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carvedilol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
vasodilators	522	72956-09-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carvedilol carvedilol phosphate carvediol carvedilol hydrochloride carvedilol HCl BM 14,190	A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION. Molecular weight: 406.48 Formula: C24H26N2O4 CLOGP: 4.04 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 75.74 ALOGS: -4.96 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carvedilol
carvedilol phosphate
carvediol
carvedilol hydrochloride
carvedilol HCl
BM 14,190

A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION.

Molecular weight: 406.48
Formula: C24H26N2O4
CLOGP: 4.04
LIPINSKI: 0
HAC: 6
HDO: 3
TPSA: 75.74
ALOGS: -4.96
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
37.50	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.40 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.30 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	0.25 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Sept. 14, 1995	FDA	SMITHKLINE BEECHAM

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	1220.73	10.48	1063	96734	91370	63299855
Myocardial infarction	411.67	10.48	629	97168	99264	63291961
Hypotension	343.56	10.48	1060	96737	271544	63119681
Cardiac failure	337.57	10.48	540	97257	88602	63302623
Bradycardia	290.20	10.48	453	97344	72774	63318451
Drug ineffective	273.86	10.48	772	97025	1043993	62347232
Synovitis	228.99	10.48	15	97782	186903	63204322
Acute kidney injury	226.40	10.48	903	96894	262512	63128713
Systemic lupus erythematosus	216.38	10.48	32	97765	208886	63182339
Hyperkalaemia	210.09	10.48	332	97465	53871	63337354

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	1129.91	10.90	1365	111201	81905	34762460
Cardiac failure	468.82	10.90	957	111609	90291	34754074
Hypotension	429.42	10.90	1625	110941	220024	34624341
Myocardial infarction	420.57	10.90	1088	111478	119997	34724368
Bradycardia	320.66	10.90	733	111833	74685	34769680
Off label use	190.62	10.90	703	111863	418821	34425544
Ejection fraction decreased	184.64	10.90	266	112300	18888	34825477
Drug abuse	180.50	10.90	48	112518	99048	34745317
Hyperkalaemia	174.79	10.90	556	112010	68833	34775532
Coronary artery disease	169.28	10.90	436	112130	47869	34796496

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	2277.21	10.04	2120	171306	140282	79430680
Myocardial infarction	890.24	10.04	1504	171922	182625	79388337
Cardiac failure	779.24	10.04	1288	172138	153554	79417408
Hypotension	708.50	10.04	2334	171092	437983	79132979
Bradycardia	657.03	10.04	1109	172317	134448	79436514
Hyperkalaemia	431.91	10.04	840	172586	113558	79457404
Acute myocardial infarction	398.10	10.04	649	172777	76387	79494575
Coronary artery disease	342.90	10.04	555	172871	64919	79506043
Acute kidney injury	281.92	10.04	2013	171413	517391	79053571
Synovitis	276.41	10.04	12	173414	150722	79420240

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07AG02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Alpha and beta blocking agents
ATC	C07FX06	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents, other combinations
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35554	cardiovascular agent
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
FDA EPC	N0000175553	alpha-Adrenergic Blocker
FDA EPC	N0000175556	beta-Adrenergic Blocker
FDA MoA	N0000000099	Adrenergic alpha-Antagonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Chronic heart failure	indication	48447003
Left ventricular cardiac dysfunction	indication	429589006
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diastolic heart failure	off-label use	418304008	DOID:9775
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation	off-label use
Bronchospasm	contraindication	4386001
Complete atrioventricular block	contraindication	27885002
Sick sinus syndrome	contraindication	36083008	DOID:13884
Anaphylaxis	contraindication	39579001

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.13	acidic
pKa2	7.88	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF CONGESTIVE HEART FAILURE
10MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF HYPERTENSION
20MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF CONGESTIVE HEART FAILURE
20MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF HYPERTENSION
40MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF CONGESTIVE HEART FAILURE
40MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF HYPERTENSION
80MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF CONGESTIVE HEART FAILURE
80MG	COREG CR	WOODWARD	N022012	Oct. 20, 2006	RX	CAPSULE, EXTENDED RELEASE	ORAL	7268156	June 27, 2023	TREATMENT OF HYPERTENSION

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Ki	9.90	IUPHAR	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	9.50	IUPHAR	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.13	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	7.31	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.40	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.46	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.93	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	6.27	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	8.48	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.93	DRUG MATRIX

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External reference:

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ID	Source
CVD	PDB_CHEM_ID
004167	NDDF
011844	NDDF
0K47UL67F2	UNII
108551001	SNOMEDCT_US
119032	MMSL
20352	RXNORM
22339	MMSL
2585	PUBCHEM_CID
265288	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0051	TABLET, FILM COATED	3.13 mg	ORAL	ANDA	26 sections
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0135	TABLET, FILM COATED	6.25 mg	ORAL	ANDA	26 sections
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7295	TABLET, FILM COATED	12.50 mg	ORAL	ANDA	26 sections
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7296	TABLET, FILM COATED	25 mg	ORAL	ANDA	26 sections
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3631	TABLET, FILM COATED	3.13 mg	ORAL	ANDA	26 sections
Carvedilol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3631	TABLET, FILM COATED	3.13 mg	ORAL	ANDA	26 sections
COREG	HUMAN PRESCRIPTION DRUG LABEL	1	0007-4139	TABLET, FILM COATED	3.13 mg	ORAL	NDA	26 sections
COREG	HUMAN PRESCRIPTION DRUG LABEL	1	0007-4139	TABLET, FILM COATED	3.13 mg	ORAL	NDA	26 sections
COREG	HUMAN PRESCRIPTION DRUG LABEL	1	0007-4140	TABLET, FILM COATED	6.25 mg	ORAL	NDA	26 sections
COREG	HUMAN PRESCRIPTION DRUG LABEL	1	0007-4140	TABLET, FILM COATED	6.25 mg	ORAL	NDA	26 sections

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