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Journal of veterinary pharmacology and therapeutics2006; 29(6); 561-568; doi: 10.1111/j.1365-2885.2006.00804.x

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.
Publication Date: 2006-11-07 PubMed ID: 17083461DOI: 10.1111/j.1365-2885.2006.00804.xGoogle Scholar: Lookup
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  • Journal Article

Summary

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This study investigated the effects and effectiveness of tilmicosin, a commonly used antibiotic, in young horses. The researchers looked at how the drug behaved in the bloodstream and lungs, and how it acted against certain common types of bacteria that harm horses.

Methodology

  • The research administered a single dose of a new formulation of tilmicosin, dissolved in a fatty acid salt, to seven healthy young foals that were 5 to 8 weeks old.
  • The dosage was given intramuscularly (injected into a muscle), at a dose rate of 10 mg per kg of body weight.
  • The researchers then measured concentrations of the drug in various locations within the foals’ bodies, including their blood serum, lung tissue, Pulmonary Epithelial Lining Fluid (PELF), Bronchoalveolar Lavage (BAL) cells, and blood neutrophils.

Findings

  • The levels of tilmicosin were different in various parts of the foals’ bodies. The drug was most concentrated in the blood neutrophils, followed by the BAL cells, then the PELF, and least concentrated in the serum.
  • The antibiotic persisted for varying times in different tissues, with the longest retention time in lung tissue, then PELF, followed by BAL cells, neutrophils, and serum.
  • In laboratory tests, tilmicosin showed potency against most of the 56 strains of the Rhodococcus equi bacteria tested. It was also effective against most types of streptococci, a group of bacteria that include the cause of ‘strep throat’ in humans, plus Staphylococcus, Actinobacillus, and Pasteurella species. However, this antibiotic was not effective against Enterococcus, Pseudomonas, and Enterobacteriaceae species.

Implications

  • This research provides valuable insights into how the drug tilmicosin behaves in the bodies of young foals. This is particularly important for the treatment of bacterial diseases in horses, as it demonstrates how the antibiotic is distributed and how long it persists in different tissues.
  • The findings will help veterinarians to plan the best dosing strategies for treating equine diseases, especially respiratory tract diseases, caused by susceptible bacteria.
  • However, the finding that this drug is not active against some bacterial species suggests that its use may be limited in some circumstances, or that other antibiotics may also be required.

Cite This Article

APA
Womble A, Giguère S, Murthy YV, Cox C, Obare E. (2006). Pulmonary disposition of tilmicosin in foals and in vitro activity against Rhodococcus equi and other common equine bacterial pathogens. J Vet Pharmacol Ther, 29(6), 561-568. https://doi.org/10.1111/j.1365-2885.2006.00804.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 29
Issue: 6
Pages: 561-568

Researcher Affiliations

Womble, A
  • Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville, FL 32610, USA.
Giguère, S
    Murthy, Y V S N
      Cox, C
        Obare, E

          MeSH Terms

          • Animals
          • Animals, Newborn / metabolism
          • Area Under Curve
          • Bronchoalveolar Lavage / veterinary
          • Female
          • Gram-Negative Bacteria / drug effects
          • Gram-Positive Bacteria / drug effects
          • Horses / metabolism
          • Lung / cytology
          • Lung / metabolism
          • Macrolides / blood
          • Macrolides / pharmacokinetics
          • Macrolides / pharmacology
          • Male
          • Microbial Sensitivity Tests / veterinary
          • Rhodococcus equi / drug effects
          • Tylosin / analogs & derivatives
          • Tylosin / blood
          • Tylosin / pharmacokinetics
          • Tylosin / pharmacology

          Citations

          This article has been cited 6 times.
          1. Wang J, Zhou X, Elazab ST, Park SC, Hsu WH. Should Airway Interstitial Fluid Be Used to Evaluate the Pharmacokinetics of Macrolide Antibiotics for Dose Regimen Determination in Respiratory Infection?. Antibiotics (Basel) 2023 Apr 3;12(4).
            doi: 10.3390/antibiotics12040700pubmed: 37107062google scholar: lookup
          2. Zhang N, Zhou M, Yan X, Liu J, Yuan S, Yang H, Ding H, Zhang D, Bai Y. Pharmacokinetic and Pharmacodynamic integration of tilmicosin against Mycoplasma gallisepticum in the target infection site in chickens. Front Vet Sci 2022;9:952599.
            doi: 10.3389/fvets.2022.952599pubmed: 36246335google scholar: lookup
          3. Bordin AI, Cohen ND, Giguère S, Bray JM, Berghaus LJ, Scott B, Johnson R, Hook M. Host-directed therapy in foals can enhance functional innate immunity and reduce severity of Rhodococcus equi pneumonia. Sci Rep 2021 Jan 28;11(1):2483.
            doi: 10.1038/s41598-021-82049-ypubmed: 33510265google scholar: lookup
          4. El-Mahmoudy A, Gheith I. The anti-nociceptive potential of tilmicosin against chemical-induced but not thermal-induced pain in mice. Int J Immunopathol Pharmacol 2016 Mar;29(1):9-16.
            doi: 10.1177/0394632015593232pubmed: 26519523google scholar: lookup
          5. Avci T, Elmas M. Milk and blood pharmacokinetics of tylosin and tilmicosin following parenteral administrations to cows. ScientificWorldJournal 2014;2014:869096.
            doi: 10.1155/2014/869096pubmed: 25177733google scholar: lookup
          6. Gallina G, Lucatello L, Drigo I, Cocchi M, Scandurra S, Agnoletti F, Montesissa C. Kinetics and intrapulmonary disposition of tilmicosin after single and repeated oral bolus administrations to rabbits. Vet Res Commun 2010 Jun;34 Suppl 1:S69-72.
            doi: 10.1007/s11259-010-9385-2pubmed: 20480234google scholar: lookup