Disposition of oral telithromycin in foals and in vitro activity of the drug against macrolide-susceptible and macrolide-resistant Rhodococcus equi isolates.
Abstract: The objectives of this study were to determine the serum and pulmonary disposition of telithromycin in foals and to determine the minimum inhibitory concentration (MIC) of telithromycin against macrolide-susceptible and macrolide-resistant Rhodococcus equi isolates. A single dose of telithromycin (15 mg/kg of body weight) was administered to six healthy 6-10-week-old foals by the intragastric route. Activity of telithromycin was measured in serum, pulmonary epithelial lining fluid (PELF), and bronchoalveolar lavage (BAL) cells using a microbiological assay. The broth macrodilution method was used to determine the MIC of telithromycin, azithromycin, clarithromycin and erythromycin against R. equi. Following intragastric administration, mean +/- SD time to peak serum telithromycin activity (T(max)) was 1.75 +/- 0.76 h, maximum serum activity (C(max)) was 1.43 +/- 0.37 microg/mL, and terminal half-life (t(1/2)) was 3.81 +/- 0.40 h. Telithromycin activity, 4 h postadministration was significantly higher in BAL cells (50.9 +/- 14.5 microg/mL) than in PELF (5.07 +/- 2.64 microg/mL), and plasma (0.84 +/- 0.25 microg/mL). The MIC(90) of telithromycin for macrolide-resistant R. equi isolates (8 microg/mL) was significantly higher than that of macrolide-susceptible isolates (0.25 microg/mL). The MIC of telithromycin for macrolide-resistant isolates (MIC(50)=4.0 microg/mL) was significantly lower than that of clarithromycin (MIC(50)=24.0 microg/mL), azithromycin (MIC(50)=256 microg/mL) and erythromycin (MIC(50)=24 microg/mL).
Publication Date: 2010-07-22 PubMed ID: 20646201DOI: 10.1111/j.1365-2885.2009.01151.xGoogle Scholar: Lookup
The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
Summary
This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.
The research study focuses on understanding the effectiveness of the drug telithromycin in foals against different strains of bacteria Rhodococcus equi, which are either sensitive or resistant to macrolide-category of antibiotics. The experiment tracks how the drug behaves in the body of the foals and compares it against other antibiotics in terms of minimal inhibitory concentration required.
Study Design
- The research was conducted on six healthy foals aged between 6 to 10 weeks. Each subject was administered with an oral dose of 15 mg/kg of body weight of telithromycin. This study was intended to map the activity of the drug in serum, pulmonary epithelial lining fluid (PELF), and bronchoalveolar lavage (BAL) cells over time.
- A laboratory technique called the broth macrodilution method was used to find the minimum concentration (MIC) of various antibiotics – telithromycin, azithromycin, clarithromycin, and erythromycin – that can inhibit the growth of the bacteria Rhodococcus equi.
Results
- Around 1.75 hours post drug administration, the peak serum activity was detected. The average maximum activity was found to be 1.43 microg/mL, with a half-life of about 3.81 hours.
- The concentration of telithromycin in BAL cells compared to PELF or plasma was distinctly higher at the 4-hour mark.
- The inhibitory concentration required of telithromycin for macrolide-resistant strains of R. equi was high at 8 microg/mL, whereas for macrolide-susceptible strains it was lower at 0.25 microg/mL. Despite this, the study noticed that telithromycin showed increased effectiveness compared to other tested antibiotics against macrolide-resistant strains.
Conclusion
- The research revealed that telithromycin concentration in the body peaked in less than 2 hours and reduced by half in about 4 hours. Also, the antibiotic accumulated in a significant manner in certain areas like BAL cells.
- While the macrolide-resistant strains of R. equi needed a higher concentration of telithromycin for inhibition, the antibiotic outperformed others like azithromycin, clarithromycin, and erythromycin, suggesting that this drug might be more effective against such resistant types of the bacteria.
Cite This Article
APA
Javsicas LH, Giguère S, Womble AY.
(2010).
Disposition of oral telithromycin in foals and in vitro activity of the drug against macrolide-susceptible and macrolide-resistant Rhodococcus equi isolates.
J Vet Pharmacol Ther, 33(4), 383-388.
https://doi.org/10.1111/j.1365-2885.2009.01151.x Publication
Researcher Affiliations
- Department of Large Animal Medicine, College of Veterinary Medicine, University of Georgia, Athens, GA 30602, USA.
MeSH Terms
- Administration, Oral
- Animals
- Anti-Bacterial Agents / blood
- Anti-Bacterial Agents / pharmacokinetics
- Anti-Bacterial Agents / pharmacology
- Azithromycin / pharmacokinetics
- Bronchoalveolar Lavage / veterinary
- Bronchoalveolar Lavage Fluid / cytology
- Clarithromycin / pharmacokinetics
- Drug Resistance, Bacterial
- Epithelium / metabolism
- Erythromycin / pharmacokinetics
- Female
- Horses
- Ketolides / blood
- Ketolides / pharmacokinetics
- Ketolides / pharmacology
- Linear Models
- Lung / metabolism
- Macrolides / pharmacology
- Male
- Microbial Sensitivity Tests / veterinary
- Rhodococcus equi / drug effects
Citations
This article has been cited 2 times.- 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).
- 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.
Use Nutrition Calculator
Check if your horse's diet meets their nutrition requirements with our easy-to-use tool Check your horse's diet with our easy-to-use tool
Talk to a Nutritionist
Discuss your horse's feeding plan with our experts over a free phone consultation Discuss your horse's diet over a phone consultation
Submit Diet Evaluation
Get a customized feeding plan for your horse formulated by our equine nutritionists Get a custom feeding plan formulated by our nutritionists