Pharmacology: Pharmacodynamics: Bisoprolol fumarate is a cardioselective inhibitor of β1-adrenoceptor. It has no significant intrinsic sympathomimetic activity or membrane stabilizing activity in its therapeutic dosage. It also exhibits β2-adrenoceptors inhibition and negative chronotropic effect.
Pharmacokinetics: 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. Bisoprolol is about 30% bound to plasma proteins. It is moderately lipid soluble and is metabolized in liver. It has plasma elimination half-life of 10 to 12 hours. Bisoprolol is excreted in urine with about 50% as unchanged drug and 50% as metabolites.