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Prevalence and migration of pharmaceutical substances in the aquatic cycles are among the most negotiable and environmentally relevant problems all over the world. On August 12, 2013 Directive 2013/39/EU of the European Parliament and Council was adopted; that Directive being the first document to contain pharmaceutical substances (diclofenac (DCF), 17-β-estradiol (E2) and 17-α-ethinylestradiol (EE2)) included in the Monitoring list. According to the right-down research it is believed that the mentioned substances can cause a harmful effect on the biota and the natural environment.To predict and to control the penetration of pharmaceutical substances into the environment, as well as to reduce their escape into it, the sources of their formation, their consumers, and the ways of their penetration into the environment are to be analyzed, their ability to change and to accumulate in the environment should be realized.To achieve this objective the legal basis applicable to the pharmaceutical substances (DCF, E2 and EE2) is analyzed in this paper, the volumes of Lithuanian sales of pharmaceutical substances (DCF, E2 and EE2) are determined, and the tendencies of sales alterations are discussed. The research done in this field is reviewed through the analyses and evaluation of the toxicological significance of these substances in the environment, through flows and sources of their penetration into the natural environment, the materials decomposition in the aquatic environment, and through the global experience in removal of pharmaceutical substances from wastewater and wastewater disposal in Lithuania.DOI: http://dx.doi.org/10.5755/j01.erem.68.2.7378