title: Penetration of telithromycin into the nasal mucosa and ethmoid bone of patients undergoing rhinosurgery for chronic sinusitis.
abstract: OBJECTIVE
  Telithromycin has a broad spectrum of activity against respiratory tract pathogens including penicillin- and macrolide-resistant streptococci. The aim of the study was to investigate the penetration of telithromycin into nasal tissue following a single oral dose of 800 mg.
  
  
  METHODS
  A total of 29 patients undergoing rhinosurgery for chronic sinusitis were evaluated. Samples of blood, nasal mucus, nasal mucosa and ethmoid bone were collected during surgery in groups of 5-6 patients after 3, 6, 9, 15 and 24 h following a single oral dose of 800 mg telithromycin. Drug concentrations were determined by HPLC with fluorimetric detection.
  
  
  RESULTS
  The highest telithromycin concentrations were observed after 3 h in plasma as well as in all tissues sampled. The mean plasma concentrations were 0.73 mg/L in the 3 h group and 0.02 mg/L in the 24 h group. The concomitant tissue concentrations were higher. The tissue penetration, expressed by the ratio of the area under the concentration-time curve in tissue versus plasma, was 1.0 for nasal mucus, 5.9 for nasal mucosa and 1.6 for ethmoid bone.
  
  
  CONCLUSIONS
  Telithromycin achieved tissue concentrations that were generally above the MIC(90) for common pathogens in upper respiratory tract infections. These results indicate that telithromycin diffuses rapidly into the nasal tissues and achieves high and prolonged concentrations in nasal mucosa and ethmoid bone.
authors.affiliation: Department of Otolaryngology, University of Regensburg, D-93053 Regensburg, Germany. Thomas.Kuehnel@klinik.uni-regensburg.de
authors.forename: T S
authors.initials: TS
authors.lastname: Kuehnel
authors.forename: C
authors.initials: C
authors.lastname: Schurr
authors.forename: K
authors.initials: K
authors.lastname: Lotter
authors.forename: F
authors.initials: F
authors.lastname: Kees
mesh_terms: D000328:Adult; D000368:Aged; D000900:Anti-Bacterial Agents / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D005004:Ethmoid Bone / Q000378:metabolism*; D005260:Female; D006801:Humans; D048628:Ketolides / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D009297:Nasal Mucosa / Q000378:metabolism*; D012852:Sinusitis / Q000188:drug therapy / Q000601:surgery*
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; C106791:telithromycin