Indications
Bisoprolol Fumarate tablet is used to treat hypertension, angina and moderate to severe heart failure. It is not recommended for the emergency treatment of hypertensive crises.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Bisoprolol Fumarate is the most selective ß1 blocker. Of all the beta-blockers available up to now, it shows the highest affinity for the ß1 receptor. It selectively blocks the ß1 adrenergic receptor in the heart and vascular smooth muscle, which reduces heart rate and cardiac output and so lowers arterial hypertension. Lipid metabolism can be adversely affected by ß-blockers in patients with non-ß1 selective ß1-blocker, but Bisoprolol does not change the cholesterol fractions in long-term therapy, including the cardioprotective HDL-cholesterol.
The pharmacokinetic properties of Bisoprolol make a single daily dose possible and give an extremely low inter and intra-individual variability in plasma concentration profiles. Its high therapeutic reliability rests on these properties.
Absorption and bioavailability: Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. Because absorption is high and the first-pass effect is small (<10%), the absolute bioavailability is 88%. Taking food at the same time does not affect absorption.
Distribution: Bisoprolol is extensively distributed. The medium distribution volume is 3.51/kg.
Metabolism: Bisoprolol is metabolized through oxidative pathways, with no conjugation afterwards. All the metabolites are very polar, so they are eliminated by the kidneys. The major metabolites found in human plasma and urine had no pharmacological activity. In vitro data from studies in human liver microsomes show that Bisoprolol is mainly metabolized via CYPSA4 (-95%), and CYP2D6 has only a minor role.
Elimination: Clearance of Bisoprolol is balanced between renal elimination of the unchanged molecule (-50%) and hepatic metabolism (-50%) to metabolites, which are also excreted by the kidneys. Total clearance is approximately 15 I/h. The elimination half-life of Bisoprolol is 10 to 12 hours.
Pregnancy & Breastfeeding
Pregnancy: In rats, bisoprolol fumarate did not cause birth defects (it was not teratogenic) at doses up to 150 mg/kg/day, which is 375 times the maximum recommended human daily dose. It was fetotoxic at 50 mg/kg/day, with an increase in late resorptions. At 150 mg/kg/day it was maternotoxic, meaning the mothers ate less and gained less body weight. In rabbits, bisoprolol fumarate was not teratogenic at doses up to 12.5 mg/kg/day, which is 31 times the maximum recommended human daily dose, but at 12.5 mg/kg/day it was embryolethal, with an increase in early resorptions. There are no studies in pregnant women. So bisoprolol fumarate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been found in the milk of lactating rats. It is not known whether the medicine passes into human milk. If bisoprolol fumarate is considered essential, mothers should stop nursing.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.