Pharmaceutical residues are not completely removed in wastewater treatment plants (WWTPs) becoming contaminants in aquatic ecosystems. Thereby, it is important to investigate their concentrations in the environment and the possible consequences of their occurrence, including for human health. Here, we briefly reviewed the paths of pharmaceuticals to reach the environment, their behavior and fate in the environment, and the possible consequences of their occurrence. Moreover, we synthetized all the studies about the detection of pharmaceuticals in Brazilian water bodies and the available ecotoxicological knowledge on their effects. In this study, when we compare the data found on these compounds worldwide, we observed that Brazilian surface waters present considerable concentrations of 17α-ethinylestradiol, 17β-estradiol, and caffeine. In general, concentrations found in aquatic systems worldwide seems to be low; however, ecotoxicological tests showed that even these low concentrations can cause sublethal effects in biota. The knowledge about the effects of continuous exposure and mixtures is sparse. In summary, new research is urgently required about the effects of these compounds in biota-including long-term exposition and mixture tests-and on specific technologies to remove these compounds in water bodies and WWTPs, besides the introduction of new policies for pharmaceutical use.