title: Serum and sputum concentrations following the oral administration of linezolid in adult patients with cystic fibrosis.
abstract: OBJECTIVE
  Linezolid is a new oxazolidinone antibiotic with efficacy against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). In this study, we have determined the serum and sputum linezolid concentrations in adults with cystic fibrosis (CF) following oral drug administration.
  
  
  METHODS
  Eleven adult patients with CF were recruited. Subjects received 600 mg of linezolid orally every 12 h for a total of six doses. Serum and sputum levels were measured just before and at 2 h after the final dose of linezolid. A further serum level was measured at 4 h.
  
  
  RESULTS
  Ten adult patients completed the study. Mean (s.d.) serum linezolid concentrations were 2.3 mg/L (1.5) at 12 h following the fifth dose. At 2 and 4 h following the sixth dose, concentrations were 13.5 (4.3) and 8.1 (3.3). Mean (s.d.) linezolid sputum concentrations were 3.6 (2.1) and 17.4 (7.2) mg/L at 0 and 2 h following drug administration.
  
  
  CONCLUSIONS
  The oral administration of linezolid results in good sputum penetration in patients with CF. Mean levels exceed the required MIC for the treatment of MRSA for >80% of the dosing period for serum and the majority of the dosing period for sputum.
authors.affiliation: Regional Adult Cystic Fibrosis Unit, Seacroft Hospital, York Road, Leeds LS14 6UH, UK.
authors.forename: Dinesh
authors.initials: D
authors.lastname: Saralaya
authors.forename: Daniel G
authors.initials: DG
authors.lastname: Peckham
authors.forename: Bill
authors.initials: B
authors.lastname: Hulme
authors.forename: Caroline M
authors.initials: CM
authors.lastname: Tobin
authors.forename: Miles
authors.initials: M
authors.lastname: Denton
authors.forename: Steve
authors.initials: S
authors.lastname: Conway
authors.forename: Christine
authors.initials: C
authors.lastname: Etherington
mesh_terms: D000081:Acetamides / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D000328:Adult; D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D003550:Cystic Fibrosis / Q000378:metabolism*; D005260:Female; D006801:Humans; D000069349:Linezolid; D008297:Male; D023303:Oxazolidinones / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D010182:Pancreatic Diseases / Q000378:metabolism; D011446:Prospective Studies; D013183:Sputum / Q000378:metabolism*
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D000069349:Linezolid