Pharmacokinetics and bioavailability of tildipirosin following intravenous and subcutaneous administration in horses

Ehab A Abu-Basha, Zuhair Bani Ismail, Mohammed M Ababneh, Eyad Hamzeh, Ronette Gehring

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

This study was designed to investigate the safety and pharmacokinetic (PK) profile of tildipirosin in horses after intravenous (i.v.) and subcutaneous (s.c.) injection of a single dose at 4 mg/kg of body weight (b.w.). A total of 12 healthy mixed breed horses were used in the study. Horses were monitored for systemic and local adverse effects, and whole blood samples were collected for hematology and plasma biochemistry analysis at time (0) and at 6, 24, and 72 h after drug administration. For PK analysis, blood samples were collected at pre-determined times before and after tildipirosin administration. Plasma concentrations of tildipirosin were determined using ultra-high-performance liquid chromatography-ultraviolet detection method (UHPLC-UV). All horses tolerated the i.v. injection of tildipirosin without showing any systemic adverse effects. However, a non-painful, soft swelling appeared at the s.c. injection site in 5 horses (41.7%). On average, tildipirosin reached a maximum plasma concentration (Cmax ) of 1257 ng/ml (geometric mean) between 0.5 and 1.5 h after s.c. administration (Tmax ). The geometric mean values for total body clearance (Cl), the apparent volume of distribution based on the terminal phase (Vz ), and the apparent volume of distribution at steady-state (Vss ) were 0.52 L/kg·h, 22 L/kg, and 10.0 L/kg, respectively. Data collected in this study suggests that tildipirosin can be used safely in horses with caution.

Original languageEnglish
Pages (from-to)544-551
Number of pages8
JournalJournal of Veterinary Pharmacology and Therapeutics
Volume44
Issue number4
DOIs
Publication statusPublished - Jul 2021

Bibliographical note

© 2021 John Wiley & Sons Ltd.

Keywords

  • adverse effects
  • bacterial pneumonia
  • equine
  • macrolide
  • pharmacokinetics
  • tildipirosin

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