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Journal of veterinary pharmacology and therapeutics2021; 44(5); 714-723; doi: 10.1111/jvp.12968

Pharmacokinetics and pulmonary distribution of Draxxin® (tulathromycin) in healthy adult horses.

Abstract: The objective of this study was to determine the pharmacokinetics and tolerability of tulathromycin (Draxxin ; 2.5 mg/kg once) after intramuscular (IM), subcutaneous (SC), and slow intravenous (IV) administration to six adult horses. A three-phase design and 4-week washout period were used. Drug concentrations in blood and bronchoalveolar lavage (BAL) samples were determined by ultra-performance liquid chromatography tandem mass spectrometry and pharmacokinetic parameters calculated using noncompartmental analysis. Following SC and IM administration, all horses exhibited sweating, discomfort, and periods of recumbency. As signs were more severe after SC administration this route was only used in 3/6 horses. Intravenous administration of tulathromycin was well tolerated in all horses. Mean bioavailability was 99.4% IM and 115% SC. Mean maximum plasma concentration was 645 ng/ml IM and 373 ng/ml SC. Mean half-life was 59.8 h, 54.8 h, and 57.9 h for IV, IM, and SC administration, respectively. Mean clearance was 3.25 ml/kg/min, and mean volume of distribution was 16.8 L/kg following IV administration. Drug was detectable in plasma and BAL samples for 120 h following all routes; however, adverse effects may prevent IM use and SC use is not recommended. Tulathromycin may be a practical and affordable antimicrobial for use in adult equine patients.
Publication Date: 2021-03-14 PubMed ID: 33719056DOI: 10.1111/jvp.12968Google Scholar: Lookup
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  • Journal Article

Summary

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The study investigates the effects, tolerance and the distribution of a drug called Tulathromycin, commercially known as Draxxin, on adult horses. The drug was given in three different methods – intramuscular (IM), subcutaneous (SC) and slow intravenous (IV) to understand its behavior in the body of the horses.

Study Design

  • The study involved a three-phase experiment with a 4-week washout period between phases. Six adult horses were used in this experiment.
  • In each phase, the drug (Tulathromycin) was administered using a different method: intramuscular (IM), subcutaneous (SC), and slow intravenous (IV).
  • The blood and bronchoalveolar lavage (BAL) samples were collected from the horses and analyzed using ultra-performance liquid chromatography tandem mass spectrometry. The results from this analysis informed about the drug concentrations in the body of the horses.

Study Findings

  • All horses experienced discomfort, sweating, and periods of recumbency (lying down) following both intramuscular and subcutaneous administration of the drug.
  • Discomfort seemed to increase after subcutaneous administration, therefore this method of application was only done on three of the six horses.
  • Slow intravenous administration method seemed to be well tolerated by all horses.
  • The bioavailability of the drug was found to be 99.4% for intramuscular and 115% for subcutaneous administration.
  • After intramuscular and subcutaneous administration, the maximum plasma concentration of the drug was observed to be 645 ng/ml and 373 ng/ml respectively.
  • Mean half-life was found to be roughly equivalent for all routes: 59.8 hours for IV, 54.8 hours for IM and 57.9 hours for SC respectively.
  • For intravenous administration, the mean clearance was 3.25 ml/kg/min and the mean volume of distribution was 16.8 L/kg.
  • Also, the drug was found in the plasma and BAL samples for 120 hours after administration, irrespective of the method of injection.

Implications

  • Given the adverse effects and the discomfort faced by the horses, intramuscular use of the drug might be avoided.
  • Subcutaneous usage is not recommended due to more severe signs of discomfort in horses.
  • Tulathromycin, administered intravenously, might be a practical and affordable antimicrobial for use in adult equine patients.

Cite This Article

APA
Leventhal HR, McKenzie HC, Estell K, Council-Troche M, Davis JL. (2021). Pharmacokinetics and pulmonary distribution of Draxxin® (tulathromycin) in healthy adult horses. J Vet Pharmacol Ther, 44(5), 714-723. https://doi.org/10.1111/jvp.12968

Publication

ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 44
Issue: 5
Pages: 714-723

Researcher Affiliations

Leventhal, Hannah R
  • Department of Large Animal Clinical Sciences, Virginia-Maryland College of Veterinary Medicine, Blacksburg, VA, USA.
McKenzie, Harold C
  • Department of Large Animal Clinical Sciences, Virginia-Maryland College of Veterinary Medicine, Blacksburg, VA, USA.
Estell, Krista
  • Marion duPont Scott Equine Medical Center, Virginia-Maryland College of Veterinary Medicine, Leesburg, VA, USA.
Council-Troche, McAlister
  • Department of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Blacksburg, VA, USA.
Davis, Jennifer L
  • Department of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Blacksburg, VA, USA.

MeSH Terms

  • Animals
  • Disaccharides
  • Half-Life
  • Heterocyclic Compounds
  • Horses
  • Injections, Intramuscular / veterinary

Grant Funding

  • Zoetis

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Citations

This article has been cited 2 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. Onzere CK, Hulbert M, Sears KP, Williams LBA, Fry LM. Tulathromycin and Diclazuril Lack Efficacy against Theileria haneyi, but Tulathromycin Is Not Associated with Adverse Clinical Effects in Six Treated Adult Horses.. Pathogens 2023 Mar 14;12(3).
    doi: 10.3390/pathogens12030453pubmed: 36986375google scholar: lookup