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Details

Stereochemistry RACEMIC
Molecular Formula C18H31NO4
Molecular Weight 325.4437
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BISOPROLOL

SMILES

CC(C)NCC(COc1ccc(cc1)COCCOC(C)C)O

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 325.4437
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.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

7.330176E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
52 μg/L
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
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
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
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
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
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%
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%
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:
unhealthy, 37 - 52 years
n = 15
Health Status: unhealthy
Condition: liver disease
Age Group: 37 - 52 years
Sex: M+F
Population Size: 15
Sources:
Other AEs: Dizziness, Tiredness...
Other AEs:
Dizziness (2 patients)
Tiredness (1 patient)
Shortness of breath (1 patient)
Faintness (1 patient)
Sources:
10 mg 1 times / day steady, oral (max)
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, adult
n = 1327
Health Status: unhealthy
Condition: heart failure
Age Group: adult
Sex: unknown
Population Size: 1327
Sources:
5 mg 1 times / day steady, intravenous (max)
Highest studied dose
Dose: 5 mg, 1 times / day
Route: intravenous
Route: steady
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
n = 37
Health Status: unhealthy
Condition: myocardial infarction
Age Group: adult
Sex: unknown
Population Size: 37
Sources:
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
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:
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Disc. AE: Bradycardia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Bradycardia (< 1%)
Fatigue (< 1%)
Sources:
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Other AEs: Headache, Hypoaesthesia...
Other AEs:
Headache (10.9%)
Hypoaesthesia (1.5%)
Sweating increased (1%)
Arthralgia (2.7%)
Dizziness (3.5%)
Dry mouth (1.3%)
Bradycardia (0.5%)
Insomnia (2.5%)
Depression (0.2%)
Diarrhea (3.5%)
Nausea (2.2%)
Vomiting (1.5%)
Sources:
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Disc. AE: Bradycardia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Bradycardia (< 1%)
Fatigue (< 1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Faintness 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 37 - 52 years
n = 15
Health Status: unhealthy
Condition: liver disease
Age Group: 37 - 52 years
Sex: M+F
Population Size: 15
Sources:
Shortness of breath 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 37 - 52 years
n = 15
Health Status: unhealthy
Condition: liver disease
Age Group: 37 - 52 years
Sex: M+F
Population Size: 15
Sources:
Tiredness 1 patient
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 37 - 52 years
n = 15
Health Status: unhealthy
Condition: liver disease
Age Group: 37 - 52 years
Sex: M+F
Population Size: 15
Sources:
Dizziness 2 patients
10 mg single, oral
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 37 - 52 years
n = 15
Health Status: unhealthy
Condition: liver disease
Age Group: 37 - 52 years
Sex: M+F
Population Size: 15
Sources:
Bradycardia 0.4%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Dry mouth 0.7%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Sweating increased 0.7%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Hypoaesthesia 1.1%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Vomiting 1.1%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Insomnia 1.5%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Nausea 1.5%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Arthralgia 2.2%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Diarrhea 2.6%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Dizziness 2.9%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Headache 8.8%
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Bradycardia < 1%
Disc. AE
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Fatigue < 1%
Disc. AE
20 mg 1 times / day steady, oral (max)
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, adult
n = 273
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 273
Sources:
Depression 0.2%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Bradycardia 0.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Sweating increased 1%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Dry mouth 1.3%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Hypoaesthesia 1.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Vomiting 1.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Headache 10.9%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Nausea 2.2%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Insomnia 2.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Arthralgia 2.7%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Diarrhea 3.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Dizziness 3.5%
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Bradycardia < 1%
Disc. AE
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
Fatigue < 1%
Disc. AE
40 mg 1 times / day steady, oral (max)
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: steady
Dose: 40 mg, 1 times / day
Sources:
unhealthy, adult
n = 404
Health Status: unhealthy
Condition: hypertension
Age Group: adult
Sex: unknown
Population Size: 404
Sources:
PubMed

PubMed

TitleDatePubMed
Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors.
1999 Apr
[Treatment of cardiac insufficiency: does treatment depend on whether its cause is ischemic or idiopathic?].
1999 Jun
Clinical improvement in patients with orthostatic intolerance after treatment with bisoprolol and fludrocortisone.
2000 Oct
Cost effectiveness of bisoprolol in the treatment of chronic congestive heart failure in Sweden: analysis using data from the Cardiac Insufficiency Bisoprolol Study II trial.
2001
Beta-blocker treatment in heart failure.
2001 Apr
[Efficacy of oncologic surgery. Does anesthesia influence the postoperative outcome?].
2001 Apr
Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium.
2001 Aug
Bisoprolol reduces cardiac death and myocardial infarction in high-risk patients as long as 2 years after successful major vascular surgery.
2001 Aug
Autoantibodies against the beta1 adrenoceptor from patients with dilated cardiomyopathy prolong action potential duration and enhance contractility in isolated cardiomyocytes.
2001 Aug
Predictors of medical events and of their competitive interactions in the Cardiac Insufficiency Bisoprolol Study 2 (CIBIS-2).
2001 Dec
Immunofluorescent imaging of beta 1- and beta 2-adrenergic receptors in rat kidney.
2001 Feb
[A must in symptomatic heart failure. Added beta blocker improves prognosis].
2001 Feb 1
Current role of beta-adrenergic blockers in the treatment of chronic congestive heart failure.
2001 Jan 15
Sex differences in the prognosis of congestive heart failure: results from the Cardiac Insufficiency Bisoprolol Study (CIBIS II).
2001 Jan 23
[Bisprolol in heart failure: efficacy and costs in a French setting according to CIBIS II].
2001 Jul-Aug
Beta-blockers to reduce mortality in patients with systolic dysfunction: a meta-analysis.
2001 Jun
A cost-effectiveness analysis of bisoprolol for heart failure.
2001 Jun
Bisoprolol treatment for cyanotic spells--a 69-year-old female with uncorrected pentalogy of Fallot.
2001 Jun 28
The effects of bisoprolol, a selective beta1-blocker, on glucose metabolism by long-term administration in essential hypertension.
2001 May
Enhanced in vivo and in vitro contractile responses to beta(2)-adrenergic receptor stimulation in dogs susceptible to lethal arrhythmias.
2001 Oct
[Role of beta-blockers in the treatment of chronic heart heart failure].
2001 Sep 16
Bisoprolol: a review of its use in chronic heart failure.
2002
Optimising the use of beta-blockers in older patients with heart failure.
2002
Differential effects of bucindolol and carvedilol on noradenaline-induced hypertrophic response in ventricular cardiomyocytes of adult rats.
2002 Apr
Metoprolol CR/XL in female patients with heart failure: analysis of the experience in Metoprolol Extended-Release Randomized Intervention Trial in Heart Failure (MERIT-HF).
2002 Apr 2
Beta-blockers work as well in women as in men.
2002 Apr 5
[Hormonal hyperactivity in heart failure. Differences in beta blockers].
2002 Aug
Integrated acquisition of analytical and biopharmaceutical screening data for beta-adrenergic-drugs employing diversified macrocycle supported potentiometric detection in HPLC systems.
2002 Aug
Beta blockers in older persons with heart failure: tolerability and impact on quality of life.
2002 Dec
Clinical results with bisoprolol 2.5 mg/hydrochlorothiazide 6.25 mg combination in systolic hypertension in the elderly.
2002 Feb
Fixed low-dose combination in first-line treatment of hypertension.
2002 Feb
Transoesophageal Doppler echocardiography provided important parameters in patients with dilated cardiomyopathy during bisoprolol therapy.
2002 Feb
[Cost-effectiveness of bisoprolol in chronic heart failure].
2002 Feb 14
beta-Blocker therapy in heart failure: scientific review.
2002 Feb 20
Perindopril reverses myocyte remodeling in the hypertensive heart.
2002 Jan
Inappropriate tachycardia detection by a biventricular implantable cardioverter defibrillator.
2002 Jan
Can beta blockers be safely initiated at home in patients with heart failure?
2002 Jan
Comparison of the affinity of beta-blockers for two states of the beta 1-adrenoceptor in ferret ventricular myocardium.
2002 Jan
Present and future pharmacotherapy for heart failure.
2002 Jul
Unique effects of carvedilol on noradrenaline release in the human heart.
2002 Mar
Beta-blocker therapy combined with low-dose pimobendan in patients with idiopathic dilated cardiomyopathy and chronic obstructive pulmonary disease: report on two cases.
2002 May
Beta-blocker/thiazide combination for treatment of hypertensive children: a randomized double-blind, placebo-controlled trial.
2002 May
Effect of beta(1)-selective adrenergic blockade on maximal blood lactate steady state in healthy men.
2002 May
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

Sample Use Guides

2.5 to 40 mg once-daily dose
Route of Administration: Oral
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 Sat Jun 26 01:41:12 UTC 2021
Edited
by admin
on Sat Jun 26 01:41:12 UTC 2021
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
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
EMD 33 512
Code English
BISOPROLOL [JAN]
Common Name English
BISOPROLOL [WHO-DD]
Common Name English
BISOPROLOL [INN]
Common Name English
Classification Tree Code System Code
WHO-VATC QC07BB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
NCI_THESAURUS C29576
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 12.4
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
LIVERTOX 111
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C09BX02
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
NDF-RT N0000175556
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 12.1
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 12.3
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-VATC QC07AB57
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C07FB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C07FX04
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
NDF-RT N0000000161
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C07BB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-VATC QC07AB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C07AB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ATC C07AB57
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-VATC QC07FB07
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 12.2
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
Code System Code Type Description
EVMPD
SUB13096MIG
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
FDA UNII
Y41JS2NL6U
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
WIKIPEDIA
BISOPROLOL
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
RXCUI
19484
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY RxNorm
MESH
D017298
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
CAS
66722-44-9
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
LACTMED
Bisoprolol
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
PUBCHEM
2405
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
DRUG BANK
DB00612
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
INN
5225
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
HSDB
8316
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
IUPHAR
7129
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
EPA CompTox
66722-44-9
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
MERCK INDEX
M2565
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C61653
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
ChEMBL
CHEMBL645
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
DRUG CENTRAL
380
Created by admin on Sat Jun 26 01:41:12 UTC 2021 , Edited by admin on Sat Jun 26 01:41:12 UTC 2021
PRIMARY
Related Record Type Details
ENANTIOMER -> RACEMATE
ENANTIOMER -> RACEMATE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
SALT/SOLVATE -> PARENT
TARGET -> AGONIST
SHORT-ACTING
SALT/SOLVATE -> PARENT
Related Record Type Details
METABOLITE -> PARENT
MAJOR
PLASMA; URINE
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
METABOLITE -> PARENT
MINOR
PLASMA; URINE
METABOLITE -> PARENT
MINOR
PLASMA; URINE
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
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
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC