title: Bronchoalveolar distribution of cefuroxime axetil and in-vitro efficacy of observed concentrations against respiratory pathogens.
abstract: The concentrations of cefuroxime in human alveolar macrophages (AM), epithelial lining fluid (ELF), bronchial mucosal biopsies and serum were measured after a single dose, equivalent to 500 mg of cefuroxime base, given in the form of the orally-administered pro-drug, cefuroxime axetil. Fourteen patients undergoing fibreoptic bronchoscopy with bronchoalveolar lavage were studied. The mean ELF concentration was 0.7 mg/L, that of bronchial biopsies was 1.8 mg/kg and that of serum 3.5 mg/L. AM-associated cefuroxime was detected in nine patients. To assess the in-vitro activity of the concentrations achieved at the potential sites of infection, clinical isolates of common respiratory pathogens were exposed to two concentrations of cefuroxime, based on the observed concentrations in ELF and bronchial mucosa. ELF and mucosal site concentrations were effective against Streptococcus pneumoniae (except one strain with reduced susceptibility to benzyl penicillin) and Haemophilus influenzae. The ELF concentration was less effective against Moraxella catarrhalis.
authors.affiliation: Department of Thoracic Medicine, Dudley Road Hospital, Birmingham, UK.
authors.forename: D R
authors.initials: DR
authors.lastname: Baldwin
authors.forename: J M
authors.initials: JM
authors.lastname: Andrews
authors.forename: R
authors.initials: R
authors.lastname: Wise
authors.forename: D
authors.initials: D
authors.lastname: Honeybourne
mesh_terms: D000368:Aged; D000369:Aged, 80 and over; D001419:Bacteria / Q000187:drug effects*; D001980:Bronchi / Q000378:metabolism; D001992:Bronchoalveolar Lavage Fluid / Q000737:chemistry / Q000378:metabolism*; D001999:Bronchoscopy; D002444:Cefuroxime / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology; D004848:Epithelium / Q000378:metabolism; D005260:Female; D006193:Haemophilus influenzae / Q000187:drug effects; D006801:Humans; D016676:Macrophages, Alveolar / Q000378:metabolism*; D008297:Male; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D001936:Moraxella catarrhalis / Q000187:drug effects; D011355:Prodrugs / Q000493:pharmacokinetics* / Q000494:pharmacology*; D013296:Streptococcus pneumoniae / Q000187:drug effects
chemical_list: D011355:Prodrugs; D002444:Cefuroxime; C040738:cefuroxime axetil