The entry of antibiotic into human monocytes

Since entry of antibiotics into mononuclear phagocytes is a pre-requisite for activity against such intracellular organism, the authors have determined the uptake of 11 radiolabelled antibiotics by human peripheral blood monocytes. beta -Lactams (penicillin G, cefamandole and cefotaxime), gentamicin...

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Bibliographic Details
Published in:Journal of antimicrobial chemotherapy 1989, Vol.23 (5), p.681-689
Main Authors: LEE HAND, W, KING-THOMPSON, N. L
Format: Article
Language:English
Subjects:
Antibacterial agents
antibiotics
Antibiotics. Antiinfectious agents. Antiparasitic agents
beta -lactam antibiotics
Biological and medical sciences
chloramphenicol
clindamycin
erythromycin propionate
gentamicin
Medical sciences
metronidazole
Pharmacology. Drug treatments
roxithromycin
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Summary:Since entry of antibiotics into mononuclear phagocytes is a pre-requisite for activity against such intracellular organism, the authors have determined the uptake of 11 radiolabelled antibiotics by human peripheral blood monocytes. beta -Lactams (penicillin G, cefamandole and cefotaxime), gentamicin, and metrondiazole had a limited ability to enter monocytes, achieving cellular concentrations which were equal to or less than extracellular levels (C/E less than or equal to 1). Imipenem, a novel beta -lactam antibiotic, rapidly bound to monocytes, but cell-associated drug progressively declined during further incubation. Chloramphenicol, a lipid-soluble drug, and trimethoprim were concentrated three-fold by human monocytes. In comparison with the other antibiotics, roxithromycin (C/E = 14), clindamycin (C/E = 6 to 7) and erythromycin propionate (C/E = 4 to 5) were markedly concentrated by human monocytes.
ISSN:0305-7453
1460-2091