[Intracellular penetration of macrolides].
CELL PENETRATION: One of the main features of macrolides is their capacity to penetrate host cells. This property is the basis of their action against intercellular microorganisms and can explain characteristic pharmacokinetics as well as interference with cell metabolism. INTRACELLULAR CONCENTRATION: Erythromycin A derivatives with a single base group (roxithromycin) accumulate rapidly to a saturation point both the cytoplasm and in granulations. Intracellular concentrations of derivatives with two base groups do not reach saturation due to slow exflux. THERAPEUTIC ACTION: Because of their intracellular concentration, macrolides are indicated for the treatment of cell-associated pathogens. Exflux allows possible selective transfer into infected tissues. Macrolides also have an effect on functional activity of the host cells.
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INSERM U294, Service d'Hématologie, et d'Immunologie biologiques, CHU Xavier Bichat, Paris.
D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics*; D001693:Biological Transport, Active; D002463:Cell Membrane Permeability; D006801:Humans; D018942:Macrolides; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D018942:Macrolides