The known occurrence of pharmaceuticals in the built and natural water environment, including in drinking water supplies, continues to raise concerns over inadvertent exposures and associated potential health risks in humans and aquatic organisms. At the same time, the number and concentrations of new and existing pharmaceuticals in the water environment are destined to increase further in the future as a result of increased consumption of pharmaceuticals by a growing and aging population and ongoing measures to decrease per-capita water consumption. This review examines the occurrence and movement of pharmaceuticals in the built and natural water environment, with special emphasis on contamination of the drinking water supply, and opportunities for sustainable pollution control. We surveyed peer-reviewed publications dealing with quantitative measurements of pharmaceuticals in U.S. drinking water, surface water, groundwater, raw and treated wastewater as well as municipal biosolids. Pharmaceuticals have been observed to reenter the built water environment contained in raw drinking water, and they remain detectable in finished drinking water at concentrations in the ng/L to μg/L range. The greatest promises for minimizing pharmaceutical contamination include source control (for example, inputs from intentional flushing of medications for safe disposal, and sewer overflows), and improving efficiency of treatment facilities.