals Canada Inc1980-12-312003-10-09Canada
Voltaren Tab 50mgtablet (delayed-release)50 mgoralNovartis Pharmaceuticals Canada Inc1980-12-31Not applicableCanada
Voltaren XRtablet, film coated, extended release100 mg/1oralNovartis Pharmaceuticals Corporation1996-03-08Not applicableUs
Zipsorcapsule, liquid filled25 mg/1oralDepomed, Inc.2009-06-16Not applicableUs
Zipsorcapsule, liquid filled25 mg/1oralPd Rx Pharmaceuticals, Inc.2010-04-30Not applicableUs
Zipsorcapsule, liquid filled25 mg/1oralLake Erie Medical DBA Quality Care Products2010-12-22Not applicableUs
Zorvolexcapsule35 mg/1oralIroko Pharmaceuticals LLC2013-10-31Not applicableUs
Zorvolexcapsule18 mg/1oralIroko Pharmaceuticals LLC2013-10-31Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-diclotablet (enteric-coated)50 mgoralApotex Inc1989-12-31Not applicableCanada
Apo-diclotablet (enteric-coated)25 mgoralApotex Inc1989-12-31Not applicableCanada
Apo-diclo Rapide 50 Mg Tabletstablet50 mgoralApotex Inc2001-05-25Not applicableCanada
Apo-diclo SRtablet (extended-release)75 mgoralApotex Inc1995-12-31Not applicableCanada
Apo-diclo SRtablet (extended-release)100 mgoralApotex Inc1994-12-31Not applicableCanada
Apo-diclofenacsolution1.5 %topicalApotex IncNot applicableNot applicableCanada
Apo-diclofenac Ophthalmicsolution0.1 %ophthalmicApotex Inc2015-09-01Not applicableCanada
Diclofenacsolution/ drops1 mg/mLophthalmicLake Erie Medical DBA Quality Care Products LLC2008-05-01Not applicableUs
Diclofenacsolution/ drops1 mg/mLophthalmicAkorn, Inc.2008-05-01Not applicableUs
Diclofenacsolution/ drops1 mg/mLophthalmicAltaire Pharmaceuticals Inc.2015-11-16Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralTeva Pharmaceuticals USA Inc1998-08-11Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-05Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralStat Rx USA2004-03-18Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralPhysicians Total Care, Inc.2008-10-15Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralAidarex Pharmaceuticals LLC1998-08-11Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralClinical Solutions Wholesale1998-11-20Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralMylan Pharmaceuticals Inc.2012-08-13Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralCarilion Materials Management1998-08-11Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralRebel Distributors Corp2010-01-21Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralPd Rx Pharmaceuticals, Inc.1998-11-20Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralREMEDYREPACK INC.2015-09-04Not applicableUs
Diclofenac Potassiumtablet50 mg/1oralREMEDYREPACK INC.2012-03-30Not applicableUs
Diclofenac Potassiumtablet50 mg/1oralApotheca, Inc2007-08-20Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralbryant ranch prepack2010-01-21Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralSandoz Inc1998-11-20Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralH.J. Harkins Company, Inc.2010-01-21Not applicableUs
Diclofenac Potassiumtablet, film coated50 mg/1oralLake Erie Medical DBA Quality Care Products LLC1998-08-11Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralUnit Dose Services1995-09-28Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralStat Rx USA1995-09-28Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralREMEDYREPACK INC.2011-06-02Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralBlenheim Pharmacal, Inc.2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralSTAT Rx USA LLC2010-03-05Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralSandoz Inc1995-11-30Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralH.J. Harkins Company, Inc.2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralAv Kare, Inc.1998-11-13Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralSt Marys Medical Park Pharmacy2014-04-21Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralUnit Dose Services2008-08-19Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalPure Tek Corporation2015-11-04Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralProficient Rx LP1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralSandoz Inc1995-09-28Not applicableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicPhysicians Total Care, Inc.2011-07-19Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralDIRECT RX2015-01-01Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralMylan Pharmaceuticals Inc.2010-05-18Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralCarilion Materials Management1995-09-28Not applicableUs
Diclofenac Sodiumsolution1 mg/mLophthalmicSandoz Inc2008-02-14Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralBlue Point Laboratories2014-02-24Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralOceanside Pharmaceuticals2000-02-28Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralbryant ranch prepack1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralKeltman Pharmaceuticals Inc.2009-07-01Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralUnit Dose Services2002-01-07Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalInternational Brand Management, Llc2016-02-04Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralBlenheim Pharmacal, Inc.2015-06-02Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalTeligent Pharma, Inc.2015-07-08Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralAv Kare, Inc.1998-11-13Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralProficient Rx LP2002-11-06Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralSandoz Inc1995-09-28Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralAphena Pharma Solutions Tennessee, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPreferred Pharmaceuticals, Inc.2012-06-04Not applicableUs
Diclofenac Sodiumgel10 mg/gtopicalAmneal Pharmaceuticals of New York, LLC2016-03-21Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralRising Pharmaceuticals, Inc.2010-12-31Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalPharmaceutica North America, Inc2015-08-13Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralBlenheim Pharmacal, Inc.2015-05-18Not applicableUs
Diclofenac Sodiumtablet, extended release100 mg/1oralPhysicians Total Care, Inc.2004-03-02Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalApotex Corp.2014-05-28Not applicableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicBausch & Lomb Incorporated2007-12-28Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralClinical Solutions Wholesale2010-12-31Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1996-03-26Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralMylan Pharmaceuticals Inc.2002-02-15Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralAmerican Health Packaging2009-04-02Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralAphena Pharma Solutions Tennessee, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPreferred Pharmaceuticals, Inc.2014-02-03Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralRising Pharmaceuticals, Inc.2010-12-31Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralAphena Pharma Solutions Tennessee, Inc.1998-11-13Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralBlenheim Pharmacal, Inc2015-05-27Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralPhysicians Total Care, Inc.2004-05-21Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralRebel Distributors Corp2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralGolden State Medical Supply, Inc.2015-07-27Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralClinical Solutions Wholesale2010-12-31Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralProficient Rx LP1996-03-08Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1996-03-26Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralActavis Elizabeth LLC2002-01-09Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralBlue Point Laboratories2015-12-21Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralDispensing Solutions, Inc.2008-08-19Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPreferred Pharmaceuticals, Inc.2014-06-02Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalSircle Laboratories, Llc2015-07-08Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2002-01-09Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralGolden State Medical Supply, Inc.2015-07-27Not applicableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicRebel Distributors Corp2007-12-28Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralProficient Rx LP2008-08-19Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalActavis Pharma, Inc.2015-04-06Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralActavis Pharma, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralBlue Point Laboratories2015-12-21Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralDispensing Solutions, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralPreferred Pharmaceuticals, Inc.2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralRising Pharmaceuticals, Inc.2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralPhysicians Total Care, Inc.1997-02-10Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalTaro Pharmaceuticals U.S.A., Inc.2014-11-26Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralBlue Point Laboratories2015-12-21Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-07-01Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPreferred Pharmaceuticals, Inc.2010-05-18Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalPreferred Pharmcacuticals Inc.2016-04-11Not applicableUs
Diclofenac Sodiumtablet, extended release100 mg/1oralREMEDYREPACK INC.2012-03-28Not applicableUs
Diclofenac Sodiumsolution/ drops3.5 mg/mLophthalmicPACK Pharmaceuticals, LLC2008-06-20Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPhysicians Total Care, Inc.1995-11-16Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-12-31Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPd Rx Pharmaceuticals, Inc.1995-09-28Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralActavis Pharma, Inc.2002-11-06Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralActavis Pharma, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalProficient Rx LP2015-07-08Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralREMEDYREPACK INC.2012-03-27Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralPd Rx Pharmaceuticals, Inc.2010-01-27Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralBlenheim Pharmacal, Inc2013-03-28Not applicableUs
Diclofenac Sodiumsolution/ drops1 mg/mLophthalmicH.J. Harkins Company, Inc.2007-12-28Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralMylan Institutional Inc.2010-06-04Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralLake Erie Medical DBA Quality Care Products LLC2008-08-19Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralRebel Distributors Corp1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralDIRECT RX2015-12-22Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalPaddock Laboratories, LLC2014-11-24Not applicableUs
Diclofenac Sodiumgel30 mg/gtopicalImpax Generics2013-11-21Not applicableUs
Diclofenac Sodiumtablet, delayed release25 mg/1oralBlue Point Laboratories2014-02-24Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralPreferred Pharmaceuticals, Inc.2010-12-31Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralREMEDYREPACK INC.2012-03-02Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralBlenheim Pharmacal, Inc.2015-07-15Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralSTAT Rx USA LLC2010-03-05Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralMylan Institutional Inc.2010-06-04Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralRebel Distributors Corp1996-03-26Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralCardinal Health1995-11-30Not applicableUs
Diclofenac Sodiumtablet, delayed release75 mg/1oralMylan Pharmaceuticals Inc.2010-05-18Not applicableUs
Diclofenac Sodiumtablet, film coated, extended release100 mg/1oralTEVA Pharmaceuticals USA Inc.2000-02-28Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralBlue Point Laboratories2014-02-24Not applicableUs
Diclofenac Sodiumtablet, extended release100 mg/1oralbryant ranch prepack2004-03-02Not applicableUs
Diclofenac Sodiumsolution16.05 mg/mLtopicalNovel Laboratories, Inc.2015-12-09Not applicableUs
Diclofenac Sodiumtablet, delayed release50 mg/1oralA S Medication Solutions1996-03-26Not applicableUs
Diclofenac Sodium D/rtablet, delayed release75 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diclofenac Sodium D/rtablet, delayed release50 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralPreferred Pharmaceuticals Inc.2015-08-31Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-04-10Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralRebel Distributors Corp2012-04-10Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralProficient Rx LP1998-11-13Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-04-10Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralBlenheim Pharmacal, Inc.2013-09-30Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralBlenheim Pharmacal, Inc.2013-11-30Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralGolden State Medical Supply, Inc.2014-08-12Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release75 mg/1oralCarlsbad Technology, Inc.1998-11-13Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralGolden State Medical Supply, Inc.2014-08-12Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralCarlsbad Technology, Inc.1998-11-13Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release25 mg/1oralCarlsbad Technology, Inc.1998-11-13Not applicableUs
Diclofenac Sodium Delayed Releasetablet, delayed release50 mg/1oralPreferred Pharmaceuticals Inc.2015-11-20Not applicableUs
Diclofenac Sodium Delayed Release Delayed Releasetablet, delayed release75 mg/1oralREMEDYREPACK INC.2013-06-24Not applicableUs
Diclofenac Sodium Delayed Release Delayed Releasetablet, delayed release75 mg/1oralREMEDYREPACK INC.2013-06-04Not applicableUs
Diclofenac Sodium Drtablet, delayed release50 mg/1oralNorthwind Pharmaceuticals2015-01-16Not applicableUs
Diclofenac Sodium Extended-releasetablet, extended release100 mg/1oralMedsource Pharmaceuticals2009-01-05Not applicableUs
Diclofenac Sodium Extended-releasetablet, extended release100 mg/1oralSt Marys Medical Park Pharmacy2002-01-07Not applicableUs
Diclofenac Sodium Extended-releasetablet, extended release100 mg/1oralRebel Distributors Corp.2002-01-07Not applicableUs
Diclofenac Sodiumdelayed Release Delayed Releasetablet, delayed release50 mg/1oralREMEDYREPACK INC.2016-03-15Not applicableUs
Flectorpatch180 mg/1topicalPhysicians Total Care, Inc.2008-11-17Not applicableUs
Flectorpatch180 mg/1topicalDIRECT RX2014-01-01Not applicableUs
Klofensaid IIsolution16.05 mg/mLtopicalPure Tek Corporation2016-03-01Not applicableUs
Previdolrx Analgesic PakkitGen Pak Solutions, Llc2015-12-15Not applicableUs
XrylixkitPure Tek Corporation2016-03-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Diclofenac Sodiumaerosol, metered30 mg/mLtopicalShoreline Pharmaceuticals, Inc.2016-01-07Not applicableUs
Diclofenac Sodiumgel3 g/100gtopicalTwo Hip Consulting, Llc2016-03-25Not applicableUs
International Brands
NameCompany
AclonacNot Available
AllvoranNot Available
EcofenacNot Available
EffektonNot Available
Nu-DicloNot Available
PrimofenacNot Available
ProphenatinNot Available
RhumalganNot Available
Voltaren EmulgelNot Available
VoltarolNot Available
Brand mixtures
NameLabellerIngredients
Act Diclo-misoActavis Pharma Company
ArthrotecG.D. Searle LLC Division of Pfizer Inc
Arthrotec 50Pfizer Canada Inc
Arthrotec 75Pfizer Canada Inc
Diclofenac MisoprostolAbri Pharmaceuticals Inc
Diclofenac Sodium and MisoprostolActavis Pharma, Inc.
Diclofenac Sodium and Misoprostol Delayed-releaseEagle Pharmaceuticals, Inc.
Dipentocaine Topical Cream Compounding KitAlvix Laboratories, LLC
Gapeam BudibacAlvix Laboratories, LLC
Gd-diclofenac/misoprostol 50Genmed A Division Of Pfizer Canada Inc
Gd-diclofenac/misoprostol 75Genmed A Division Of Pfizer Canada Inc
Infla-ezeAlvix Laboratories, LLC
PMS-diclofenac-misoprostolPharmascience Inc
Sandoz Diclofenac MisoprostolSandoz Canada Incorporated
Salts
Name/CASStructureProperties
Diclofenac epolamine
ThumbNot applicableDBSALT001398
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
UNII144O8QL0L1
CAS number15307-86-5
WeightAverage: 296.149
Monoisotopic: 295.016684015
Chemical FormulaC14H11Cl2NO2
InChI KeyInChIKey=DCOPUUMXTXDBNB-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.
Related Articles
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 inhibitorInhibitor0.6786
CYP450 2D6 inhibitorNon-inhibitor0.848
CYP450 2C19 inhibitorNon-inhibitor0.8947
CYP450 3A4 inhibitorNon-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
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
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
Tablet (enteric-coated)oral
Tablet (enteric-coated)oral25 mg
Tablet (enteric-coated)oral50 mg
Solutionophthalmic0.1 %
Tablet, film coatedoral
Tabletoral
Powder for solutionoral50 mg
Powder, for solutionoral1 mg/mg
Powder, for solutionoral50 mg/1
Tablet, sugar coatedoral50 mg/1
Solution/ dropsophthalmic1 mg/mL
Tabletoral50 mg/1
Tablet, film coatedoral50 mg/1
Aerosol, meteredtopical30 mg/mL
Geltopical3 g/100g
Geltopical30 mg/g
Solutiontopical16.05 mg/mL
Solution/ dropsophthalmic3.5 mg/mL
Tablet, delayed releaseoral25 mg/1
Tablet, delayed releaseoral50 mg/1
Tablet, delayed releaseoral75 mg/1
Tablet, delayed releaseoral
Tablet, extended releaseoral100 mg/1
Kittopical
Injection, solutionintravenous37.5 mg/mL
Patchtopical180 mg/1
Patchtopical180 mg/14g
Liquidtopical16.05 mg/mL
Solutiontopical1.5 %
Solutiontopical20 mg/g
Tabletoral25 mg
Kit
Tablet (delayed-release)oral25 mg
Suppositoryrectal100 mg
Suppositoryrectal50 mg
Tablet (extended-release)oral100 mg
Tablet (extended-release)oral75 mg
Liquidophthalmic0.1 %
Geltopical10 mg/g
Solutionophthalmic1 mg/mL
Tabletoral50 mg
Tablet (delayed-release)oral50 mg
Tablet, film coated, extended releaseoral100 mg/1
Capsule, liquid filledoral25 mg/1
Capsuleoral18 mg/1
Capsuleoral35 mg/1
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
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5607690 No1999-04-132019-04-13Us
US5792753 No1995-08-112015-08-11Us
US5914322 No1995-08-112015-08-11Us
US5985850 No1995-08-112015-08-11Us
US6287594 No1999-01-152019-01-15Us
US6365180 No1999-07-152019-07-15Us
US6407079 No1999-06-182019-06-18Us
US6974595 No1997-05-152017-05-15Us
US7482377 No1997-05-152017-05-15Us
US7662858 No2009-02-242029-02-24Us
US7759394 No2006-06-162026-06-16Us
US7884095 No2009-02-242029-02-24Us
US7939518 No2009-02-242029-02-24Us
US8097651 No2006-06-162026-06-16Us
US8110606 No2009-02-242029-02-24Us
US8217078 No2009-07-102029-07-10Us
US8252838 No2008-04-212028-04-21Us
US8546450 No2010-08-092030-08-09Us
US8563613 No2007-10-172027-10-17Us
US8618164 No2009-07-102029-07-10Us
US8623920 No2009-02-242029-02-24Us
US8679544 No2010-04-232030-04-23Us
US8741956 No2009-07-102029-07-10Us
US8871809 No2007-10-172027-10-17Us
US8927604 No2006-06-162026-06-16Us
US8946292 No2007-03-222027-03-22Us
US8999387 No2010-04-232030-04-23Us
US9017721 No2010-04-232030-04-23Us
US9066913 No2007-10-172027-10-17Us
US9101591 No2007-10-172027-10-17Us
US9132110 No2007-10-172027-10-17Us
US9168304 No2007-10-172027-10-17Us
US9168305 No2007-10-172027-10-17Us
US9173854 No2010-04-232030-04-23Us
US9180095 No2010-04-232030-04-23Us
US9180096 No2010-04-232030-04-23Us
US9186328 No2010-04-232030-04-23Us
US9220784 No2007-10-172027-10-17Us
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
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
MSMass Spectrum (Electron Ionization)splash10-03xv-1290000000-8fb3ce6f68fc69b5218eView in MoNA
References
Synthesis Reference

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

US4670254
General References
  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:16740558 ]
  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:16645966 ]
  3. FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med. 2001 Aug 9;345(6):433-42. [PubMed:11496855 ]
  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:16968830 ]
  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:11992745 ]
  6. Gan TJ: Diclofenac: an update on its mechanism of action and safety profile. Curr Med Res Opin. 2010 Jul;26(7):1715-31. doi: 10.1185/03007995.2010.486301. [PubMed:20470236 ]
  7. Link [Link]
External Links
ATC CodesD11AX18M01AB05M01AB55M02AA15S01BC03S01CC01
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
AbciximabDiclofenac may increase the anticoagulant activities of Abciximab.
AcenocoumarolDiclofenac may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Diclofenac is combined with Acetylsalicylic acid.
AliskirenDiclofenac may decrease the antihypertensive activities of Aliskiren.
AlteplaseDiclofenac may increase the anticoagulant activities of Alteplase.
AmikacinDiclofenac may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmitriptylineAmitriptyline may increase the antiplatelet activities of Diclofenac.
AnistreplaseDiclofenac may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Diclofenac is combined with Apixaban.
AprepitantThe serum concentration of Diclofenac can be decreased when it is combined with Aprepitant.
ArbekacinDiclofenac may decrease the excretion rate of Arbekacin which could result in a lower serum level and potentially a reduction in efficacy.
BalsalazideDiclofenac may increase the nephrotoxic activities of Balsalazide.
CapecitabineThe serum concentration of Diclofenac can be increased when it is combined with Capecitabine.
CarbamazepineThe serum concentration of Diclofenac can be decreased when it is combined with Carbamazepine.
Citric AcidDiclofenac may increase the anticoagulant activities of Citric Acid.
ColesevelamColesevelam can cause a decrease in the absorption of Diclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
CollagenaseThe risk or severity of adverse effects can be increased when Diclofenac is combined with Collagenase.
CyclosporineDiclofenac may increase the nephrotoxic activities of Cyclosporine.
Dabigatran etexilateDiclofenac may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinDiclofenac may increase the anticoagulant activities of Dalteparin.
DasatinibDasatinib may increase the anticoagulant activities of Diclofenac.
DeferasiroxThe risk or severity of adverse effects can be increased when Diclofenac is combined with Deferasirox.
DeferiproneThe serum concentration of Deferiprone can be increased when it is combined with Diclofenac.
DelavirdineThe serum concentration of Diclofenac can be increased when it is combined with Delavirdine.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Diclofenac is combined with Deoxycholic Acid.
DesmopressinThe risk or severity of adverse effects can be increased when Diclofenac is combined with Desmopressin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Diclofenac.
DicoumarolDiclofenac may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diclofenac is combined with Diflunisal.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Diclofenac.
DrospirenoneDiclofenac may increase the hyperkalemic activities of Drospirenone.
Edetic AcidDiclofenac may increase the anticoagulant activities of Edetic Acid.
EnoxaparinDiclofenac may increase the anticoagulant activities of Enoxaparin.
EplerenoneDiclofenac may decrease the antihypertensive activities of Eplerenone.
ErythromycinThe serum concentration of Diclofenac can be increased when it is combined with Erythromycin.
Ethyl biscoumacetateDiclofenac may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Etodolac.
FenoprofenThe risk or severity of adverse effects can be increased when Diclofenac is combined with Fenoprofen.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Diclofenac.
FloxuridineThe serum concentration of Diclofenac can be increased when it is combined with Floxuridine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Diclofenac.
FluorouracilThe serum concentration of Diclofenac can be increased when it is combined with Fluorouracil.
FlurbiprofenThe risk or severity of adverse effects can be increased when Diclofenac is combined with Flurbiprofen.
Fondaparinux sodiumDiclofenac may increase the anticoagulant activities of Fondaparinux sodium.
FosphenytoinThe serum concentration of Diclofenac can be decreased when it is combined with Fosphenytoin.
FramycetinDiclofenac may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
GemfibrozilThe serum concentration of Diclofenac can be increased when it is combined with Gemfibrozil.
GentamicinDiclofenac may decrease the excretion rate of Gentamicin which could result in a lower serum level and potentially a reduction in efficacy.
GlucosamineGlucosamine may increase the antiplatelet activities of Diclofenac.
HaloperidolThe risk or severity of adverse effects can be increased when Diclofenac is combined with Haloperidol.
HeparinDiclofenac may increase the anticoagulant activities of Heparin.
HomoharringtonineThe risk or severity of adverse effects can be increased when Diclofenac is combined with Homoharringtonine.
HydralazineDiclofenac may decrease the antihypertensive activities of Hydralazine.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Diclofenac is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Diclofenac.
IbuprofenThe risk or severity of adverse effects can be increased when Diclofenac is combined with Ibuprofen.
IcosapentThe risk or severity of adverse effects can be increased when Diclofenac is combined with Icosapent.
IndomethacinThe risk or severity of adverse effects can be increased when Diclofenac is combined with Indomethacin.
InfliximabThe risk or severity of adverse effects can be increased when Diclofenac is combined with Infliximab.
KanamycinDiclofenac may decrease the excretion rate of Kanamycin which could result in a lower serum level and potentially a reduction in efficacy.
KetoprofenThe risk or severity of adverse effects can be increased when Diclofenac is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Diclofenac.
LimaprostLimaprost may increase the antiplatelet activities of Diclofenac.
LithiumThe serum concentration of Lithium can be increased when it is combined with Diclofenac.
Mefenamic acidThe risk or severity of adverse effects can be increased when Diclofenac is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Diclofenac is combined with Meloxicam.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Diclofenac.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Diclofenac.
NabumetoneThe risk or severity of adverse effects can be increased when Diclofenac is combined with Nabumetone.
NadololDiclofenac may decrease the antihypertensive activities of Nadolol.
NaproxenThe risk or severity of adverse effects can be increased when Diclofenac is combined with Naproxen.
NeomycinDiclofenac may decrease the excretion rate of Neomycin which could result in a lower serum level and potentially a reduction in efficacy.
NetilmicinDiclofenac may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
NicardipineThe serum concentration of Diclofenac can be increased when it is combined with Nicardipine.
ObinutuzumabThe risk or severity of adverse effects can be increased when Diclofenac is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Diclofenac.
OxaprozinThe risk or severity of adverse effects can be increased when Diclofenac is combined with Oxaprozin.
PamidronateThe risk or severity of adverse effects can be increased when Diclofenac is combined with Pamidronate.
ParoxetineParoxetine may increase the antiplatelet activities of Diclofenac.
PemetrexedThe serum concentration of Pemetrexed can be increased when it is combined with Diclofenac.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Diclofenac.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Diclofenac.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Diclofenac.
PhenindioneDiclofenac may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Diclofenac can be decreased when it is combined with Phenobarbital.
PhenprocoumonDiclofenac may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Diclofenac can be decreased when it is combined with Phenytoin.
PiroxicamThe risk or severity of adverse effects can be increased when Diclofenac is combined with Piroxicam.
PorfimerDiclofenac may increase the photosensitizing activities of Porfimer.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Diclofenac.
PrimidoneThe serum concentration of Diclofenac can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Diclofenac can be increased when it is combined with Probenecid.
ReteplaseDiclofenac may increase the anticoagulant activities of Reteplase.
RibostamycinDiclofenac may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RidogrelDiclofenac may increase the anticoagulant activities of Ridogrel.
RifampicinThe serum concentration of Diclofenac can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Diclofenac can be decreased when it is combined with Rifapentine.
RivaroxabanDiclofenac may increase the anticoagulant activities of Rivaroxaban.
SecobarbitalThe serum concentration of Diclofenac can be decreased when it is combined with Secobarbital.
SparfloxacinDiclofenac may increase the neuroexcitatory activities of Sparfloxacin.
SpectinomycinDiclofenac may decrease the excretion rate of Spectinomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptokinaseDiclofenac may increase the anticoagulant activities of Streptokinase.
StreptomycinDiclofenac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
SulfadiazineThe serum concentration of Diclofenac can be increased when it is combined with Sulfadiazine.
SulfisoxazoleThe serum concentration of Diclofenac can be increased when it is combined with Sulfisoxazole.
SulindacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Sulindac.
SulodexideDiclofenac may increase the anticoagulant activities of Sulodexide.
TacrolimusDiclofenac may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Diclofenac.
TenecteplaseDiclofenac may increase the anticoagulant activities of Tenecteplase.
TenofovirThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tenofovir.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tiaprofenic acid.
TipranavirTipranavir may increase the antiplatelet activities of Diclofenac.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Diclofenac.
TobramycinDiclofenac may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TolbutamideThe serum concentration of Diclofenac can be increased when it is combined with Tolbutamide.
TolmetinThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tolmetin.
TorasemideDiclofenac may decrease the diuretic activities of Torasemide.
TositumomabThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tositumomab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Diclofenac.
TriamtereneDiclofenac may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Diclofenac.
UnoprostoneThe therapeutic efficacy of Unoprostone can be decreased when used in combination with Diclofenac.
UrokinaseDiclofenac may increase the anticoagulant activities of Urokinase.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Diclofenac.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Diclofenac.
VenlafaxineVenlafaxine may increase the antiplatelet activities of Diclofenac.
VerteporfinDiclofenac may increase the photosensitizing activities of Verteporfin.
Vitamin EVitamin E may increase the antiplatelet activities of Diclofenac.
VoriconazoleThe serum concentration of Diclofenac can be increased when it is combined with Voriconazole.
WarfarinDiclofenac may increase the anticoagulant activities of Warfarin.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
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:12534640 ]
  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:12588370 ]
  3. Beubler E: [Pharmacology of cyclooxygenase 2 inhibition]. Wien Med Wochenschr. 2003;153(5-6):95-9. [PubMed:12705061 ]
  4. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. [PubMed:12852704 ]
  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:12925531 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
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:12414874 ]
  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:12534640 ]
  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:12713596 ]
  4. Chavez ML, DeKorte CJ: Valdecoxib: a review. Clin Ther. 2003 Mar;25(3):817-51. [PubMed:12852704 ]
  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:12966366 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Iron ion binding
Specific Function:
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
Gene Name:
ALOX5
Uniprot ID:
P09917
Molecular Weight:
77982.595 Da
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:12932896 ]
  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:12826271 ]
  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:15525540 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity
Specific Function:
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. This sodium channel may be present in both denervated and innervated skeleta...
Gene Name:
SCN4A
Uniprot ID:
P35499
Molecular Weight:
208059.175 Da
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:15824190 ]
  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:15032643 ]
  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:15574747 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ligand-gated sodium channel activity
Specific Function:
Isoform 2 and isoform 3 function as proton-gated sodium channels; they are activated by a drop of the extracellular pH and then become rapidly desensitized. The channel generates a biphasic current with a fast inactivating and a slow sustained phase. Has high selectivity for sodium ions and can also transport lithium ions with high efficiency. Isoform 2 can also transport potassium, but with lo...
Gene Name:
ASIC1
Uniprot ID:
P78348
Molecular Weight:
59908.915 Da
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:11588175 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
other
General Function:
Voltage-gated potassium channel activity
Specific Function:
Probably important in the regulation of neuronal excitability. Associates with KCNQ3 to form a potassium channel with essentially identical properties to the channel underlying the native M-current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons as well as the responsiveness to synaptic in...
Gene Name:
KCNQ2
Uniprot ID:
O43526
Molecular Weight:
95846.575 Da
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:15598972 ]
  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. doi: 10.1016/j.tips.2007.11.010. Epub 2008 Jan 18. [PubMed:18206251 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
other
General Function:
Voltage-gated potassium channel activity
Specific Function:
Probably important in the regulation of neuronal excitability. Associates with KCNQ2 or KCNQ5 to form a potassium channel with essentially identical properties to the channel underlying the native M-current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons as well as the responsiveness to sy...
Gene Name:
KCNQ3
Uniprot ID:
O43525
Molecular Weight:
96741.515 Da
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. doi: 10.1016/j.tips.2007.11.010. Epub 2008 Jan 18. [PubMed:18206251 ]
  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:15598972 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Phospholipid binding
Specific Function:
Thought to participate in the regulation of the phospholipid metabolism in biomembranes including eicosanoid biosynthesis. Catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides.
Gene Name:
PLA2G2A
Uniprot ID:
P14555
Molecular Weight:
16082.525 Da
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:15906762 ]
  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:16552142 ]
  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:9279965 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
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:20167001 ]
  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:19515014 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  4. 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:12065442 ]
  5. 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:8417277 ]
  6. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
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:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Glucuronosyltransferase activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites. Is also active with androsterone, hyodeoxycholic acid and tetrachlorocatechol...
Gene Name:
UGT2B7
Uniprot ID:
P16662
Molecular Weight:
60694.12 Da
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:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
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:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
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:19515014 ]
  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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Identical protein binding
Specific Function:
Thyroid hormone-binding protein. Probably transports thyroxine from the bloodstream to the brain.
Gene Name:
TTR
Uniprot ID:
P02766
Molecular Weight:
15886.88 Da
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:14968122 ]
  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:15080795 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
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:14727845 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
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:12835412 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
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:11743742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
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:12835412 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
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:10991954 ]
  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:9880528 ]
  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:10220563 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
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:11306713 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol, estrone-3-sulfate and sulfobromophthalein (BSP) are transported with much lower efficiency. May play a signifiant role in regulating T4 flux into and out of the brain (By similarity).
Gene Name:
SLCO1C1
Uniprot ID:
Q9NYB5
Molecular Weight:
78695.625 Da
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. doi: 10.1210/en.2008-0188. Epub 2008 Oct 9. [PubMed:18845642 ]
  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:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name:
SLC22A11
Uniprot ID:
Q9NSA0
Molecular Weight:
59970.945 Da
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:10660625 ]
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Drug created on June 13, 2005 07:24 / Updated on June 28, 2016 01:53