Currently, thanks to the development of sensitive analytical techniques, the presence of different emerging pollutants in aquatic ecosystems has been evidenced; however, most of them have not been submitted to any regulation so far. Among emerging contaminants, antimicrobials have received particular attention in recent decades, mainly due to the concerning development of antibiotic resistance observed in bacteria, but little is known about the toxicological and ecological impact that antimicrobials can have on aquatic ecosystems. Their high consumption in human and veterinary medicine, food-producing animals and aquaculture, as well as persistence and poor absorption have caused antimicrobials to be discharged into receiving waters, with or without prior treatment, where they have been detected at ng-mg L−1 levels with the potential to cause effects on the various organisms living within aquatic systems. This review presents the current knowledge on the occurrence of antimicrobials in aquatic ecosystems, emphasizing their occurrence in different environmental matrixes and the effects on aquatic organisms (cyanobacteria, microalgae, invertebrates and vertebrates).