Pharmacology: Bisoprolol fumarate, a cardioselective inhibitor of beta (1)-adrenoceptor, has no significant intrinsic sympathomimetic activity or membrane stabilizing activity in its therapeutic dosage. It also exhibits beta (2)-adrenoceptors inhibition and negative chronotropic effect.
Pharmacokinetics: Absorption: Bisoprolol is almost completely absorbed from the gastrointestinal tract and undergoes only minimal first-pass metabolism resulting in an oral bioavailability of about 90%. Peak plasma concentrations occur 2 to 4 hours after oral doses.
Distribution: Bisoprolol is about 30% bound to plasma proteins. Bisoprolol is moderately lipid-soluble.
Metabolism: It is metabolized in the liver.
Elimination: It has a plasma elimination half-life of 10 to 12 hours. It is excreted in urine, about 50% as unchanged drug and 50% as metabolites.