Half-Life of Bisoprolol
The plasma elimination half-life of bisoprolol in adults with normal renal and hepatic function is 9-12 hours, allowing for once-daily dosing. 1
Pharmacokinetic Profile in Normal Function
- The FDA-approved drug label specifies a plasma elimination half-life of 9-12 hours in patients with normal organ function 1
- This half-life is slightly longer in elderly patients, partly due to age-related decline in renal function 1
- Steady-state plasma concentrations are achieved within 5 days of once-daily dosing 1
- The accumulation factor with once-daily dosing ranges from 1.1 to 1.3, which is minimal and expected from first-order kinetics 1
Comparative Context with Other Beta-Blockers
- Bisoprolol's half-life is longer than metoprolol (3-5 hours) but shorter than atenolol (6-9 hours in normal renal function) 2
- During hemodialysis, bisoprolol's half-life is 7.8 hours, demonstrating moderate dialyzability compared to atenolol (4.6 hours HD half-life) or propranolol (3.42 hours HD half-life) 2
Clinical Implications of Balanced Clearance
- Bisoprolol exhibits balanced clearance with approximately 50% renal elimination (unchanged drug in urine) and 50% hepatic metabolism to inactive metabolites 1, 3
- This balanced elimination pathway means that even with complete failure of one clearance organ (kidney or liver), the half-life would only double, preventing excessive drug accumulation 4, 3
- In patients with severe renal impairment (creatinine clearance <40 mL/min), the half-life increases approximately threefold 1
- In end-stage renal disease (CLCR <5 mL/min), the elimination half-life extends to 24.2 hours 5
- In patients with liver cirrhosis, the half-life ranges from 8.3 to 21.7 hours (mean 13.5 hours), which is more variable than in renal disease 1, 5
Dosing Considerations Based on Half-Life
- The 10-12 hour half-life supports once-daily administration in patients with normal organ function 6, 7
- Peak plasma concentrations occur 2-4 hours after oral dosing 1
- In severe renal or hepatic failure, maximum dose should not exceed 10 mg once daily to prevent accumulation beyond a factor of 2 4, 5
- No dose adjustment is necessary for patients with mild to moderate renal or hepatic dysfunction 4