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CARVEDILOL Drug Record

  • Summary
  • Interactions
  • Claims
  • CARVEDILOL chembl:CHEMBL723 Approved

    Alternate Names:

    COREG
    EUCARDIC 3.125
    SKF-105517
    BM-14-190
    C07AG02
    DQ-2466
    EUCARDIC 12.5
    CARVEDILOL
    COREG CR
    BM-14.190
    BM-14190
    BM 14.190
    EUCARDIC 25
    EUCARDIC 6.25
    DQ 2466
    SKF 105517
    (+-)-1-(CARBAZOL-4-YLOXY)-3-((2-(O-METHOXYPHENOXY)ETHYL)AMINO)-2-PROPANOL
    CARVEDILOLUM
    drugbank:01136
    rxcui:20352
    chemidplus:72956-09-3
    chembl:CHEMBL723
    pubchem.compound:2585

    Drug Info:

    Drug Indications cardiovascular agent
    FDA Approval not approved
    Drug Class Small Molecule
    Drug Indications for treatment of congestive heart failure
    Year of Approval 1995
    Drug Class antihypertensive agents
    (5 More Sources)

    Publications:

    McCrink KA et al., 2016, β<sub>1</sub>-adrenoceptor Arg389Gly polymorphism confers differential β-arrestin-binding tropism in cardiac myocytes., Pharmacogenomics
    Rau T et al., 2012, Impact of the β1-adrenoceptor Arg389Gly polymorphism on heart-rate responses to bisoprolol and carvedilol in heart-failure patients., Clin Pharmacol Ther
    Huntgeburth M et al., 2011, The Arg389Gly β1-adrenoceptor gene polymorphism influences the acute effects of β-adrenoceptor blockade on contractility in the human heart., Clin Res Cardiol
    Baudhuin LM et al., 2010, Relation of ADRB1, CYP2D6, and UGT1A1 polymorphisms with dose of, and response to, carvedilol or metoprolol therapy in patients with chronic heart failure., Am J Cardiol
    Metra M et al., 2010, Role of beta-adrenergic receptor gene polymorphisms in the long-term effects of beta-blockade with carvedilol in patients with chronic heart failure., Cardiovasc Drugs Ther
    Filigheddu F et al., 2010, Haplotypes of the adrenergic system predict the blood pressure response to beta-blockers in women with essential hypertension., Pharmacogenomics
    Chen L et al., 2007, Arg389Gly-beta1-adrenergic receptors determine improvement in left ventricular systolic function in nonischemic cardiomyopathy patients with heart failure after chronic treatment with carvedilol., Pharmacogenet Genomics
    Lobmeyer MT et al., 2007, Synergistic polymorphisms of beta1 and alpha2C-adrenergic receptors and the influence on left ventricular ejection fraction response to beta-blocker therapy in heart failure., Pharmacogenet Genomics
    Liu J et al., 2006, beta1-Adrenergic receptor polymorphisms influence the response to metoprolol monotherapy in patients with essential hypertension., Clin Pharmacol Ther
    Terra SG et al., 2005, Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy., Pharmacogenet Genomics
    de Groote P et al., 2005, Association between beta-1 and beta-2 adrenergic receptor gene polymorphisms and the response to beta-blockade in patients with stable congestive heart failure., Pharmacogenet Genomics
    Terra SG et al., 2005, beta-Adrenergic receptor polymorphisms and responses during titration of metoprolol controlled release/extended release in heart failure., Clin Pharmacol Ther
    Liu et al., 2003, Gly389Arg polymorphism of beta1-adrenergic receptor is associated with the cardiovascular response to metoprolol., Clin. Pharmacol. Ther.
    Mialet Perez J et al., 2003, Beta 1-adrenergic receptor polymorphisms confer differential function and predisposition to heart failure., Nat Med
    White HL et al., 2003, An evaluation of the beta-1 adrenergic receptor Arg389Gly polymorphism in individuals with heart failure: a MERIT-HF sub-study., Eur J Heart Fail
    Johnson et al., 2003, Beta 1-adrenergic receptor polymorphisms and antihypertensive response to metoprolol., Clin. Pharmacol. Ther.
    Sofowora GG et al., 2003, A common beta1-adrenergic receptor polymorphism (Arg389Gly) affects blood pressure response to beta-blockade., Clin Pharmacol Ther
    Nichols et al., 1989, The interaction of the enantiomers of carvedilol with alpha 1- and beta 1-adrenoceptors., Chirality
    Nichols et al., 1989, In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilol., Pharmacology
    de Mey et al., 1994, 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.
    Nichols et al., 1991, Studies on the mechanism of arterial vasodilation produced by the novel antihypertensive agent, carvedilol., Fundam Clin Pharmacol
    Yeh et al., 2006, Reduced expression of endothelial connexins 43 and 37 in hypertensive rats is rectified after 7-day carvedilol treatment., Am. J. Hypertens.
    Fan et al., 2005, [Effects and the mechanism of carvedilol on gap junctional intercellular communication in rat myocardium]., Zhonghua Xin Xue Guan Bing Za Zhi
    Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.
    Sehrt D et al., 2011, Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics., Pharmacogenomics
    Kaye et al., 2003, Beta-adrenoceptor genotype influences the response to carvedilol in patients with congestive heart failure., Pharmacogenetics
    Maebara et al., 2002, Nightmares and panic disorder associated with carvedilol overdose., Ann Pharmacother
    Irodova et al., 2002, [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.
    Okajima et al., 2004, Activation of capsaicin-sensitive sensory neurons by carvedilol, a nonselective beta-blocker, in spontaneous hypertensive rats., J. Pharmacol. Exp. Ther.
    Yang et al., 2006, [Beneficial effects of carvedilol on cardiomyocyte apoptosis and bcl-2/bax expression after acute myocardial infarction an experiment with rats]., Zhonghua Yi Xue Za Zhi
    Zeng et al., 2003, Effects of carvedilol on cardiomyocyte apoptosis and gene expression in vivo after ischemia-reperfusion in rats., J. Huazhong Univ. Sci. Technol. Med. Sci.
    Oliveira et al., 2005, Are the antioxidant properties of carvedilol important for the protection of cardiac mitochondria?, Curr Vasc Pharmacol
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    O'Connell TD et al., 2013, Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance., Pharmacol Rev
    Jensen BC et al., 2009, {alpha}1-Adrenergic receptor subtypes in nonfailing and failing human myocardium., Circ Heart Fail
    Hryniewicz et al., 2003, Partial reversal of cachexia by beta-adrenergic receptor blocker therapy in patients with chronic heart failure., J. Card. Fail.
    Afonso et al., 2006, Carvedilol action is dependent on endogenous production of nitric oxide., Am. J. Hypertens.
    Oldham et al., 1997, In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol., Drug Metab. Dispos.
    Bajcetic et al., 2008, Effects of carvedilol on left ventricular function and oxidative stress in infants and children with idiopathic dilated cardiomyopathy: a 12-month, two-center, open-label study., Clin Ther
    Takekuma Y et al., 2006, Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol., J Pharm Pharm Sci
  • CARVEDILOL   GJA1

    Interaction Score: 1.72

    Interaction Types & Directionality:
    other/unknown

    Interaction Info:

    PMIDs:
    16448880 16563290


    Sources:
    NCI

  • CARVEDILOL   ADRB1

    Interaction Score: 1.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name carvedilol,Coreg
    Novel drug target Established target
    Mechanism of Interaction Adrenergic receptor beta antagonist

    PMIDs:
    27643874 22617224 21311897 20643254 20352314 20235788 18075464 17496726 16815314 15864115 15861037 15735607 14534524 14502278 12921807 12844134 12709726 2577144 2575762 7908256 1712335


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • CARVEDILOL   GSR

    Interaction Score: 0.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18498919


    Sources:
    NCI

  • CARVEDILOL   LEP

    Interaction Score: 0.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14966787


    Sources:
    NCI

  • CARVEDILOL   ADRB2

    Interaction Score: 0.35

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name carvedilol,Coreg
    Novel drug target Established target
    Direct Interaction yes

    PMIDs:
    21599570 20352314 15861037 12835612 12398570 12360591 14764656 1712335


    Sources:
    TdgClinicalTrial ChemblInteractions NCI TEND PharmGKB

  • CARVEDILOL   XDH

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15853634


    Sources:
    NCI

  • CARVEDILOL   UGT1A1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20643254 16849011


    Sources:
    PharmGKB

  • CARVEDILOL   ADRA1A

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)
    potentiator

    Interaction Info:
    Mechanism of Interaction Adrenergic receptor alpha-1 antagonist
    Direct Interaction yes
    Trial Name carvedilol, Coreg

    PMIDs:
    17016423 17139284 24368739 19919991


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • CARVEDILOL   BAX

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16759520 12973927


    Sources:
    NCI

  • CARVEDILOL   NOS1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16580580


    Sources:
    NCI

  • CARVEDILOL   ADRB3

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Adrenergic receptor beta antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CARVEDILOL   ADRA1B

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Adrenergic receptor alpha-1 antagonist
    Direct Interaction yes

    PMIDs:
    15306222


    Sources:
    ChemblInteractions

  • CARVEDILOL   DRD1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CARVEDILOL   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CARVEDILOL   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9280405


    Sources:
    NCI

  • CARVEDILOL   KDM4E

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CARVEDILOL   BAZ2B

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CARVEDILOL   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA

  • TEND: CARVEDILOL

    • Version: 01-August-2011

    Alternate Names:
    CARVEDILOL Primary Drug Name

    Drug Info:
    Drug Class antihypertensive agents
    Year of Approval 1995

    Publications:

  • TdgClinicalTrial: CARVEDILOL

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications for treatment of congestive heart failure
    Drug Class Small Molecule
    FDA Approval not approved

    Publications:

  • NCI: CARVEDILOL

    • Version: 14-September-2017

    Alternate Names:
    C28906 NCI drug code

    Drug Info:

    Publications:
    Afonso et al., 2006, Carvedilol action is dependent on endogenous production of nitric oxide., Am. J. Hypertens.
    Bajcetic et al., 2008, Effects of carvedilol on left ventricular function and oxidative stress in infants and children with idiopathic dilated cardiomyopathy: a 12-month, two-center, open-label study., Clin Ther
    Kaye et al., 2003, Beta-adrenoceptor genotype influences the response to carvedilol in patients with congestive heart failure., Pharmacogenetics

  • PharmGKB: carvedilol

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Baudhuin LM et al., 2010, Relation of ADRB1, CYP2D6, and UGT1A1 polymorphisms with dose of, and response to, carvedilol or metoprolol therapy in patients with chronic heart failure., Am J Cardiol
    Takekuma Y et al., 2006, Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol., J Pharm Pharm Sci
    Terra SG et al., 2005, Beta1-adrenergic receptor polymorphisms and left ventricular remodeling changes in response to beta-blocker therapy., Pharmacogenet Genomics

  • TTD: Carvedilol

    • Version: 2020.06.01

    Alternate Names:
    D0W9LX TTD Drug ID

    Drug Info:

    Publications:

  • DTC: CARVEDILOL

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL723 ChEMBL Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL723

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL723

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Carvedilol

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21