• Pharmacol. Res. · Nov 2016

    Review

    Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity.

    • Maija Dambrova, Marina Makrecka-Kuka, Reinis Vilskersts, Elina Makarova, Janis Kuka, and Edgars Liepinsh.
    • Latvian Institute of Organic Synthesis, Aizkraukles Str. 21, Riga LV-1006, Latvia; Riga Stradins University, Dzirciema Str. 16, Riga LV-1007, Latvia. Electronic address: maija.dambrova@farm.osi.lv.
    • Pharmacol. Res. 2016 Nov 1; 113 (Pt B): 771-780.

    AbstractMeldonium (mildronate; 3-(2,2,2-trimethylhydrazinium)propionate; THP; MET-88) is a clinically used cardioprotective drug, which mechanism of action is based on the regulation of energy metabolism pathways through l-carnitine lowering effect. l-Carnitine biosynthesis enzyme γ-butyrobetaine hydroxylase and carnitine/organic cation transporter type 2 (OCTN2) are the main known drug targets of meldonium, and through inhibition of these activities meldonium induces adaptive changes in the cellular energy homeostasis. Since l-carnitine is involved in the metabolism of fatty acids, the decline in its levels stimulates glucose metabolism and decreases concentrations of l-carnitine related metabolites, such as long-chain acylcarnitines and trimethylamine-N-oxide. Here, we briefly reviewed the pharmacological effects and mechanisms of meldonium in treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis and diabetes.Copyright © 2016 Elsevier Ltd. All rights reserved.

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