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Aim: to form modern ideas about the properties of creatine as a pharmaconutrient, its biological role in the body, and rational dosage during physical exertion. Materials and methods. To determine the level of development of the research problem, a search was conducted in the databases MEDLINE, PubMed, Scopus, Directory of Open Access Journals and ScienceDirect; the keywords used included physical exercise, creatine supplementation, oxidative stress, mitochondria, energy metabolism. We focused on English-language articles published between 2019 and 2025. Results. The use of creatine loading schemes during high-intensity interval training provides an increase in physical fitness indicators by an average of 10–20 % due to an increase in the concentration of muscle phosphocreatine. According to modern ideas, creatine belongs, on the one hand, to the group of myostatin inhibitors, and on the other hand, to the protectors of mitochondrial function. The results of 50 studies showed that compared to placebo, creatine, both alone and in combination with bicarbonate, produced a statistically significant increase in average and peak power in martial artists. Increasing cellular creatine levels promoted metabolic channeling, demonstrated antiapoptotic properties, promoted the survival of dopaminergic neurons, and produced a pronounced antidepressant effect, helping athletes remain psychologically stable during training, and before competitions. Conclusions. Thus, from the literature data, it becomes clear that the course use of creatine leads to a significant increase in the efficiency of the training process, and this makes it an indispensable tool for improving the indicators of physical and functional fitness, as well as the overall quality of life of athletes. Creatine is a universal ergogenic food supplement, but due to its predominantly positive effect on the body with chiefly aerobic energy supply, typical of Olympic martial arts, it is fully suitable for improving the effectiveness of the training process in boxing, judo, taekwondo, jiu-jitsu (jujutsu), fencing, etc. The neuroprotective and antidepressant effects of ergogenic supplements with creatine are very important in sports such as martial arts, as they contribute to the development of discipline, emotional control, mental stability, and help athletes’ brains become more resistant to stress, especially before competitions. The course use of such a pharmaconutrient as creatine can rightfully be attributed to health-saving technologies – a new direction in sports pharmacology, and nutriology.