title: Antimicrobial disposition in pulmonary epithelial lining fluid of horses, part III. cefquinome.
abstract: Cefquinome concentrations, following intravenous and aerosol administration to horses, in pulmonary epithelial lining fluid (PELF) were examined and compared to plasma concentrations. Single dose of cefquinome sulphate (1 mg/kg) was administered intravenously to six horses followed by a single aerosol administration (225 mg) with a wash-out period of 14 days between treatments. After each drug administration, cefquinome concentrations in plasma and PELF, obtained by intrabronchial cotton swabs, were determined. After intravenous administration, cefquinome concentrations in plasma declined fast and were not detectable after 12 h. After aerosol administration, plasma concentrations were low or below limit of quantification (LOQ) during the entire sampling period. The degree of penetration of cefquinome into PELF after intravenous administration as described by the AUC(PELF) /AUC(plasma) ratio was 0.33. Following aerosol administration, cefquinome concentrations in PELF were high, but only detectable for 4 h. Based on AUC values, total cefquinome concentrations in PELF were one-third of total plasma concentrations after intravenous administration together with shorter time above Minimum Inhibitory Concentrations (T > MIC) in PELF, thus twice daily dosing may be required when treating lower airway infections in horses. Lower doses of cefquinome can be administered as aerosols providing high local drug concentrations in lung, but additional optimization of formulation is needed to improve distribution and persistence in lung.
authors.affiliation: Faculty of Life Sciences, Department of Large Animal Sciences, University of Copenhagen, Copenhagen, Denmark. low@dkma.dk
authors.forename: L
authors.initials: L
authors.lastname: Winther
authors.forename: K E
authors.initials: KE
authors.lastname: Baptiste
authors.forename: C
authors.initials: C
authors.lastname: Friis
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001826:Body Fluids / Q000737:chemistry; D002511:Cephalosporins / Q000378:metabolism / Q000493:pharmacokinetics*; D006207:Half-Life; D006736:Horses / Q000378:metabolism*; D008168:Lung / Q000378:metabolism*; D020545:Respiratory Mucosa / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D000900:Anti-Bacterial Agents; D002511:Cephalosporins; C068212:cefquinome