Pharmacokinetics and behavioral effects of methylphenidate in Thoroughbred horses.
Abstract: In horses given (rapid IV) methylphenidate (Ritalin, alpha-phenyl-2-piperidinacetic acid methyl ester; 0.70 mg/kg), plasma concentrations of the drug decreased rapidly at first, with an apparent alpha half-life of about 19 minutes, and then more slowly, with an apparent beta half-life of about 2.4 hours. These data were well fitted by a 2-compartment open model. In blood, about 40% of the methylphenidate present was in the plasma fraction, and of this, about 80% was plasma-protein bound. If given by subcutaneous or IM injection, plasma concentrations of methylphenidate peaked in about 1 hour and were no longer detectable (cleared) from plasma by 6 hours. Urinary clearance time, however, was longer, and between 12 and 24 hours should be allowed for a dose of methylphenidate to "clear" from urine. Using a variable-interval responding apparatus, methylphenidate was shown to stimulate the responding rate of horses up to 6 times above base line, making it the most potent central stimulant tested in this responding apparatus to date. Peak central stimulation at 30 minutes after IV dosing was seen in horses given 0.4 to 1.0 mg of methylphenidate/kg.
Publication Date: 1981-05-01 PubMed ID: 7258793
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- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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The research article presents a study on the effects of the drug methylphenidate, commonly sold as Ritalin, on Thoroughbred horses. It explores how the drug is processed in the horses’ system and its impact on their behavior.
Pharmacokinetics of Methylphenidate in Horses
- Methylphenidate was administered to Thoroughbred horses intravenously (IV). The dosage given was 0.70 mg/kg.
- Upon administration, the initial plasma concentrations of the drug decreased quickly, with an alpha half-life of about 19 minutes. This means the drug was breaking down relatively quickly in the body.
- After this initial rapid decline, the drug concentration decreased more slowly, with a beta half-life of about 2.4 hours. This shows that the drug persisted in the horses’ systems for a period of time after the rapid initial breakdown occurred.
- The study used a 2-compartment open model to accurately depict how the drug was absorbed, distributed, metabolized, and then excreted by the horse’s body.
- About 40% of the methylphenidate in the horse’s blood was found in the plasma fraction, and of this, approximately 80% was bound to plasma-proteins.
Subcutaneous or Intramuscular Administration
- If the drug was administered either subcutaneously or intramuscularly, the plasma concentrations of methylphenidate peaked in about 1 hour.
- The drug was detectable in plasma up to 6 hours after administration, signifying that it takes that long for the drug to be cleared from the plasma.
- Urinary clearance time of the drug was longer, and a dose of methylphenidate would take between 12 and 24 hours to be cleared from urine.
Behavioral Effects of Methylphenidate
- The study also documented the behavioral impact of the drug using a variable-interval responding apparatus.
- Methylphenidate was able to stimulate the response rate of horses to up to six times the baseline rate, thereby classifying it as a potent central stimulant in the apparatus used in the study.
- Peak central stimulation was observed at 30 minutes after intravenous dosing when horses were given 0.4 to 1.0 mg of methylphenidate per kg of body weight.
Cite This Article
APA
Shults T, Kownacki AA, Woods WE, Valentine R, Dougherty J, Tobin T.
(1981).
Pharmacokinetics and behavioral effects of methylphenidate in Thoroughbred horses.
Am J Vet Res, 42(5), 722-726.
Publication
Researcher Affiliations
MeSH Terms
- Animals
- Behavior, Animal / drug effects
- Horses / metabolism
- Methylphenidate / administration & dosage
- Methylphenidate / metabolism
- Methylphenidate / pharmacology
Citations
This article has been cited 1 times.- Moeller BC, Flores L, Clifford A, Alarcio G, Mosburg M, Arthur RM. Detection of Methylphenidate in Equine Hair Using Liquid Chromatography-High-Resolution Mass Spectrometry. Molecules 2021 Sep 24;26(19).
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