<p>Perfluorooctane sulfonate and perfluorooctanoic acid have been used since the 1950s and detected in various environmental compartments, posing risks to human and environmental health. This study aims to evaluate the environmental behavior, review their global occurrence in water, and assess international legislation regarding perfluorooctane sulfonate and perfluorooctanoic acid to conduct an initial health risk assessment associated with drinking water. A systematic review of 161 papers published between 2002 and 2022 was conducted. Asia emerged as the continent with the most research, with 97 papers, while Africa, South America, and Oceania had fewer than seven papers each. Across all analyzed matrices, concentrations of perfluorooctanoic acid showed a broader range compared to perfluorooctane sulfonate. The highest reported perfluorooctane sulfonate concentration was 110,000&#xa0;ng.L⁻¹ in North American groundwater, whereas the highest perfluorooctanoic acid concentration was 1,707,290&#xa0;ng.L⁻¹ in surface water in Asia. Evaluated concentrations were frequently found near fluorochemical industries and military installations. Preliminary health risk assessment suggests that reported concentrations in global drinking water generally adhere to established standards, with few exceptions. Nevertheless, further research is necessary to fully comprehend the risks of exposure to perfluorooctane sulfonate and perfluorooctanoic acid through drinking water. Monitoring and evaluation of these microcontaminants are essential to safeguard drinking water quality and public health.</p>