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Pharmacokinetics and Tissue Penetration of Linezolid following Multiple Oral Doses

The pharmacokinetics of multiple-dose linezolid were determined following administration of five 600-mg oral doses given every 12 h to each of six healthy male volunteers. Concentrations of the drug were determined in plasma and inflammatory blister fluid using high-pressure liquid chromatography. A...

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Detalhes bibliográficos
Main Authors: Gee, Thekli, Ellis, Richard, Marshall, Gillian, Andrews, Jenny, Ashby, Janet, Wise, Richard
Formato: Artigo
Idioma:en
Publicado em: American Society for Microbiology 2001
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Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC90555/
https://ncbi.nlm.nih.gov/pubmed/11353635
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.45.6.1843-1846.2001
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Resumo:The pharmacokinetics of multiple-dose linezolid were determined following administration of five 600-mg oral doses given every 12 h to each of six healthy male volunteers. Concentrations of the drug were determined in plasma and inflammatory blister fluid using high-pressure liquid chromatography. A mean peak concentration in plasma of 18.3 μg/ml (standard deviation [SD], 6.0) was attained at a mean time of 0.7 h (SD, 0.3) after the final dose. The penetration into the inflammatory fluid was 104% (SD, 20.7). A mean peak concentration of 16.4 μg/ml (SD, 10.6) was attained in the inflammatory fluid at 3 h (SD, 0.6) after the final dose. The elimination half-life from serum and inflammatory fluid was 4.9 (SD, 1.8) and 5.7 (SD, 1.7) h, respectively. The area under the concentration-time curve in plasma and blister fluid was 140.3 (SD, 73.1) and 155.3 (SD, 80.1) μg · h/ml, respectively. These data suggest that linezolid has good tissue penetration, and we can predict that it will be successful in the treatment of a variety of gram-positive infections.