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Pharmacokinetics of Oral AcetylcysteineAbsorption, Binding and Metabolism in Patients w...
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Pharmacokinetics of Oral AcetylcysteineAbsorption, Binding and Metabolism in Patients with Respiratory Disorders
作者:
D. Rodenstein,
A. De Coster,
A. Gazzaniga,
期刊:
Clinical Pharmacokinetics
(ADIS Available online 1978)
卷期:
Volume 3,
issue 3
页码: 247-254
ISSN:0312-5963
年代: 1978
出版商: ADIS
数据来源: ADIS
摘要:
The fate of an oral 100mg dose of35S-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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