The article deals with historical information dedicated to the discovery of bioflavonoids and their effect on the human cardiovascular system, also considering the modern classification of phlebotrophic agents, followed by generalization and analysis of their mechanisms of action, as well as detailed discussion of different forms of diosmin. Summing up contains generalization of the Russian, European, and American guidelines on using phlebotrophic drugs for various forms and stages of chronic venous diseases.