Today an important task of sports pharmacology and cardiology is the rational search for and assessment of the efficiency of athlete cardiovascular system protection, which limits physical work capacity stimulation in most sports events and may result in health and life quality worsening and even sudden death under inadequate conditions of cardioprotection. Wide spectrum of physiological and biochemical action of pharmacological means on the basis of gamma-butirobetaine (L-carnitine) allows their application at all preparation stages with high efficiency of cardioprotective and ergogenic action. Usage of these cardioprotectors allows to avoid doping sanctions and disorders of training and competitive process, which is of tremendous significance for elite sport.