Bisoprolol

Bisoprolol is a beta-1 adrenergic blocking agent used to prevent myocardial infarction and heart failure and to treat mild to moderate hypertension.

Bisoprolol is a cardioselective β1-adrenergic blocking agent used to treat high blood pressure. 4,16 It is considered a potent drug with a long-half life that can be used once daily to reduce the need for multiple doses of antihypertensive drugs. 4 Bisoprolol is generally well tolerated, likely due to its β1-adrenergic receptor selectivity and is a useful alternative to non-selective β-blocker drugs in the treatment of hypertension such as Carvedilol and Labetalol. It may be used alone or in combination with other drugs to manage hypertension 16 and can be useful in patients with chronic obstructive pulmonary disease (COPD) due to its receptor selectivity. 13

Type Small Molecule Groups Approved Structure

Structure for Bisoprolol (DB00612)

  • (+-)-1-((alpha-(2-Isopropoxyethoxy)-p-tolyl)oxy)-3-(isopropylamino)-2-propanol
  • (RS)-1-(4-(2-Isopropoxyethoxymethyl)phenoxy)-3-(isopropylamino)-2-propanol
  • Bisoprolol
  • CL 297,939
  • CL 297939
  • EMD 33 512
  • EMD 33512

Pharmacology

Bisoprolol is indicated for the treatment of mild to moderate hypertension. 16 It may be used off-label to treat heart failure, atrial fibrillation, and angina pectoris. 1,2

Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Bisoprolol decreases heart rate (chronotropy), decreases contractility (inotropy), and reduces blood pressure. 14,16 The results of various clinical studies indicate that bisoprolol reduces cardiovascular mortality and all-cause mortality in patients with heart failure and decreased cardiac ejection fraction (EF). 3,8

Mechanism of action

Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension, it is thought that therapeutic effects are achieved through the antagonism of β-1adrenoceptors to result in lower cardiac output. Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors (located mainly in the heart) 14 are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, leading to greater cardiovascular work, increasing the demand for oxygen. Bisoprolol reduces cardiac workload by decreasing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors. 7,14

Bisoprolol is also thought to reduce the output of renin in the kidneys, which normally increases blood pressure. Additionally, some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate. 16

Bisoprolol is well absorbed in the gastrointestinal tract. 17 The AUC is 642.87 g.hr/mL and bioavailability of bisoprolol is about 90% due to the minimal first pass effects. 1 Absorption is unaffected by food intake. Peak plasma concentrations of bisoprolol are attained within 2-4 hours and steady-state concentrations are achieved within 5 days of administration. 16 In a pharmacokinetic study, the mean peak concentration of bisoprolol was 52 micrograms/L. 6 Cmax at steady state concentrations of bisoprolol is 64±21 ng/ml administered at 10 mg daily. 17

Volume of distribution

The volume of distribution of bisoprolol is 3.5 L/kg. 17 The mean volume of distribution was found to be 230 L/kg in heart failure patients, which was similar to the volume of distribution in healthy patients. 10 Bisoprolol is known to cross the placenta. 15

Binding to serum proteins is approximately 30%. 9,17

About 50% of a single bisoprolol dose is metabolized mainly by the enzyme CYP3A4 to inactive metabolites. 16

Route of elimination

Bisoprolol is eliminated equally by both renal and hepatic pathways. About 50% of an oral dose is excreted unchanged in the urine with the remainder of the dose excreted as inactive bisoprolol metabolites. Under 2% of the ingested dose is found to be excreted in the feces. 16,17

A pharmacokinetic study in 12 healthy individuals determined the mean plasma half-life of bisoprolol to be 10-12 hours. 4 Another study comprised of healthy patients determined the elimination half-life to be approximately 10 hours. 6 Renal impairment increased the half-life to 18.5 hours. 6

Total body clearance in healthy patients was determined to be 14.2 L/h. In patients with renal impairment, clearance was reduced to 7.8 L/h. Hepatic dysfunction also reduced the clearance of bisoprolol. 6

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.

LD50 information Oral LD50 of bisoprolol in the mouse was 730 mg/kg. 20

Signs of a β-blocker overdose include cardiovascular symptoms such as hypotension, congestive heart failure, and bradycardia. Other symptoms such as bronchospasm, and hypoglycemia may occur. If an overdose occurs with bisoprolol, supportive treatment should be initiated. Glucagon has been shown to be beneficial in bradycardia and hypotension associated with beta-blocker overdosage. 11 Hypoglycemia may be managed by administering IV glucose. 16 Monitor the patient and administer atropine in cases of bradycardia, pressors and fluids in the case of hypotension, and conventional heart failure therapy if heart failure occurs. If heart block occurs, the patient must be closely monitored and isoproterenol infusion or transvenous cardiac pacemaker insertion should take place. 16 For the management of overdose-related bronchospasm, administer bronchodilators with or without IV aminophylline. Limited research suggests that bisoprolol fumarate is not removed adequately by hemodialysis sessions. 12,16

Pathways

Pathway Category
Bisoprolol Action Pathway Drug action

Pharmacogenomic Effects/ADRs

Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

  • Take with or without food. The absorption is unaffected by food.

Products

Our datasets provide approved product information including: dosage, form, labeller, route of administration, and marketing period.

Ingredient UNII CAS InChI Key
Bisoprolol fumarate UR59KN573L 104344-23-2 VMDFASMUILANOL-WXXKFALUSA-N

Product Images
International/Other Brands Bisocor / Cardicor (Bayer) / Concor (Merck) / Concore (Merck) / Detensiel (Merck Santé) / Emconcor (Merck) / Emcor (Merck) / Euradal (Lacer) / Isoten (Meda) / Monocor (Biovail Pharmaceuticals) / Soprol (Helsinn) Brand Name Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Bisoprolol Tablet 5 mg Oral Sivem Pharmaceuticals Ulc 2012-06-12 2020-07-21 Canada
Bisoprolol Tablet 5 mg Oral Sanis Health Inc 2012-10-01 Not applicable Canada
Bisoprolol Tablet 10 mg Oral Sorres Pharma Inc 2009-02-26 2014-06-20 Canada
Bisoprolol Tablet 5 mg Oral Sorres Pharma Inc 2009-02-26 2014-06-20 Canada
Bisoprolol Tablet 10 mg Oral Sivem Pharmaceuticals Ulc 2012-06-12 2020-07-21 Canada
Bisoprolol Tablet 10 mg Oral Sanis Health Inc 2012-10-01 Not applicable Canada
Bisoprolol Fumarate Tablet 10 mg Oral Sanis Health Inc Not applicable Not applicable Canada
Bisoprolol Fumarate Tablet 5 mg Oral Sanis Health Inc Not applicable Not applicable Canada
Bisoprolol Tablets Tablet 5 mg Oral Sivem Pharmaceuticals Ulc 2020-05-26 Not applicable Canada
Bisoprolol Tablets Tablet 10 mg Oral Sivem Pharmaceuticals Ulc 2020-05-26 Not applicable Canada

Generic Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Ag-bisoprolol Tablet 10 mg Oral Angita Pharma Inc. 2022-03-18 Not applicable Canada
Ag-bisoprolol Tablet 5 mg Oral Angita Pharma Inc. 2022-03-18 Not applicable Canada
Apo-bisoprolol Tablet 5 mg Oral Apotex Corporation 2004-08-10 Not applicable Canada
Apo-bisoprolol Tablet 10 mg Oral Apotex Corporation 2004-08-10 Not applicable Canada
Ava-bisoprolol Tablet 10 mg Oral Avanstra Inc 2011-08-22 2014-08-21 Canada
Ava-bisoprolol Tablet 5 mg Oral Avanstra Inc 2011-08-22 2014-08-21 Canada
Bisoprolol Tablet, film coated 5 mg/1 Oral Trupharma, Llc 2019-06-20 Not applicable US
Bisoprolol Tablet, film coated 5 mg/1 Oral Nucare Pharmaceuticals,inc. 2019-06-20 Not applicable US
Bisoprolol Tablet, film coated 5 mg/1 Oral bryant ranch prepack 2019-06-20 Not applicable US
Bisoprolol Tablet, film coated 10 mg/1 Oral bryant ranch prepack 2019-06-20 Not applicable US

Mixture Products

Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
BIRAMLO 10MG/10MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 10MG/10MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 10MG/10MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 10MG/5MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (5 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 10MG/5MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (5 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 10MG/5MG Bisoprolol fumarate (10 mg/1) + Amlodipine besylate (5 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 5MG/10MG Bisoprolol fumarate (5 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 5MG/10MG Bisoprolol fumarate (5 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 5MG/10MG Bisoprolol fumarate (5 mg/1) + Amlodipine besylate (10 mg/1) Tablet Oral 2018-10-01 Not applicable Germany
BIRAMLO 5MG/5MG Bisoprolol fumarate (5 mg/1) + Amlodipine besylate (5 mg/1) Tablet Oral 2018-10-01 Not applicable Germany

Unapproved/Other Products

Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
CONCOR 10 MG 30 LAK TABLET Bisoprolol fumarate (10 mg) Tablet Oral DAİİCHİ SANKYO İLAÇ TİC. LTD. ŞTİ. 2020-08-14 Not applicable Turkey
CONCOR 5 MG 30 LAK TABLET Bisoprolol fumarate (5 mg) Tablet Oral DAİİCHİ SANKYO İLAÇ TİC. LTD. ŞTİ. 2020-08-14 Not applicable Turkey

Categories

Chemical Identifiers

References

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

  1. Lancaster SG, Sorkin EM: Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. Drugs. 1988 Sep;36(3):256-85. doi: 10.2165/00003495-198836030-00002. [Article]
  2. Ishiguro H, Ikeda T, Abe A, Tsukada T, Mera H, Nakamura K, Yusu S, Yoshino H: Antiarrhythmic effect of bisoprolol, a highly selective beta1-blocker, in patients with paroxysmal atrial fibrillation. Int Heart J. 2008 May;49(3):281-93. [Article]
  3. Metra M, Nodari S, Bordonali T, Milani P, Lombardi C, Bugatti S, Fontanella B, Verzura G, Danesi R, Dei Cas L: Bisoprolol in the treatment of chronic heart failure: from pathophysiology to clinical pharmacology and trial results. Ther Clin Risk Manag. 2007 Aug;3(4):569-78. [Article]
  4. Leopold G, Ungethum W, Pabst J, Simane Z, Buhring KU, Wiemann H: Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist. Br J Clin Pharmacol. 1986 Sep;22(3):293-300. doi: 10.1111/j.1365-2125.1986.tb02890.x. [Article]
  5. Nuttall SL, Routledge HC, Kendall MJ: A comparison of the beta1-selectivity of three beta1-selective beta-blockers. J Clin Pharm Ther. 2003 Jun;28(3):179-86. [Article]
  6. Kirch W, Rose I, Demers HG, Leopold G, Pabst J, Ohnhaus EE: Pharmacokinetics of bisoprolol during repeated oral administration to healthy volunteers and patients with kidney or liver disease. Clin Pharmacokinet. 1987 Aug;13(2):110-7. doi: 10.2165/00003088-198713020-00003. [Article]
  7. Chatterjee SS: The cardioselective and hypotensive effects of bisoprolol in hypertensive asthmatics. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S74-7. [Article]
  8. Dezsi CA, Szentes V: The Real Role of beta-Blockers in Daily Cardiovascular Therapy. Am J Cardiovasc Drugs. 2017 Oct;17(5):361-373. doi: 10.1007/s40256-017-0221-8. [Article]
  9. Leopold G: Balanced pharmacokinetics and metabolism of bisoprolol. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S16-20. [Article]
  10. Cvan Trobec K, Grabnar I, Kerec Kos M, Vovk T, Trontelj J, Anker SD, Rosano G, Lainscak M: Bisoprolol pharmacokinetics and body composition in patients with chronic heart failure: a longitudinal study. Eur J Clin Pharmacol. 2016 Jul;72(7):813-22. doi: 10.1007/s00228-016-2041-1. Epub 2016 Mar 21. [Article]
  11. Peterson CD, Leeder JS, Sterner S: Glucagon therapy for beta-blocker overdose. Drug Intell Clin Pharm. 1984 May;18(5):394-8. [Article]
  12. Shroff GR, Herzog CA: beta-Blockers in dialysis patients: a nephrocardiology perspective. J Am Soc Nephrol. 2015 Apr;26(4):774-6. doi: 10.1681/ASN.2014080831. Epub 2014 Oct 30. [Article]
  13. Albouaini K, Andron M, Alahmar A, Egred M: Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions. Int J Chron Obstruct Pulmon Dis. 2007;2(4):535-40. [Article]
  14. William D. Tucker; Pramod Theetha Kariyanna (2019). Selective B1 blockers. Stat Pearls Publishing.
  15. National Collaborating Centre for Women’s and Children’s Health (UK) (2010). NICE Guidelines for hypertension in pregnancy. RCOG Press.
  16. Bisoprolol monograph [Link]
  17. Summary of product characteristics [Link]
  18. Bisoprolol, health links AU [Link]
  19. CaymanChem: Bisoprolol MSDS [Link]
  20. Monograph, Bisoprolol [Link]
  21. DailyMed Label: Bisoprolol fumarate Oral Tablets [Link]

Clinical Trials

Phase Status Purpose Conditions Count
4 Completed Health Services Research High Blood Pressure (Hypertension) / Syndrome, Metabolic 1
4 Completed Prevention Adverse Side Effects / Coronary Artery Atherosclerosis / Insulin resistance syndrome 1
4 Completed Prevention Atrial Fibrillation / Coronary Artery Bypass Grafting (CABG) / Prevention 1
4 Completed Prevention High Blood Pressure (Hypertension) 1
4 Completed Supportive Care High Blood Pressure (Hypertension) 1
4 Completed Treatment Atrial Fibrillation (Permanent) 1
4 Completed Treatment Blood Pressures 2
4 Completed Treatment Chronic Heart Failure (CHF) 2
4 Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) 2
4 Completed Treatment Congestive Heart Failure (CHF) 1

Pharmacoeconomics

  • 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
  • Atlantic Biologicals Corporation
  • Aurobindo Pharma Ltd.
  • Duramed
  • Eon Labs
  • Greenstone LLC
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Novopharm Ltd.
  • Physicians Total Care Inc.
  • Resource Optimization and Innovation LLC
  • Teva Pharmaceutical Industries Ltd.
  • Unichem Laboratories Ltd.
  • Watson Pharmaceuticals
  • Wyeth Pharmaceuticals

Dosage Forms

Form Route Strength
Tablet Oral
Tablet, film coated Oral
Tablet, film coated Oral 2.5 mg
Tablet, film coated Oral 5 mg
Tablet Oral 10 mg/1
Tablet Oral 5 mg/1
Tablet, coated Oral 10 mg/1
Tablet, coated Oral 5 mg/1
Tablet, film coated Oral 10 mg/1
Tablet, film coated Oral 5 mg/1
Tablet Oral
Tablet, coated Oral
Tablet, film coated Oral
Tablet, film coated Oral 1.25 mg
Tablet, film coated Oral 10 mg
Tablet Oral 1.25 mg
Tablet Oral 10 mg
Tablet Oral 2.5 mg
Tablet Oral 3.75 mg
Tablet Oral 5 mg
Tablet Oral 7.5 mg
Tablet, film coated Oral 1.06 MG
Tablet, film coated Oral 2.50 MG
Tablet, coated Oral 10 mg
Tablet, film coated Oral 3.75 mg
Tablet, film coated Oral 7.5 mg
Tablet Oral 10 mg
Tablet Oral 5 mg
Tablet, coated Oral 1.25 mg
Tablet, film coated Oral 10 mg
Tablet, film coated Oral 5 mg
Tablet, coated Oral 5 mg
Tablet, coated Oral 2.5 mg

Prices

Unit description Cost Unit
Condylox 0.5% Gel 3.5 gm Tube 304.93USD tube
Condylox 0.5% Solution 3.5ml Bottle 143.4USD bottle
Condylox 0.5% gel 97.73USD g
Zebeta 10 mg tablet 3.6USD tablet
Zebeta 5 mg tablet 3.6USD tablet
Bisoprolol fumarate 5 mg tablet 1.78USD tablet
Bisoprolol fumarate 10 mg tablet 1.24USD tablet
Bisoprolol-Hydrochlorothiazide 10-6.25 mg tablet 1.19USD tablet
Bisoprolol-Hydrochlorothiazide 2.5-6.25 mg tablet 1.19USD tablet
Bisoprolol-Hydrochlorothiazide 5-6.25 mg tablet 1.19USD tablet
Apo-Bisoprolol 10 mg Tablet 0.38USD tablet
Novo-Bisoprolol 10 mg Tablet 0.38USD tablet
Pms-Bisoprolol 10 mg Tablet 0.38USD tablet
Sandoz Bisoprolol 10 mg Tablet 0.38USD tablet
Apo-Bisoprolol 5 mg Tablet 0.23USD tablet
Novo-Bisoprolol 5 mg Tablet 0.23USD tablet
Pms-Bisoprolol 5 mg Tablet 0.23USD tablet
Sandoz Bisoprolol 5 mg Tablet 0.23USD tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Properties

State Solid Experimental Properties

Property Value Source
melting point (°C) 100-103 https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf
boiling point (°C) 445.0±45.0 http://www.chemspider.com/Chemical-Structure.2312.html
logP 2.2 http://www.hmdb.ca/metabolites/HMDB0014750
logS -3.7 http://www.hmdb.ca/metabolites/HMDB0014750
pKa 9.5 https://www.sandoz.ca/sites/www.sandoz.ca/files/Bisoprolol_TAB_Monograph.pdf

Predicted Properties

Property Value Source
Water Solubility 0.0707 mg/mL ALOGPS
logP 2.3 ALOGPS
logP 2.2 ChemAxon
logS -3.7 ALOGPS
pKa (Strongest Acidic) 14.09 ChemAxon
pKa (Strongest Basic) 9.67 ChemAxon
Physiological Charge 1 ChemAxon
Hydrogen Acceptor Count 5 ChemAxon
Hydrogen Donor Count 2 ChemAxon
Polar Surface Area 59.95 Å 2 ChemAxon
Rotatable Bond Count 12 ChemAxon
Refractivity 92.15 m 3 ·mol -1 ChemAxon
Polarizability 38.5 Å 3 ChemAxon
Number of Rings 1 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter Yes ChemAxon
Veber’s Rule No ChemAxon
MDDR-like Rule No ChemAxon

Predicted ADMET Features

Property Value Probability
Human Intestinal Absorption + 0.9445
Blood Brain Barrier 0.9077
Caco-2 permeable + 0.6149
P-glycoprotein substrate Substrate 0.7785
P-glycoprotein inhibitor I Non-inhibitor 0.807
P-glycoprotein inhibitor II Non-inhibitor 0.7821
Renal organic cation transporter Non-inhibitor 0.8568
CYP450 2C9 substrate Non-substrate 0.8134
CYP450 2D6 substrate Substrate 0.8919
CYP450 3A4 substrate Non-substrate 0.6113
CYP450 1A2 substrate Non-inhibitor 0.9046
CYP450 2C9 inhibitor Non-inhibitor 0.9071
CYP450 2D6 inhibitor Non-inhibitor 0.923
CYP450 2C19 inhibitor Non-inhibitor 0.9485
CYP450 3A4 inhibitor Non-inhibitor 0.8373
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9766
Ames test Non AMES toxic 0.9064
Carcinogenicity Non-carcinogens 0.9267
Biodegradation Not ready biodegradable 0.8962
Rat acute toxicity 2.0089 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.7877
hERG inhibition (predictor II) Non-inhibitor 0.6611

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST) Not Available Spectra

Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum – GC-MS Predicted GC-MS Not Available
Predicted MS/MS Spectrum – 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum – 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-004i-0109000000-564ffde4ea3f59c4126f
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-014i-2903000000-5e5b905ef2026aa7f011
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-00xr-9800000000-99ce6ca7b3171d63af09
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-00di-9600000000-bfefc02f00a4439a34ba
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-05fr-9500000000-4b91d206ced038eff35c
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-0ab9-9400000000-dd6baeb57f900d719aa9
LC-MS/MS Spectrum – LC-ESI-QTOF , positive LC-MS/MS splash10-004i-0209000000-0f37dcfed3fc1c82c470
LC-MS/MS Spectrum – LC-ESI-QTOF , positive LC-MS/MS splash10-014i-5902000000-dae2a435db6b3ea664cd
LC-MS/MS Spectrum – LC-ESI-QTOF , positive LC-MS/MS splash10-05fr-9200000000-1cce569461a677bb6467
MS/MS Spectrum – , positive LC-MS/MS splash10-004i-0209000000-65dd49cd88f0ec134445
LC-MS/MS Spectrum – LC-ESI-QFT , positive LC-MS/MS splash10-00or-5709000000-360e67ed724045a9c01b

Targets

Binding Properties
Property Measurement pH Temperature (°C) References
Kd (nM) 15 7.4 37 A15307
Ki (nM) 22.4 N/A N/A A15544

General Function Receptor signaling protein activity Specific Function Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e. Gene Name ADRB1 Uniprot ID P08588 Uniprot Name Beta-1 adrenergic receptor Molecular Weight 51322.1 Da

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Curator comments At higher doses, bisoprolol antagonizes the B2 receptors, but is normally selective for B1 receptors.

General Function Protein homodimerization activity Specific Function Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately . Gene Name ADRB2 Uniprot ID P07550 Uniprot Name Beta-2 adrenergic receptor Molecular Weight 46458.32 Da

References
  1. Mark G. Papich (2016). Saunders Handbook of Veterinary Drugs (4th ed.). Saunders.
  2. Summary of product characteristics [Link]

Enzymes

General Function Vitamin d3 25-hydroxylase activity Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react. Gene Name CYP3A4 Uniprot ID P08684 Uniprot Name Cytochrome P450 3A4 Molecular Weight 57342.67 Da

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. [Article]
  2. Zisaki A, Miskovic L, Hatzimanikatis V: Antihypertensive drugs metabolism: an update to pharmacokinetic profiles and computational approaches. Curr Pharm Des. 2015;21(6):806-22. [Article]
  3. Bisoprolol monograph [Link]

Transporters

General Function Xenobiotic-transporting atpase activity Specific Function Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells. Gene Name ABCB1 Uniprot ID P08183 Uniprot Name Multidrug resistance protein 1 Molecular Weight 141477.255 Da