The single dose pharmacokinetics of bisoprolol (10 mg) in renal insufficiency: the clinical significance of balanced clearance.

Abstract

The pharmacokinetics of the beta-blocking agents presently available render some subject to accumulation in renal or hepatic failure. Bisoprolol is one of the beta blockers possessing balanced clearance (both renal and hepatic clearance) which prevents such accumulation even in the case of complete failure of kidneys or liver. The single dose pharmacokinetics of bisoprolol were studied in patients with varying degrees of renal impairment and in healthy controls. Correlations were demonstrated between creatinine clearance and elimination half-life, mean residence time, area under the curve, total clearance and maximum concentration in those with renal dysfunction. The elimination half-life increased by a factor of 1.96 in those with severe renal dysfunction. Because of its balanced clearance, it is unlikely that accumulation of bisoprolol would occur beyond a factor of 2 on dosing to a steady state. The 48 hour plasma levels in the patients on dialysis were similar to those of the patients with severe renal dysfunction. This suggest that accumulation is unlikely, even in end stage renal failure. Bisoprolol may be used safely in patients with renal dysfunction. No adjustment of dose is necessary for those with mild to moderate dysfunction, but in severe or end stage renal failure the dose should not exceed 10 mg once daily.