The object of the investigation is Ca2+ regulating role in glutathione antioxidant system function in blood lymphocytes. The aim of the work: to define the connection between the function of the glutathione-dependent antioxidant system, lipids peroxidation and ionized calcium, using as the model the mononuclear human peripheral blood lymphocytes. Methods of research and equipment: biochemical, spectrophotometer, pH-meter, microscope, centrifuge, electronic and torsion scales. Innovation: for the first time the separate links of glutathione antioxidant system and cation-transporting enzymatic system and their sensitiveness to Ca2+ were studied in complex. Theoretical and practical results: it had been established the Са2+ ability for the regulation of lipid peroxidation process and the system of their detoxication with the help of glutathione antioxidant system. The dependence of glutathione peroxidase, glutathione reductase, glutathione transferase and Na+,K+-ATPase, Ca2+,Mg2+-АТPase activity from intensity of the oxidative stress, inducing by adriamycine was shown. It was revealed that saponin application uncovered the latent activities of the glutathione-dependent enzymes, such as glutathione peroxidase, glutathione reductase, glutathione transferase, Na+,K+-ATPase and Ca2+,Mg2+-АТPase, that gives the opportunity to define the functional relationships between the activities of these enzymes. The optimal conditions (concentration of saponin, protein and ATP; pH, time of the incubation, cations correlation) for enzymatic reactions by the work with the permeabilized mononuclear human peripheral blood lymphocytes were defined. It was revealed, that the general link in the expression of different by pharmacological effect drugs, like Curiosin, Quamatel, Midokalm, is their action on the activity of glutathione-dependent antioxidant system and the transporting ATPases function. Inculcation: the obtained results may be used for the work out of methods of pathological changes of cellular homeostasis correction, give the possibility of new drugs synthesis and the selection of existent pharmacological preparations, modulating the activity of the ATPases and the enzymes of glutathione antioxidant system. The materials of the investigation may be used for lectures in universities and institutes. The branches are biochemistry, normal and pathological physiology, membranology, enzymology and pharmacology.