Bisoprolol

pharmacological · digestive · renal · Oral

Bisoprolol. Most β₁-selective of clinical β-blockers (~75:1 β₁:β₂). One of four β-blockers with evidence base for HFrEF (along with carvedilol… Oral half-life 11 h.

Most β₁-selective of clinical β-blockers (~75:1 β₁:β₂). One of four β-blockers with evidence base for HFrEF (along with carvedilol, metoprolol-succinate, nebivolol). Half renal / half hepatic clearance.

PK: the best-supported record in this batch. Leopold 1986 (PMID:2878941), 23 healthy volunteers, verbatim "mean elimination half-lives of 11 hours for the unchanged drug" and "yielded an absolute bioavailability of 90%", both stored correctly. Volume corrected 210 -> 226 L, the paper own figure, verbatim "The volume of distribution was 226 L". Because that bioavailability is ABSOLUTE, measured against an intravenous comparison, the volume and F pair legitimately here — unlike most records in this batch. The absence of an absorption rate was already honest; the abstract says only that enteral absorption "was nearly complete".

Pharmacokinetics

• Oral — t½ 11 h · F 90% · Vd 226 L

Sources: PMID:1982759, PMID:7516019, PMID:1691366, PMID:2439789