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American journal of veterinary research2006; 67(4); 654-662; doi: 10.2460/ajvr.67.4.654

Pharmacokinetics of methylprednisolone acetate after intra-articular administration and its effect on endogenous hydrocortisone and cortisone secretion in horses.

Abstract: To determine the pharmacokinetics of methylprednisolone (MP) and develop a pharmacokinetic-pharmacodynamic model of the related changes in plasma concentrations of endogenous hydrocortisone (HYD) and cortisone (COR) following intra-articular administration of methylprednisolone acetate (MPA) in horses. Methods: 6 Thoroughbreds. Methods: In each horse, 200 mg of MPA was injected intrasynovially into a carpal joint, and plasma MP, HYD, and COR concentrations were determined via liquid chromatography-mass spectrometry. Results: A 5-compartment pharmacokinetic-pharmacodynamic model was used to describe the concatenated changes in the plasma concentrations of MP, HYD, and COR and to estimate the instantaneous rate of endogenous HYD production. The median transfer half-life (t(1/2t)) of methylprednisolone from the joint to plasma and elimination half-life (t(1/2e)) from plasma were 1.7 and 19.2 hours, respectively. Maximum plasma concentration of methylprednisolone was 7.26 +/- 3.3 ng/mL at 8 hours, which decreased to 0.11 +/- 0.08 ng/mL at 144 hours after injection. At 3 hours after MPA administration, plasma COR and HYD concentrations were significantly decreased from baseline values (from 2.9 +/- 0.28 ng/mL to 2.10 +/- 1.0 ng/mL and from 61.1 +/- 18.9 ng/mL to 25.7 +/- 12.1 ng/mL, respectively). Conclusions: The sensitivity of the analytic method used allowed complete description of the related kinetics of MP, HYD, and COR following intra-articular administration of MPA. A single intra-articular administration of MPA profoundly affected the secretion of HYD and COR in horses; secretion of endogenous corticosteroids remained suppressed for as long as 240 hours after injection.
Publication Date: 2006-04-04 PubMed ID: 16579759DOI: 10.2460/ajvr.67.4.654Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research investigated how methylprednisolone acetate, injected directly into the joint of a horse, affected the levels of the horse’s naturally occurring steroids, hydrocortisone and cortisone. The study found that this treatment significantly reduced hydrocortisone and cortisone levels for as long as 240 hours after the injection.

Research Methods

The research methods consisted of several steps:

  • Six thoroughbred horses participated in the study.
  • Each horse received an intra-articular injection of 200 mg of methylprednisolone acetate (MPA) into a carpal joint. An intra-articular injection is an injection given directly into a joint.
  • Scientists used liquid chromatography-mass spectrometry, a technique used to identify and quantify compounds in a sample, to determine the plasma concentrations of methylprednisolone (MP), hydrocortisone (HYD), and cortisone (COR) in the horses.

Research Findings

After performing these steps and analyzing the data, the researchers arrived at several findings:

  • The transfer half-life of MP from the joint to the plasma was 1.7 hours, and the elimination half-life from plasma was 19.2 hours. Half-life refers to the time it takes for the quantity of a drug in the body to reduce by half.
  • The maximum plasma concentration of MP was 7.26 +/- 3.3 ng/mL at 8 hours after the injection, which dropped to 0.11 +/- 0.08 ng/mL at 144 hours after the injection.
  • Three hours after the MPA injection, the plasma concentrations of COR and HYD significantly decreased from their baseline values.
  • The secretion of endogenous corticosteroids remained suppressed for as long as 240 hours after the injection.

Conclusion

The researchers concluded that intra-articular administration of MPA had a profound effect on HYD and COR secretion in horses, and that this effect lasted for up to 240 hours after the injection. This demonstrates the potential impact of this treatment on a horse’s naturally occurring steroids. The researchers also noted that the method used in the research was sensitive enough to fully describe the kinetics of MP, HYD, and COR after MPA administration.

Cite This Article

APA
Soma LR, Uboh CE, Luo Y, Guan F, Moate PJ, Boston RC. (2006). Pharmacokinetics of methylprednisolone acetate after intra-articular administration and its effect on endogenous hydrocortisone and cortisone secretion in horses. Am J Vet Res, 67(4), 654-662. https://doi.org/10.2460/ajvr.67.4.654

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 67
Issue: 4
Pages: 654-662

Researcher Affiliations

Soma, Lawrence R
  • New Bolton Center Campus, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, PA 19348, USA.
Uboh, Cornelius E
    Luo, Yi
      Guan, Fuyu
        Moate, Peter J
          Boston, Ray C

            MeSH Terms

            • Animals
            • Anti-Inflammatory Agents / administration & dosage
            • Anti-Inflammatory Agents / pharmacokinetics
            • Cortisone / blood
            • Cortisone / metabolism
            • Horses / blood
            • Hydrocortisone / blood
            • Hydrocortisone / metabolism
            • Injections, Intra-Articular
            • Kinetics
            • Methylprednisolone / administration & dosage
            • Methylprednisolone / analogs & derivatives
            • Methylprednisolone / pharmacokinetics
            • Methylprednisolone Acetate

            Citations

            This article has been cited 5 times.
            1. Kikuchi M, Nagata SI, Ishige T, Minamijima Y, Hirota KI, Tozaki T, Kakoi H, Kizaki K. Evaluation of the effect of glucocorticoid treatment on adrenocortical functions by monitoring endogenous hydrocortisone in horses. J Vet Med Sci 2023 Jun 13;85(6):647-652.
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            4. Yu R, Jusko WJ. Meta-Analysis and Mechanism-Based Modeling of Synovial and Plasma Pharmacokinetics and Adrenal Suppression Following Intra-Articular Injection of Methylprednisolone Acetate in Horses. J Vet Pharmacol Ther 2025 Jul;48(4):260-273.
              doi: 10.1111/jvp.13504pubmed: 40059579google scholar: lookup
            5. Knych HK. Administration Studies in Equine Antidoping Research: Designing Scientific Investigations to Effectively Direct Medication Control in Racehorses. Drug Test Anal 2025 Sep;17(9):1560-1566.
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