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