A new model examining intracellular and extracellular activity of amoxicillin, azithromycin, and clarithromycin in infected cells.
An in vitro infection model was created using a suspension of macrophages, polymorphonuclear leukocytes, lymphocytes, fibroblasts, and human serum to which pathogen and antibiotic were added. Separate intracellular and extracellular antibiotic concentrations and activity against Staphylococcus aureus and Legionella pneumophila were assessed for three antimicrobial agents: amoxicillin, azithromycin and clarithromycin. Amoxicillin was found almost exclusively in extracellular fluid, where it was active; intracellularly, it was ineffective. Azithromycin, in contrast, was primarily concentrated and active intracellularly, with little activity in extracellular fluid. Clarithromycin was present in both compartments and possessed significant activity both intracellularly and extracellularly.
Scaglione
F
F
Department of Pharmacology, Chemotherapy and Toxicology, University of Milan, Italy.
Demartini
G
G
Dugnani
S
S
Fraschini
F
F
D000658:Amoxicillin / Q000494:pharmacology*; D017963:Azithromycin / Q000494:pharmacology*; D001424:Bacterial Infections; D017291:Clarithromycin / Q000494:pharmacology*; D005110:Extracellular Space / Q000737:chemistry*; D005347:Fibroblasts / Q000382:microbiology; D006801:Humans; D007424:Intracellular Fluid / Q000737:chemistry*; D016952:Legionella pneumophila / Q000187:drug effects; D007962:Leukocytes / Q000382:microbiology; D008214:Lymphocytes / Q000382:microbiology; D008264:Macrophages / Q000382:microbiology; D008826:Microbial Sensitivity Tests; D008954:Models, Biological; D009504:Neutrophils / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects
D000658:Amoxicillin; D017963:Azithromycin; D017291:Clarithromycin