Intracellular bioactivity of macrolides.
A brief overview is provided of the bioactivity of macrolides against a range of bacterial species. Topics considered include the cellular pharmacokinetics of uptake and efflux of these drugs and the importance of intra- or extracellular and cytoplasmic or granular location on their activity. Emphasis is placed on the importance of synergy between macrolides and host defenses, with drug accumulation producing modification of cellular function, such as enhancement of phagocytosis, and exocytosis of polymorphonuclear neutrophils. Such interaction may explain the activity of such agents against organisms which normally inhibit fusion of phagolysosomes.
Labro
Marie Thérèse
MT
INSERM U294, CHU Xavier Bichat, Service d'Hématologie et d'Immunologie Biologiques, 46 rue Henri Huchard, 75018 Paris, France.