Pharmacokinetics and pharmacodynamics of meldonium in exercised thoroughbred horses

Drug Testing and Analysis
H K KnychPhilip H Kass

Abstract

Although developed as a therapeutic medication, meldonium has found widespread use in human sports and was recently added to the World Anti-Doping Agency's list of prohibited substances. Its reported abuse potential in human sports has led to concern by regulatory authorities about the possible misuse of meldonium in equine athletics. The potential abuse in equine athletes along with the limited data available regarding the pharmacokinetics and pharmacodynamics of meldonium in horses necessitates further study. Eight exercised adult thoroughbred horses received a single oral dose of 3.5, 7.1, 14.3 or 21.4 mg/kg of meldonium. Blood and urine samples were collected and analyzed using liquid chromatography tandem mass spectrometry. Pharmacokinetic parameters were determined using non-compartmental analysis. Maximum serum concentrations ranged from 440.2 to 1147 ng/mL and the elimination half-life from 422 to 647.8 h. Serum concentrations were below the limit of quantitation by days 4, 7, 12 and 12 for doses of 3.5, 7.1, 14.3 and 21.4 mg/kg, respectively. Urine concentrations were below the limit of detection by day 44 following administration of 3.5 mg/kg and day 51 for all other dose groups. No adverse effects were observed follo...Continue Reading

References

Jul 15, 2009·British Journal of Pharmacology·Edgars LiepinshMaija Dambrova
Feb 2, 2010·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Ye PengAiDong Wen
Sep 10, 2011·Journal of Cardiovascular Pharmacology and Therapeutics·Janis KukaEdgars Liepinsh
Feb 22, 2012·Journal of Veterinary Pharmacology and Therapeutics·H K KnychR M Arthur
Feb 7, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Maija DambrovaEdgars Liepinsh
Jun 6, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Edgars Liepinsh, Maija Dambrova
Jul 29, 2016·British Journal of Sports Medicine·Wolfgang SchobersbergerCornelia Blank
Dec 17, 2016·Basic & Clinical Pharmacology & Toxicology·Edgars LiepinshMaija Dambrova

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Citations

Jun 21, 2017·Drug Testing and Analysis·Adam Cawley
Jan 14, 2021·Drug Testing and Analysis·Fernando MoreiraMaria de Lourdes Bastos

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