Pharmacokinetics and pharmacodynamics of pantoprazole in clinically normal neonatal foals

Equine Vet J. 2005 Jul;37(4):336-41. doi: 10.2746/0425164054529427.

Abstract

Reasons for performing study: Proton pump inhibitors (PPIs) are a mainstay of treatment for acid-related ulceration in man and horses. Currently, only an oral preparation of omeprazole is approved for use in horses in the USA. Intravenous administration of a PPI would provide a useful therapeutic alternative for those foals in which oral medication is not feasible.

Objective: To investigate the pharmacokinetics and pharmacodynamics of pantoprazole following i.v. or intragastric administration in healthy neonatal foals.

Methods: Seven healthy foals age 6-12 days at the start of the study were evaluated. Treatments included no drug administration, i.v. pantoprazole (1.5 mg/kg bwt) and intragastric pantoprazole (1.5 mg/kg bwt). Intragastric pH was recorded for 24 h after drug administration for pharmacodynamic evaluation. Plasma pantoprazole concentrations were measured using high-performance liquid chromatography.

Results: Plasma concentrations of pantoprazole were detectable at the 5 min sampling point following i.v. or intragastric administration. Bioavailability of intragastric-administered pantoprazole was 41%. Baseline mean hourly pH was 1.5-6.1. There was a statistically significant increase in mean hourly pH relative to untreated foals 2-24 h after i.v. or intragastric pantoprazole administration.

Conclusions: Based on these data, i.v. or intragastric administration of pantoprazole results in a significant, prolonged increase in intragastric pH.

Potential relevance: The i.v. formulation of pantoprazole may provide a clinically useful alternative means of acid suppression in foals unable to tolerate enteral administration of a PPI, such as those with pyloric outflow obstruction.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Administration, Oral
  • Animals
  • Animals, Newborn
  • Anti-Ulcer Agents / adverse effects
  • Anti-Ulcer Agents / blood
  • Anti-Ulcer Agents / pharmacokinetics*
  • Benzimidazoles / adverse effects
  • Benzimidazoles / blood
  • Benzimidazoles / pharmacokinetics*
  • Biological Availability
  • Chromatography, High Pressure Liquid / veterinary
  • Female
  • Gastric Acidity Determination / veterinary
  • Gastric Mucosa / metabolism
  • Horses / metabolism*
  • Hydrogen-Ion Concentration / drug effects
  • Injections, Intravenous / methods
  • Injections, Intravenous / veterinary
  • Male
  • Omeprazole / adverse effects
  • Omeprazole / analogs & derivatives*
  • Omeprazole / blood
  • Omeprazole / pharmacokinetics
  • Pantoprazole
  • Proton Pump Inhibitors
  • Random Allocation
  • Stomach / drug effects
  • Sulfoxides / adverse effects
  • Sulfoxides / blood
  • Sulfoxides / pharmacokinetics*

Substances

  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Anti-Ulcer Agents
  • Benzimidazoles
  • Proton Pump Inhibitors
  • Sulfoxides
  • Pantoprazole
  • Omeprazole