Epibloc Mechanism of Action

Pharmacologic Classification: Beta Blocking Agent, selective.
Pharmacology: Pharmacodynamics: Bisoprolol is a highly beta₁-selective-adrenoreceptor blocking agent, lacking intrinsic sympathomimetic and relevant membrane stabilizing activity. It only shows low affinity to the beta₂-receptor of the smooth muscles of the 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 is used for the treatment of hypertension, angina pectoris and heart failure. As with other beta₁-blocking agents, the method of acting in hypertension is unclear. However, it is known that bisoprolol reduces plasma renin activity markedly.
Antianginal mechanism: Bisoprolol by inhibiting the cardiac beta receptors inhibits the response given to sympathetic activation. That results in the decrease of heart rate and contractility this way decreasing the oxygen demand of the cardiac muscle.
Pharmacokinetics: Absorption: Bisoprolol is absorbed and has a biological availability of about 90% after oral administration.
Distribution: The plasma protein binding of bisoprolol is about 30%. The distribution volume is 3.5 L/kg.
Biotransformation and elimination: 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 metabolized by the liver to inactive metabolites which are then excreted by the kidneys. The remaining 50% is excreted by the kidneys in metabolized 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.
Linearity/non-linearity: The kinetics of bisoprolol are linear and independent of age.