Eur J Clin Microbiol Infect Dis 1991 Feb;10(2):100-6

Intracellular distribution and activity of antibiotics.

Tulkens PM

Laboratory of Physiological Chemistry, Catholic University of Louvain, Brussels,
Belgium.

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.

Publication Types:
Review
Review, tutorial

PMID: 1864271, UI: 91323313