Myocor 2.5 | 1 Strip

Bisoprolol Fumarate is a highly selective β₁-adrenergic receptor blocker, demonstrating the greatest affinity for cardiac β₁ receptors compared to other available beta-blockers. By selectively inhibiting β₁-receptors in the heart and vascular smooth muscle, it lowers heart rate and cardiac output, resulting in reduced arterial blood pressure. Unlike non-selective beta-blockers, Bisoprolol does not negatively affect lipid metabolism and has no adverse impact on cholesterol fractions, including HDL, during long-term therapy.

Pharmacokinetics:

Absorption & Bioavailability: Bisoprolol is almost completely absorbed (>90%) from the gastrointestinal tract with a minimal first-pass effect (<10%), leading to an absolute bioavailability of approximately 88%. Food does not influence its absorption.

Distribution: The drug exhibits extensive distribution with an average distribution volume of 3.5 L/kg.

Metabolism: It undergoes oxidative metabolism primarily via the CYP3A4 enzyme (≈95%), with CYP2D6 playing a minor role. Its metabolites are pharmacologically inactive and are excreted through the kidneys.

Elimination: Approximately half of the drug is excreted unchanged via the kidneys, while the remainder is metabolized hepatically and then eliminated renally. The total clearance is about 15 L/h, and the elimination half-life is between 10–12 hours, allowing for once-daily dosing.