Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease
作者:
W. Kirch,
I. Rose,
H.G. Demers,
G. Leopold,
J. Pabst,
E.E. Ohnhaus,
期刊:
Clinical Pharmacokinetics
(ADIS Available online 1987)
卷期:
Volume 13,
issue 2
页码: 110-117
ISSN:0312-5963
年代: 1987
出版商: ADIS
数据来源: ADIS
摘要:
The pharmacokinetics of bisoprolol were investigated following oral administration of 10mg once daily for 7 days in 8 healthy subjects, in 14 patients with different degrees of renal impairment and in 18 patients with liver disease.In healthy subjects peak and trough steady-state concentrations of 52 μg/L and 11 μg/L, respectively, an elimination half-life of 10.0 hours and total body clearance of 14.2 L/h were observed. 5.21 mg/24 hours of unchanged bisoprolol were recovered following urinary excretion during the dosage interval. In 11 patients with renal impairment (mean CLCR=28 ± 5 ml/min/1.72m2) half-life was prolonged to 18.5 hours, and peak and trough concentrations were 74 and 32 μg/L, respectively. Correspondingly, urinary excretion decreased to 3.35 mg/24 hours and total body clearance to 7.8 L/h. In uraemic patients (CLCR<5 ml/min/1.73m2) the total clearance of bisoprolol was 5.0 L/h and the elimination half-life was 24.2 hours. In patients with liver cirrhosis half-life increased to 13.5 hours, steady-state peak and trough concentrations increased to 62 and 22 μg/L, respectively, and total body clearance decreased to 10.8 L/h.The present study indicates that in patients with impairment of kidney or liver function accumulation of bisoprolol above a factor of 2 did not occur. However, in the terminal stages of insufficiency of kidney or liver function bisoprolol dosage should not exceed 10mg.
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