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Pharmacokinetics after a single oral dose of bopindolol in patients with cirrhosis
Authors:G. Wensing  R. A. Branch  H. Humbert  E. E. Ohnhaus  Prof. Dr. W. Kirch
Affiliation:(1) I. Medizinische Klinik, Christian-Albrechts-Universität, Kiel, FRG;(2) Division of Clinical Pharmacology, Department of Pharmacology, Vanderbilt University, Nashville, USA;(3) Sandoz Laboratories, Preclinical Research Centre, Rueil-Malmaison, Paris, France;(4) Present address: Medizinische Klinik I, Friedrich-Alexander-Universität, Krankenhausstra"beta"e 12, W-8520 Erlangen, FRG
Abstract:
Summary The plasma concentration-time curve of the hydrolysis product of bopindolol has been investigated in 14 patients with cirrhosis and in 15 healthy volunteers given a single oral dose of 2 mg bopindolol. Cirrhosis was confirmed by history and clinical examination or liver biopsy.The time to maximum concentration, maximum concentration and AUC of hydrolyzed bopindolol were similar in the patients and controls. However, the elimination half-life was 6.0 h in controls and 9.5 h in cirrhotics. Antipyrine clearance was markedly decreased in patients with cirrhosis, but no correlation was found with the pharmacokinetic parameters of hydrolysed bopindolol.Although the AUC was not significantly altered in patients with cirrhosis, the longer half-life of hydrolysed bopindolol suggests impairment of its disposition in liver disease, which could lead to significant accumulation of drug during chronic dosing.
Keywords:Bopindolol  cirrhosis  antipyrine  pharmacokinetics  side effects
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