Description

Simple

A medication used to treat high blood pressure and chest pain, as well as to prevent heart attacks and heart failure.

Clinical

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

Overview

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.[Read more

Pharmacology

Indication

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.[ Read more

Pharmacodynamic

Bisoprolol decreases heart rate (chronotropy), decreases contractility (inotropy), and reduces blood pressure.[14, Read more

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... Read more

Absorption

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.[ Read more

Protein binding

Binding to serum proteins is approximately 30%.[9, Read more

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 pat... Read more

Clearance

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.[ Read more

Half life

A pharmacokinetic study in 12 healthy individuals determined the mean plasma half-life of bisoprolol to be 10-12 hours.[ Read more

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.[ Read more

Toxicity

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

Overdose information

Signs of a β-blocker overdose include cardiovascular symptoms such as hypotension, congestive heart failure, and bra... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Sinus bradycardia/bradycardia
      • Drugbank Id: DBCOND0100360
  • Regions: US
  • Patient Conditions:
      • Name: Right Ventricular Failure
      • Drugbank Id: DBCOND0048252
  • Patient Conditions Associated With:
      • Name: Hypertension, Pulmonary
      • Drugbank Id: DBCOND0028009
  • Regions: US
  • Patient Conditions:
      • Name: Third degree AV block
      • Drugbank Id: DBCOND0107810
  • Regions: US
  • Patient Conditions:
      • Name: Second degree AV block
      • Drugbank Id: DBCOND0095721
  • Regions: US
  • Patient Conditions:
      • Name: Overt cardiac failure
      • Drugbank Id: DBCOND0107647
  • Regions: US
  • Patient Conditions:
      • Name: Cardiogenic Shock
      • Drugbank Id: DBCOND0030788

Food Interactions

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

Interactions

Type in a drug name to check for interaction with Bisoprolol
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Bisoprolol.
1,10-Phenanthroline
1,10-Phenanthroline may increase the bradycardic activities of Bisoprolol.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Bisoprolol.
2,5-Dimethoxy-4-ethylamphetamine
The therapeutic efficacy of Bisoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of Bisoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
25-desacetylrifapentine
The metabolism of Bisoprolol can be increased when combined with 25-desacetylrifapentine.
3-isobutyl-1-methyl-7H-xanthine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of Bisoprolol can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamine
The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Bisoprolol.
4-Methoxyamphetamine
The therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Bisoprolol.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Bisoprolol.
6-O-benzylguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 6-O-benzylguanine.
7-Deazaguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 7-Deazaguanine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Bisoprolol.
7,9-Dimethylguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 7,9-Dimethylguanine.
8-azaguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 8-azaguanine.
8-chlorotheophylline
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 8-chlorotheophylline.
9-Deazaguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 9-Deazaguanine.
9-Methylguanine
The risk or severity of adverse effects can be increased when Bisoprolol is combined with 9-Methylguanine.
Abacavir
Bisoprolol may decrease the excretion rate of Abacavir which could result in a higher serum level.
20 References
  1. 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.PubMed: 2903820
  2. 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.PubMed: 18612186
  3. 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.PubMed: 18472978
  4. 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.PubMed: 2876722
  5. 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.PubMed: 12795776
  6. 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.PubMed: 2887325
  7. 7 . Chatterjee SS: The cardioselective and hypotensive effects of bisoprolol in hypertensive asthmatics. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S74-7.PubMed: 2439803
  8. 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.PubMed: 28357786
  9. 9 . Leopold G: Balanced pharmacokinetics and metabolism of bisoprolol. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S16-20.PubMed: 2439789
  10. 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.PubMed: 26996442
  11. 11 . Peterson CD, Leeder JS, Sterner S: Glucagon therapy for beta-blocker overdose. Drug Intell Clin Pharm. 1984 May;18(5):394-8.PubMed: 6144498
  12. 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.PubMed: 25359873
  13. 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.PubMed: 18268926
  14. 14 . William D. Tucker; Pramod Theetha Kariyanna (2019). Selective B1 blockers. Stat Pearls Publishing.
  15. 15 . National Collaborating Centre for Women's and Children's Health (UK) (2010). NICE Guidelines for hypertension in pregnancy. RCOG Press.
  16. 16 . Bisoprolol monograph Link
  17. 17 . Summary of product characteristics Link
  18. 18 . Bisoprolol, health links AU Link
  19. 19 . CaymanChem: Bisoprolol MSDS Link
  20. 20 . Monograph, Bisoprolol Link