Pharmacokinetics and pharmacodynamics of intravenous esomeprazole at 2 different dosages in dogs

J Vet Intern Med. 2019 Mar;33(2):531-535. doi: 10.1111/jvim.15383. Epub 2018 Dec 13.

Abstract

Background: Although the demand for esomeprazole is increasing in veterinary medicine, the pharmacokinetics (PK) and pharmacodynamics of esomeprazole have been described in only a few studies.

Objective: To determine the PK of 0.5 and 1 mg/kg esomeprazole administered IV q12h and to investigate its effects on intragastric pH in healthy dogs.

Animals: Six adult Beagles.

Methods: Open-label, randomized, and crossover design. The dogs received 0.5 or 1 mg/kg esomeprazole IV q12h for 48 hours. Plasma concentrations of esomeprazole were measured by high-performance liquid chromatography-tandem mass spectrometry. Intragastric pH was determined using the Bravo pH monitoring system and recorded as mean percentage time (MPT) for which pH was ≥3 and ≥4 for 24 hours in each group.

Results: The peak plasma concentration and area under the curve from the time of dosing to the last measurable concentration in the 1 mg/kg group were higher than those in the 0.5 mg/kg group. However, when the dosage normalized, intergroup differences were not significant. The MPTs for which intragastric pH was ≥3 and ≥4 for 48 hours were 88% ± 7% and 81% ± 9% for the 0.5 mg/kg group and 90% ± 9% and 85% ± 11% for the 1 mg/kg group, respectively, with no significant intergroup differences.

Conclusions and clinical importance: The pharmacokinetic parameters and acid suppressant effect for 0.5 and 1 mg/kg esomeprazole were not significantly different. Furthermore, the efficacy of esomeprazole 0.5 mg/kg IV q12h was sufficient to increase intragastric pH in Beagles.

Keywords: Bravo pH monitoring system; IV; S-omeprazole; canine; q12h.

Publication types

  • Clinical Trial, Veterinary

MeSH terms

  • Animals
  • Anti-Ulcer Agents / administration & dosage
  • Anti-Ulcer Agents / pharmacokinetics
  • Anti-Ulcer Agents / pharmacology*
  • Area Under Curve
  • Chromatography, High Pressure Liquid / veterinary
  • Cross-Over Studies
  • Dogs / blood
  • Dogs / metabolism*
  • Dose-Response Relationship, Drug
  • Esomeprazole / administration & dosage
  • Esomeprazole / pharmacokinetics
  • Esomeprazole / pharmacology*
  • Gastric Acid / metabolism
  • Gastric Acidity Determination / veterinary
  • Hydrogen-Ion Concentration / drug effects
  • Injections, Intravenous / veterinary
  • Random Allocation

Substances

  • Anti-Ulcer Agents
  • Esomeprazole