Bisorif 2.5mg

Bisoprolol Fumarate is the most selective ß1 blocker. It displays highest level of affinity for the ß1 receptor than any other beta-blocker available up to now. Selectively blocks ß1 adrenergic receptor in the heart and vascular smooth muscle and reduces heart rate and cardiac output resulting in decrease of arterial hypertension. Lipid metabolism can be adversely affected by ß-blockers, in patients with non-ß1 selective ß1-blocker, but Bisoprolol does not cause any change in the cholesterol fraction including the cardioprotective HDL-cholesterol, in long-term therapy.

The pharmacokinetic properties of Bisoprolol provide the prerequisite for a single daily dose and ensure an extremely low inter and intra-individual variability of the plasma concentration profiles. The high therapeutic reliability of Bisoprolol is based on these properties.

Absorption and bioavailability: Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. The high absorption rate and the small first-pass effect (<10%) lead to an absolute bioavailability of 88%. Concomitant food intake does not affect the absorption. Distribution: Bisoprolol is extensively distributed. The medium distribution volume is 3.51/kg.

Metabolism: Bisoprolol is metabolized via oxidative pathways with no subsequent conjugation. All metabolites, being very polar, are renally eliminated. The major metabolites in human plasma and urine were found to be without pharmacological activity. In vitro data from studies in human liver microsomes show that Bisoprolol is primarily metabolized via CYPSA4 (-95%) with CYP2D6 having only a minor role.

Elimination: The clearance of Bisoprolol is balanced between renal elimination of the unchanged molecule (-50%) and hepatic metabolism (-50%) to metabolites which are also renally excreted. The total clearance of Bisoprolol is approximately 15 I/h. Bisoprolol has an elimination half-life of 10-12 hours.

Adult: In the treatment of mild to moderate hypertension, Bisoprolol fumarate must be individualized to the needs of the patient. The usual starting dose is 5 mg once daily either added to a diuretic or alone. If the response to 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily. An appropriate interval for dose titration is 2 weeks. Increasing the dose beyond 20 mg once daily produces only a small incremental benefit.

Children: Safety and effectiveness in children have not been established.

Patients With Renal or Hepatic Impairment: In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min) as in other patients, the initial daily dose should be 5 mg. Because of the possibility of accumulation, caution must be used in dose titration. Since limited data suggest that bisoprolol fumarate is not dialysable, drug replacement is not necessary in patients undergoing dialysis.

Geriatrics: In the elderly, it is not usually necessary to adjust the dose, unless there is also significant renal or hepatic dysfunction