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Pharmacokinetics of Oral Acetylcysteine: Absorption, Binding and Metabolism in Patients with Respiratory Disorders

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Summary

The fate of an oral 100mg dose of 35S-acetylcysteine, a mucolytic agent, was studied in 10 patients with respiratory disorders, 5 of whom underwent pneumonectomy or lobectomy a few hours after administration of the drug. In the 5 nonoperated patients, plasma radioactivity concentrations were maximal after 2 to 3 hours and remained high after 24 hours: about 22% of radioactivity was excreted in urine after 24 hours. In the 5 operated patients, plasma radioactivity concentrations were comparable with those in the nonoperated patients. Lung tissue radioactivity concentrations after 5 hours were comparable with those in plasma, while the presence of small amounts of radioactivity in the bronchial secretions indicates that acetylcysteine passes into the mucus.

Total radioactivity after 5 hours consisted of free, unchanged drug and metabolites (about 22% of total in plasma, 48% in lung tissue), unchanged drug bound to protein by means of labile disulphide bridges (about 14% in plasma, 47% in lung tissue), and drug firmly bound to protein (about 64% in plasma, 5% in lung tissue).

Oral acetylcysteine is rapidly absorbed and slowly excreted and is available in the lung in an active form for at least 5 hours at high concentrations.

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Authors and Affiliations

  1. Department of Pulmonary Diseases, Hopital Universitaire Saint-Pierre, 322 rue Haute, 1000, Bruxelles, Belgium

    D. Rodenstein, A. De Coster & A. Gazzaniga

  2. The Biochemistry Department of Zambon SpA, Bresso, Milan, Italy

    D. Rodenstein, A. De Coster & A. Gazzaniga

Authors
  1. D. Rodenstein
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  2. A. De Coster
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  3. A. Gazzaniga
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Rodenstein, D., De Coster, A. & Gazzaniga, A. Pharmacokinetics of Oral Acetylcysteine: Absorption, Binding and Metabolism in Patients with Respiratory Disorders. Clin Pharmacokinet 3, 247–254 (1978). https://doi.org/10.2165/00003088-197803030-00005

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  • DOI: https://doi.org/10.2165/00003088-197803030-00005

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