cefoxitin and furazlocillin

The effect of protein binding upon the penetration of six-beta-lactam (three penicillins and three cephalosporins) antibiotics into tissue fluid was studied in humans. A cantharides blister technique was used. It was found that there was a linear relationship between the percentage of protein binding and the penetration into the blister fluid of the antibiotic as measured by the area under the curve of the protein-free fraction. This finding is further evidence that protein binding may have important influence upon the likely efficacy of an antimicrobial agent.

Topics: Adult; Amoxicillin; Anti-Bacterial Agents; Azlocillin; beta-Lactams; Blister; Cefoxitin; Cefsulodin; Cefuroxime; Cephalosporins; Floxacillin; Humans; Imidazolidines; Male; Penicillins; Protein Binding

Bay k 4999 and piperacillin, two new substituted ampicillins, were compared with other beta-lactam antibiotics, including carbenicillin, azlocillin, mezlocillin, benzylpenicillin, ampicillin, and cefoxitin, against a wide range of gram-positive and -negative organisms. Bay k 4999 and piperacillin were extremely active against Pseudomonas aeruginosa (50% inhibited by 2 mug/ml), being about 16-fold more active than carbenicillin. Bay k 4999 was the most active drug against Escherichia coli (50% inhibited by 0.5 mug/ml) and Klebsiella spp. (50% inhibited by 2 mug/ml). Piperacillin and Bay k 4999 were equally active against Proteus spp., and piperacillin had high activity against Bacteroides fragilis (50% inhibited by between 1 and 2 mug/ml).

Topics: Azlocillin; Bacteria; Bacteroides fragilis; Cefoxitin; Cephalosporins; Enterobacteriaceae; Haemophilus influenzae; Imidazolidines; Neisseria gonorrhoeae; Penicillins; Pseudomonas aeruginosa; Staphylococcus aureus; Streptococcus