Changes in today’s human existence and functioning that include the high pace of life, significant deterioration of ecological safety, and professional stresses result in overstrain and overfatigue. In the long run, this leads to significant depletion of the body defensive and adaptive resources, the development of dysimmune changes. This tends to affect the level of physical and mental work capacity of the representatives of extreme professions, such as elite athletes, military servicemen, aircraft pilots, etc. and to impair the efficiency of their professional activity. All this creates prerequisites for the formation and implementation of pharmacological support system for persons subjected to constant influence of such negative factors, and above of all, the professional ones. The first step in this direction is the separation of those metabolic shifts that underlie further pathophysiological processes, which, in general, are responsible for decrease in the general and special physical work capacity as well as mental toughness. This review paper addresses all the main homeostatic links and physiological mechanisms, changes of which are accompanied by the development of overfatigue. It is at these vulnerable links that the action of pharmacological and nutritiological means cardioprotectors, antioxidants and anti-hypoxants, actoprotectors, regulators of blood aggregate state, metabolic regulators with polyprotective action (L-glutamine, amber acid, ATP), neuroprotectors, etc. should be directed. The article presents the main representatives of different groups and specific dietary supplements that can be used for homeostatic shift regulation. It is also accentuated that only those means that are not prohibited under the current rules of the World Anti-Doping Agency should be used. Pride of place in the work goes to the description of new national pharmacological developments, some of which have been already implemented in medical practice, while others are at the stage of clinical trials. The use of a complex of pharmacological and nutritiological means has been substantiated, which is based on due account for professional activity specifics, a set of factors negatively influencing physical and mental work capacity of highly skilled athletes and representatives of other extreme professions, and will improve their functional state, contribute to prevention of overstrain and overfatigue development and become an important factor in work-related disease prevention.
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