Antibiotics act as crucial tools in healthcare, veterinary medicine, and agriculture against bacterial infections. However, a major amount of the antibioticsAntibiotics used for the treatment of humans and other domestic animals are spent in waste water through their feces and urine in the form of metabolitesMetabolites or even in unmodified states, thereby acting as emerging pollutants. AntibioticsAntibiotics and their metabolitesMetabolites pose significant environmental concerns due to their potential adverse effects on aquatic ecosystems, agriculture, and human health. The ubiquitous presence of antibiotics often leads to the selection of antibiotic-resistant bacteria in the environment. Thus, understanding the distribution of antibiotics and their metabolitesMetabolites in wastewater and implementing effective remediation strategies for further elimination from the environment are imperative for mitigating their environmental impacts. Different physicalCoagulation (coagulation, filtrationFiltration, ion exchangeIon exchange, sedimentationSedimentation, adsorptionAdsorption, etc.) and chemical (chlorination, oxidation, ozonation, etc.) techniques are frequently used to remove antibioticsAntibiotics from the environmental samples. However, bioremediationBioremediation is a cost-effective, environmentally sustainable method that uses living organisms and their derivatives to eliminate or detoxify antibiotics from a specific environment. Overall, this chapter provides insights into the distribution of antibioticsAntibiotics and their metabolitesMetabolites in wastewater, as well as their toxicity in living organisms, and emphasizes the importance of adopting sustainable bioremediationBioremediation approaches for the elimination of antibioticsAntibiotics and their metabolitesMetabolites for environmental protection and human health preservation.