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Equine veterinary journal1996; 28(2); 121-125; doi: 10.1111/j.2042-3306.1996.tb01603.x

Regulatory significance of procaine residues in plasma and urine samples: preliminary communication.

Abstract: Plasma and urinary concentrations of procaine and the duration of response to procaine after its administration as a local anaesthetic to horses were studied. Following injection of a clinical dose of procaine HCl (80 mg), the concentration of procaine in plasma was less than the lower limit of quantitation and unsuitable for threshold determination. Therefore, the urinary concentration of procaine was determined after injection of a dose of 5 mg procaine HCl, the highest no-effect dose (HNED) of this agent. Free unconjugated procaine in equine urine reached a peak concentration of 23.7 ng/mL, while total (unconjugated plus conjugated) procaine peaked at 37.9 ng/mL (mean urine pH of 8.5). Because a basic drug may concentrate substantially in acidic urine, a threshold concentration of 25 ng/mL of unconjugated procaine is a reasonable and conservative threshold for procaine at this time. Horses were administered abaxial sesamoid blocks containing 2% procaine HCl (40, 80, 160 and 320 mg) and 2% procaine HCl (40 and 320 mg) with epinephrine (1:100,000) in local anaesthetic experiments. There was a significant local anaesthetic (LA) effect for all doses of procaine HCl with the duration of effect ranging from 30 min (40 mg) to 60 min (320 mg). The addition of epinephrine significantly increased the duration of local anaesthesia to 180 min for a 40 mg dose and 420 min for a 320 mg dose. Because epinephrine may extend the duration of local anaesthesia beyond a reasonable period of confinement for horses before the starting time of a race, the increased LA effect following the addition of epinephrine to procaine has regulatory significance.
Publication Date: 1996-03-01 PubMed ID: 8706643DOI: 10.1111/j.2042-3306.1996.tb01603.xGoogle Scholar: Lookup
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  • Journal Article
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  • Non-U.S. Gov't

Summary

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This research studied the presence and effects of procaine, a local anaesthetic, in horses. Specifically, the investigation focused on the concentration of procaine in horse plasma and urine, the duration of its effects, and the significant alteration of effects when combined with epinephrine.

Study on Plasma and Urinary Concentrations of Procaine

  • The experiment scrutinized the levels of procaine, a local anaesthetic, found in horses’ plasma and urine after it was administered.
  • Initially, a clinical dose of 80mg procaine was used, but the resulting concentration in plasma was below the lower quantification limit, rendering it unsuitable to set a threshold.
  • Subsequently, the concentration of procaine was measured in the horses’ urine. This was done using a dose of 5mg procaine, representing the highest dose that showed no effect (HNED) on horses.

Threshold Findings for Procaine in Horses’ Urine

  • The research identified the peak concentration of free unconjugated procaine in equine urine as 23.7 ng/mL. The highest level of total procaine, comprising both unconjugated and conjugated, was 37.9 ng/mL.
  • Given that basic drugs like procaine can accumulate greatly in acidic urine, the study proposed a reasonable and conservative threshold concentration of 25 ng/mL of unconjugated procaine.

Study on the Effects of Procaine and Epinephrine in Horses

  • Horses were administered various doses of procaine for local anaesthetic experiments. The horses were also given doses of 2% procaine with added epinephrine.
  • Even without epinephrine, all doses of procaine produced a local anaesthetic effect with durations that varied depending on the dose. However, when epinephrine was added, the duration of the anaesthetic effect significantly increased.
  • The longest effects without epinephrine lasted for 60 minutes (320mg dose), while the effects after adding epinephrine could extend up to 420 minutes (320mg dose).

Regulatory Implications

  • The research highlights regulatory implications as the addition of epinephrine to procaine increases the duration of the local anaesthesia. This extension could surpass a reasonable confinement period for horses before a race, which could potentially lead to unfair sporting outcomes or animal welfare issues.

Cite This Article

APA
Harkins JD, Mundy GD, Stanley S, Woods WE, Boyles J, Arthur RA, Sams RA, Tobin T. (1996). Regulatory significance of procaine residues in plasma and urine samples: preliminary communication. Equine Vet J, 28(2), 121-125. https://doi.org/10.1111/j.2042-3306.1996.tb01603.x

Publication

ISSN: 0425-1644
NlmUniqueID: 0173320
Country: United States
Language: English
Volume: 28
Issue: 2
Pages: 121-125

Researcher Affiliations

Harkins, J D
  • Maxwell H. Gluck Equine Research Center, University of Kentucky, Lexington 40506, USA.
Mundy, G D
    Stanley, S
      Woods, W E
        Boyles, J
          Arthur, R A
            Sams, R A
              Tobin, T

                MeSH Terms

                • Anesthetics, Local / administration & dosage
                • Anesthetics, Local / blood
                • Anesthetics, Local / urine
                • Animals
                • Dose-Response Relationship, Drug
                • Drug Combinations
                • Drug Residues / pharmacokinetics
                • Epinephrine / administration & dosage
                • Female
                • Horses / metabolism
                • Injections, Subcutaneous / veterinary
                • Procaine / administration & dosage
                • Procaine / blood
                • Procaine / urine
                • Sesamoid Bones
                • Time Factors

                Citations

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