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

Maija Dambrova, Marina Makrecka-Kuka, Reinis Vilskersts, Elina Makarova, Janis Kuka, Edgars Liepinsh

Research output: Contribution to journalReview articlepeer-review

42 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)771-780
JournalPharmacological Research
Volume113
Issue numberPart B
DOIs
Publication statusPublished - 1 Nov 2016

Keywords

  • Cardioprotective
  • L-Carnitine
  • Long-chain acylcarnitines
  • Meldonium
  • Trimethylamine-N-oxide

Field of Science

  • 3.1 Basic medicine

Publication Type

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database

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