title: Lung concentrations of telithromycin after oral dosing.
abstract: Concentrations of telithromycin were measured in plasma, bronchial mucosa (BM), epithelial lining fluid (ELF) and alveolar macrophages (AM) following multiple oral doses. Concentrations were determined using a microbiological assay. There were 20 subjects in the study, allocated to three nominal time periods: 2, 12 and 24 h. Mean concentrations in plasma, BM, ELF and AM for 2, 12 and 24 h were as follows: 2 h, 1.86 mg/L, 3.88 mg/kg, 14.89 mg/L and 69.32 mg/L; 12 h, 0.23 mg/L, 1.41 mg/kg, 3.27 mg/L and 318.1 mg/L; and 24 h, 0.08 mg/L, 0.78 mg/kg, 0.97 mg/L and 161.57 mg/L. These concentrations of telithromycin in BM and ELF exceeded for 24 h the mean MIC90s of the common respiratory pathogens Streptococcus pneumoniae (0.12 mg/L) and Moraxella catarrhalis (0.03 mg/L), as well as the atypical microorganism Mycoplasma pneumoniae (0.001 mg/L), and suggest that telithromycin may be effective for the treatment of community-acquired pneumonia and chronic obstructive pulmonary disease.
authors.affiliation: Department of Medical Microbiology, City Hospital NHS Trust, Birmingham B18 7QH, UK.
authors.forename: O A
authors.initials: OA
authors.lastname: Khair
authors.forename: J M
authors.initials: JM
authors.lastname: Andrews
authors.forename: D
authors.initials: D
authors.lastname: Honeybourne
authors.forename: G
authors.initials: G
authors.lastname: Jevons
authors.forename: F
authors.initials: F
authors.lastname: Vacheron
authors.forename: R
authors.initials: R
authors.lastname: Wise
mesh_terms: D000284:Administration, Oral; D000900:Anti-Bacterial Agents / Q000097:blood / Q000493:pharmacokinetics*; D001980:Bronchi / Q000166:cytology / Q000378:metabolism; D001999:Bronchoscopy; D005260:Female; D006801:Humans; D048628:Ketolides; D008168:Lung / Q000378:metabolism*; D018942:Macrolides; D016676:Macrophages, Alveolar / Q000378:metabolism; D008297:Male; D008875:Middle Aged; D009092:Mucous Membrane / Q000378:metabolism; D017698:Postmenopause
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D018942:Macrolides; C106791:telithromycin