The phenomenon of insulin resistance as a factor of polymorbidity is increasingly discussed in the literature. The evidence base on the pathogenetic role of insulin resistance for the formation of a number of socially significant diseases that reduce the quality and life expectancy of patients has been accumulated. The role of cellular transporter proteins in the regulation of glucose metabolism as one of the links of therapeutic action is discussed. Attention is focused on the effect of insulin on the processes of neurogenesis, its angio- and neuroprotective properties. The levels of insulin resistance development that determine the optimization of pharmacotherapeutic effects, the choice of the most accessible method for determining insulin resistance for clinical and outpatient conditions, the evaluation of the results of which will allow evaluating the effectiveness of the treatment. Various methods of determining this pathology are proposed and new approaches to its treatment are being sought. This article provides an overview of the existing information about the currently known pathogenetic mechanisms of insulin resistance, as well as the methods used in clinical practice for its diagnosis and therapeutic correction. An overview of the most modern and promising oral hypoglycemic drugs and their pleotropic effects is given.