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Intracellular distribution and activity of antibiotics.

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Tulkens, Paul M. [UCL]

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 of Staphylococcus aureus-infected J774 macrophages has revealed low activity of clindamycin, whereas macrolides, and even more so fluoroquinolones, easily reduce the original inoculum.

Document type Article de périodique (Journal article) – Journal Article, Research Support, Non-U.S. Gov't, Review
Access type Accès restreint
Publication date 1991
Journal information "European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology" - Vol. 10, no. 2, p. 100-6 (1991)
Peer reviewed yes
issn 0934-9723
Publication status Publié
Affiliation UCL
MESH Subject 4-Quinolones ; Aminoglycosides ; Anti-Bacterial Agents - classification - pharmacokinetics - pharmacology ; Anti-Infective Agents - pharmacokinetics - pharmacology ; Bacteria - drug effects - metabolism ; Humans ; Lactams ; Macrolides ; Macrophages - metabolism ; Staphylococcus aureus - drug effects - metabolism
Links
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Bibliographic reference Tulkens, Paul M.. Intracellular distribution and activity of antibiotics.. In: European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology, Vol. 10, no. 2, p. 100-6 (1991)
Permanent URL http://hdl.handle.net/2078.1/24735