Ryan C A, Sanchez L C, Giguère S, Vickroy T
Island Whirl Equine Colic Research Laboratory, Department of Large Animal Clinical Sciences, College of Veterinary Medicine, PO Box 100136, University of Florida, Gainesville, Florida 32610-0136, USA.
Equine Vet J. 2005 Jul;37(4):336-41. doi: 10.2746/0425164054529427.
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.
To investigate the pharmacokinetics and pharmacodynamics of pantoprazole following i.v. or intragastric administration in healthy neonatal foals.
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.
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.
Based on these data, i.v. or intragastric administration of pantoprazole results in a significant, prolonged increase in intragastric pH.
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.
质子泵抑制剂（PPIs）是治疗人和马酸相关性溃疡的主要药物。目前，在美国仅奥美拉唑口服制剂被批准用于马匹。对于无法口服给药的幼驹，静脉注射PPI将提供一种有效的治疗选择。
研究泮托拉唑在健康新生幼驹静脉注射或胃内给药后的药代动力学和药效学。
对研究开始时年龄为6 - 12天的7匹健康幼驹进行评估。治疗包括不给药、静脉注射泮托拉唑（1.5mg/kg体重）和胃内给予泮托拉唑（1.5mg/kg体重）。给药后记录24小时胃内pH值以进行药效学评估。使用高效液相色谱法测量血浆泮托拉唑浓度。
静脉注射或胃内给药后5分钟采样点可检测到血浆泮托拉唑浓度。胃内给予泮托拉唑的生物利用度为41%。基线平均每小时pH值为1.5 - 6.1。静脉注射或胃内给予泮托拉唑后2 - 24小时，相对于未治疗的幼驹，平均每小时pH值有统计学显著升高。
基于这些数据，静脉注射或胃内给予泮托拉唑可导致胃内pH值显著、持续升高。
泮托拉唑静脉制剂可为无法耐受PPI肠内给药的幼驹（如患有幽门流出道梗阻的幼驹）提供一种临床上有用的抑酸替代方法。
