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Intracellular distribution and activity of antibiotics

  • P. M. Tulkens
Current Topic: Review

Abstract

Intracellular penetration, accumulation and disposition are important parameters governing the activity of antibiotics against intracellular bacteria. Beta-lactams diffuse into but do not accumulate in phagocytes, probably because of their acidic character. Aminoglycosides are too polar to pass across membranes and are therefore only taken up slowly by endocytosis, which results in an exclusively lysosomal localization. Lincosaminides, macrolides and fluoroquinolones all accumulate in phagocytes, the two former classes of drugs showing both a cytosolic and a lysosomal localization. Fluoroquinolones appear to be entirely soluble in cells. Analysis of their activity in a model ofStaphylococcus aureus-infected J774 macrophages has revealed low activity of clindamycin, whereas macrolides, and even more so fluoroquinolones, easily reduce the original inoculum.

Keywords

Internal Medicine Fluoroquinolones Aminoglycosides Macrolides Clindamycin 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Friedr. Vieweg & Sohn Verlagsgesellschaft mbH 1991

Authors and Affiliations

  • P. M. Tulkens
    • 1
  1. 1.Laboratory of Physiological ChemistryCatholic University of Louvain, and International Institute of Cellular and Molecular PathologyBrusselsBelgium

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