-Conguard® is a B1-selective (cardioselective) adrenoreceptor blocking agent
without significant membrane stabilizing activity or intrinsic sympathomimetic
activity in its therapeutic dosage range.
Cardioselectivity is not absolute, however, and at higher doses (>/=20mg),
bisoprolol fumarate also inhibits B2- adrenoreceptors, chiefly located in the
bronchial and vascular musculature; to retain selectivity, it is therefore important to
use the lowest effective dose.
-The absolute bioavailability after a 10mg oral dose of bisoprolol fumarate is about
-Absorption is not affected by the presence of food.
-The first pass metabolism of bisoprolol fumarate is about 20%.
-Binding to serum proteins is approximately 30%. Bisoprolol shows linear kinetics
and the plasma concentrations are proportional to the administered dose over the
dose range 5 to 20 mg.Peak plasma concentration occur within (2 - 3) hours of
dosing with 5 to 20 mg.
-The half-life of bisoprolol in plasma is ranging between 10- 12 hours.
-It is metabolised in the liver. Approximately 50% of an orally administered dose is
excreted in urine as unchanged drug and the remains appearing in the form of
inactive metabolites. In subjects with creatinine clearance < 40 ml/min, the plasma
half-life is increased approximately threefold compared to healthy subjects.
-In subjects with cirrhosis of the liver, the elimination of Conguard® is more
variable in rate and slower than that in healthy subjects. In normal volunteers
bisoprolol therapy resulted in a reduction of exercise, and isoproterenol-induced
tachycardia. The maximal effect occurred within (1- 4) hours post-dosing. Effects
persisted for 24 hours at doses equal to or greater than 5 mg.