Abstract
ABSTRACT. The ability of the third generation cephalosporins to penetrate human polymorphonuclear leukocytes (PMNs) and their antibacterial activity against cell-associated Staphylococcus aureus (SA) and Haemophilus influenzae, type b (Hib) were studied. Utilizing radioactive uptake experiments, the cellular to extracellular concentration ratios were determined to be less than one for all cephalosporins at 10 and 120 min cefotaxime (0.08 ± 0.02, 0.34 ± 0.08), ceftizoxime (0.21 ± 0.11, 0.52 ± 0.18), ceftriaxone (0.12 ± 0.04, 0.38 ± 0.23), and N-formimidoyl thienamycin (0.18 ± 0.09, 0.33 ± 0.14). Third generation cephalosporins were similar to penicillin in their exclusion from PMNs. The killing of cell-associated SA and Hib were evaluated in a preopsonized cell-associated bacterial assay with radiolabelled SA/Hib (cfu/cpm) comparing activity of PMNs + antibiotics to the PMN cell control (no antibiotics) at 0.5, 2, and 4 h. PMNs alone killed ≤0.5 log SA/Hib over 4 h. Clindamycin killed significantly more SA (p < 0.01) than all other antibiotics; nafcillin killed significantly fewer SA (p < 0.05) than all other antibiotics. Although each third generation cephalosporin showed good activity against cell-associated Hib, chloramphenicol had a significantly greater effect (p < 0.05). N-formimidoyl thienamycin demonstrated good activity only after the concentration was increased in vitro to 8 μg/ml. Although cellular penetration of antibiotics may be important in the eradication of cell-associated pathogens, the overall cellular activity would appear to be multifactorial.
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Jacobs, R., Thompson, J., Kiel, D. et al. Cellular Uptake and Cell-Associated Activity of Third Generation Cephalosporins. Pediatr Res 20, 909–912 (1986). https://doi.org/10.1203/00006450-198609000-00021
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DOI: https://doi.org/10.1203/00006450-198609000-00021
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