U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry RACEMIC
Molecular Formula C18H31NO4
Molecular Weight 325.443
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BISOPROLOL

SMILES

CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1

InChI

InChIKey=VHYCDWMUTMEGQY-UHFFFAOYSA-N
InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3

HIDE SMILES / InChI
Molecular Formula C18H31NO4
Molecular Weight 325.443
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: description was created based on several sources, including: http://www.healthline.com/drugs/bisoprolol/oral-tablet#Highlights1 https://www.drugs.com/ppa/bisoprolol.html http://pharm-sci.tbzmed.ac.ir/Drug-Information/Integrative%20Medicine%20Professional%20Access/ProfDrugs/Bisoprololpd.html http://www.drugbank.ca/drugs/DB00612 https://en.wikipedia.org/wiki/Bisoprolol

Bisoprolol is a cardioselective beta1-adrenergic blocking agent. It lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, ischemic heart diseases, and myocardial infarction after the acute event. General side effects are: fatigue, asthenia, chest pain, malaise, edema, weight gain, angioedema. Concurrent use of rifampin increases the metabolic clearance of bisoprolol fumarate, shortening its elimination half-life.

CNS Activity

Originator

Approval Year

1992
113
Targets

Targets

Primary TargetPharmacologyConditionPotency
Blocker
555
 8.8 nM [IC50]
Substrate
661
Substrate
661
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
ZIAC

Approved Use

BISOPROLOL FUMARATE is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.

Launch Date

1993
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
52 μg/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2887325/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
40.37 ng/mL
DRUG LABEL
https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
661 μg × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2887325/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
609.8 ng × h/mL
DRUG LABEL
https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2887325/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
11.07 h
DRUG LABEL
https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2887325/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
70%
DRUG LABEL
https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BISOPROLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
unhealthy, 37 - 52 years
Health Status: unhealthy
Age Group: 37 - 52 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
Other AEs: Dizziness, Tiredness...
Other AEs:
Dizziness (2 patients)
Tiredness (1 patient)
Shortness of breath (1 patient)
Faintness (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
10 mg 1 times / day steady, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10023943/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/10023943/
Sources:
https://pubmed.ncbi.nlm.nih.gov/10023943/
5 mg 1 times / day steady, intravenous
Highest studied dose
Dose: 5 mg, 1 times / day
Route: intravenous
Route: steady
Dose: 5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/11527129/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/11527129/
Sources:
https://pubmed.ncbi.nlm.nih.gov/11527129/
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Disc. AE: Bradycardia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Bradycardia (< 1%)
Fatigue (< 1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Other AEs: Sweating increased, Arthralgia...
Other AEs:
Sweating increased (0.7%)
Arthralgia (2.2%)
Dizziness (2.9%)
Headache (8.8%)
Hypoaesthesia (1.1%)
Dry mouth (0.7%)
Bradycardia (0.4%)
Insomnia (1.5%)
Diarrhea (2.6%)
Nausea (1.5%)
Vomiting (1.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Disc. AE: Bradycardia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Bradycardia (< 1%)
Fatigue (< 1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Other AEs: Sweating increased, Arthralgia...
Other AEs:
Sweating increased (1%)
Arthralgia (2.7%)
Dizziness (3.5%)
Headache (10.9%)
Hypoaesthesia (1.5%)
Dry mouth (1.3%)
Bradycardia (0.5%)
Insomnia (2.5%)
Depression (0.2%)
Diarrhea (3.5%)
Nausea (2.2%)
Vomiting (1.5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Faintness 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
unhealthy, 37 - 52 years
Health Status: unhealthy
Age Group: 37 - 52 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
Shortness of breath 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
unhealthy, 37 - 52 years
Health Status: unhealthy
Age Group: 37 - 52 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
Tiredness 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
unhealthy, 37 - 52 years
Health Status: unhealthy
Age Group: 37 - 52 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
Dizziness 2 patients
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
unhealthy, 37 - 52 years
Health Status: unhealthy
Age Group: 37 - 52 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/2897298/
Bradycardia < 1%
Disc. AE
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Fatigue < 1%
Disc. AE
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Bradycardia 0.4%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Dry mouth 0.7%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Sweating increased 0.7%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Hypoaesthesia 1.1%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Vomiting 1.1%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Insomnia 1.5%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Nausea 1.5%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Arthralgia 2.2%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Diarrhea 2.6%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Dizziness 2.9%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Headache 8.8%
20 mg 1 times / day steady, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Bradycardia < 1%
Disc. AE
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Fatigue < 1%
Disc. AE
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Depression 0.2%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Bradycardia 0.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Sweating increased 1%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Dry mouth 1.3%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Hypoaesthesia 1.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Vomiting 1.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Headache 10.9%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Nausea 2.2%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Insomnia 2.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Arthralgia 2.7%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Diarrhea 3.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Dizziness 3.5%
40 mg 1 times / day steady, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019982s014lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946
substrate
1388

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741

OCT2
779

OCT1
620

OCT3
159

OCTN1
32

OCTN2
71
P-gp
2052
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OCT3
161
 no
OCTN1
32
 no
OCTN2
71
 no
OCT2
782
 yes [IC50 2.4 uM]
OCT1
656
 yes
P-gp
1932
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2D6
1388
 yes
CYP3A4
1946
 yes
P-gp
2052
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:3127
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3127
ChemicalBook
CB03118896
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB03118896
ChemicalBook
CB13118893
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB13118893
ChemicalBook
CB33118897
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB33118897
ChemicalBook
CB73118895
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB73118895
ChemicalBook
CB83118892
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB83118892
eMolecules
901481
https://www.emolecules.com/cgi-bin/more?vid=901481
MolPort
MolPort-003-666-876
https://www.molport.com/shop/molecule-link/MolPort-003-666-876
MolPort
MolPort-005-937-320
https://www.molport.com/shop/molecule-link/MolPort-005-937-320
PubMed

PubMed

TitleDatePubMed
Carvedilol versus other beta-blockers in heart failure.
2001 May
[Cost-effectiveness of bisoprolol in chronic heart failure].
2002 Feb 14
Beta-blocker decreases the increase in QT dispersion and transmural dispersion of repolarization induced by bepridil.
2002 Nov
Influence of drugs and gender on the arterial pulse wave and natriuretic peptide secretion in untreated patients with essential hypertension.
2002 Nov
Functional beta1- and beta2-adrenoceptors in the left and right atrium of pre-hypertensive rats.
2002 Oct
[Beta blockers in heart failure. Start with low and slowly increase the dosage!].
2002 Sep 19
Storms of ventricular tachyarrhythmias associated with primary hyperparathyroidism in a patient with dilated cardiomyopathy.
2003 Jan
Patents

Patents

BE 859425
4
US 4258062
4

Sample Use Guides

In Vivo Use Guide
2.5 to 40 mg once-daily dose
Route of Administration: Oral
In Vitro Use Guide
Positive test results were obtained in the in vitro CHO Sister Chromatid Exchange (clastogenicity) test and in the mouse Lymphoma Cell (mutagenicity) assays, using concentrations of hydrochlorothiazide of 43-1300 µg/mL.
Substance Class Chemical
Created
by admin
on Mon Mar 31 19:29:58 GMT 2025
Edited
by admin
on Mon Mar 31 19:29:58 GMT 2025
Record UNII
Y41JS2NL6U
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BISOPROLOL
INN   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
EMD 33 512
Preferred Name English
BISOPROLOL [USAN]
Common Name English
BISOPROLOL [VANDF]
Common Name English
BISOPROLOL [MI]
Common Name English
2-PROPANOL, 1-(4-((2-(1-METHYLETHOXY)ETHOXY)METHYL)PHENOXY)-3-((1-METHYLETHYL)AMINO)-, (±)-
Systematic Name English
(±)-1-((.ALPHA.-(2-ISOPROPOXYETHOXY)-P-TOLYL)OXY)-3-(ISOPROPYLAMINO)-2-PROPANOL
Common Name English
BISOPROLOL [JAN]
Common Name English
bisoprolol [INN]
Common Name English
Bisoprolol [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-VATC QC07BB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
NCI_THESAURUS C29576
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 12.4
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
LIVERTOX NBK548471
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C09BX02
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
NDF-RT N0000175556
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 12.1
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 12.3
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-VATC QC07AB57
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C07FB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C07FX04
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
NDF-RT N0000000161
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C07BB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-VATC QC07AB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C07AB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ATC C07AB57
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-VATC QC07FB07
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 12.2
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
Code System Code Type Description
SMS_ID
100000092277
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
EVMPD
SUB13096MIG
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
FDA UNII
Y41JS2NL6U
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
DAILYMED
Y41JS2NL6U
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
CHEBI
3127
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
USAN
Y-69
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
WIKIPEDIA
BISOPROLOL
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
RXCUI
19484
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY RxNorm
MESH
D017298
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
CAS
66722-44-9
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
LACTMED
Bisoprolol
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
PUBCHEM
2405
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
DRUG BANK
DB00612
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
INN
5225
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
HSDB
8316
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
IUPHAR
7129
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
EPA CompTox
DTXSID6022682
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
MERCK INDEX
m2565
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY Merck Index
NCI_THESAURUS
C61653
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
ChEMBL
CHEMBL645
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
DRUG CENTRAL
380
Created by admin on Mon Mar 31 19:29:58 GMT 2025 , Edited by admin on Mon Mar 31 19:29:58 GMT 2025
PRIMARY
Related Record Type Details
Structure of BISOPROLOL, (R)-
ENANTIOMER -> RACEMATE
Structure of BISOPROLOL, (S)-
ENANTIOMER -> RACEMATE
Structure of BISOPROLOL MONOFUMARATE
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
BETA-1 ADRENERGIC RECEPTOR
TARGET -> AGONIST
Structure of BISOPROLOL FUMARATE
SALT/SOLVATE -> PARENT
Structure of BISOPROLOL HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of O-(DESISOPROPYL) BISOPROLOL ACID
METABOLITE -> PARENT
MAJOR
PLASMA; URINE
Structure of O-(DESISOPROPYL)-O-(1-CARBOXYETHYL) BISOPROLOL
METABOLITE -> PARENT
The AUC and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol. In vitro: stereoselectively of CYP2D6 (R > S) and CYP3A4 was not stereoselective.
IN-VITRO
Structure of 4-(2-HYDROXY-3-((1-METHYLETHYL)AMINO)PROPOXY)BENZOIC ACID
METABOLITE -> PARENT
MINOR
PLASMA; URINE
Structure of O-(DESISOPROPYL)-O-(1-CARBOXYETHYL) BISOPROLOL
METABOLITE -> PARENT
MINOR
PLASMA; URINE
Structure of O-(DESISOPROPYL) BISOPROLOL ACID
METABOLITE -> PARENT
The AUC and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol. In vitro: stereoselectively of CYP2D6 (R > S) and CYP3A4 was not stereoselective.
IN-VITRO
Structure of 4-(2-HYDROXY-3-((1-METHYLETHYL)AMINO)PROPOXY)BENZOIC ACID
METABOLITE -> PARENT
The AUC and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol. In vitro: stereoselectively of CYP2D6 (R > S) and CYP3A4 was not stereoselective.
IN-VITRO
Related Record Type Details
Structure of BISOPROLOL
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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