title: Pulmonary disposition of tilmicosin in foals and in vitro activity against Rhodococcus equi and other common equine bacterial pathogens.
abstract: The objectives of this study were to determine the serum and pulmonary disposition of tilmicosin in foals and to investigate the in vitro activity of the drug against Rhodococcus equi and other common bacterial pathogens of horses. A single dose of a new fatty acid salt formulation of tilmicosin (10 mg/kg of body weight) was administered to seven healthy 5- to 8-week-old foals by the intramuscular route. Concentrations of tilmicosin were measured in serum, lung tissue, pulmonary epithelial lining fluid (PELF), bronchoalveolar lavage (BAL) cells, and blood neutrophils. Mean peak tilmicosin concentrations were significantly different between sampling sites with highest concentrations measured in blood neutrophils (66.01+/-15.97 microg/mL) followed by BAL cells (20.1+/-5.1 microg/mL), PELF (2.91+/-1.15 microg/mL), lung tissue (1.90+/-0.65 microg/mL), and serum (0.19+/-0.09 microg/mL). Harmonic mean terminal half-life in lung tissue (193.3 h) was significantly longer than that of PELF (73.3 h), bronchoalveolar cells (62.2 h), neutrophils (47.9 h), and serum (18.4 h). The MIC90 of 56 R. equi isolates was 32 microg/mL. Tilmicosin was active in vitro against most streptococci, Staphylococcus spp., Actinobacillus spp., and Pasteurella spp. The drug was not active against Enterococcus spp., Pseudomonas spp., and Enterobacteriaceae.
authors.affiliation: Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville, FL 32610, USA.
authors.forename: A
authors.initials: A
authors.lastname: Womble
authors.forename: S
authors.initials: S
authors.lastname: Giguère
authors.forename: Y V S N
authors.initials: YV
authors.lastname: Murthy
authors.forename: C
authors.initials: C
authors.lastname: Cox
authors.forename: E
authors.initials: E
authors.lastname: Obare
mesh_terms: D000818:Animals; D000831:Animals, Newborn / Q000378:metabolism; D019540:Area Under Curve; D018893:Bronchoalveolar Lavage / Q000662:veterinary; D005260:Female; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006736:Horses / Q000378:metabolism*; D008168:Lung / Q000166:cytology / Q000378:metabolism*; D018942:Macrolides / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D008826:Microbial Sensitivity Tests / Q000662:veterinary; D016929:Rhodococcus equi / Q000187:drug effects*; D015645:Tylosin / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D018942:Macrolides; C052319:tilmicosin; D015645:Tylosin