The concern on the presence of pesticides in Italian water resources historically broke out around 1980 after severe episodes of ambient, raw water and drinking water contamination due to some herbicides, atrazine (ATR), its metabolites desethylatrazine (DEA) and deisopropylatrazine (DIA), simazine, cyanazine, bentazone, molinate, which affected mainly the maize, grain and rice producing floodplains and karst areas of the northern Regions. Due to the risks of human exposure, in the early 1990 the use of atrazine was banned in Italy and was replaced by terbuthylazine (TERB). In a few years, TERB became a chemical of concern, together with its main metabolite desethylterbuthylazine (DET), because of alerting detections in surface and groundwater resources. Up to now, the risk of contamination of water resources by TERB, DET, DEA and, in some extent ATR, is of relevance in Italy due to their present and past wide employment in agriculture, the discharges or seepages in particularly vulnerable areas, their unfavorable intrinsic properties, e.g. poor sorption and high persistence, their mobility by drift, leaching and runoff in vadose zones, aquifers and surface water. So, unsurprisingly, results from national monitoring of ambient water and raw water indicate that TERB, DET, DEA and residual ATR, despite its withdrawal, are detected at remarkable frequencies and, sometimes, at levels higher than pesticide quality standards under the Italian Decrees for the protection of surface water (specifically, raw waters doomed at the drinking water abstraction), groundwater and drinking water (tap water), that is 0.1–0.5μg/l for individual pesticides and for total pesticides, respectively, including relevant metabolites. On the other hand, in these last years, the control measures in drinking water production adopted by the waterworks Companies and the regional and central health Authorities, also in the view of the recent WHO approaches under the Water Safety Plans, ensure that levels of any pesticide residue (also involving TERB, DET, DEA, ATR) in finished tap water meet parametric values for pesticides. Therefore, in these last years, no derogation to the parametric values for drinking water has been required. The aim of this paper is to contribute to widen the knowledge on the water impact of these important water pollutants giving sound details on present usages, levels and frequencies of detection in water bodies in Italy, on their key chemiodynamic properties, e.g. soil half-lives (DT50) and soil to organic carbon partition (Koc) available in the open literature, particularly for TERB metabolites, and some details on legal provision adopted at the national level. In fact, a more effective protection of water supplies, particularly against TERB and DET, has been pursued in the late 2000s by the Italian Health Ministry through the adoption of consistent provisions aimed at mitigating emissions of TERB in routine agricultural activities, and by the Italian Ministry of the Environment through the adoption of specific Environmental Quality Standards for TERB and its metabolite DET, ATR, SIM for the protection of surface waters.