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. 2001 Jun;45(6):1843-6.
doi: 10.1128/AAC.45.6.1843-1846.2001.

Pharmacokinetics and tissue penetration of linezolid following multiple oral doses

T Gee  1 , R Ellis, G Marshall, J Andrews, J Ashby, R Wise
Affiliations

Pharmacokinetics and tissue penetration of linezolid following multiple oral doses

T Gee et al. Antimicrob Agents Chemother. 2001 Jun.

Abstract

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 microg/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 microg/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) microg x 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.

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Figures

FIG. 1
FIG. 1
Concentration of linezolid in plasma and inflammatory fluid versus time after final dose.
See this image and copyright information in PMC

References

    1. Ford C, Hamel J, Stapert D, Moerman J, Hutchinson H, Barbachyn M, Zurenko G. Oxazolidinones: a new class of antimicrobials. Infect Med. 1999;16:435–445.
    1. Ford C W, Hamel J C, Wilson D M, Moerman J K, Stapert D, Yancey R J, et al. In vivo activities of U-100 592 and U-100 766, novel oxazolidinone antimicrobial agents against experimental bacterial infections. Antimicrob Agents Chemother. 1996;40:1508–1513. - PMC - PubMed
    1. Forrest A, Nix D E, Ballow C H, Goss T F, Birmingham M C, Schentag J J. Pharmacodynamics of intravenous ciprofloxacin in seriously ill patients. Antimicrob Agents Chemother. 1993;37:1073–1081. - PMC - PubMed
    1. Hyatt J M, McKinnon P S, Zimmer G S, Schentag J J. The importance of pharmacokinetic/pharmacodynamic surrogate markers of outcome. Focus on antibacterial agents. Clin Pharmacokinet. 1995;28:143–160. - PubMed
    1. Lasher-Sisson T, Jungbluth G, Hopkins N K. A pharmacokinetic evaluation of concomitant administration of linezolid and aztreonam. J Clin Pharmacol. 1999;39:1277–1282. - PubMed

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