Source: Υπουργείο Υγείας (CY) Revision Year: 2022 Publisher: Merck A.E. Hellas, 41-45 Kifissias av. (Building B), 15123 Marousi, Athens, Greece
Pharmacotherapeutic group: Beta blocking agents, selective
ATC code: C07AB07
Bisoprolol is a highly beta1-selective-adrenoceptor blocking agent, lacking intrinsic stimulating and relevant membrane stabilising activity. It only shows low affinity to the beta2-receptor of the smooth muscles of bronchi and vessels as well as to the beta2-receptors concerned with metabolic regulation. Therefore, bisoprolol is generally not to be expected to influence the airway resistance and beta2-mediated metabolic effects. Its beta1-selectivity extends beyond the therapeutic dose range.
Bisoprolol has a negative inotropic and cronotropic effect.
Bisoprolol reaches its maximal effect 3-4 hours after oral administration.
The maximal antihypertensive effect of bisoprolol is generally reached after 2 weeks.
In acute administration, bisoprolol reduces the heart rate and stroke volume, thus reducing cardiac output. In chronic administration the initially elevated peripheral resistance decreases.
Bisoprolol is absorbed and has a biological availability of about 90% after oral administration. The plasma protein binding of bisoprolol is about 30%. The distribution volume is 3.5 l/kg. Total clearance is approximately 15 l/h. The half-life in plasma of 10-12 hours gives a 24 hour effect after dosing once daily.
Bisoprolol is excreted from the body by two routes. 50% is metabolised by the liver to inactive metabolites which are then excreted by the kidneys. The remaining 50% is excreted by the kidneys in an unmetabolised form. Since the elimination takes place in the kidneys and the liver to the same extent a dosage adjustment is not required for patients with impaired liver function or renal insufficiency.
The kinetics of bisoprolol are linear and independent of age.
Preclinical data reveal no special hazard for humans based on conventional studies of general toxicity, genotoxicity or carcinogenicity. Like other beta-blockers, bisoprolol caused maternal (decreased food intake and decreased body weight) and embryo/fetal toxicity (increased incidence of resorptions, reduced birth weight of the offspring, retarded physical development) at high doses but was not teratogenic.
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