Bisoprolol

Bisoprolol
ATC Code C07AB07
Formula C18H31NO4
Molar Mass (g·mol−1) 325,45
Physical State solid
Melting Point (°C) 100
PKS Value 9.5
CAS Number 66722-44-9
PUB Number 2405
Drugbank ID DB00612
Solubility low in water

Basics

Bisoprolol is a representative of the so-called beta-blockers, which are most often used for heart disease. These include in particular hypertension, chest pain due to insufficient blood flow to the heart and heart failure. Within the beta blocker family, it has a special position in that it binds selectively to the beta1 adrenoreceptor and not to the beta2 subtype. It is taken by mouth. Bisoprolol is on the WHO list of essential medicines. The drug is available only on prescription.

Pharmacology

Pharmacodynamics

Bisoprolol acts cardioprotectively by selectively and competitively blocking stimulation of β1-adrenoreceptors by catecholamines (epinephrine), which are found primarily in cardiac myocytes and cardiac conduction tissue, but also in cells in the kidney. Normally, stimulation of the β1-adrenoreceptor by epinephrine and norepinephrine activates a signaling cascade that ultimately leads to increased myocardial contractility and heart rate, respectively. Bisoprolol competitively blocks activation of this cascade, thereby decreasing adrenergic stimulation of myocardial and pacemaker cells. Decreased adrenergic tone indicates decreased contractility of the myocardium and decreased heart rate of the pacemaker cells. This spares the heavily stressed heart and relieves the patient's symptoms.

Pharmacokinetics

Bisoprolol has both lipid and water soluble properties. It has high bioavailability (approximately 90%) after ingestion and approximately 30% is present bound to plasma proteins. 50% of the dose is excreted unchanged by the kidney. The remaining 50% is metabolized in the liver and then also excreted in the urine. Bisoprolol has an approximate half-life of 10-12 hours.

Toxicity

Side effects

Common side effects are headache, fatigue, diarrhea, and swelling in the legs.

More severe side effects include worsening asthma, blocking the ability to detect low blood sugar, and worsening heart failure.

There are concerns that taking it during pregnancy may be harmful to the baby. Therefore, it is not recommended to be taken during pregnancy.

Toxicological data

LD50 (mouse, oral): 100 mg-kg-1

Sources

  • PubChem
  • Drugbank
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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