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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	380	66722-44-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bisoprolol hemifumarate bisoprolol bisoprolol fumarate	A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. Molecular weight: 325.45 Formula: C18H31NO4 CLOGP: 1.79 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 59.95 ALOGS: -3.66 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

bisoprolol hemifumarate
bisoprolol
bisoprolol fumarate

A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.

Molecular weight: 325.45
Formula: C18H31NO4
CLOGP: 1.79
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 59.95
ALOGS: -3.66
ROTB: 12

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	88 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	63 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	3.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	2.40 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	10 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.88 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.66 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
July 31, 1992	FDA	TEVA WOMENS
June 28, 2013	PMDA	TOA EIYO LTD.

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
Acute kidney injury	1783.64	10.42	2957	184416	260458	63041191
Bradycardia	1293.48	10.42	1323	186050	71904	63229745
Drug interaction	878.23	10.42	2026	185347	227105	63074544
Cardiac failure	824.85	10.42	1159	186214	87983	63213666
Hyponatraemia	754.37	10.42	1256	186117	110644	63191005
Hyperkalaemia	742.71	10.42	857	186516	53346	63248303
Atrial fibrillation	628.50	10.42	1187	186186	115449	63186200
Drug ineffective	585.67	10.42	1400	185973	1043365	62258284
General physical health deterioration	577.48	10.42	1596	185777	199806	63101843
Hypotension	498.77	10.42	1851	185522	270753	63030896

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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
Acute kidney injury	828.08	10.89	3604	189786	301384	34462157
Bradycardia	760.03	10.89	1437	191953	73981	34689560
Cardiac failure	712.34	10.89	1564	191826	89684	34673857
Death	513.96	10.89	886	192504	397163	34366378
Hyperkalaemia	493.88	10.89	1147	192243	68242	34695299
Drug ineffective	445.43	10.89	1190	192200	455561	34307980
Drug interaction	426.97	10.89	2412	190978	223534	34540007
Atrial fibrillation	373.55	10.89	1502	191888	120891	34642650
Completed suicide	336.47	10.89	67	193323	98101	34665440
General physical health deterioration	296.49	10.89	1449	191941	126820	34636721

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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
Acute kidney injury	2512.26	10.08	6360	340008	513044	78884976
Bradycardia	1981.24	10.08	2683	343685	132874	79265146
Cardiac failure	1459.81	10.08	2500	343868	152342	79245678
Hyperkalaemia	1220.15	10.08	1953	344415	112445	79285575
Drug interaction	1178.80	10.08	4219	342149	410964	78987056
Atrial fibrillation	936.71	10.08	2409	343959	195477	79202543
General physical health deterioration	783.06	10.08	2801	343567	272437	79125583
Drug ineffective	732.20	10.08	2342	344026	1078571	78319449
Completed suicide	720.32	10.08	105	346263	245662	79152358
Hypotension	681.62	10.08	3734	342634	436583	78961437

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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
Small for dates baby	31.92	30.45	41	248	2768	86735

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Pharmacologic Action:

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Source	Code	Description
ATC	C07AB07	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective
ATC	C07BB07	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Beta blocking agents, selective, and thiazides
ATC	C07FB07	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents and calcium channel blockers
ATC	C07FX04	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents, other combinations
ATC	C09BX02	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors, other combinations
ATC	C09BX04	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors, other combinations
ATC	C09BX05	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors, other combinations
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent

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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
Atrial fibrillation	indication	49436004	DOID:0060224
Chronic heart failure	off-label use	48447003
Angina pectoris	off-label use	194828000
Diastolic heart failure	off-label use	418304008	DOID:9775
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation	off-label use
Anuria	contraindication	2472002	DOID:2983
Psoriasis	contraindication	9014002	DOID:8893
Hypercholesterolemia	contraindication	13644009
Secondary angle-closure glaucoma	contraindication	21571006

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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	7.65	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.94	WOMBAT-PK
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	5.04	WOMBAT-PK
Beta-1 adrenergic receptor	GPCR		ADRB1_MOUSE		Ki	8.28	CHEMBL

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External reference:

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ID	Source
003703	NDDF
003704	NDDF
104344-23-2	SECONDARY_CAS_RN
108547003	SNOMEDCT_US
142146	RXNORM
2405	PUBCHEM_CID
38369	MMSL
386868003	SNOMEDCT_US
386869006	SNOMEDCT_US
4020862	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BISOPROLOL FUMARATE	Human Prescription Drug Label	1	15955-373	TABLET, FILM COATED	5 mg	ORAL	ANDA	11 sections
BISOPROLOL FUMARATE	Human Prescription Drug Label	1	15955-374	TABLET, FILM COATED	10 mg	ORAL	ANDA	11 sections
Bisoprolol Fumarate	Human Prescription Drug Label	1	16714-529	TABLET, FILM COATED	5 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	Human Prescription Drug Label	1	16714-530	TABLET, FILM COATED	10 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	21695-667	TABLET	5 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	21695-670	TABLET	10 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	29300-126	TABLET	5 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	29300-126	TABLET	5 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	29300-127	TABLET	10 mg	ORAL	ANDA	18 sections
Bisoprolol Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	29300-127	TABLET	10 mg	ORAL	ANDA	18 sections

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