Pharmacokinetics of multiple-dose administration of eltenac in horses.
Abstract: To compare pharmacokinetics of eltenac after first and last IV administrations (0.5 mg/kg), using a multiple dosing schedule. Methods: 6 adult mares. Methods: Eltenac (50 mg/ml) was administered IV at a dosage of 0.5 mg/kg of body weight every 24 hours for days 0 through 4. On days 0 and 4, blood samples were collected before, then periodically for 8 hours after eltanac administration. Concentration of eltenac in plasma samples was determined by use of high-performance liquid chromatography. Results: On day 0, median area under the plasma eltenac concentration versus time curve (AUC) was 6.77 microg.h/ml (range, 5.61 to 8.08 microg.h/ml), median plasma clearance was 1.23 ml/min/kg (range, 1.03 to 1.40 ml/min/kg), and median steady-state volume of distribution was 191 ml/kg (range, 178 to 218 ml/kg). Median terminal half-life of eltenac was 2.36 hours (range, 2.30 to 2.98 hours). On day 4, median eltenac AUC was 6.70 microg.h/ml (range, 5.21 to 7.44 microg.h/ml), median plasma clearance was 1.23 ml/min/kg (range, 1.12 to 1.53 ml/min/kg), and median steady-state volume of distribution was 193 ml/kg (range, 172 to 205 ml/kg). Median terminal half-life of eltenac was 2.40 hours (range, 2.11 to 3.25 hours). Protein binding of eltenac, determined by ultrafiltration, was > 99% at a total plasma concentration of 36 microg/ml. Conclusions: Pharmacokinetic variables determined for each horse were not different between days 0 and 4. Conclusions: Under conditions of this study, there was no clinically relevant accumulation of eltenac in equine plasma or alteration of pharmacokinetic variables after multiple IV dosing of 0.5 mg/kg of eltenac.
Publication Date: 1998-11-26 PubMed ID: 9829405
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- Journal Article
Summary
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This research investigated the pharmacokinetics of eltenac in horses to determine if any changes occurred between the first and final intravenous administrations. It was found that there was no significant accumulation of eltenac in the horse’s blood or changes to its pharmacokinetics after multiple 0.5 mg/kg doses.
Study Design and Methodology
The study included the following design and methodology:
- Six adult mares were given an intravenous (IV) dose of eltenac every 24 hours for five consecutive days. The dosage was calculated at 0.5 mg/kg of body weight.
- Blood samples were collected on the first and last day of administration – both before administering the dose and at periodic intervals over an eight-hour period post-administration.
- The concentration of eltenac in these plasma samples was identified using a process called high-performance liquid chromatography, a method used to separate the components in a mixture, to measure the concentration of such substances.
Results
- On both the first (day 0) and last day (day 4) of eltenac administration, the median area under the curve (AUC), a parameter used in pharmacokinetics to determine the total body exposure to a drug, was found to be similar (6.77 microg.h/ml and 6.70 microg.h/ml, respectively).
- Similarly, the median plasma clearance rate, which measures how quickly the drug is eliminated from the body, and the median steady-state volume of distribution, a pharmacokinetic term referring to the apparent volume in which a drug is distributed in the body, were roughly the same on both days.
- The terminal half-life of eltenac, or the time it takes for the concentration of the drug in the body to reduce by half, was approximately 2.36 hours on the first day and 2.40 hours on the last day.
- The study also found that eltenac displayed high protein binding capacity, indicating that the drug readily binds to proteins in the blood.
Conclusions
- The pharmacokinetic variables determined were not found to be significantly different between the first and last day, indicating that there might not be any important accumulation of the drug in the horses’ bodies with multiple doses.
- The research concluded that under the conditions of this study, no clinically significant accumulation of eltenac or alterations to its pharmacokinetic variables were detected after multiple intravenous doses of 0.5 mg/kg of the substance.
This research provides valuable insights into the pharmacokinetics of eltenac in horses following multiple dosing.
Cite This Article
APA
Dyke TM, Sams RA, Thompson KG, Ashcraft SM.
(1998).
Pharmacokinetics of multiple-dose administration of eltenac in horses.
Am J Vet Res, 59(11), 1447-1450.
Publication
Researcher Affiliations
- Analytical Toxicology Laboratory, College of Veterinary Medicine, The Ohio State University, Columbus 43210-1089, USA.
MeSH Terms
- Aniline Compounds / administration & dosage
- Aniline Compounds / pharmacokinetics
- Animals
- Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
- Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
- Chromatography, High Pressure Liquid / veterinary
- Drug Administration Schedule / veterinary
- Drug Evaluation / veterinary
- Female
- Horses / metabolism
- Injections, Intravenous / veterinary
- Thiophenes / administration & dosage
- Thiophenes / pharmacokinetics
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