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Pharmacokinetics and protein binding of morphine in horses.

Abstract: Morphine could be detected in horses dosed with 0.1 mg of drug/kg of body weight for up to 48 hours in blood and 144 hours in urine. This dose of morphine elicited no observable effects and is a suggested analgesic dose. Computer analysis revealed that a 3-compartment open system was the best fitting model with a serum half life (t1/2(beta)) of 87.9 minutes and a urine t1/2(beta) of 101.1 minutes. Binding to equine serum proteins was linear over a drug concentration range of 3.88 X 10(-5)M to 3.50 X 10(-8)M and averaged 31.6%. In RBC-partitioning experiments, 78.1% of the drug was found in the plasma fraction. The data indicated that a horse should not be given morphine closer than 1 week before a race.
Publication Date: 1983-05-01 PubMed ID: 6869996
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  • Comparative Study
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research paper examines the pharmacokinetics—or how the body processes—a dose of morphine in horses. It found that a 0.1 mg/kg dose can be detected for up to 48 hours in blood and 144 hours in urine, with no observable side effects, making it a possible painkiller dose.

Study Method

  • The researchers administered to horses a dose of 0.1 mg of morphine per kg of body weight.
  • They then monitored and measured the amount of morphine present in the horses’ blood and urine for extended periods.
  • They also used computer analysis to create the most fitting model for the horses’ physiological processes and responses to the drug—finding that a three-compartment open system model was most appropriate.

Morphine Persistence

  • This study found that morphine can be detected in a horse’s system for quite a while. In the blood, it is detectable for up to 48 hours. In the urine, the detection window extends to up to 144 hours (or six days).
  • Despite the long presence in the body, the dose did not result in any observable effects on horses, suggesting it can be used as a non-disruptive analgesic.

Morphine Metabolism and Binding

  • The metabolism of the drug was modeled using a three-compartment open system, which produced a serum half-life (t1/2(beta)) of 87.9 minutes and a urine half-life of 101.1 minutes.
  • It was also found that morphine binds linearly to equine serum proteins across the drug concentration range studied, with an average binding of 31.6%.
  • Red Blood Cell (RBC) partitioning experiments showed that 78.1% of the drug ended up in the plasma fraction, indicating the major location of the drug after administration.

Implications for Horse Racing

  • The lingering detectability of morphine in the system of a horse has implications for horse racing. According to the data, a horse should not be administered morphine one week prior to a race due to the lengthy detection period.
  • This is particularly relevant within the context of horse racing regulations, which prohibit the use of certain substances, including morphine, for a specified period before races to ensure fair competition.

Cite This Article

APA
Combie JD, Nugent TE, Tobin T. (1983). Pharmacokinetics and protein binding of morphine in horses. Am J Vet Res, 44(5), 870-874.

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 44
Issue: 5
Pages: 870-874

Researcher Affiliations

Combie, J D
    Nugent, T E
      Tobin, T

        MeSH Terms

        • Animals
        • Blood Specimen Collection / veterinary
        • Computers
        • Dialysis / veterinary
        • Erythrocytes / metabolism
        • Female
        • Half-Life
        • Horses / metabolism
        • Humans
        • Kinetics
        • Models, Biological
        • Morphine / administration & dosage
        • Morphine / analysis
        • Morphine / metabolism
        • Protein Binding / drug effects
        • Serum Albumin / pharmacology
        • Time Factors

        Citations

        This article has been cited 1 times.
        1. Toutain PL. Pharmacokinetic/pharmacodynamic integration in drug development and dosage-regimen optimization for veterinary medicine.. AAPS PharmSci 2002;4(4):E38.
          doi: 10.1208/ps040438pubmed: 12646010google scholar: lookup