The presence of psychoactive stimulatory drugs in raw waters used for drinking water production and in finished drinking water was evaluated in a Spanish drinking water treatment plant (DWTP). Contamination of the river basin which provides raw water to this DWTP was also studied. In surface waters, illicit drugs such as cocaine, benzoylecgonine (cocaine metabolite), amphetamine, methamphetamine, MDMA (ecstasy), and MDA were detected at mean concentrations ranging from 4 to 350 ng/L. Nicotine, caffeine, and their metabolites were also found at the microg/L level. The elimination of these compounds during drinking water treatment was investigated in a real waterworks. Amphetamine-type stimulants (except MDMA) were completely removed during prechlorination, flocculation, and sand filtration steps, yielding concentrations lowerthan their limits of detection (LODs). Further, ozone treatment was shown to be effective in partially eliminating caffeine (76%), while subsequent granulated activated carbon (GAC) filtration removed cocaine (100%), MDMA(88%), benzoylecgonine (72%), and cotinine (63%). Postchlorination achieved the complete elimination of cocaine and nicotine and only one parent compound (caffeine) and two metabolites (cotinine and benzoylecgonine) persisted throughout treatment although reductions of 90% for caffeine and benzoylecgonine and 74% for cotinine were obtained.