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

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

Author information

1
Laboratory of Veterinary Internal Medicine, College of Veterinary Medicine, Chungnam National University, Daejeon, Republic of Korea.
2
Laboratory of Veterinary Internal Medicine, College of Veterinary Medicine, Kangwon National University, Chuncheon-si, Republic of Korea.
3
Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon, Republic of Korea.

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

PMID:
30548689
PMCID:
PMC6430889
DOI:
10.1111/jvim.15383
[Indexed for MEDLINE]
Free PMC Article

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