Pharmaceutically active compounds are increasingly detected in raw and treated wastewater, surface water, and drinking water worldwide. These compounds can cause adverse effects to the ecosystem even at low concentrations and, to assess these impacts, toxicity tests are essential. However, the toxicity data are scarce for many PhACs, and when available, they are dispersed in the literature. The values of pharmaceuticals concentration in the environment and toxicity data are essential for measuring their environmental and human health risks. Thus this review verified the concentrations of pharmaceuticals in the aquatic environment and the toxicity related to them. The risk assessment was also carried out. Diclofenac, naproxen, erythromycin, roxithromycin, and 17β-estradiol presented a high environment risk and 17α-ethinylestradiol presented a high human health risk. This shows the potential of these pharmaceuticals to cause adverse effects to the ecosystem and humans and establishes the necessity of their removal through advanced technologies.