The problem of protection and maintenance of myocardial function and cardiovascular system on the whole in athletes under conditions of intense muscular activity continues to be one of the major in sports cardiology and pharmacology. Due to tightening of the WADA requirements for the use of cardioprotective agents and prohibition of the most commonly used in sport trimetazidine and meldonium, new directions for their use are required, which determined the purpose of the present review of the scientific literature on the subject. The paper highlights metabolic and functional prerequisites of application of cardioprotective means at the preparatory stages and presents the current classifications of these pharmacological agents. It is particularly emphasized the use of metabolitotropic agents with low toxicity and broad spectrum of action on the mechanisms a particular agent energy homeostasis; application of controlling during physical loads with different energy supply mechanism has been substantiated. New groups of cardioprotectors (inhibitors of potassium and sodium channels, inhibitors of fatty acid β-oxidation, natriuretic peptide based agents) are described, which have been already used in clinical cardiology.