Bisoprolol Half-Life

Bisoprolol has a plasma elimination half-life of 9-12 hours, which allows for once-daily dosing. 1

Pharmacokinetic Properties

Bisoprolol is a beta-1 selective (cardioselective) adrenoceptor blocking agent with a long half-life of 9-12 hours in healthy individuals 1
The half-life is slightly longer in elderly patients, primarily due to decreased renal function in this population 1
Bisoprolol has high oral bioavailability (approximately 80%) with absorption not affected by food 1
Peak plasma concentrations occur within 2-4 hours after oral administration 1
Steady state is attained within 5 days of once-daily dosing, with low plasma accumulation (accumulation factor 1.1-1.3) 1
Plasma protein binding is approximately 30%, which makes it less susceptible to protein-binding drug interactions 2

Bisoprolol features "balanced clearance" with elimination equally distributed between renal and non-renal (hepatic) pathways 1, 2
Approximately 50% of the dose appears unchanged in urine, with the remainder appearing as inactive metabolites 1
Less than 2% of the dose is excreted in feces 1
Bisoprolol is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase) 1
The balanced clearance mechanism provides an advantage in patients with either renal or hepatic impairment, as complete failure of one clearance pathway would only double the half-life 2

In patients with creatinine clearance less than 40 mL/min, the plasma half-life increases approximately threefold compared to healthy subjects 1
In patients with severe renal dysfunction, the elimination half-life increases by a factor of 1.96 3
In patients with liver cirrhosis, the elimination is more variable and significantly slower, with plasma half-life ranging from 8.3 to 21.7 hours 1
In uremic patients (CrCl < 5 mL/min), the elimination half-life extends to 24.2 hours 4

The long half-life of bisoprolol allows for once-daily dosing, which can improve patient adherence 5, 2
To achieve 24-hour efficacy in angina treatment, bisoprolol's long half-life makes it suitable for once-daily administration 5
When initiating bisoprolol in heart failure patients, the long half-life should be considered during dose titration, with dose adjustments made at not less than 2-week intervals 5
Due to its balanced clearance, accumulation of bisoprolol beyond a factor of 2 is unlikely even in patients with severe renal or hepatic impairment 3, 4

Bisoprolol's half-life (9-12 hours) is longer than metoprolol (3-7 hours) and propranolol (3-6 hours), but shorter than nadolol (20-24 hours) 5
The balanced clearance of bisoprolol provides advantages over beta-blockers that rely predominantly on either renal or hepatic clearance 2
Bisoprolol's predictable pharmacokinetics lead to small intra- and interindividual variability of plasma concentration time curves 2

When using bisoprolol for perioperative beta blockade, the long half-life should be considered when determining the timing of initiation before surgery 5
In patients with severe renal or hepatic impairment, the dose should not exceed 10 mg once daily due to the extended half-life 3, 4
If bisoprolol needs to be discontinued, the long half-life should be considered to avoid potential rebound effects 5