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Identification
NameCarvedilol
Accession NumberDB01136  (APRD00091)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Carvedilol is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors.

Structure
Thumb
Synonyms
(+-)-1-(Carbazol-4-yloxy)-3-((2-(O-methoxyphenoxy)ethyl)amino)-2-propanol
Carvedilol
Carvedilolum
SKF 105517
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Auro-carvediloltablet6.25 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-carvediloltablet3.125 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-carvediloltablet25 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-carvediloltablet12.5 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Ava-carvediloltablet12.5 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-carvediloltablet6.25 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-carvediloltablet3.125 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-carvediloltablet25 mgoralAvanstra Inc2011-10-112014-08-21Canada
Carvediloltablet12.5 mgoralSivem Pharmaceuticals Ulc2004-04-06Not applicableCanada
Carvediloltablet25 mgoralSivem Pharmaceuticals Ulc2004-04-06Not applicableCanada
Carvediloltablet3.125 mgoralSanis Health Inc2011-06-10Not applicableCanada
Carvediloltablet6.25 mgoralSivem Pharmaceuticals Ulc2004-04-06Not applicableCanada
Carvediloltablet3.125 mgoralSivem Pharmaceuticals Ulc2004-04-06Not applicableCanada
Carvediloltablet12.5 mgoralMeliapharm Inc2010-05-172014-06-25Canada
Carvediloltablet25.0 mgoralPro Doc Limitee2009-06-12Not applicableCanada
Carvediloltablet6.25 mgoralMeliapharm Inc2010-05-172014-06-25Canada
Carvediloltablet12.5 mgoralPro Doc Limitee2009-06-12Not applicableCanada
Carvediloltablet25 mgoralSanis Health Inc2011-06-10Not applicableCanada
Carvediloltablet3.125 mgoralMeliapharm Inc2010-06-012014-06-25Canada
Carvediloltablet6.25 mgoralPro Doc Limitee2009-06-12Not applicableCanada
Carvediloltablet12.5 mgoralSanis Health Inc2011-06-10Not applicableCanada
Carvediloltablet3.125 mgoralPro Doc Limitee2009-06-12Not applicableCanada
Carvediloltablet6.25 mgoralSanis Health Inc2011-06-10Not applicableCanada
Coregtablet, film coated3.125 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-21Not applicableUs
Coregtablet, film coated6.25 mg/1oralPhysicians Total Care, Inc.2000-11-28Not applicableUs
Coregtablet, film coated25 mg/1oralGlaxo Smith Kline Llc1997-06-03Not applicableUs
Coregtablet, film coated3.125 mg/1oralPhysicians Total Care, Inc.2000-11-28Not applicableUs
Coregtablet, film coated12.5 mg/1oralGlaxo Smith Kline Llc1997-06-03Not applicableUs
Coregtablet, film coated12.5 mg/1oralPhysicians Total Care, Inc.2002-05-23Not applicableUs
Coregtablet, film coated6.25 mg/1oralGlaxo Smith Kline Llc1997-06-03Not applicableUs
Coregtablet, film coated25 mg/1oralPhysicians Total Care, Inc.2003-06-20Not applicableUs
Coregtablet, film coated3.125 mg/1oralGlaxo Smith Kline Llc1997-06-03Not applicableUs
Coregtablet, film coated12.5 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-21Not applicableUs
Coregtablet, film coated25 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-21Not applicableUs
Coreg (carvedilol) Tablets, 12.5mgtablet12.5 mgoralGlaxosmithkline Inc1996-10-172006-10-11Canada
Coreg (carvedilol) Tablets, 25mgtablet25 mgoralGlaxosmithkline Inc1996-10-172006-10-11Canada
Coreg (carvedilol) Tablets, 3.125 mgtablet3.125 mgoralGlaxosmithkline Inc1996-10-172006-10-11Canada
Coreg (carvedilol) Tablets, 6.25mgtablet6.25 mgoralGlaxosmithkline Inc1996-10-172006-10-11Canada
Coreg 12.5mgtablet12.5 mgoralHoffmann La Roche Limited2000-04-192001-07-18Canada
Coreg 25mgtablet25 mgoralHoffmann La Roche Limited2000-03-222001-07-18Canada
Coreg 3.125mgtablet3.125 mgoralHoffmann La Roche Limited2000-05-292001-07-18Canada
Coreg 6.25mgtablet6.25 mgoralHoffmann La Roche Limited2000-12-062001-07-18Canada
Coreg CRcapsule, extended release10 mg/1oralGlaxo Smith Kline Llc2007-02-09Not applicableUs
Coreg CRcapsule, extended release80 mg/1oralCarilion Materials Management2007-02-20Not applicableUs
Coreg CRcapsule, extended release40 mg/1oralCarilion Materials Management2007-02-14Not applicableUs
Coreg CRcapsule, extended release20 mg/1oralCarilion Materials Management2007-02-06Not applicableUs
Coreg CRcapsule, extended release80 mg/1oralGlaxo Smith Kline Llc2007-02-20Not applicableUs
Coreg CRcapsule, extended release10 mg/1oralCarilion Materials Management2007-02-09Not applicableUs
Coreg CRcapsule, extended release40 mg/1oralGlaxo Smith Kline Llc2007-02-14Not applicableUs
Coreg CRcapsule, extended release20 mg/1oralGlaxo Smith Kline Llc2007-02-06Not applicableUs
Coregcr CRcapsule, extended release80 mg/1oralPhysicians Total Care, Inc.2007-05-23Not applicableUs
Coregcr CRcapsule, extended release40 mg/1oralPhysicians Total Care, Inc.2008-05-09Not applicableUs
Coregcr CRcapsule, extended release20 mg/1oralPhysicians Total Care, Inc.2008-08-25Not applicableUs
Coregcr CRcapsule, extended release10 mg/1oralPhysicians Total Care, Inc.2009-04-15Not applicableUs
Dilatrend - Tab 25mgtablet25 mgoralHoffmann La Roche LimitedNot applicableNot applicableCanada
Dilatrend - Tab 50mgtablet50 mgoralHoffmann La Roche LimitedNot applicableNot applicableCanada
Dom-carvediloltablet25 mgoralDominion Pharmacal2004-03-01Not applicableCanada
Dom-carvediloltablet12.5 mgoralDominion Pharmacal2004-03-01Not applicableCanada
Dom-carvediloltablet6.25 mgoralDominion Pharmacal2004-03-01Not applicableCanada
Dom-carvediloltablet3.125 mgoralDominion Pharmacal2004-03-01Not applicableCanada
Jamp-carvediloltablet25 mgoralJamp Pharma Corporation2011-06-17Not applicableCanada
Jamp-carvediloltablet12.5 mgoralJamp Pharma Corporation2011-06-17Not applicableCanada
Jamp-carvediloltablet6.25 mgoralJamp Pharma Corporation2011-06-17Not applicableCanada
Jamp-carvediloltablet3.125 mgoralJamp Pharma Corporation2011-06-17Not applicableCanada
Mylan-carvediloltablet25 mgoralMylan Pharmaceuticals Ulc2010-03-30Not applicableCanada
Mylan-carvediloltablet12.5 mgoralMylan Pharmaceuticals Ulc2010-03-30Not applicableCanada
Mylan-carvediloltablet6.25 mgoralMylan Pharmaceuticals Ulc2010-03-30Not applicableCanada
Mylan-carvediloltablet3.125 mgoralMylan Pharmaceuticals Ulc2010-03-30Not applicableCanada
Novo-carvedilol Tabletstablet3.125 mgoralNovopharm Limited2003-12-022015-10-26Canada
Novo-carvedilol Tabletstablet6.25 mgoralNovopharm Limited2003-11-282015-10-26Canada
Novo-carvedilol Tabletstablet25 mgoralNovopharm Limited2003-11-282015-10-26Canada
Novo-carvedilol Tabletstablet12.5 mgoralNovopharm Limited2003-11-282015-10-26Canada
Ntp-carvediloltablet25 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-carvediloltablet12.5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-carvediloltablet6.25 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-carvediloltablet3.125 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-carvediloltablet25 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-carvediloltablet12.5 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-carvediloltablet6.25 mgoralNu Pharm IncNot applicableNot applicableCanada
Nu-carvediloltablet3.125 mgoralNu Pharm IncNot applicableNot applicableCanada
PMS-carvediloltablet12.5 mgoralPharmascience Inc2003-08-04Not applicableCanada
PMS-carvediloltablet6.25 mgoralPharmascience Inc2003-08-04Not applicableCanada
PMS-carvediloltablet3.125 mgoralPharmascience Inc2003-08-04Not applicableCanada
PMS-carvediloltablet25 mgoralPharmascience Inc2003-08-04Not applicableCanada
Ran-carvediloltablet25 mgoralRanbaxy Pharmaceuticals Canada Inc.2005-07-22Not applicableCanada
Ran-carvediloltablet12.5 mgoralRanbaxy Pharmaceuticals Canada Inc.2005-07-22Not applicableCanada
Ran-carvediloltablet6.25 mgoralRanbaxy Pharmaceuticals Canada Inc.2005-07-22Not applicableCanada
Ran-carvediloltablet3.125 mgoralRanbaxy Pharmaceuticals Canada Inc.2005-07-22Not applicableCanada
Ratio-carvediloltablet25 mgoralTeva Canada Limited2004-05-04Not applicableCanada
Ratio-carvediloltablet12.5 mgoralTeva Canada Limited2004-05-04Not applicableCanada
Ratio-carvediloltablet6.25 mgoralTeva Canada Limited2004-05-04Not applicableCanada
Ratio-carvediloltablet3.125 mgoralTeva Canada Limited2004-05-04Not applicableCanada
Zym-carvediloltablet3.125 mgoralZymcan Pharmaceuticals Inc2009-12-292014-06-16Canada
Zym-carvediloltablet6.25 mgoralZymcan Pharmaceuticals Inc2009-12-292014-06-16Canada
Zym-carvediloltablet25 mgoralZymcan Pharmaceuticals Inc2009-12-292014-06-16Canada
Zym-carvediloltablet12.5 mgoralZymcan Pharmaceuticals Inc2009-12-292014-06-16Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-carvediloltablet3.125 mgoralApotex Inc2003-08-06Not applicableCanada
Apo-carvediloltablet6.25 mgoralApotex Inc2003-08-06Not applicableCanada
Apo-carvediloltablet25 mgoralApotex Inc2003-08-06Not applicableCanada
Apo-carvediloltablet12.5 mgoralApotex Inc2003-08-06Not applicableCanada
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralClinical Solutions Wholesale, Llc2010-06-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralProficient Rx LP2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralSun Pharmaceutical Industries, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2015-04-16Not applicableUs
Carvediloltablet, film coated25 mg/1oralBlue Point Laboratories2014-04-22Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralApotex Corp.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAurobindo Pharma Limited2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralGlenmark Pharmaceuticals Inc., Usa2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralbryant ranch prepack2009-03-23Not applicableUs
Carvediloltablet, film coated25 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralBlue Point Laboratories2014-04-22Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralPreferred Pharmaceuticals, Inc.2013-03-27Not applicableUs
Carvediloltablet3.125 mg/1oralCipla USA Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralLegacy Pharmaceutical Packaging2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAvera Mc Kennan Hospital2015-10-19Not applicableUs
Carvediloltablet6.25 mg/1oralCipla USA Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-03-112016-04-05Us
Carvediloltablet, film coated6.25 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Carvediloltablet12.5 mg/1oralMajor Pharmaceuticals2010-06-18Not applicableUs
Carvediloltablet25 mg/1oralMajor Pharmaceuticals2010-06-04Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralPd Rx Pharmaceuticals, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralTeva Pharmaceuticals USA Inc2007-09-06Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2013-03-292016-04-05Us
Carvediloltablet, film coated25 mg/1oralAidarex Pharmaceuticals LLC2007-09-05Not applicableUs
Carvediloltablet3.125 mg/1oralREMEDYREPACK INC.2011-08-02Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2013-05-13Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2013-03-25Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralUnit Dose Services2007-09-05Not applicableUs
Carvediloltablet12.5 mg/1oralH.J. Harkins Company, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralCardinal Health2010-06-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-05-15Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralDr. Reddy's Laboratories Limited2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralSun Pharmaceutical Industries, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2011-02-18Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralHikma Pharmaceutical2007-10-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralCadila Healthcare Limited2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Carvediloltablet, film coated25 mg/1oralAmerican Health Packaging2008-07-032015-11-30Us
Carvediloltablet, film coated25 mg/1oralPreferred Pharmaceuticals,Inc.2014-12-03Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2013-12-11Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAvera Mc Kennan Hospital2015-11-11Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralREMEDYREPACK INC.2013-03-112016-04-05Us
Carvediloltablet, film coated3.125 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Carvediloltablet, film coated25 mg/1oralSandoz Inc2007-09-06Not applicableUs
Carvediloltablet, film coated25 mg/1oralMylan Pharmaceuticals Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralPd Rx Pharmaceuticals, Inc.2009-03-23Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-05-14Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralREMEDYREPACK INC.2013-07-082016-04-05Us
Carvediloltablet, film coated6.25 mg/1oralNorthwind Pharmaceuticals, LLC2015-02-09Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralLucid Pharma Llc2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCardinal Health2010-06-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralPhysicians Total Care, Inc.2007-09-17Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralSun Pharmaceutical Industries, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralCardinal Health2011-02-18Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralHikma Pharmaceutical2007-10-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralClinical Solutions Wholesale, Llc2010-06-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralProficient Rx LP2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralSt Marys Medical Park Pharmacy2013-04-25Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralBlue Point Laboratories2014-04-22Not applicableUs
Carvediloltablet, film coated25 mg/1oralMc Kesson Contract Packaging2011-09-21Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralPreferred Pharmaceuticals, Inc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralUnit Dose Services2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAvera Mc Kennan Hospital2015-11-10Not applicableUs
Carvediloltablet, film coated25 mg/1oralAurolife Pharma LLC2009-03-23Not applicableUs
Carvediloltablet, film coated25 mg/1oralMajor Pharmaceuticals2012-11-14Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralSandoz Inc2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralMylan Pharmaceuticals Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralPd Rx Pharmaceuticals, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet12.5 mg/1oralREMEDYREPACK INC.2012-01-17Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-05-13Not applicableUs
Carvediloltablet, film coated12.5 mg/301oralNorthwind Pharmaceuticals2014-05-16Not applicableUs
Carvediloltablet3.125 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralLucid Pharma Llc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralCardinal Health2010-06-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralPhysicians Total Care, Inc.2009-08-12Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralSun Pharmaceutical Industries, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCardinal Health2011-02-18Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralHikma Pharmaceutical2007-10-01Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralClinical Solutions Wholesale, Llc2010-06-01Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralProficient Rx LP2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralSt Marys Medical Park Pharmacy2013-04-25Not applicableUs
Carvediloltablet12.5 mg/1oralRed Pharm Drug Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCadila Healthcare Limited2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralGlenmark Pharmaceuticals Inc., Usa2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAurolife Pharma LLC2009-03-23Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralMajor Pharmaceuticals2012-11-14Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralSandoz Inc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralMylan Pharmaceuticals Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralAv Kare, Inc.2014-01-14Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-05-10Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-12-112016-04-05Us
Carvediloltablet, film coated25 mg/1oralMylan Institutional Inc.2007-09-14Not applicableUs
Carvediloltablet25 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralLucid Pharma Llc2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2010-06-01Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralPhysicians Total Care, Inc.2007-09-24Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2008-07-03Not applicableUs
Carvediloltablet, film coated25 mg/1oralHikma Pharmaceutical2007-10-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralClinical Solutions Wholesale, Llc2010-06-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralProficient Rx LP2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralSt Marys Medical Park Pharmacy2013-04-25Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralMed Vantx, Inc.2007-09-06Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralCadila Healthcare Limited2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralGlenmark Pharmaceuticals Inc., Usa2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAmerican Health Packaging2014-12-15Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralMc Kesson Contract Packaging2011-09-21Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralPreferred Pharmaceuticals, Inc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralUnit Dose Services2009-03-23Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAvera Mc Kennan Hospital2015-11-04Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAurolife Pharma LLC2009-03-23Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralMajor Pharmaceuticals2012-11-14Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralSandoz Inc2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralMylan Pharmaceuticals Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAv Kare, Inc.2014-01-14Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralREMEDYREPACK INC.2013-03-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralREMEDYREPACK INC.2013-03-18Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralMylan Institutional Inc.2007-09-14Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralLucid Pharma Llc2007-09-05Not applicableUs
Carvediloltablet25 mg/1oralCardinal Health2010-06-04Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralPhysicians Total Care, Inc.2007-11-09Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralClinical Solutions Wholesale2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralClinical Solutions Wholesale, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralProficient Rx LP2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralSt Marys Medical Park Pharmacy2013-04-25Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralMed Vantx, Inc.2011-09-13Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCadila Healthcare Limited2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralZydus Pharmaceuticals (USA) Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAmerican Health Packaging2008-07-032016-02-29Us
Carvediloltablet, film coated6.25 mg/1oralMc Kesson Contract Packaging2011-09-22Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralPreferred Pharmaceuticals, Inc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralSolco Healthcare US LLC2010-06-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAv Kare, Inc.2014-01-14Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAidarex Pharmaceuticals LLC2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-03-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-02-092016-04-05Us
Carvediloltablet, film coated6.25 mg/1oralMylan Institutional Inc.2007-09-14Not applicableUs
Carvediloltablet12.5 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralREMEDYREPACK INC.2014-03-19Not applicableUs
Carvediloltablet, film coated25 mg/1oralDr. Reddy's Laboratories Limited2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralState of Florida DOH Central Pharmacy2014-11-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralClinical Solutions Wholesale2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralClinical Solutions Wholesale, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralDIRECT RX2014-01-01Not applicableUs
Carvediloltablet, film coated25 mg/1oralApotex Corp.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralAurobindo Pharma Limited2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralbryant ranch prepack2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralZydus Pharmaceuticals (USA) Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAmerican Health Packaging2008-07-032016-01-31Us
Carvediloltablet, film coated3.125 mg/1oralMc Kesson Contract Packaging2011-09-20Not applicableUs
Carvediloltablet, film coated25 mg/1oralLegacy Pharmaceutical Packaging2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralSolco Healthcare US LLC2010-06-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralPd Rx Pharmaceuticals, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAurolife Pharma LLC2009-03-23Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralMajor Pharmaceuticals2012-11-14Not applicableUs
Carvediloltablet, film coated25 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-09-06Not applicableUs
Carvediloltablet, film coated25 mg/1oralTeva Pharmaceuticals USA Inc2007-09-06Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-04-02Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralMylan Institutional Inc.2007-09-14Not applicableUs
Carvediloltablet6.25 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralREMEDYREPACK INC.2013-05-22Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralDr. Reddy's Laboratories Limited2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCardinal Health2008-07-03Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralClinical Solutions Wholesale2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralClinical Solutions Wholesale, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2015-12-16Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralApotex Corp.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAurobindo Pharma Limited2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralbryant ranch prepack2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralZydus Pharmaceuticals (USA) Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAmerican Health Packaging2008-07-03Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralPreferred Pharmaceuticals,Inc.2012-06-04Not applicableUs
Carvediloltablet, film coated25 mg/1oralLegacy Pharmaceutical Packaging2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralSolco Healthcare US LLC2010-06-01Not applicableUs
Carvediloltablet25 mg/1oralCipla USA Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Carvediloltablet6.25 mg/1oralMajor Pharmaceuticals2010-06-18Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralTeva Pharmaceuticals USA Inc2007-09-06Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralAv Kare, Inc.2014-01-14Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralAidarex Pharmaceuticals LLC2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-04-152016-04-05Us
Carvediloltablet, film coated6.25 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralDr. Reddy's Laboratories Limited2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralCardinal Health2011-02-18Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralCardinal Health2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralClinical Solutions Wholesale2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralClinical Solutions Wholesale, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2015-05-15Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralApotex Corp.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAurobindo Pharma Limited2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralbryant ranch prepack2009-03-23Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralZydus Pharmaceuticals (USA) Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralBlue Point Laboratories2014-04-22Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralPreferred Pharmaceuticals, Inc.2012-10-01Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralLegacy Pharmaceutical Packaging2007-09-05Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralSolco Healthcare US LLC2010-06-01Not applicableUs
Carvediloltablet12.5 mg/1oralCipla USA Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated12.5 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Carvediloltablet3.125 mg/1oralMajor Pharmaceuticals2010-06-07Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralTeva Pharmaceuticals USA Inc2007-09-06Not applicableUs
Carvediloltablet, film coated3.125 mg/1oralRebel Distributors Corp2009-03-23Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralAidarex Pharmaceuticals LLC2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-04-112016-04-05Us
Carvediloltablet, film coated25 mg/1oralAphena Pharma Solutions Tennessee, Llc2007-09-05Not applicableUs
Carvediloltablet, film coated25 mg/1oralREMEDYREPACK INC.2013-03-052016-04-05Us
Carvediloltablet, film coated3.125 mg/1oralUnit Dose Services2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralH.J. Harkins Company, Inc.2007-09-05Not applicableUs
Carvediloltablet, film coated6.25 mg/1oralREMEDYREPACK INC.2013-05-16Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
COREGCRNot Available
Brand mixtures
NameLabellerIngredients
Hypertenevide-12.5Physician Therapeutics Llc
Salts
Name/CASStructureProperties
Carvedilol phosphate
ThumbNot applicableDBSALT001201
Categories
UNII0K47UL67F2
CAS number72956-09-3
WeightAverage: 406.4742
Monoisotopic: 406.18925733
Chemical FormulaC24H26N2O4
InChI KeyInChIKey=OGHNVEJMJSYVRP-UHFFFAOYSA-N
InChI
InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
IUPAC Name
1-(9H-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol
SMILES
COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=C1C1=CC=CC=C1N2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassCarbazoles
Direct ParentCarbazoles
Alternative Parents
Substituents
  • Carbazole
  • Indole
  • Methoxybenzene
  • Phenol ether
  • Anisole
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Pyrrole
  • Secondary alcohol
  • 1,2-aminoalcohol
  • Azacycle
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin.
PharmacodynamicsCarvedilol is a nonselective beta-adrenergic blocking agent with alpha1-blocking activity and is indicated for the treatment of hypertension and mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Carvedilol is a racemic mixture in which nonselective b-adrenoreceptor blocking activity is present in the S(-) enantiomer and a-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol has no intrinsic sympathomimetic activity. The effect of carvedilol's b-adrenoreceptor blocking activity has been demonstrated in animal and human studies showing that carvedilol (1) reduces cardiac output in normal subjects; (2) reduces exercise-and/or isoproterenol-induced tachycardia and (3) reduces reflex orthostatic tachycardia.
Mechanism of actionCarvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol's beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca2+ in OH- free radical-treated myocardium. Carvedilol and its metabolites also prevent OH- radical-induced decrease in sarcoplasmic reticulum Ca2+-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage.
Related Articles
AbsorptionCarvedilol is rapidly and extensively absorbed following oral administration, with an absolute bioavailability of approximately 25% to 35% due to a significant degree of first-pass metabolism.
Volume of distribution
  • 115 L
Protein binding98%
Metabolism

Hepatic. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. Demethylation and hydroxylation at the phenol ring produce three active metabolites with b-receptor blocking activity. The 4'-hydroxyphenyl metabolite is approximately 13 times more potent than carvedilol for b-blockade.

SubstrateEnzymesProduct
Carvedilol
8-HydroxycarvedilolDetails
Carvedilol
4'-HydroxycarvedilolDetails
Carvedilol
5'-HydroxycarvedilolDetails
Carvedilol
O-DesmethylcarvedilolDetails
Carvedilol
1-HydroxycarvedilolDetails
Carvedilol
Not Available
4'-hydroxyphenyl CarvedilolDetails
Route of eliminationCarvedilol is extensively metabolized. Less than 2% of the dose was excreted unchanged in the urine. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. The metabolites of carvedilol are excreted primarily via the bile into the feces.
Half life7-10 hours
Clearance
  • 500-700 mL/min
ToxicityNot expected to be toxic following ingestion.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Carvedilol Action PathwayDrug actionSMP00367
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Beta-1 adrenergic receptor
Gene symbol: ADRB1
UniProt: P08588
rs1801253 Not AvailableC AlleleImproved response to blood pressure medication12844134
Beta-1 adrenergic receptor
Gene symbol: ADRB1
UniProt: P08588
rs1801252 Not AvailableA AlleleImproved response to blood pressure medication12844134
Beta-1 adrenergic receptor
Gene symbol: ADRB1
UniProt: P08588
rs1801253 Not AvailableG > CBetter response to drug therapy22192668
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9706
Blood Brain Barrier-0.6814
Caco-2 permeable-0.6308
P-glycoprotein substrateSubstrate0.8552
P-glycoprotein inhibitor INon-inhibitor0.8729
P-glycoprotein inhibitor IINon-inhibitor0.6521
Renal organic cation transporterNon-inhibitor0.5405
CYP450 2C9 substrateNon-substrate0.7517
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.5408
CYP450 1A2 substrateInhibitor0.524
CYP450 2C9 inhibitorNon-inhibitor0.8496
CYP450 2D6 inhibitorNon-inhibitor0.7274
CYP450 2C19 inhibitorNon-inhibitor0.5676
CYP450 3A4 inhibitorNon-inhibitor0.6352
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6048
Ames testNon AMES toxic0.8261
CarcinogenicityNon-carcinogens0.9692
BiodegradationNot ready biodegradable0.963
Rat acute toxicity2.4566 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5725
hERG inhibition (predictor II)Inhibitor0.8889
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral12.5 mg/1
Tabletoral25 mg/1
Tabletoral25.0 mg
Tabletoral3.125 mg/1
Tabletoral6.25 mg/1
Tablet, film coatedoral12.5 mg/301
Tablet, film coatedoral12.5 mg/1
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral3.125 mg/1
Tablet, film coatedoral6.25 mg/1
Capsule, extended releaseoral10 mg/1
Capsule, extended releaseoral20 mg/1
Capsule, extended releaseoral40 mg/1
Capsule, extended releaseoral80 mg/1
Tabletoral50 mg
Kit
Tabletoral12.5 mg
Tabletoral25 mg
Tabletoral3.125 mg
Tabletoral6.25 mg
Prices
Unit descriptionCostUnit
Coreg CR 10 mg 24 Hour Capsule4.77USD capsule
Coreg CR 20 mg 24 Hour Capsule4.77USD capsule
Coreg CR 40 mg 24 Hour Capsule4.77USD capsule
Coreg CR 80 mg 24 Hour Capsule4.77USD capsule
Coreg cr 10 mg capsule4.59USD capsule
Coreg cr 20 mg capsule4.59USD capsule
Coreg cr 40 mg capsule4.59USD capsule
Coreg cr 80 mg capsule4.59USD capsule
Coreg 12.5 mg tablet2.54USD tablet
Coreg 25 mg tablet2.54USD tablet
Coreg 3.125 mg tablet2.54USD tablet
Coreg 6.25 mg tablet2.54USD tablet
Carvedilol 12.5 mg tablet2.18USD tablet
Carvedilol 25 mg tablet2.18USD tablet
Carvedilol 3.125 mg tablet2.18USD tablet
Carvedilol 6.25 mg tablet2.18USD tablet
Apo-Carvedilol 12.5 mg Tablet0.84USD tablet
Apo-Carvedilol 25 mg Tablet0.84USD tablet
Apo-Carvedilol 3.125 mg Tablet0.84USD tablet
Apo-Carvedilol 6.25 mg Tablet0.84USD tablet
Phl-Carvedilol 12.5 mg Tablet0.79USD tablet
Phl-Carvedilol 3.125 mg Tablet0.79USD tablet
Phl-Carvedilol 6.25 mg Tablet0.79USD tablet
Pms-Carvedilol 12.5 mg Tablet0.79USD tablet
Pms-Carvedilol 25 mg Tablet0.79USD tablet
Pms-Carvedilol 3.125 mg Tablet0.79USD tablet
Pms-Carvedilol 6.25 mg Tablet0.79USD tablet
Ran-Carvedilol 12.5 mg Tablet0.79USD tablet
Ran-Carvedilol 25 mg Tablet0.79USD tablet
Ran-Carvedilol 3.125 mg Tablet0.79USD tablet
Ran-Carvedilol 6.25 mg Tablet0.79USD tablet
Ratio-Carvedilol 12.5 mg Tablet0.79USD tablet
Ratio-Carvedilol 25 mg Tablet0.79USD tablet
Ratio-Carvedilol 3.125 mg Tablet0.79USD tablet
Ratio-Carvedilol 6.25 mg Tablet0.79USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6022562 Yes1996-04-172016-04-17Us
US7268156 Yes2003-12-272023-12-27Us
US8101209 Yes2006-03-112026-03-11Us
USRE40000 Yes1995-12-072015-12-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point114.5 °CPhysProp
water solubilityPractically insoluble (0.583 mg/L)Not Available
logP4.19AVDEEF,A (1997)
Predicted Properties
PropertyValueSource
Water Solubility0.00444 mg/mLALOGPS
logP3.05ALOGPS
logP3.42ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)14.03ChemAxon
pKa (Strongest Basic)8.74ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area75.74 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity115.64 m3·mol-1ChemAxon
Polarizability45.03 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Ilan Kor, “Crystalline solids of carvedilol and processes for their preparation.” U.S. Patent US20030166702, issued September 04, 2003.

US20030166702
General References
  1. Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Staiger C, Holcslaw TL, Amann-Zalan I, DeMets DL: Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study. Circulation. 2002 Oct 22;106(17):2194-9. [PubMed:12390947 ]
  2. Packer M, Coats AJ, Fowler MB, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Castaigne A, Roecker EB, Schultz MK, DeMets DL: Effect of carvedilol on survival in severe chronic heart failure. N Engl J Med. 2001 May 31;344(22):1651-8. [PubMed:11386263 ]
  3. Vanderhoff BT, Ruppel HM, Amsterdam PB: Carvedilol: the new role of beta blockers in congestive heart failure. Am Fam Physician. 1998 Nov 1;58(7):1627-34, 1641-2. [PubMed:9824960 ]
External Links
ATC CodesC07AG02
AHFS Codes
  • 24:04.00
  • 24:24.00
PDB EntriesNot Available
FDA labelDownload (1.25 MB)
MSDSDownload (32.9 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Carvedilol can be increased when it is combined with Abiraterone.
AcepromazineAcepromazine may increase the hypotensive activities of Carvedilol.
AcetylcholineThe risk or severity of adverse effects can be increased when Carvedilol is combined with Acetylcholine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Carvedilol.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Carvedilol.
AlfuzosinCarvedilol may increase the orthostatic hypotensive activities of Alfuzosin.
AmifostineCarvedilol may increase the hypotensive activities of Amifostine.
AmiodaroneThe serum concentration of Carvedilol can be increased when it is combined with Amiodarone.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Carvedilol.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Carvedilol.
BretyliumBretylium may increase the bradycardic activities of Carvedilol.
BrimonidineBrimonidine may increase the antihypertensive activities of Carvedilol.
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Carvedilol.
ButabarbitalThe serum concentration of Carvedilol can be decreased when it is combined with Butabarbital.
ButethalThe serum concentration of Carvedilol can be decreased when it is combined with Butethal.
CabergolineCarvedilol may increase the vasoconstricting activities of Cabergoline.
CapecitabineThe serum concentration of Carvedilol can be increased when it is combined with Capecitabine.
CarbacholThe risk or severity of adverse effects can be increased when Carvedilol is combined with Carbachol.
CeritinibCarvedilol may increase the bradycardic activities of Ceritinib.
ChloroquineThe metabolism of Carvedilol can be decreased when combined with Chloroquine.
ChlorpropamideCarvedilol may increase the hypoglycemic activities of Chlorpropamide.
CimetidineThe serum concentration of Carvedilol can be increased when it is combined with Cimetidine.
CobicistatThe serum concentration of Carvedilol can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Carvedilol.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Carvedilol.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Carvedilol.
DarunavirThe serum concentration of Carvedilol can be increased when it is combined with Darunavir.
DiazoxideDiazoxide may increase the hypotensive activities of Carvedilol.
DigoxinDigoxin may increase the bradycardic activities of Carvedilol.
DipivefrinDipivefrin may increase the atrioventricular blocking (AV block) activities of Carvedilol.
DipyridamoleDipyridamole may increase the bradycardic activities of Carvedilol.
DisopyramideDisopyramide may increase the bradycardic activities of Carvedilol.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Carvedilol.
DronedaroneDronedarone may increase the bradycardic activities of Carvedilol.
DuloxetineCarvedilol may increase the orthostatic hypotensive activities of Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Carvedilol.
EfavirenzThe serum concentration of Carvedilol can be increased when it is combined with Efavirenz.
EsmololEsmolol may increase the bradycardic activities of Carvedilol.
EtravirineThe serum concentration of Carvedilol can be increased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Carvedilol.
FingolimodCarvedilol may increase the bradycardic activities of Fingolimod.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Carvedilol.
FloxuridineThe serum concentration of Carvedilol can be increased when it is combined with Floxuridine.
FluconazoleThe serum concentration of Carvedilol can be increased when it is combined with Fluconazole.
FluorouracilThe serum concentration of Carvedilol can be increased when it is combined with Fluorouracil.
FluoxetineThe metabolism of Carvedilol can be decreased when combined with Fluoxetine.
FluvastatinThe serum concentration of Carvedilol can be increased when it is combined with Fluvastatin.
GemfibrozilThe serum concentration of Carvedilol can be increased when it is combined with Gemfibrozil.
HeptabarbitalThe serum concentration of Carvedilol can be decreased when it is combined with Heptabarbital.
HexobarbitalThe serum concentration of Carvedilol can be decreased when it is combined with Hexobarbital.
InfliximabInfliximab may decrease the antihypertensive activities of Carvedilol.
IrbesartanThe serum concentration of Carvedilol can be increased when it is combined with Irbesartan.
IvabradineCarvedilol may increase the bradycardic activities of Ivabradine.
KetoconazoleThe serum concentration of Carvedilol can be increased when it is combined with Ketoconazole.
LacosamideCarvedilol may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Carvedilol.
LeflunomideThe serum concentration of Carvedilol can be increased when it is combined with Leflunomide.
LevodopaCarvedilol may increase the orthostatic hypotensive activities of Levodopa.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Carvedilol.
LosartanThe serum concentration of Carvedilol can be increased when it is combined with Losartan.
LumacaftorThe serum concentration of Carvedilol can be decreased when it is combined with Lumacaftor.
MepivacaineThe serum concentration of Mepivacaine can be increased when it is combined with Carvedilol.
MethacholineThe risk or severity of adverse effects can be increased when Carvedilol is combined with Methacholine.
MethohexitalThe serum concentration of Carvedilol can be decreased when it is combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Carvedilol.
MidodrineCarvedilol may increase the bradycardic activities of Midodrine.
MolsidomineMolsidomine may increase the hypotensive activities of Carvedilol.
MoxonidineMoxonidine may increase the hypotensive activities of Carvedilol.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Carvedilol.
NicardipineNicardipine may increase the hypotensive activities of Carvedilol.
NicorandilNicorandil may increase the hypotensive activities of Carvedilol.
NifedipineNifedipine may increase the hypotensive activities of Carvedilol.
ObinutuzumabCarvedilol may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Carvedilol.
OmeprazoleThe serum concentration of Carvedilol can be increased when it is combined with Omeprazole.
OrciprenalineCarvedilol may decrease the activities of Orciprenaline.
PanobinostatThe serum concentration of Carvedilol can be increased when it is combined with Panobinostat.
ParoxetineThe serum concentration of Carvedilol can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Carvedilol.
Peginterferon alfa-2bThe serum concentration of Carvedilol can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe serum concentration of Carvedilol can be decreased when it is combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Carvedilol.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Carvedilol.
PrazosinCarvedilol may increase the orthostatic hypotensive activities of Prazosin.
PrimidoneThe serum concentration of Carvedilol can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Carvedilol can be increased when it is combined with Propafenone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Carvedilol.
PyrimethamineThe serum concentration of Carvedilol can be increased when it is combined with Pyrimethamine.
QuinineThe serum concentration of Carvedilol can be increased when it is combined with Quinine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Carvedilol.
RegorafenibRegorafenib may increase the bradycardic activities of Carvedilol.
ReserpineReserpine may increase the hypotensive activities of Carvedilol.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Carvedilol.
RisperidoneCarvedilol may increase the hypotensive activities of Risperidone.
RitonavirThe metabolism of Carvedilol can be decreased when combined with Ritonavir.
RituximabCarvedilol may increase the hypotensive activities of Rituximab.
RivastigmineRivastigmine may increase the bradycardic activities of Carvedilol.
RuxolitinibRuxolitinib may increase the bradycardic activities of Carvedilol.
SaquinavirThe serum concentration of Carvedilol can be increased when it is combined with Saquinavir.
SecobarbitalThe serum concentration of Carvedilol can be decreased when it is combined with Secobarbital.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Carvedilol.
SorafenibThe serum concentration of Carvedilol can be increased when it is combined with Sorafenib.
SufentanilSufentanil may increase the bradycardic activities of Carvedilol.
SulfadiazineThe serum concentration of Carvedilol can be increased when it is combined with Sulfadiazine.
SulfisoxazoleThe serum concentration of Carvedilol can be increased when it is combined with Sulfisoxazole.
TacrineTacrine may increase the bradycardic activities of Carvedilol.
TadalafilTadalafil may increase the antihypertensive activities of Carvedilol.
TesmilifeneThe serum concentration of Carvedilol can be decreased when it is combined with Tesmilifene.
TheophyllineCarvedilol may decrease the activities of Theophylline.
TicagrelorThe serum concentration of Carvedilol can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Carvedilol can be decreased when combined with Ticlopidine.
TofacitinibTofacitinib may increase the bradycardic activities of Carvedilol.
TolbutamideThe serum concentration of Carvedilol can be increased when it is combined with Tolbutamide.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Carvedilol.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Carvedilol.
TreprostinilTreprostinil may increase the hypotensive activities of Carvedilol.
TrimethoprimThe serum concentration of Carvedilol can be increased when it is combined with Trimethoprim.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Carvedilol.
VardenafilVardenafil may increase the antihypertensive activities of Carvedilol.
VerapamilThe serum concentration of Carvedilol can be increased when it is combined with Verapamil.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Carvedilol.
VoriconazoleThe serum concentration of Carvedilol can be increased when it is combined with Voriconazole.
YohimbineYohimbine may decrease the antihypertensive activities of Carvedilol.
ZafirlukastThe serum concentration of Carvedilol can be increased when it is combined with Zafirlukast.
Food Interactions
  • Take with food, food slows the absorption rate and reduces the incidence of adverse effects (extent of absorption is not affected).

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Nichols AJ, Gellai M, Ruffolo RR Jr: Studies on the mechanism of arterial vasodilation produced by the novel antihypertensive agent, carvedilol. Fundam Clin Pharmacol. 1991;5(1):25-38. [PubMed:1712335 ]
  2. Nichols AJ, Sulpizio AC, Ashton DJ, Hieble JP, Ruffolo RR Jr: In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilol. Pharmacology. 1989;39(5):327-36. [PubMed:2575762 ]
  3. Nichols AJ, Sulpizio AC, Ashton DJ, Hieble JP, Ruffolo RR Jr: The interaction of the enantiomers of carvedilol with alpha 1- and beta 1-adrenoceptors. Chirality. 1989;1(4):265-70. [PubMed:2577144 ]
  4. de Mey C, Breithaupt K, Schloos J, Neugebauer G, Palm D, Belz GG: Dose-effect and pharmacokinetic-pharmacodynamic relationships of the beta 1-adrenergic receptor blocking properties of various doses of carvedilol in healthy humans. Clin Pharmacol Ther. 1994 Mar;55(3):329-37. [PubMed:7908256 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Nadh dehydrogenase (ubiquinone) activity
Specific Function:
Accessory subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I), that is believed not to be involved in catalysis. Complex I functions in the transfer of electrons from NADH to the respiratory chain. The immediate electron acceptor for the enzyme is believed to be ubiquinone.
Gene Name:
NDUFC2
Uniprot ID:
O95298
Molecular Weight:
14187.33 Da
References
  1. Oliveira PJ, Santos DJ, Moreno AJ: Carvedilol inhibits the exogenous NADH dehydrogenase in rat heart mitochondria. Arch Biochem Biophys. 2000 Feb 15;374(2):279-85. [PubMed:10666308 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Irodova NL, Krasnikova TL, Masenko VP, Kochetov AG, Chazova IE: [Carvedilol in treating primary pulmonary hypertension patients: effect on severity of cardiac failure, degree of pulmonary hypertension, concentration of catecholamines in blood plasma and dependence of cyclic AMP synthesis in lymphocytes on beta-adrenergic receptors]. Ter Arkh. 2002;74(8):30-4. [PubMed:12360591 ]
  2. Maebara C, Ohtani H, Sugahara H, Mine K, Kubo C, Sawada Y: Nightmares and panic disorder associated with carvedilol overdose. Ann Pharmacother. 2002 Nov;36(11):1736-40. [PubMed:12398570 ]
  3. Okajima K, Harada N, Uchiba M, Isobe H: Activation of capsaicin-sensitive sensory neurons by carvedilol, a nonselective beta-blocker, in spontaneous hypertensive rats. J Pharmacol Exp Ther. 2004 May;309(2):684-91. Epub 2004 Feb 5. [PubMed:14764656 ]
  4. Nichols AJ, Gellai M, Ruffolo RR Jr: Studies on the mechanism of arterial vasodilation produced by the novel antihypertensive agent, carvedilol. Fundam Clin Pharmacol. 1991;5(1):25-38. [PubMed:1712335 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Vascular endothelial growth factor receptor binding
Specific Function:
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activ...
Gene Name:
VEGFA
Uniprot ID:
P15692
Molecular Weight:
27042.205 Da
References
  1. de Boer RA, Siebelink HJ, Tio RA, Boomsma F, van Veldhuisen DJ: Carvedilol increases plasma vascular endothelial growth factor (VEGF) in patients with chronic heart failure. Eur J Heart Fail. 2001 Jun;3(3):331-3. [PubMed:11378004 ]
  2. Saijonmaa O, Nyman T, Fyhrquist F: Carvedilol inhibits basal and stimulated ACE production in human endothelial cells. J Cardiovasc Pharmacol. 2004 May;43(5):616-21. [PubMed:15071347 ]
  3. Shyu KG, Lu MJ, Chang H, Sun HY, Wang BW, Kuan P: Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure. J Card Fail. 2005 Mar;11(2):152-9. [PubMed:15732037 ]
  4. Shyu KG, Liou JY, Wang BW, Fang WJ, Chang H: Carvedilol prevents cardiac hypertrophy and overexpression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in pressure-overloaded rat heart. J Biomed Sci. 2005;12(2):409-20. [PubMed:15942707 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Receptor binding
Specific Function:
Cardiac hormone which may function as a paracrine antifibrotic factor in the heart. Also plays a key role in cardiovascular homeostasis through natriuresis, diuresis, vasorelaxation, and inhibition of renin and aldosterone secretion. Specifically binds and stimulates the cGMP production of the NPR1 receptor. Binds the clearance receptor NPR3.
Gene Name:
NPPB
Uniprot ID:
P16860
Molecular Weight:
14725.825 Da
References
  1. Ohta Y, Watanabe K, Nakazawa M, Yamamoto T, Ma M, Fuse K, Ito M, Hirono S, Tanabe T, Hanawa H, Kato K, Kodama M, Aizawa Y: Carvedilol enhances atrial and brain natriuretic peptide mRNA expression and release in rat heart. J Cardiovasc Pharmacol. 2000;36 Suppl 2:S19-23. [PubMed:11206715 ]
  2. Richards AM, Doughty R, Nicholls MG, MacMahon S, Sharpe N, Murphy J, Espiner EA, Frampton C, Yandle TG: Plasma N-terminal pro-brain natriuretic peptide and adrenomedullin: prognostic utility and prediction of benefit from carvedilol in chronic ischemic left ventricular dysfunction. Australia-New Zealand Heart Failure Group. J Am Coll Cardiol. 2001 Jun 1;37(7):1781-7. [PubMed:11401111 ]
  3. Konishi H, Nishio S, Tsutamoto T, Minouchi T, Yamaji A: Serum carvedilol concentration and its relation to change in plasma brain natriuretic peptide level in the treatment of heart failure: a preliminary study. Int J Clin Pharmacol Ther. 2003 Dec;41(12):578-86. [PubMed:14692707 ]
  4. Takeda Y, Fukutomi T, Suzuki S, Yamamoto K, Ogata M, Kondo H, Sugiura M, Shigeyama J, Itoh M: Effects of carvedilol on plasma B-type natriuretic peptide concentration and symptoms in patients with heart failure and preserved ejection fraction. Am J Cardiol. 2004 Aug 15;94(4):448-53. [PubMed:15325927 ]
  5. Frantz RP, Olson LJ, Grill D, Moualla SK, Nelson SM, Nobrega TP, Hanna RD, Backes RJ, Mookadam F, Heublein D, Bailey KR, Burnett JC: Carvedilol therapy is associated with a sustained decline in brain natriuretic peptide levels in patients with congestive heart failure. Am Heart J. 2005 Mar;149(3):541-7. [PubMed:15864245 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
other
General Function:
Signal transducer activity
Specific Function:
Gap junction protein that acts as a regulator of bladder capacity. A gap junction consists of a cluster of closely packed pairs of transmembrane channels, the connexons, through which materials of low MW diffuse from one cell to a neighboring cell. May play a critical role in the physiology of hearing by participating in the recycling of potassium to the cochlear endolymph. Negative regulator o...
Gene Name:
GJA1
Uniprot ID:
P17302
Molecular Weight:
43008.005 Da
References
  1. Yeh HI, Lee PY, Su CH, Tian TY, Ko YS, Tsai CH: Reduced expression of endothelial connexins 43 and 37 in hypertensive rats is rectified after 7-day carvedilol treatment. Am J Hypertens. 2006 Feb;19(2):129-35. [PubMed:16448880 ]
  2. Fan SY, Ke YN, Zeng YJ, Wang Y, Cheng WL, Yang JR: [Effects and the mechanism of carvedilol on gap junctional intercellular communication in rat myocardium]. Zhonghua Xin Xue Guan Bing Za Zhi. 2005 Dec;33(12):1141-5. [PubMed:16563290 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. Karle CA, Kreye VA, Thomas D, Rockl K, Kathofer S, Zhang W, Kiehn J: Antiarrhythmic drug carvedilol inhibits HERG potassium channels. Cardiovasc Res. 2001 Feb 1;49(2):361-70. [PubMed:11164846 ]
  2. Kawakami K, Nagatomo T, Abe H, Kikuchi K, Takemasa H, Anson BD, Delisle BP, January CT, Nakashima Y: Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. [PubMed:16314852 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Primary amine oxidase activity
Specific Function:
Important in cell-cell recognition. Appears to function in leukocyte-endothelial cell adhesion. Interacts with integrin alpha-4/beta-1 (ITGA4/ITGB1) on leukocytes, and mediates both adhesion and signal transduction. The VCAM1/ITGA4/ITGB1 interaction may play a pathophysiologic role both in immune responses and in leukocyte emigration to sites of inflammation.
Gene Name:
VCAM1
Uniprot ID:
P19320
Molecular Weight:
81275.43 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Chen JW, Lin FY, Chen YH, Wu TC, Chen YL, Lin SJ: Carvedilol inhibits tumor necrosis factor-alpha-induced endothelial transcription factor activation, adhesion molecule expression, and adhesiveness to human mononuclear cells. Arterioscler Thromb Vasc Biol. 2004 Nov;24(11):2075-81. Epub 2004 Sep 16. [PubMed:15374848 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Koshimizu TA, Tsujimoto G, Hirasawa A, Kitagawa Y, Tanoue A: Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. [PubMed:15306222 ]
  2. Van Tassell BW, Rondina MT, Huggins F, Gilbert EM, Munger MA: Carvedilol increases blood pressure response to phenylephrine infusion in heart failure subjects with systolic dysfunction: evidence of improved vascular alpha1-adrenoreceptor signal transduction. Am Heart J. 2008 Aug;156(2):315-21. doi: 10.1016/j.ahj.2008.04.004. Epub 2008 Jun 20. [PubMed:18657662 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Koshimizu TA, Tsujimoto G, Hirasawa A, Kitagawa Y, Tanoue A: Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. [PubMed:15306222 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Koshimizu TA, Tsujimoto G, Hirasawa A, Kitagawa Y, Tanoue A: Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. [PubMed:15306222 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Koshimizu TA, Tsujimoto G, Hirasawa A, Kitagawa Y, Tanoue A: Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. [PubMed:15306222 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Koshimizu TA, Tsujimoto G, Hirasawa A, Kitagawa Y, Tanoue A: Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72. [PubMed:15306222 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transmembrane signaling receptor activity
Specific Function:
Cell-surface glycoprotein having a role in immunoadhesion. Mediates in the adhesion of blood neutrophils in cytokine-activated endothelium through interaction with PSGL1/SELPLG. May have a role in capillary morphogenesis.
Gene Name:
SELE
Uniprot ID:
P16581
Molecular Weight:
66654.575 Da
References
  1. Chen JW, Lin FY, Chen YH, Wu TC, Chen YL, Lin SJ: Carvedilol inhibits tumor necrosis factor-alpha-induced endothelial transcription factor activation, adhesion molecule expression, and adhesiveness to human mononuclear cells. Arterioscler Thromb Vasc Biol. 2004 Nov;24(11):2075-81. Epub 2004 Sep 16. [PubMed:15374848 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
modulator
General Function:
Ubiquitin protein ligase binding
Specific Function:
Functions as a master transcriptional regulator of the adaptive response to hypoxia. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia. Plays an essentia...
Gene Name:
HIF1A
Uniprot ID:
Q16665
Molecular Weight:
92669.595 Da
References
  1. Shyu KG, Lu MJ, Chang H, Sun HY, Wang BW, Kuan P: Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure. J Card Fail. 2005 Mar;11(2):152-9. [PubMed:15732037 ]

Enzymes

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. 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. 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:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Xanthine oxidase activity
Specific Function:
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro).
Gene Name:
XDH
Uniprot ID:
P47989
Molecular Weight:
146422.99 Da
References
  1. Yue TL, McKenna PJ, Gu JL, Cheng HY, Ruffolo RE Jr, Feuerstein GZ: Carvedilol, a new vasodilating beta adrenoceptor blocker antihypertensive drug, protects endothelial cells from damage initiated by xanthine-xanthine oxidase and neutrophils. Cardiovasc Res. 1994 Mar;28(3):400-6. [PubMed:7909721 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. 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 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. 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:
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. 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:
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 ]

Transporters

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 EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  2. Takara K, Kakumoto M, Tanigawara Y, Funakoshi J, Sakaeda T, Okumura K: Interaction of digoxin with antihypertensive drugs via MDR1. Life Sci. 2002 Feb 15;70(13):1491-500. [PubMed:11895100 ]
  3. Jonsson O, Behnam-Motlagh P, Persson M, Henriksson R, Grankvist K: Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. Biochem Pharmacol. 1999 Dec 1;58(11):1801-6. [PubMed:10571255 ]
  4. Neuhoff S, Langguth P, Dressler C, Andersson TB, Regardh CG, Spahn-Langguth H: Affinities at the verapamil binding site of MDR1-encoded P-glycoprotein: drugs and analogs, stereoisomers and metabolites. Int J Clin Pharmacol Ther. 2000 Apr;38(4):168-79. [PubMed:10783826 ]
  5. Hokama N, Hobara N, Sakai M, Kameya H, Ohshiro S, Sakanashi M: Influence of nicardipine and nifedipine on plasma carvedilol disposition after oral administration in rats. J Pharm Pharmacol. 2002 Jun;54(6):821-5. [PubMed:12078998 ]
  6. Kakumoto M, Sakaeda T, Takara K, Nakamura T, Kita T, Yagami T, Kobayashi H, Okamura N, Okumura K: Effects of carvedilol on MDR1-mediated multidrug resistance: comparison with verapamil. Cancer Sci. 2003 Jan;94(1):81-6. [PubMed:12708479 ]
  7. Brodde OE, Kroemer HK: Drug-drug interactions of beta-adrenoceptor blockers. Arzneimittelforschung. 2003;53(12):814-22. [PubMed:14732961 ]
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Drug created on June 13, 2005 07:24 / Updated on June 30, 2016 03:04