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.
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Chatterjee SS: The cardioselective and hypotensive effects of bisoprolol in hypertensive asthmatics. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S74-7. [Article]
- 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]
- Leopold G: Balanced pharmacokinetics and metabolism of bisoprolol. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S16-20. [Article]
- 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]
- Peterson CD, Leeder JS, Sterner S: Glucagon therapy for beta-blocker overdose. Drug Intell Clin Pharm. 1984 May;18(5):394-8. [Article]
- 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]
- 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]
- William D. Tucker; Pramod Theetha Kariyanna (2019). Selective B1 blockers. Stat Pearls Publishing.
- National Collaborating Centre for Women’s and Children’s Health (UK) (2010). NICE Guidelines for hypertension in pregnancy. RCOG Press.
- Bisoprolol monograph [Link]
- Summary of product characteristics [Link]
- Bisoprolol, health links AU [Link]
- CaymanChem: Bisoprolol MSDS [Link]
- Monograph, Bisoprolol [Link]
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- Mark G. Papich (2016). Saunders Handbook of Veterinary Drugs (4th ed.). Saunders.
- 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
- Horikiri Y, Suzuki T, Mizobe M: Pharmacokinetics and metabolism of bisoprolol enantiomers in humans. J Pharm Sci. 1998 Mar;87(3):289-94. [Article]
- 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]
- 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
