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Effect of Liver Function on β-Blocker Kinetics

  • Section 2A: Pharmacodynamics, Pharmacokinetics and Drug Interactions
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Summary

The role of the liver on the kinetics of β-blockers metabolised by hepatic enzyme systems (propranolol) or eliminated unchanged (atenolol and sotalol) was investigated in 55 patients with diagnostic liver biopsy, who also required β-blockers for cardiovascular diseases. Microsomal enzyme activity assay in vivo (antipyrine) and in vitro (cytochrome P-450 content), and conventional liver tests were used to reflect liver function in subjects classified by histology.

Plasma levels and clearance rate of propranolol, but not of atenolol and sotalol, were related to liver changes, rate of antipyrine elimination and cytochrome P- 450 content. Subjects with reduced serum albumin metabolised propranolol slowly but the values of other liver function tests were not useful when predicting the elimination rate of the β-blockers. The findings show that the kinetics of β-blockers eliminated unchanged are independent of the liver and these drugs are hence recommendable for patients with activated, impaired or with time- altering liver metabolism.

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Authors and Affiliations

  1. Clinical Research Unit, Department of Internal Medicine, University of Oulu and Research Center of Farmos Group Ltd, Turku, Oulu 22, SF, 90220, Finland

    Eero A. Sotaniemi (Associate Professor), R. Olavi Pelkonen, Arno J. Arranto, Sakari Säkö & Markku Anttila

  2. Clinical Research Unit, Department of Pharmacology, University of Oulu and Research Center of Farmos Group Ltd, Turku, Finland

    R. Olavi Pelkonen, Arno J. Arranto, Sakari Säkö & Markku Anttila

Authors
  1. Eero A. Sotaniemi
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  2. R. Olavi Pelkonen
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  3. Arno J. Arranto
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  4. Sakari Säkö
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  5. Markku Anttila
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Sotaniemi, E.A., Pelkonen, R.O., Arranto, A.J. et al. Effect of Liver Function on β-Blocker Kinetics. Drugs 25 (Suppl 2), 113–120 (1983). https://doi.org/10.2165/00003495-198300252-00035

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  • DOI: https://doi.org/10.2165/00003495-198300252-00035

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