[Role of cefuroxime-axetil in the treatment of respiratory tract infections. Bacteriological and pharmacological data].
Cefuroxime-axetil, the 1-acetoxyethyl ester of cefuroxime, is a prodrug for oral administration. The indication of this new formulation in the treatment of community acquired RTI required an updating of its activity against respiratory pathogens. A total of 260 isolates were included in a study using MIC determination (agar dilution technique): the mode MICs for Haemophilus spp., Branhamella catarrhalis, streptococci, S. pneumoniae ranged from 0.016 to 0.5 mg/l; no difference was noted between beta-lactamase producers and non producers in Haemophilus and B. catarrhalis; coagulase positive staphylococci, E. coli, K. pneumoniae isolated from RTI exhibited mode MICs not exceeding 4 mg/l (except for methicillin-R staphylococci mode MIC greater than 128 mg/l). Simultaneously the pharmacokinetic parameters were determined in healthy volunteers after a loading dose (500 mg) of the drug: 7 consecutive samples collected after a light meal provided the following data: Cmax = 7.77 +/- 2.2 mg/l; Tmax = 2.33 +/- 0.23 hrs; t1/2 beta = 1.18 +/- 0.19 hrs; AUC = 22.17 +/- 6.4 h.mg/l. Cmax and AUC were half of these values after administration of 250 mg. These results, together with the known intrinsic beta-lactamase stability of cefuroxime, should ensure sufficient in vivo concentrations and effective in vivo antibacterial activity against most respiratory pathogens after oral administration of cefuroxime-axetil.
Bergogne-Berezin
E
E
Service de Microbiologie, CHU Bichat-Claude Bernard, Paris.
Vallée
E
E
Muller-Serieys
C
C
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002444:Cefuroxime / Q000031:analogs & derivatives / Q000097:blood / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004359:Drug Therapy, Combination / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000302:isolation & purification; D006193:Haemophilus influenzae / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D066298:In Vitro Techniques; D007711:Klebsiella pneumoniae / Q000187:drug effects / Q000302:isolation & purification; D001936:Moraxella catarrhalis / Q000187:drug effects* / Q000302:isolation & purification; D012141:Respiratory Tract Infections / Q000382:microbiology*; D013291:Streptococcus / Q000187:drug effects* / Q000302:isolation & purification
D000900:Anti-Bacterial Agents; D002444:Cefuroxime
Place du céfuroxime-axetil dans le traitement des infections respiratoires. Bases bactérologiques et pharmacologiques.