Pharmacokinetics of ketorolac tromethamine in horses after intravenous, intramuscular, and oral single-dose administration.
Abstract: Nonsteroidal anti-inflammatory drugs (NSAIDs) are an integral component of equine analgesia, yet currently available NSAIDs are both limited in their analgesic efficacy and have adverse effects. The NSAID ketorolac tromethamine (KT) is widely used in humans as a potent morphine-sparing analgesic drug but has not been fully evaluated in horses. The purpose of this study was to determine the pharmacokinetic profile of KT in horses after intravenous (i.v.), intramuscular (i.m.), and oral (p.o.) administration. Nine healthy adult horses received a single 0.5-mg/kg dose of KT via each route of administration. Plasma was collected up to 48 h postadministration and analyzed for KT concentration using HPLC/MS/MS. Noncompartmental analysis of i.v. dosage indicated a mean plasma clearance of 8.4 (mL/min)/kg and an estimated mean volume of distribution at steady-state of 0.77 L/kg. Noncompartmental analysis of i.v., i.m., and p.o. dosages indicated mean residence times of 2.0, 2.6, and 7.1 h, respectively. The drug was rapidly absorbed after i.m. and p.o. administration, and mean bioavailability was 71% and 57% for i.m. and p.o. administration, respectively. Adverse effects were not observed after i.v., i.m., and p.o. administration. More studies are needed to evaluate the analgesic and anti-inflammatory properties of KT in horses.
© 2015 John Wiley & Sons Ltd.
Publication Date: 2015-09-28 PubMed ID: 26416348DOI: 10.1111/jvp.12260Google Scholar: Lookup
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- Journal Article
- Randomized Controlled Trial
- Research Support
- Non-U.S. Gov't
- Adult Horses
- Adverse Effects
- Analgesia
- Biological Half-Life
- Clinical Study
- Drug
- Equine Health
- High-performance Liquid Chromatography (HPLC)
- Horses
- Intramuscular Administration
- Intravenous Administration
- NSAID
- Oral Administration
- Pharmaceuticals
- Pharmacokinetics
- Plasma
- Veterinary Care
- Veterinary Medicine
- Veterinary Research
Summary
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The study investigates the pharmacokinetics, or how a drug is absorbed, distributed, metabolized, and excreted, of ketorolac tromethamine (KT) in horses. The researchers administered a single dose of KT to horses via intravenous, intramuscular, and oral methods, then analyzed plasma samples to determine KT concentration, absorption rate, and any potential adverse effects.
Study Design and Methodology
- The experiment involved nine healthy adult horses. Each horse was subjected to a single 0.5-mg/kg dose of KT. This dosage was administered via three different routes: intravenous (i.v.), intramuscular (i.m.), and oral (p.o.). The different routes were chosen to better understand how different modes of administration might affect the drug’s pharmacokinetic properties.
- After the administration of KT, plasma was collected from the horses over a period of 48 hours for analysis.
- The plasma samples were then analyzed using High-Performance Liquid Chromatography-Tandem Mass Spectrometry (HPLC/MS/MS) for KT concentration. This method is extremely sensitive and allows for precise quantification of the drug present in the blood sample.
Findings and Conclusions
- The analysis showed that KT was rapidly absorbed after both i.m. and p.o. administration. This suggests that the drug can be absorbed into the system and begin working quite quickly, which would be beneficial for pain and inflammation relief.
- Mean bioavailability, a measure of how much of the drug is available to exert its therapeutic effects, was found to be 71% and 57% for i.m. and p.o. administration, respectively. This information is crucial because it provides insights into the drug’s effectiveness and the speed at which it can produce the desired effects.
- No adverse effects were observed in the horses during the study, indicating the potential safety of KT administration in equine subjects.
- Based on the observed pharmacokinetic properties, the study concludes that more research is necessary to explore KT’s potential as an analgesic and anti-inflammatory drug for horses.
Cite This Article
APA
Bianco AW, Constable PD, Cooper BR, Taylor SD.
(2015).
Pharmacokinetics of ketorolac tromethamine in horses after intravenous, intramuscular, and oral single-dose administration.
J Vet Pharmacol Ther, 39(2), 167-175.
https://doi.org/10.1111/jvp.12260 Publication
Researcher Affiliations
- Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Purdue University, West Lafayette, IN, USA.
- Department of Veterinary Clinical Medicine, College of Veterinary Medicine, University of Illinois, Urbana-Champaign, IL, USA.
- Bindley Bioscience Center, Purdue University, West Lafayette, IN, USA.
- Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Purdue University, West Lafayette, IN, USA.
MeSH Terms
- Animals
- Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
- Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
- Cross-Over Studies
- Drug Administration Routes
- Female
- Horses / blood
- Ketorolac Tromethamine / administration & dosage
- Ketorolac Tromethamine / pharmacokinetics
- Male
Citations
This article has been cited 3 times.- Wongrakpanich A, Khunkitchai N, Achayawat Y, Suksiriworapong J. Ketorolac-Loaded PLGA-/PLA-Based Microparticles Stabilized by Hyaluronic Acid: Effects of Formulation Composition and Emulsification Technique on Particle Characteristics and Drug Release Behaviors. Polymers (Basel) 2023 Jan 4;15(2).
- Jacobs CC, Schnabel LV, McIlwraith CW, Blikslager AT. Non-steroidal anti-inflammatory drugs in equine orthopaedics. Equine Vet J 2022 Jan 25;54(4):636-48.
- Woodland AN, Van der Saag D, Kimble B, White PJ, Govendir M, Lomax S. Plasma pharmacokinetic profile and efficacy of meloxicam administered subcutaneously and intramuscularly to sheep. PLoS One 2019;14(4):e0215842.
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