The effects of dose and diet on the pharmacodynamics of esomeprazole in the horse

Abstract

with glandular disease [1]. When compared with omeprazole; esomeprazole, the S-enantiomer of omeprazole, has a lower first-pass hepatic metabolism, slower plasma clearance, higher peak plasma concentration, higher area under the plasma concentration-time curve and greater clinical efficacy in man. In horses, esomeprazole suppresses gastric acid production for longer than omeprazole [2]; however, efficacy in clinical cases has not been reported. Objectives: To report the outcome of esomeprazole treatment for squamous and glandular gastric disease in horses that had failed to respond to treatment with omeprazole. Study design: Case series. Methods: Regular clinical examinations and gastroscopy were performed in five horses that were treated with omeprazole (4 mg/kg per os s.i.d.) and, in the absence of improvement, were treated subsequently with esomeprazole (2 mg/kg per os s.i.d.). Management and dietary recommendations remained consistent throughout the treatment period although levels of compliance varied. Results: Esomeprazole treatment was associated with resolution of squamous and glandular gastric disease in 4/5 horses. Conclusions: Esomeprazole may be a more effective treatment for squamous and glandular gastric disease than omeprazole. Blinded case-controlled studies with larger numbers of horses are warranted. Ethical animal research: Informed client consent was obtained. Abstracts Objectives: To describe the surrounding circumstances, clinical signs, progression and outcome of i.v. catheter-associated air embolism in hospitalised horses. Study design: Multicentre retrospective study.

Preliminary investigations into a novel, long‐acting, injectable, intramuscular formulation of omeprazole in the horse

“…It is unclear which measurement location more accurately reflects healing conditions at the level of the mucosa, but it has been proposed previously that measurement location 1 may be more predictive as it is fixed in a known position 10–20 mm from the glandular mucosa, and the level of acid suppression reported at measurement location 1 in a previous study evaluating omeprazole correlates well with reported healing rates in clinical trials for the doses studied. By contrast, the exact location of the tip of the probe, and thus of measurement location 2, is not known but it can reasonably be expected to be buried in the ingesta .…”

Courses for horses: Rethinking the use of proton pump inhibitors in the treatment of equine gastric ulcer syndrome

“…Although the pharmacokinetics of oral esomeprazole have not been described in the horse, the pharmacodynamics of a novel, enteric coated formulation of esomeprazole has recently been described (Sykes et al . ). When administered to horses following the withholding of feed overnight, the magnitude and duration of acid suppression observed following the administration of 0.5 and 2.0 mg/kg bwt by mouth once daily was comparable to that achieved in the same horses receiving 1.0 and 4.0 mg/kg bwt by mouth once daily, respectively, of commercial, buffered omeprazole paste (Sykes et al .…”

“…When administered to horses following the withholding of feed overnight, the magnitude and duration of acid suppression observed following the administration of 0.5 and 2.0 mg/kg bwt by mouth once daily was comparable to that achieved in the same horses receiving 1.0 and 4.0 mg/kg bwt by mouth once daily, respectively, of commercial, buffered omeprazole paste (Sykes et al . ,d). However, when administered to horses consuming ad libitum roughage at a dose a 2.0 mg/kg bwt by mouth once daily a more pronounced and consistent acid suppressive response was observed with esomeprazole when compared with the administration of 4.0 mg/kg bwt by mouth once daily of commercial, buffered omeprazole paste in the same horses under the same conditions (Sykes et al .…”

“…However, when administered to horses consuming ad libitum roughage at a dose a 2.0 mg/kg bwt by mouth once daily a more pronounced and consistent acid suppressive response was observed with esomeprazole when compared with the administration of 4.0 mg/kg bwt by mouth once daily of commercial, buffered omeprazole paste in the same horses under the same conditions (Sykes et al . ,d). Specifically, on Day 5 the therapeutic threshold for healing, as reported in other species, was exceeded in 5/6 horses on esomeprazole at 2.0 mg/kg bwt by mouth once daily paste (Sykes et al .…”

“…Specifically, on Day 5 the therapeutic threshold for healing, as reported in other species, was exceeded in 5/6 horses on esomeprazole at 2.0 mg/kg bwt by mouth once daily paste (Sykes et al . ) compared with 3/6 horses on omeprazole at 4.0 mg/kg bwt by mouth once daily (Sykes et al . ).…”