Pharmacological effects of meldonium : Biochemical mechanisms andbiomarkers of cardiometabolic activity / Maija Dambrovaa, Marina Makrecka-Kukaa, Reinis Vilskersts, Elina Makarovaa, Janis Kukaa, Edgars Liepinshaa. - (Pharmacological Research 15 (2016, 2 February) p. 1-10) doi:10.1016/j.phrs.2016.01.019
PMID: 26850121
Abstract
Meldonium (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.
