This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrowReprints and Permissions
Right arrow Copyright Information
Right arrow Books from ASM Press
Right arrow MicrobeWorld
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Gee, T.
Right arrow Articles by Wise, R.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Gee, T.
Right arrow Articles by Wise, R.

 Previous Article  |  Next Article 

Antimicrobial Agents and Chemotherapy, June 2001, p. 1843-1846, Vol. 45, No. 6
0066-4804/01/$04.00+0   DOI: 10.1128/AAC.45.6.1843-1846.2001
Copyright © 2001, American Society for Microbiology. All rights reserved.

Pharmacokinetics and Tissue Penetration of Linezolid following Multiple Oral Doses

Thekli Gee, Richard Ellis,dagger Gillian Marshall, Jenny Andrews, Janet Ashby, and Richard Wise*

Department of Microbiology, City Hospital NHS Trust, Birmingham, B18 7QH, United Kingdom

Received 7 August 2000/Returned for modification 17 December 2000/Accepted 26 March 2001

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.

* Corresponding author. Mailing address: Department of Microbiology, City Hospital NHS Trust, Birmingham, B18 7QH, United Kingdom. Phone: 121 507 4255. Fax: 121 551 7763. E-mail: r.wise{at}bham.ac.uk.

dagger Present address: Department of Microbiology, Tyneside District Hospital, South Shields, Tyne and Wear, NE34 0PL, England.

Antimicrobial Agents and Chemotherapy, June 2001, p. 1843-1846, Vol. 45, No. 6
0066-4804/01/$04.00+0   DOI: 10.1128/AAC.45.6.1843-1846.2001
Copyright © 2001, American Society for Microbiology. All rights reserved.


This article has been cited by other articles:

  • Schmidt, S., Sabarinath, S. N., Barbour, A., Abbanat, D., Manitpisitkul, P., Sha, S., Derendorf, H. (2009). Pharmacokinetic-Pharmacodynamic Modeling of the In Vitro Activities of Oxazolidinone Antimicrobial Agents against Methicillin-Resistant Staphylococcus aureus. Antimicrob. Agents Chemother. 53: 5039-5045 [Abstract] [Full Text]  
  • LaPlante, K. L., Sakoulas, G. (2009). Evaluating Aztreonam and Ceftazidime Pharmacodynamics with Escherichia coli in Combination with Daptomycin, Linezolid, or Vancomycin in an In Vitro Pharmacodynamic Model. Antimicrob. Agents Chemother. 53: 4549-4555 [Abstract] [Full Text]  
  • Williams, K. N., Brickner, S. J., Stover, C. K., Zhu, T., Ogden, A., Tasneen, R., Tyagi, S., Grosset, J. H., Nuermberger, E. L. (2009). Addition of PNU-100480 to First-Line Drugs Shortens the Time Needed to Cure Murine Tuberculosis. Am. J. Respir. Crit. Care Med. 180: 371-376 [Abstract] [Full Text]  
  • Williams, K. N., Stover, C. K., Zhu, T., Tasneen, R., Tyagi, S., Grosset, J. H., Nuermberger, E. (2009). Promising Antituberculosis Activity of the Oxazolidinone PNU-100480 Relative to That of Linezolid in a Murine Model. Antimicrob. Agents Chemother. 53: 1314-1319 [Abstract] [Full Text]  
  • Baldoni, D., Haschke, M., Rajacic, Z., Zimmerli, W., Trampuz, A. (2009). Linezolid Alone or Combined with Rifampin against Methicillin-Resistant Staphylococcus aureus in Experimental Foreign-Body Infection. Antimicrob. Agents Chemother. 53: 1142-1148 [Abstract] [Full Text]  
  • LaPlante, K. L., Leonard, S. N., Andes, D. R., Craig, W. A., Rybak, M. J. (2008). Activities of Clindamycin, Daptomycin, Doxycycline, Linezolid, Trimethoprim-Sulfamethoxazole, and Vancomycin against Community-Associated Methicillin-Resistant Staphylococcus aureus with Inducible Clindamycin Resistance in Murine Thigh Infection and In Vitro Pharmacodynamic Models. Antimicrob. Agents Chemother. 52: 2156-2162 [Abstract] [Full Text]  
  • Moise, P. A, Castro, R. S, Sul, C., Forrest, A., Sakoulas, G. (2008). Relationship of Linezolid Minimum Inhibitory Concentration and Time to Bacterial Eradication in Treatment for Methicillin-Resistant Staphylococcus aureus Infection. The Annals of Pharmacotherapy 42: 592-593 [Full Text]  
  • Kohno, S., Yamaguchi, K., Aikawa, N., Sumiyama, Y., Odagiri, S., Aoki, N., Niki, Y., Watanabe, S., Furue, M., Ito, T., Croos-Dabrera, R., Tack, K. J. (2007). Linezolid versus vancomycin for the treatment of infections caused by methicillin-resistant Staphylococcus aureus in Japan. J Antimicrob Chemother 60: 1361-1369 [Abstract] [Full Text]  
  • Stein, G. E., Schooley, S., Peloquin, C. A., Missavage, A., Havlichek, D. H. (2007). Linezolid tissue penetration and serum activity against strains of methicillin-resistant Staphylococcus aureus with reduced vancomycin susceptibility in diabetic patients with foot infections. J Antimicrob Chemother 60: 819-823 [Abstract] [Full Text]  
  • Richter, E., Rusch-Gerdes, S., Hillemann, D. (2007). First Linezolid-Resistant Clinical Isolates of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 51: 1534-1536 [Abstract] [Full Text]  
  • Myrianthefs, P., Markantonis, S. L., Vlachos, K., Anagnostaki, M., Boutzouka, E., Panidis, D., Baltopoulos, G. (2006). Serum and Cerebrospinal Fluid Concentrations of Linezolid in Neurosurgical Patients. Antimicrob. Agents Chemother. 50: 3971-3976 [Abstract] [Full Text]  
  • Buerger, C., Plock, N., Dehghanyar, P., Joukhadar, C., Kloft, C. (2006). Pharmacokinetics of unbound linezolid in plasma and tissue interstitium of critically ill patients after multiple dosing using microdialysis.. Antimicrob. Agents Chemother. 50: 2455-2463 [Abstract] [Full Text]  
  • Weigelt, J., Itani, K., Stevens, D., Lau, W., Dryden, M., Knirsch, C., the Linezolid CSSTI Study Group, (2005). Linezolid versus Vancomycin in Treatment of Complicated Skin and Soft Tissue Infections. Antimicrob. Agents Chemother. 49: 2260-2266 [Abstract] [Full Text]  
  • Dehghanyar, P., Burger, C., Zeitlinger, M., Islinger, F., Kovar, F., Muller, M., Kloft, C., Joukhadar, C. (2005). Penetration of Linezolid into Soft Tissues of Healthy Volunteers after Single and Multiple Doses. Antimicrob. Agents Chemother. 49: 2367-2371 [Abstract] [Full Text]  
  • Schriever, C., Zeitz-Colaizzi, L., Quinn, A., Schriever, A. E., Cannon, J. P. (2005). Considerations for the Management of Gram-Positive Pathogens in the Intensive Care Unit. Journal of Pharmacy Practice 18: 100-108 [Abstract]  
  • Mersfelder, T. L., Smith, C. L. (2005). Linezolid pharmacokinetics in an obese patient. Am J Health Syst Pharm 62: 464-467 [Full Text]  
  • Whitehouse, T., Cepeda, J. A., Shulman, R., Aarons, L., Nalda-Molina, R., Tobin, C., MacGowan, A., Shaw, S., Kibbler, C., Singer, M., Wilson, A. P. R. (2005). Pharmacokinetic studies of linezolid and teicoplanin in the critically ill. J Antimicrob Chemother 55: 333-340 [Abstract] [Full Text]  
  • LaPlante, K. L., Rybak, M. J. (2004). Impact of High-Inoculum Staphylococcus aureus on the Activities of Nafcillin, Vancomycin, Linezolid, and Daptomycin, Alone and in Combination with Gentamicin, in an In Vitro Pharmacodynamic Model. Antimicrob. Agents Chemother. 48: 4665-4672 [Abstract] [Full Text]  
  • Rodriguez, J. C., Cebrian, L., Lopez, M., Ruiz, M., Jimenez, I., Royo, G. (2004). Mutant prevention concentration: comparison of fluoroquinolones and linezolid with Mycobacterium tuberculosis. J Antimicrob Chemother 53: 441-444 [Abstract] [Full Text]  
  • Saralaya, D., Peckham, D. G., Hulme, B., Tobin, C. M., Denton, M., Conway, S., Etherington, C. (2004). Serum and sputum concentrations following the oral administration of linezolid in adult patients with cystic fibrosis. J Antimicrob Chemother 53: 325-328 [Abstract] [Full Text]  
  • Kutscha-Lissberg, F., Hebler, U., Muhr, G., Koller, M. (2003). Linezolid Penetration into Bone and Joint Tissues Infected with Methicillin-Resistant Staphylococci. Antimicrob. Agents Chemother. 47: 3964-3966 [Abstract] [Full Text]  
  • Gordi, T., Tan, L. H., Hong, C., Hopkins, N. J., Francom, S. F., Slatter, J. G., Antal, E. J. (2003). The Pharmacokinetics of Linezolid Are Not Affected by Concomitant Intake of the Antioxidant Vitamins C and E. J Clin Pharmacol 43: 1161-1167 [Abstract] [Full Text]  
  • Honeybourne, D., Tobin, C., Jevons, G., Andrews, J., Wise, R. (2003). Intrapulmonary penetration of linezolid. J Antimicrob Chemother 51: 1431-1434 [Abstract] [Full Text]  
  • Andes, D., van Ogtrop, M. L., Peng, J., Craig, W. A. (2002). In Vivo Pharmacodynamics of a New Oxazolidinone (Linezolid). Antimicrob. Agents Chemother. 46: 3484-3489 [Abstract] [Full Text]  
  • Burkhardt, O., Borner, K., von der Hoh, N., Koppe, P., Pletz, M. W., Nord, C. E., Lode, H. (2002). Single- and multiple-dose pharmacokinetics of linezolid and co-amoxiclav in healthy human volunteers. J Antimicrob Chemother 50: 707-712 [Abstract] [Full Text]  
  • Buchanan, L. V., Dailey, C. F., LeMay, R. J., Zielinski, R. J., Kuo, M.-S. T., Gibson, J. K. (2002). Time-dependent antibacterial effects of linezolid in experimental rabbit endocarditis. J Antimicrob Chemother 50: 440-442 [Full Text]  
  • Lovering, A. M., Zhang, J., Bannister, G. C., Lankester, B. J. A., Brown, J. H. M., Narendra, G., MacGowan, A. P. (2002). Penetration of linezolid into bone, fat, muscle and haematoma of patients undergoing routine hip replacement. J Antimicrob Chemother 50: 73-77 [Abstract] [Full Text]  


Copyright © 2009 by the American Society for Microbiology.   For an alternate route to Journals.ASM.org, visit: http://intl-journals.asm.org | More Info»