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Pharmacokinetics of oral acetylcysteine: absorption, binding and metabolism in patients with respiratory disorders

par Rodenstein, Daniel Oscar;De Coster, Armand ;Gazzaniga, Annibale
Référence Clinical pharmacokinetics, 3, 3, page (247-254)
Publication Publié, 1978

Article révisé par les pairs

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Résumé :

The fate of an oral 100 mg 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 hr and remained high after 24 hr; about 22% of radioactivity was excreted in urine after 24 hr. In the 5 operated patients, plasma radioactivity concentrations were comparable with those in the nonoperated patients. Lung tissue radioactivity concentrations after 5 hr 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 hr 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 hr at high concentrations.