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Journal of veterinary pharmacology and therapeutics2010; 34(5); 482-486; doi: 10.1111/j.1365-2885.2010.01248.x

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.
Publication Date: 2010-11-18 PubMed ID: 21083664DOI: 10.1111/j.1365-2885.2010.01248.xGoogle Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research is a study testing the effectiveness of Cefquinome, an antibiotic, when it is administered intravenously and through aerosols. The goal is to analyze its concentration in the lung lining fluid and compare it to its concentration in the blood, providing insights into the treatment of lower airway infections in horses.

Experiment Procedure

  • The research took place where Cefquinome sulphate was given to six horses, first as an intravenous injection of 1 mg/kg dosage, and after a 14-day rest period, as an aerosol spray of 225 mg.
  • Tests were done to measure the drug’s concentrations in the blood (plasma) and the lung lining fluid (Pulmonary Epithelial Lining Fluid, or PELF), using cotton swabs inserted intrabronchially.
  • The presence of Cefquinome was monitored over time after each type of administration—intravenous and aerosol.

Findings and Interpretations

  • Post intravenous injection, the quantity of Cefquinome in the plasma dropped quickly and could not be detected after 12 hours.
  • However, following aerosol administration, it was seen that the plasma concentrations of the drug were low or undetectable throughout the entire sampling period.
  • The penetration level of Cefquinome into PELF as described by its Area Under Curve(AUC) was 0.33, which denotes that overall drug concentrations in PELF were one-third the total plasma concentrations post intravenous administration.
  • After aerosol treatment, the PELF concentrations of Cefquinome were high, but those levels could only be detected for 4 hours.
  • Bearing these observations in mind, it is possible that twice-daily dosage might prove necessary in treatment of lower airway infections in horses.

Conclusions and Recommendations

  • Lower doses of Cefquinome could be given as aerosols, resulting in high local drug concentrations in the lungs, which would be beneficial in targeting lung infections.
  • However, further work is needed to better formulate the medication and improve its persistence and distribution in the lungs after it’s been sprayed as an aerosol.

Cite This Article

APA
Winther L, Baptiste KE, Friis C. (2010). Antimicrobial disposition in pulmonary epithelial lining fluid of horses, part III. cefquinome. J Vet Pharmacol Ther, 34(5), 482-486. https://doi.org/10.1111/j.1365-2885.2010.01248.x

Publication

ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 34
Issue: 5
Pages: 482-486

Researcher Affiliations

Winther, L
  • Faculty of Life Sciences, Department of Large Animal Sciences, University of Copenhagen, Copenhagen, Denmark. low@dkma.dk
Baptiste, K E
    Friis, C

      MeSH Terms

      • Animals
      • Anti-Bacterial Agents / metabolism
      • Anti-Bacterial Agents / pharmacokinetics
      • Area Under Curve
      • Body Fluids / chemistry
      • Cephalosporins / metabolism
      • Cephalosporins / pharmacokinetics
      • Half-Life
      • Horses / metabolism
      • Lung / metabolism
      • Respiratory Mucosa / metabolism
      • Tissue Distribution

      Citations

      This article has been cited 6 times.
      1. Hossain MA, Park HC, Jeong K, Jang YH, Kim DG, Kang J, Lee KJ. Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin in Pig against Korean Local Isolates of Actinobacillus pleuropneumoniae. Biomed Res Int 2017;2017:2469826.
        doi: 10.1155/2017/2469826pubmed: 28484709google scholar: lookup
      2. Taverne FJ, van Geijlswijk IM, Heederik DJ, Wagenaar JA, Mouton JW. Modelling concentrations of antimicrobial drugs: comparative pharmacokinetics of cephalosporin antimicrobials and accuracy of allometric scaling in food-producing and companion animals. BMC Vet Res 2016 Sep 6;12(1):185.
        doi: 10.1186/s12917-016-0817-2pubmed: 27596044google scholar: lookup
      3. Ahmad I, Hao H, Huang L, Sanders P, Wang X, Chen D, Tao Y, Xie S, Xiuhua K, Li J, Dan W, Yuan Z. Integration of PK/PD for dose optimization of Cefquinome against Staphylococcus aureus causing septicemia in cattle. Front Microbiol 2015;6:588.
        doi: 10.3389/fmicb.2015.00588pubmed: 26136730google scholar: lookup
      4. Dinakaran V, Dumka VK, Ranjan B, Balaje R, Sidhu PK. Pharmacokinetics following intravenous administration and pharmacodynamics of cefquinome in buffalo calves. Trop Anim Health Prod 2013 Oct;45(7):1509-12.
        doi: 10.1007/s11250-013-0390-7pubmed: 23456794google scholar: lookup
      5. Rodvold KA, George JM, Yoo L. Penetration of anti-infective agents into pulmonary epithelial lining fluid: focus on antibacterial agents. Clin Pharmacokinet 2011 Oct;50(10):637-64.
      6. Gao T, Liu X, Qiu D, Li Y, Qiu Z, Qi J, Li S, Guo X, Zhang Y, Wang Z, Gao X, Ma Y, Ma T. Ex Vivo Pharmacokinetic/Pharmacodynamic Integration Model of Cefquinome Against Escherichia coli in Foals. Vet Sci 2025 Mar 22;12(4).
        doi: 10.3390/vetsci12040294pubmed: 40284796google scholar: lookup