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Identification
NameBisoprolol
Accession NumberDB00612  (APRD00257)
TypeSmall Molecule
GroupsApproved
Description

Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At lower doses (less than 20 mg daily), bisoprolol selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with daily doses of 20 mg or greater. Unlike propranolol and pindolol, bisoprolol does not exhibit membrane-stabilizing or sympathomimetic activity. Bisoprolol possesses a single chiral centre and is administered as a racemic mixture. Only l-bisoprolol exhibits significant β-blocking activity.

Structure
Thumb
Synonyms
SynonymLanguageCode
(+-)-1-((alpha-(2-Isopropoxyethoxy)-P-tolyl)oxy)-3-(isopropylamino)-2-propanolNot AvailableNot Available
(RS)-1-(4-(2-isopropoxyethoxymethyl)phenoxy)-3-(isopropylamino)-2-propanolNot AvailableNot Available
BisoprololFrench/German/SpanishINN
BisoprololumLatinINN
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zebetatablet5 mgoralDuramed Pharmaceuticals, Inc.1992-07-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Zebetatablet10 mgoralDuramed Pharmaceuticals, Inc.1992-07-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bisoprolol Fumaratetablet, film coated5 mgoralTeva Pharmaceuticals USA Inc2004-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated10 mgoralTeva Pharmaceuticals USA Inc2004-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, coated5 mgoralEon Labs, Inc.2000-11-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, coated10 mgoralEon Labs, Inc.2000-11-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated5 mgoralMylan Pharmaceuticals Inc.2012-09-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated10 mgoralMylan Pharmaceuticals Inc.2012-09-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet5 mgoralRebel Distributors Corp2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet10 mgoralRebel Distributors Corp2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet5 mgoralUnichem Pharmaceuticals (USA), Inc.2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet10 mgoralUnichem Pharmaceuticals (USA), Inc.2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated10 mgoralPhysicians Total Care, Inc.2009-07-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated5 mgoralPhysicians Total Care, Inc.2009-08-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated10 mgoralGreenstone LLC2006-12-272015-03-31Us 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet5 mgoralbryant ranch prepack2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated5 mgoralAurobindo Pharma Limited2006-12-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, film coated10 mgoralAurobindo Pharma Limited2006-12-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet, coated5 mgoralAmerican Health Packaging2011-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprolol Fumaratetablet5 mgoralCarilion Materials Management2009-09-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Bisoprololtablet5 mgoralSivem Pharmaceuticals UlcNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Bisoprololtablet10 mgoralSivem Pharmaceuticals UlcNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Bisoprololtablet5 mgoralSanis Health IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Bisoprololtablet10 mgoralSanis Health IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot Available
International Brands
NameCompany
CardicorBayer
ConcorMerck
ConcoreMerck
DetensielMerck Santé
EmconcorMerck
EmcorMerck
EuradalLacer
IsotenMeda
MonocorBiovail Pharmaceuticals
SoprolHelsinn
Brand mixtures
Brand NameIngredients
Concor plus bisoprolol + hydrochlorothiazide
Emcoreticbisoprolol + hydrochlorothiazide
Lodozbisoprolol + hydrochlorothiazide
Maxsotenbisoprolol + hydrochlorothiazide
Tebisbisoprolol + hydrochlorothiazide
Wytensbisoprolol + hydrochlorothiazide
Zabesta-XLObisoprolol + hydrochlorothiazide
Ziacbisoprolol + hydrochlorothiazide
Salts
Name/CASStructureProperties
Bisoprolol Fumarate
ThumbNot applicableDBSALT001015
Categories
CAS number66722-44-9
WeightAverage: 325.443
Monoisotopic: 325.225308485
Chemical FormulaC18H31NO4
InChI KeyVHYCDWMUTMEGQY-UHFFFAOYSA-N
InChI
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
IUPAC Name
1-[(propan-2-yl)amino]-3-(4-{[2-(propan-2-yloxy)ethoxy]methyl}phenoxy)propan-2-ol
SMILES
CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzylethers. These are aromatic ethers with the general formula ROCR' (R = alkyl, aryl; R'=benzene).
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzylethers
Direct ParentBenzylethers
Alternative Parents
Substituents
  • Benzylether
  • Phenol ether
  • Alkyl aryl ether
  • Secondary alcohol
  • 1,2-aminoalcohol
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI).
PharmacodynamicsBisoprolol is a competitive, cardioselective β1-adrenergic antagonist. Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. They are routinely prescribed in patients with ischemic heart disease. In addition, β1-selective blockers prevent the release of renin, a hormone produced by the kidneys causes constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane-stabilizing activity.
Mechanism of actionBisoprolol selectively blocks catecholamine stimulation of β1-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block β2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation.
AbsorptionWell absorbed. Bioavailability > 80%. Absorption is not affected by food. Peak plasma concentrations occur within 2-4 hours.
Volume of distributionNot Available
Protein bindingBinding to serum proteins is approximately 30%
Metabolism

Approximately 50% of the dose is metabolized primarily metabolized by CYP3A4 to inactive metabolites. In vitro studies have shown that bisoprolol is also metabolized by CYP2D6 though this does not appear to be clinically significant. Approximately half the administered dose is excreted in unchanged in urine.

Route of eliminationEliminated equally by renal and non-renal pathways. Approximately 50% of the total orally administered dose is excreted unchanged in urine with the remainder appearing as inactive metabolites. Less than 2% of the dose is excreted in the feces.
Half life9-12 hours; prolonged in the elderly and those with decreased renal function
ClearanceNot Available
ToxicityOral, mouse: LD50 = 100 mg/kg; Skin, rabbit: LD50 = 200 mg/kg; Skin, rat: LD50 = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9445
Blood Brain Barrier-0.9077
Caco-2 permeable+0.6149
P-glycoprotein substrateSubstrate0.7785
P-glycoprotein inhibitor INon-inhibitor0.807
P-glycoprotein inhibitor IINon-inhibitor0.7821
Renal organic cation transporterNon-inhibitor0.8568
CYP450 2C9 substrateNon-substrate0.8134
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.6113
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 substrateNon-inhibitor0.9071
CYP450 2D6 substrateNon-inhibitor0.923
CYP450 2C19 substrateNon-inhibitor0.9485
CYP450 3A4 substrateNon-inhibitor0.8373
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9766
Ames testNon AMES toxic0.9064
CarcinogenicityNon-carcinogens0.9267
BiodegradationNot ready biodegradable0.8962
Rat acute toxicity2.0089 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7877
hERG inhibition (predictor II)Non-inhibitor0.6611
Pharmacoeconomics
Manufacturers
  • Aurobindo pharma ltd
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Unichem pharmaceuticals (usa) inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral5 mg
Tablet, coatedoral10 mg
Tablet, coatedoral5 mg
Tablet, film coatedoral10 mg
Tablet, film coatedoral5 mg
Prices
Unit descriptionCostUnit
Condylox 0.5% Gel 3.5 gm Tube304.93USD tube
Condylox 0.5% Solution 3.5ml Bottle143.4USD bottle
Condylox 0.5% gel97.73USD g
Zebeta 10 mg tablet3.6USD tablet
Zebeta 5 mg tablet3.6USD tablet
Bisoprolol fumarate 5 mg tablet1.78USD tablet
Bisoprolol fumarate 10 mg tablet1.24USD tablet
Bisoprolol-Hydrochlorothiazide 10-6.25 mg tablet1.19USD tablet
Bisoprolol-Hydrochlorothiazide 2.5-6.25 mg tablet1.19USD tablet
Bisoprolol-Hydrochlorothiazide 5-6.25 mg tablet1.19USD tablet
Apo-Bisoprolol 10 mg Tablet0.38USD tablet
Novo-Bisoprolol 10 mg Tablet0.38USD tablet
Pms-Bisoprolol 10 mg Tablet0.38USD tablet
Sandoz Bisoprolol 10 mg Tablet0.38USD tablet
Apo-Bisoprolol 5 mg Tablet0.23USD tablet
Novo-Bisoprolol 5 mg Tablet0.23USD tablet
Pms-Bisoprolol 5 mg Tablet0.23USD tablet
Sandoz Bisoprolol 5 mg Tablet0.23USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point100 °CPhysProp
water solubility2240 mg/LNot Available
logP1.87RECANATINI,M (1992)
Predicted Properties
PropertyValueSource
Water Solubility0.0707 mg/mLALOGPS
logP2.3ALOGPS
logP2.2ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)14.09ChemAxon
pKa (Strongest Basic)9.67ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area59.95 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity92.15 m3·mol-1ChemAxon
Polarizability38.5 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Yoshihiro Iwao, Katsuyuki Ookubo, Katsuhiro Okada, Kunihiro Minami, Shuichiro Yuasa, “Adhesive Pharmaceutical Preparation Containing Bisoprolol.” U.S. Patent US20090169604, issued July 02, 2009.

US20090169604
General ReferenceNot Available
External Links
ATC CodesC07AB07
AHFS Codes
  • 24:24.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.1 KB)
Interactions
Drug Interactions
Drug
AcetylcholineBeta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction.
AmifostineAntihypertensives may enhance the hypotensive effect of Amifostine.
AmiodaroneMay enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
BretyliumMay enhance the bradycardic effect of Bradycardia-Causing Agents. Bretylium may also enhance atrioventricular (AV) blockade in patients receiving AV blocking agents.
BupivacaineBeta-Blockers may increase the serum concentration of Bupivacaine.
ButabarbitalMay decrease the serum concentration of Beta-Blockers.
ButethalMay decrease the serum concentration of Beta-Blockers.
CarbacholBeta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DasatinibMay increase the serum concentration of CYP3A4 Substrates.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DiazoxideMay enhance the hypotensive effect of Antihypertensives.
DipyridamoleMay enhance the bradycardic effect of Beta-Blockers.
DisopyramideMay enhance the bradycardic effect of Beta-Blockers. Beta-Blockers may enhance the negative inotropic effect of Disopyramide.
DronedaroneMay enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6.
DuloxetineHypotensive Agents may enhance the orthostatic hypotensive effect of DULoxetine.
FingolimodBeta-Blockers may enhance the bradycardic effect of Fingolimod.
FloctafenineMay enhance the adverse/toxic effect of Beta-Blockers.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
HeptabarbitalMay decrease the serum concentration of Beta-Blockers.
HexobarbitalMay decrease the serum concentration of Beta-Blockers.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
LacosamideBradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
MepivacaineBeta-Blockers may increase the serum concentration of Mepivacaine.
MethacholineBeta-Blockers may enhance the adverse/toxic effect of Methacholine.
MethohexitalMay decrease the serum concentration of Beta-Blockers.
MethylphenidateMay diminish the antihypertensive effect of Antihypertensives.
MidodrineBeta-Blockers may enhance the bradycardic effect of Midodrine.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
ObinutuzumabAntihypertensives may enhance the hypotensive effect of Obinutuzumab.
PentobarbitalMay decrease the serum concentration of Beta-Blockers.
PentoxifyllineMay enhance the hypotensive effect of Antihypertensives.
PrimidoneMay decrease the serum concentration of Beta-Blockers.
PropafenoneMay increase the serum concentration of Beta-Blockers. Propafenone possesses some independent beta blocking activity.
RegorafenibMay enhance the bradycardic effect of Beta-Blockers.
ReserpineMay enhance the hypotensive effect of Beta-Blockers.
RisperidoneHypotensive Agents may enhance the hypotensive effect of RisperiDONE.
RituximabAntihypertensives may enhance the hypotensive effect of RiTUXimab.
RivastigmineMay enhance the bradycardic effect of Beta-Blockers.
RuxolitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
SecobarbitalMay decrease the serum concentration of Beta-Blockers.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of CYP3A4 Substrates.
TadalafilMay enhance the antihypertensive effect of Antihypertensives.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TofacitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
VardenafilMay enhance the antihypertensive effect of Antihypertensives.
YohimbineMay diminish the antihypertensive effect of Antihypertensives.
Food Interactions
  • Take without regard to meals.

Targets

1. Beta-1 adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Beta-1 adrenergic receptor P08588 Details

References:

  1. Breed JG, Ciampricotti R, Tromp GP, Valster FA, Lageweg E, Van Bortel LM: Quality of life perception during antihypertensive treatment: a comparative study of bisoprolol and enalapril. J Cardiovasc Pharmacol. 1992;20(5):750-5. Pubmed
  2. Brouri F, Hanoun N, Mediani O, Saurini F, Hamon M, Vanhoutte PM, Lechat P: Blockade of beta 1- and desensitization of beta 2-adrenoceptors reduce isoprenaline-induced cardiac fibrosis. Eur J Pharmacol. 2004 Feb 6;485(1-3):227-34. Pubmed
  3. Bruck H, Leineweber K, Temme T, Weber M, Heusch G, Philipp T, Brodde OE: The Arg389Gly beta1-adrenoceptor polymorphism and catecholamine effects on plasma-renin activity. J Am Coll Cardiol. 2005 Dec 6;46(11):2111-5. Epub 2005 Nov 4. Pubmed
  4. Lipworth BJ, Irvine NA, McDevitt DG: A dose-ranging study to evaluate the beta 1-adrenoceptor selectivity of bisoprolol. Eur J Clin Pharmacol. 1991;40(2):135-9. Pubmed
  5. Mauz AB, Pelzer H: Beta-adrenoceptor-binding studies of the cardioselective beta blockers bisoprolol, H-I 42 BS, and HX-CH 44 BS to heart membranes and intact ventricular myocytes of adult rats: two beta 1-binding sites for bisoprolol. J Cardiovasc Pharmacol. 1990 Mar;15(3):421-7. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Beta-2 adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Beta-2 adrenergic receptor P07550 Details

References:

  1. Brouri F, Hanoun N, Mediani O, Saurini F, Hamon M, Vanhoutte PM, Lechat P: Blockade of beta 1- and desensitization of beta 2-adrenoceptors reduce isoprenaline-induced cardiac fibrosis. Eur J Pharmacol. 2004 Feb 6;485(1-3):227-34. Pubmed
  2. Bruck H, Poller U, Lussenhop H, Ponicke K, Temme T, Heusch G, Philipp T, Brodde OE: Beta 2-adrenoceptor-mediated intrinsic sympathomimetic activity of carteolol: an in vivo study. Naunyn Schmiedebergs Arch Pharmacol. 2004 Nov;370(5):361-8. Epub 2004 Oct 23. Pubmed
  3. Motomura S, Reinhard-Zerkowski H, Daul A, Brodde OE: On the physiologic role of beta-2 adrenoceptors in the human heart: in vitro and in vivo studies. Am Heart J. 1990 Mar;119(3 Pt 1):608-19. Pubmed
  4. Brodde OE: Bisoprolol (EMD 33512), a highly selective beta 1-adrenoceptor antagonist: in vitro and in vivo studies. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S29-35. Pubmed
  5. Daul A, Johnston T, Reher M, Kruger M, Brodde OE: Differential haemodynamic effects induced by beta 1-(bisoprolol) or beta 2-(ICI 118,551) adrenoceptor blockade in man. J Hypertens Suppl. 1986 Dec;4(6):S99-102. Pubmed

Enzymes

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Horikiri Y, Suzuki T, Mizobe M: Pharmacokinetics and metabolism of bisoprolol enantiomers in humans. J Pharm Sci. 1998 Mar;87(3):289-94. Pubmed
  2. Horikiri Y, Suzuki T, Mizobe M: Stereoselective metabolism of bisoprolol enantiomers in dogs and humans. Life Sci. 1998;63(13):1097-108. Pubmed
  3. Nozawa T, Taguchi M, Tahara K, Hashimoto Y, Igarashi N, Nonomura M, Kato B, Igawa A, Inoue H: Influence of CYP2D6 genotype on metoprolol plasma concentration and beta-adrenergic inhibition during long-term treatment: a comparison with bisoprolol. J Cardiovasc Pharmacol. 2005 Nov;46(5):713-20. Pubmed
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Horikiri Y, Suzuki T, Mizobe M: Pharmacokinetics and metabolism of bisoprolol enantiomers in humans. J Pharm Sci. 1998 Mar;87(3):289-94. Pubmed
  2. Horikiri Y, Suzuki T, Mizobe M: Stereoselective metabolism of bisoprolol enantiomers in dogs and humans. Life Sci. 1998;63(13):1097-108. Pubmed
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11