ABSTRACT Sulfonamides are antimicrobials whose major components and metabolites enter the natural environment through pharmaceutical and aquaculture effluents. Sulfonamides have increased in recent years in response to the increased use of sulfonamides in pharmaceuticals and aquaculture. Sulfonamides are currently detected in almost all major rivers on all continents and their distribution in ecosystems, especially in drinking water sources. Studies on sulfonamides have focused on their effects on aquatic organisms and human health, and the results show that sulfonamides can affect fish development and reproduction, disrupt the structure of soil microbial communities, reduce the activity of soil enzymes, and affect higher organisms through the food chain. In humans, they can cause allergic reactions and neurotoxicity, among other effects. This paper reviews the sources, distribution, and effects of sulfonamides on aquatic organisms and humans and discusses in detail the contamination and potential hazards of sulfonamides in water sources. In the future, it is necessary to conduct more in‐depth studies on the potential adverse effects of sulfonamides on human organs such as the liver and kidney, to set strict standards for their release, and to strengthen the monitoring of water sources.