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Meldonium is the active molecule from Mildronate® with similar chemical structure to an amino acid, and it is known as (3-(2,2,2-trimethylhydrazine) propionate) (CAS 76144-81-5). This pharmaceutical substance is approved in Eastern Europe for cerebral and myocardial ischemia and has been on the World Doping Association’s banned substances list since January 2016. The goal of this review is to relate the use of meldonium as a doping agent, considering its pharmacological, toxicological, and analytical aspects. This review is based on the scientific literature from digital platforms. The main mechanism of action of meldonium is based on a decrease in l-carnitine levels and increase of peroxisomes activity in the cytosol. Females were more susceptible to the substance in animal experiments for toxicological tests. There is currently no report in the scientific literature about acute or chronic intoxication cases by meldonium in humans. Based on the literature findings, meldonium showed ergogenic effect in animals and human volunteers. For anti-doping analysis, urine is the biological matrix of choice, and dilute-and-shoot is the most common sample treatment in addition to liquid chromatography–mass spectrometry analysis. Other approaches could be used to determine meldonium levels, mainly for screening tests, such as l-carnitine or gamma-butyrobetaine levels.

Meldonium: Pharmacological, toxicological, and analytical aspects