Details of the Drug

General Information of Drug (ID: DMHTEAO)

Drug Name
Carvedilol
Synonyms
Artist; Carvedilolum; Coreg; Coropres; Coropress; Dibloc; Dilatrend; Eucardic; Kredex; Querto; Atlana Pharma brand of carvedilol; Carvedilolum [Latin]; Coreg CR; GlaxoSmithKline brand of carvedilol; Lakeside brand of carvedilol; Roche brand of carvedilol; BM 14190; DQ 2466; SKF 105517; Artist (TN); BM-14190; Carloc (TN); Coreg (TN); DQ-2466; Dilatrend (TN); EG-P042; Eucardic (TN); BM-14-190; BM-14.190; Carvedilol, 14C-labeled; SK&F-105517; Carvedilol (JAN/USAN/INN); Carvedilol [USAN:INN:BAN:JAN]; Carvedilol, (R)-isomer; Carvedilol, (S)-isomer; Carvedilol, (+-)-isomer; (+-)-1-(Carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol; (+-)-1-Carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol; (+/-)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol; 1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol; 1-(9H-carbazol-4-yloxy)-3-[(2-{[2-(methyloxy)phenyl]oxy}ethyl)amino]propan-2-ol; 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol; 1-(9H-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol
Indication
Disease Entry ICD 11 Status REF
Chronic heart failure BD1Z Approved [1]
Congestive heart failure BD10 Approved [2]
Pulmonary hypertension BB01 Approved [1]
Coronavirus Disease 2019 (COVID-19) 1D6Y Investigative [3]
Therapeutic Class
Vasodilator Agents
Affected Organisms
Humans and other mammals
ATC Code
C07AG02: Carvedilol
C07AG: Alpha and beta blocking agents
C07A: BETA BLOCKING AGENTS
C07: BETA BLOCKING AGENTS
C: CARDIOVASCULAR SYSTEM
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 406.5
Logarithm of the Partition Coefficient (xlogp) 4.2
Rotatable Bond Count (rotbonds) 10
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 7.8 mL/min/kg [5]
Elimination
1% of drug is excreted from urine in the unchanged form [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 2.4 hours [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.02587 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.02% [5]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 1.3 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 0.01 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Vascular disorders Not Available KDR FLK1 VEGFR2 OT15797V [7]
Vascular disorders Not Available SRC SRC1 OTETYX40 [7]
Chemical Identifiers
Formula
C24H26N2O4
IUPAC Name
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Canonical SMILES
COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
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
InChIKey
OGHNVEJMJSYVRP-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2585
ChEBI ID
CHEBI:3441
CAS Number
72956-09-3
UNII
0K47UL67F2
DrugBank ID
DB01136
TTD ID
D0W9LX
VARIDT ID
DR00689
INTEDE ID
DR0282
ACDINA ID
D00103
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor Alpha-1 (ADRA1) TTG28O6 NOUNIPROTAC Antagonist [8]
HUAMN alpha-1 adrenergic receptor (ADRA1) TTDBOI7 ADA1A_HUMAN ; ADA1B_HUMAN ; ADA1D_HUMAN Inhibitor [9]
HUMAN beta adrenergic receptor (BAR) TTJB8UY ADRB1_HUMAN ; ADRB2_HUMAN ; ADRB3_HUMAN Antagonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [11]
Cytochrome P450 2E1 (CYP2E1) DEVDYN7 CP2E1_HUMAN Substrate [12]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [13]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [14]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [15]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [16]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [15]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Adiponectin (ADIPOQ) OTNX23LE ADIPO_HUMAN Gene/Protein Processing [17]
Angiotensinogen (AGT) OTBZLYR3 ANGT_HUMAN Gene/Protein Processing [18]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Regulation of Drug Effects [19]
Beta-1 adrenergic receptor (ADRB1) OTQBWN4U ADRB1_HUMAN Gene/Protein Processing [20]
Beta-2 adrenergic receptor (ADRB2) OTSDOX4Q ADRB2_HUMAN Post-Translational Modifications [21]
C-reactive protein (CRP) OT0RFT8F CRP_HUMAN Gene/Protein Processing [22]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Gene/Protein Processing [23]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Gene/Protein Processing [23]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Biotransformations [24]
Endothelin-1 (EDN1) OTZCACEG EDN1_HUMAN Gene/Protein Processing [25]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Carvedilol (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Gilteritinib DMTI0ZO Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [26]
Bepridil DM0RKS4 Moderate Increased risk of cardiac depression by the combination of Carvedilol and Bepridil. Angina pectoris [BA40] [27]
Dronedarone DMA8FS5 Moderate Increased risk of atrioventricular block by the combination of Carvedilol and Dronedarone. Angina pectoris [BA40] [28]
Desipramine DMT2FDC Moderate Increased plasma concentrations of Carvedilol and Desipramine due to competitive inhibition of the same metabolic pathway. Attention deficit hyperactivity disorder [6A05] [29]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Carvedilol and Cariprazine. Bipolar disorder [6A60] [30]
Talazoparib DM1KS78 Major Decreased clearance of Carvedilol due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [26]
Alpelisib DMEXMYK Moderate Increased metabolism of Carvedilol caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [31]
Atracurium DM42HXN Moderate Additive neuromuscular blocking effects by the combination of Carvedilol and Atracurium. Corneal disease [9A76-9A78] [32]
Mivacurium DM473VD Moderate Additive neuromuscular blocking effects by the combination of Carvedilol and Mivacurium. Corneal disease [9A76-9A78] [32]
Pancuronium DMB0VY8 Moderate Additive neuromuscular blocking effects by the combination of Carvedilol and Pancuronium. Corneal disease [9A76-9A78] [32]
Pasireotide DMHM7JS Moderate Increased risk of atrioventricular block by the combination of Carvedilol and Pasireotide. Cushing syndrome [5A70] [33]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Carvedilol caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [34]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Carvedilol and OPC-34712. Depression [6A70-6A7Z] [30]
Clomipramine DMINRKW Moderate Increased plasma concentrations of Carvedilol and Clomipramine due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [29]
Doxepin DMPI98T Moderate Increased plasma concentrations of Carvedilol and Doxepin due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [35]
Mepenzolate DM8YU2F Moderate Antagonize the effect of Carvedilol when combined with Mepenzolate. Digestive system disease [DE2Z] [26]
Stiripentol DMMSDOY Moderate Decreased metabolism of Carvedilol caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [36]
Phenobarbital DMXZOCG Moderate Increased metabolism of Carvedilol caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [37]
Mirabegron DMS1GYT Moderate Decreased metabolism of Carvedilol caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [38]
Ripretinib DM958QB Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Ripretinib. Gastrointestinal stromal tumour [2B5B] [39]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Carvedilol caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [40]
Aliskiren DM1BV7W Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [33]
Levamlodipine DM92S6N Moderate Increased risk of cardiac depression by the combination of Carvedilol and Levamlodipine. Hypertension [BA00-BA04] [27]
Hydralazine DMU8JGH Minor Decreased metabolism of Carvedilol caused by Hydralazine mediated interference with first-pass metabolism. Hypertension [BA00-BA04] [41]
Clevidipine butyrate DMW4M97 Moderate Increased risk of cardiac depression by the combination of Carvedilol and Clevidipine butyrate. Hypertension [BA00-BA04] [27]
Belladonna DM2RBWK Moderate Antagonize the effect of Carvedilol when combined with Belladonna. Infectious gastroenteritis/colitis [1A40] [26]
Berotralstat DMWA2DZ Major Decreased clearance of Carvedilol due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [42]
Amobarbital DM0GQ8N Moderate Increased metabolism of Carvedilol caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [37]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Carvedilol and ITI-007. Insomnia [7A00-7A0Z] [30]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Carvedilol caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [26]
PF-06463922 DMKM7EW Moderate Increased metabolism of Carvedilol caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [39]
Dacomitinib DMOH8VY Moderate Decreased metabolism of Carvedilol caused by Dacomitinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [43]
Lumefantrine DM29GAD Moderate Decreased metabolism of Carvedilol caused by Lumefantrine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [39]
GDC-0199 DMH0QKA Major Decreased clearance of Carvedilol due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [39]
Vemurafenib DM62UG5 Moderate Decreased metabolism of Carvedilol caused by Vemurafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [44]
Ubrogepant DM749I3 Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Ubrogepant. Migraine [8A80] [45]
Lanthanum carbonate DMMJQSH Moderate Decreased absorption of Carvedilol due to formation of complexes caused by Lanthanum carbonate. Mineral absorption/transport disorder [5C64] [33]
Panobinostat DM58WKG Moderate Decreased metabolism of Carvedilol caused by Panobinostat mediated inhibition of CYP450 enzyme. Multiple myeloma [2A83] [46]
Siponimod DM2R86O Major Increased risk of atrioventricular block by the combination of Carvedilol and Siponimod. Multiple sclerosis [8A40] [39]
Fingolimod DM5JVAN Major Increased risk of bradycardia by the combination of Carvedilol and Fingolimod. Multiple sclerosis [8A40] [47]
Ozanimod DMT6AM2 Moderate Increased risk of bradycardia by the combination of Carvedilol and Ozanimod. Multiple sclerosis [8A40] [48]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Carvedilol caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [26]
Nilotinib DM7HXWT Moderate Decreased metabolism of Carvedilol caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [49]
Rolapitant DM8XP26 Moderate Decreased metabolism of Carvedilol caused by Rolapitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [50]
Bupropion DM5PCS7 Moderate Decreased metabolism of Carvedilol caused by Bupropion mediated inhibition of CYP450 enzyme. Nicotine use disorder [6C4A] [51]
Lorcaserin DMG6OYJ Moderate Decreased metabolism of Carvedilol caused by Lorcaserin mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [52]
Polythiazide DMCH80F Moderate Increased risk of ventricular arrhythmias by the combination of Carvedilol and Polythiazide. Oedema [MG29] [53]
S-297995 DM26IH8 Moderate Decreased clearance of Carvedilol due to the transporter inhibition by S-297995. Opioid use disorder [6C43] [26]
Methylscopolamine DM5VWOB Moderate Altered absorption of Carvedilol due to GI dynamics variation caused by Methylscopolamine. Peptic ulcer [DA61] [26]
Lefamulin DME6G97 Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Lefamulin. Pneumonia [CA40] [54]
ABIRATERONE DM8V75C Moderate Decreased metabolism of Carvedilol caused by ABIRATERONE mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [55]
Relugolix DMK7IWL Major Decreased clearance of Carvedilol due to the transporter inhibition by Relugolix. Prostate cancer [2C82] [56]
Terazosin DM3JCVS Moderate Additive hypotensive effects by the combination of Carvedilol and Terazosin. Prostate hyperplasia [GA90] [57]
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Carvedilol and Silodosin. Prostate hyperplasia [GA90] [57]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Carvedilol and Levomepromazine. Psychotic disorder [6A20-6A25] [30]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Carvedilol and Quetiapine. Schizophrenia [6A20] [30]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Carvedilol and Aripiprazole. Schizophrenia [6A20] [30]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Carvedilol and Iloperidone. Schizophrenia [6A20] [30]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Carvedilol and Paliperidone. Schizophrenia [6A20] [30]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Carvedilol and Molindone. Schizophrenia [6A20] [30]
Thiothixene DMDINC4 Moderate Increased plasma concentrations of Carvedilol and Thiothixene due to competitive inhibition of the same metabolic pathway. Schizophrenia [6A20] [58]
Amisulpride DMSJVAM Moderate Increased risk of ventricular arrhythmias by the combination of Carvedilol and Amisulpride. Schizophrenia [6A20] [26]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Carvedilol and Asenapine. Schizophrenia [6A20] [30]
Larotrectinib DM26CQR Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [39]
Docetaxel DMDI269 Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Docetaxel. Solid tumour/cancer [2A00-2F9Z] [59]
Taxol DMUOT9V Moderate Decreased clearance of Carvedilol due to the transporter inhibition by Taxol. Solid tumour/cancer [2A00-2F9Z] [59]
Pipecuronium DM5F84A Moderate Additive neuromuscular blocking effects by the combination of Carvedilol and Pipecuronium. Tonus and reflex abnormality [MB47] [32]
Vecuronium DMP0UK2 Moderate Additive neuromuscular blocking effects by the combination of Carvedilol and Vecuronium. Tonus and reflex abnormality [MB47] [32]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Carvedilol and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [60]
Propafenone DMPIBJK Moderate Decreased metabolism of Carvedilol caused by Propafenone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [61]
⏷ Show the Full List of 70 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Allura red AC dye E00338 33258 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Hydrazine yellow E00409 164825 Colorant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Quinoline yellow WS E00309 24671 Colorant
Sodium citrate anhydrous E00102 6224 Alkalizing agent; Buffering agent; Complexing agent; Emulsifying agent
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Ammonia E00007 222 Alkalizing agent
Beta-D-galactose E00415 439353 Complexing agent; Flavoring agent
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sucrose 1,6-distearate E00593 71587490 Dispersing agent; Emulsifying agent; Modified-release agent; Solubilizing agent; Surfactant; lubricant
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triethyl citrate E00128 6506 Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 31 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Carvedilol 40 mg capsule 40 mg 24 HR Extended Release Oral Capsule Oral
Carvedilol 10 mg capsule 10 mg 24 HR Extended Release Oral Capsule Oral
Carvedilol 80 mg capsule 80 mg 24 HR Extended Release Oral Capsule Oral
Carvedilol 20 mg capsule 20 mg 24 HR Extended Release Oral Capsule Oral
Carvedilol 12.5 mg tablet 12.5 mg Oral Tablet Oral
Carvedilol 25 mg tablet 25 mg Oral Tablet Oral
Carvedilol 3.125 mg tablet 3.125 mg Oral Tablet Oral
Carvedilol 6.25 mg tablet 6.25 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Carvedilol FDA Label
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