The aim of the present paper was to give a complete picture on the drinking water contamination by pharmaceutical residues all over the world. For this purpose, a systematic review was carried out for identifying all available research reporting original data resulting by sampling campaign and analysis of "real" drinking water samples to detect pharmaceutical residues. The investigated databases were PubMed, Scopus, and Web of Science. A total of 124 studies were included; among these, 33 did not find target analytes (all below the limit of detection), while the remaining 91 studies reported the presence for one or more compounds, in concentrations ranging from a few units to a few tens of nanograms. The majority of the studies were performed in Europe and the most represented categories were nonsteroidal anti-inflammatory drugs and analgesics. The most common analytical approach used is the preparation and analysis of the samples by solid-phase extraction and chromatography coupled to mass spectrometry. The main implications resulting from our review are the need for (a) further studies aimed to allow more accurate environmental, wildlife, and human health risk assessments and (b) developing integrated policies promoting less environmentally persistent drugs, the reduction of pharmaceuticals in livestock breeding, and the update of wastewater and drinking water treatment plants for a better removal of drugs and their metabolites.