BISOPROLOL MONOFUMARATE

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H31NO4.C4H4O4
Molecular Weight	441.5152
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C\C(O)=O.CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1

InChI

InChIKey=RZPZLFIUFMNCLY-WLHGVMLRSA-N

InChI=1S/C18H31NO4.C4H4O4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4;5-3(6)1-2-4(7)8/h5-8,14-15,17,19-20H,9-13H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1+

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	( + / - )

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020186s027s028lbl.pdf
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

Targets

Primary Target	Pharmacology	Potency
Beta-1 adrenergic receptor 163 Target ID: CHEMBL213 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020186s027s028lbl.pdf	Blocker 555	8.8 nM [IC50]
Cytochrome P450 2D6 62 Target ID: CHEMBL289 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9523980	Substrate 661
Cytochrome P450 3A4 127 Target ID: CHEMBL340 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9523980	Substrate 661

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020186s027s028lbl.pdf	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

C_max

Value	Dose	Co-administered	Analyte	Population
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

Value	Dose	Co-administered	Analyte	Population
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946		substrate 1388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 OCT2 779 OCT1 620 OCT3 159 OCTN1 32 OCTN2 71	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
OCT3 161	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	no
OCTN1 32	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	no
OCTN2 71	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	no
OCT2 782	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/19740083/	yes [IC50 2.4 uM]
OCT1 656	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21641380/	yes
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/16671962/	yes

Drug as victim

Target	Modality	Activity
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/9523980/	yes
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/9523980/	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/18974611/ \| https://pubmed.ncbi.nlm.nih.gov/16671962/	yes

Sourcing

Vendor/Aggregator	ID	URL
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

Title	Date	PubMed
Storms of ventricular tachyarrhythmias associated with primary hyperparathyroidism in a patient with dilated cardiomyopathy.	2003-01	12468064
Beta blockers in older persons with heart failure: tolerability and impact on quality of life.	2002-12	12433890
Beta-blocker decreases the increase in QT dispersion and transmural dispersion of repolarization induced by bepridil.	2002-11	12419934
Influence of drugs and gender on the arterial pulse wave and natriuretic peptide secretion in untreated patients with essential hypertension.	2002-11	12401122
Functional beta1- and beta2-adrenoceptors in the left and right atrium of pre-hypertensive rats.	2002-10	12396304
[Beta blockers in heart failure. Start with low and slowly increase the dosage!].	2002-09-19	12395713
[Hormonal hyperactivity in heart failure. Differences in beta blockers].	2002-08	12229258
[Pharmacology of beta blockers and their significance for therapy of hypertension].	2002-08	12229254
Integrated acquisition of analytical and biopharmaceutical screening data for beta-adrenergic-drugs employing diversified macrocycle supported potentiometric detection in HPLC systems.	2002-08	12171563
Current research on carvedilol in heart failure.	2002-08	12166050
Efficacy of domestic bisoprolol,enalapril and nifedipine retard in mild to moderate hypertension: a randomized double-blind multicenter clinical trial in China.	2002-07	12189112
Present and future pharmacotherapy for heart failure.	2002-07	12083991
[Heart failure. Only every fifth patient is properly treated?].	2002-06-20	12136677
Beta-blocker therapy combined with low-dose pimobendan in patients with idiopathic dilated cardiomyopathy and chronic obstructive pulmonary disease: report on two cases.	2002-05	12374905
Beta-blocker/thiazide combination for treatment of hypertensive children: a randomized double-blind, placebo-controlled trial.	2002-05	12042891
Effect of beta(1)-selective adrenergic blockade on maximal blood lactate steady state in healthy men.	2002-05	12012078
Beta-blockers work as well in women as in men.	2002-04-05	12452171
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).	2002-04-02	11927527
Effects of bisoprolol fumarate on left ventricular size, function, and exercise capacity in patients with heart failure: analysis with magnetic resonance myocardial tagging.	2002-04	11923805
Maintainance of sinus rhythm after electrical cardioversion of persistent atrial fibrillation.	2002-04	11922651
Double-blind, placebo-controlled crossover comparison of five classes of antihypertensive drugs.	2002-04	11910315
Differential effects of bucindolol and carvedilol on noradenaline-induced hypertrophic response in ventricular cardiomyocytes of adult rats.	2002-04	11907159
Factors related to the occurrence of microalbuminuria during antihypertensive treatment in essential hypertension.	2002-03-01	11897766
Unique effects of carvedilol on noradrenaline release in the human heart.	2002-03	11959042
Beta-blockers are associated with lower C-reactive protein concentrations in patients with coronary artery disease.	2002-03	11893365
[Beta blockers for hypertension. No negative influence on insulin resistance].	2002-02-21	11910826
beta-Blocker therapy in heart failure: scientific review.	2002-02-20	11851582
[Cost-effectiveness of bisoprolol in chronic heart failure].	2002-02-14	11887711
Clinical results with bisoprolol 2.5 mg/hydrochlorothiazide 6.25 mg combination in systolic hypertension in the elderly.	2002-02	11996196
Fixed low-dose combination in first-line treatment of hypertension.	2002-02	11996195
Transoesophageal Doppler echocardiography provided important parameters in patients with dilated cardiomyopathy during bisoprolol therapy.	2002-02	11918138
[New and old beta-blockers in the treatment of heart failure].	2002-02	11887345
Bisoprolol for the treatment of chronic heart failure: a meta-analysis on individual data of two placebo-controlled studies--CIBIS and CIBIS II. Cardiac Insufficiency Bisoprolol Study.	2002-02	11835035
[Therapy relevant differences in beta blockers and ACE inhibitors. Innovation or plagiarism?].	2002-01-17	11847884
Perindopril reverses myocyte remodeling in the hypertensive heart.	2002-01	11924731
Inappropriate tachycardia detection by a biventricular implantable cardioverter defibrillator.	2002-01	11877928
Can beta blockers be safely initiated at home in patients with heart failure?	2002-01	11834774
Comparison of the affinity of beta-blockers for two states of the beta 1-adrenoceptor in ferret ventricular myocardium.	2002-01	11815381
Bisoprolol: a review of its use in chronic heart failure.	2002	12466013
Optimising the use of beta-blockers in older patients with heart failure.	2002	12381236
[The effect of aspirin on rheological properties of erythrocytes in essential hypertension].	2002	12152252
[Comparison beta-blockers and their relevance to pharmacologic therapy of cardiovascular diseases].	2002	11878202
Predictors of medical events and of their competitive interactions in the Cardiac Insufficiency Bisoprolol Study 2 (CIBIS-2).	2001-12	11717602
Bisoprolol improves survival in rats with heart failure.	2001-10	11811360
Chiral separation of beta-blockers after derivatization with (-)-alphamethoxy-alpha-(trifluoromethyl)phenylacetyl chloride by gas chromatography.	2001-10	11693539
[Differential therapy with beta blockers. What is their value, what are the risks?].	2001-09-27	11680926
Effect of cibenzoline, a class ia antiarrhythmic agent, on left ventricular diastolic function in hypertrophic cardiomyopathy.	2001-09	11855665
Prevention of experimental autoimmune cardiomyopathy in rabbits by receptor blockers.	2001	11908781
Beta-blockers in heart failure.	2001	11725388
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	11700777

Patents

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 20:57:35 GMT 2025` Edited by `admin` on `Mon Mar 31 20:57:35 GMT 2025`
Record UNII	U057CX04H0
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BISOPROLOL MONOFUMARATE

Common Name

English

2-PROPANOL, 1-(4-((2-(1-METHYLETHOXY)ETHOXY)METHYL)PHENOXY)-3-((1-METHYLETHYL)AMINO)-, (2E)-2-BUTENEDIOATE (1:1)

Preferred Name

English

2-PROPANOL, 1-(4-((2-(1-METHYLETHOXY)ETHOXY)METHYL)PHENOXY)-3-((1-METHYLETHYL)AMINO)-, (2E)-2-BUTENEDIOATE (1:1) (SALT)

Systematic Name

English

2-PROPANOL, 1-(4-((2-(1-METHYLETHOXY)ETHOXY)METHYL)PHENOXY)-3-((1-METHYLETHYL)AMINO)-, (E)-2-BUTENEDIOATE (1:1) (SALT)

Systematic Name

English

Code System Code Type Description

CAS

105878-43-1

Created by admin on Mon Mar 31 20:57:35 GMT 2025 , Edited by admin on Mon Mar 31 20:57:35 GMT 2025

PRIMARY

PUBCHEM

6917733

Created by admin on Mon Mar 31 20:57:35 GMT 2025 , Edited by admin on Mon Mar 31 20:57:35 GMT 2025

PRIMARY

FDA UNII

U057CX04H0

Created by admin on Mon Mar 31 20:57:35 GMT 2025 , Edited by admin on Mon Mar 31 20:57:35 GMT 2025

PRIMARY

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ACTIVE MOIETY

AE	Significance	Dose	Population
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

Details

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Funbound

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Overview

OverviewOther

Drug as perpetrator​

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PubMed

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Drug as perpetrator