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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	1786	51384-51-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: metoprolol fumarate metoprolol metoprolol succinate beatrolol metoprolol tartrate	A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS. Molecular weight: 267.37 Formula: C15H25NO3 CLOGP: 1.49 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 50.72 ALOGS: -2.82 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metoprolol fumarate
metoprolol
metoprolol succinate
beatrolol
metoprolol tartrate

A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.

Molecular weight: 267.37
Formula: C15H25NO3
CLOGP: 1.49
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 50.72
ALOGS: -2.82
ROTB: 9

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.15	g	O
0.15	g	P

ADMET properties:

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Property	Value	Reference
S (Water solubility)	50 mg/mL	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	38 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	3.60 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.10 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	24.95 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	13 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.88 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 7, 1978	FDA	US PHARMS HOLDINGS I

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
Myocardial infarction	1148.02	9.87	1903	314890	97990	63074239
Cardiac failure congestive	925.61	9.87	1657	315136	90776	63081453
Atrial fibrillation	891.52	9.87	1865	314928	114771	63057458
Pemphigus	841.34	9.87	15	316778	183711	62988518
Systemic lupus erythematosus	726.12	9.87	93	316700	208825	62963404
Synovitis	712.01	9.87	59	316734	186859	62985370
Hand deformity	699.27	9.87	21	316772	159436	63012793
Glossodynia	668.96	9.87	61	316732	178815	62993414
Bradycardia	659.00	9.87	1254	315539	71973	63100256
Coronary artery disease	629.25	9.87	792	316001	31585	63140644

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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
Myocardial infarction	1286.51	10.92	2889	270609	118196	34565237
Cardiac failure congestive	707.86	10.92	1824	271674	81446	34601987
Coronary artery disease	632.97	10.92	1257	272241	47048	34636385
Bradycardia	563.15	10.92	1575	271923	73843	34609590
Atrial fibrillation	551.58	10.92	2153	271345	120240	34563193
Off label use	432.84	10.92	1755	271743	417769	34265664
Acute myocardial infarction	366.06	10.92	1086	272412	52633	34630800
Drug abuse	351.07	10.92	168	273330	98928	34584505
Hypotension	333.54	10.92	2911	270587	218738	34464695
Coronary artery bypass	333.13	10.92	289	273209	4613	34678820

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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
Myocardial infarction	2597.25	9.92	4263	475935	179866	79084324
Cardiac failure congestive	1534.64	9.92	2932	477266	139470	79124720
Coronary artery disease	1300.85	9.92	1781	478417	63693	79200497
Bradycardia	1251.53	9.92	2617	477581	132940	79131250
Atrial fibrillation	1223.08	9.92	3266	476932	194620	79069570
Acute myocardial infarction	864.90	9.92	1615	478583	75421	79188769
Hypotension	745.66	9.92	4867	475331	435450	78828740
Synovitis	690.90	9.92	58	480140	150676	79113514
Off label use	639.64	9.92	3053	477145	904162	78360028
Completed suicide	621.48	9.92	3027	477171	242740	79021450

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FDA Adverse Event Reporting System (Pediatric)

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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
Neonatal respiratory failure	49.94	28.07	34	977	251	88530

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Pharmacologic Action:

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Source	Code	Description
ATC	C07AB02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
ATC	C07BB02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, selective, and thiazides
ATC	C07BB52	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, selective, and thiazides
ATC	C07CB02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Beta blocking agents, selective, and other diuretics
ATC	C07FB02	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents and calcium channel blockers
ATC	C07FB13	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents and calcium channel blockers
ATC	C07FX03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents, other combinations
ATC	C07FX05	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:35674	antihypertensive drugs

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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
Myocardial infarction	indication	22298006	DOID:5844
Hypertensive disorder	indication	38341003	DOID:10763
Chronic heart failure	indication	48447003
Angina pectoris	indication	194828000
Acute coronary syndrome	indication	394659003
Myocardial Reinfarction Prevention	indication
Supraventricular tachycardia	off-label use	6456007
Ventricular tachycardia	off-label use	25569003
Atrial fibrillation	off-label use	49436004	DOID:0060224
Multifocal atrial tachycardia	off-label use	49982000

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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	9.19	Basic

Orange Book patent data (new drug applications)

None

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-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	7.60	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	6.30	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		Kd	6.79	CHEMBL
Beta-1 adrenergic receptor	GPCR		B0FL73_CAVPO		Kd	7.83	CHEMBL
Adrenergic receptor beta	GPCR		ADRB2_RAT ADRB1_RAT ADRB3_RAT		IC50	6.30	CHEMBL
Beta-1 adrenergic receptor	GPCR		ADRB1_MOUSE		Ki	7.31	CHEMBL

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External reference:

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ID	Source
001853	NDDF
003627	NDDF
003628	NDDF
004135	NDDF
102313	RXNORM
1073	MMSL
3471	INN_ID
372826007	SNOMEDCT_US
4018393	VANDF
4019836	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4595	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4595	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4595	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4595	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4596	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4596	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Metoprolol Succinate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4596	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Metoprolol Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9660	INJECTION, SOLUTION	5 mg	INTRAVENOUS	ANDA	26 sections
Metoprolol Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9873	INJECTION, SOLUTION	5 mg	INTRAVENOUS	ANDA	26 sections
Metoprolol Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0018	TABLET, FILM COATED	25 mg	ORAL	ANDA	23 sections

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