In the article, the authors, based on their own research, as well as based on the results of other scientists, gave an idea of such concepts as metabolitotropic therapy and metabolic and metabolitotropic drugs, their place in the basic therapy of diseases, the cardiovascular system, the central nervous system, the hepatobiliary system, etc. The authors provided a classiћcation of metabolitotropic agents depending on their chemical structure and mechanism of action. The general principle of action of metabolitotropic agents is described. Molecular and biochemical mechanisms of energizing, antioxidant, neuroprotective, stress-protective, cardioprotective action of arachidonic acid, liposomes, magnesium preparations, mexidol, L-lysine, L-carnitine and taurine are described in detail. The article provides an experimental rationale for the use of metabolitotropic agents in neonatology and pediatrics.