Apart from the studies which reported the occurrence of steroid hormones and antibiotics in wastewater treatment plants (WWTPs) back in 2004, 2007 and 2012, the evidence for monitoring of pharmaceuticals in South African water bodies intensified from 2014. Therefore, this study reviewed the analytical methods developed and applied in South Africa for the purpose of monitoring pharmaceuticals and their metabolites in water. At the same time, pharmaceuticals and their metabolites detected in South African waters are reviewed. To date, there is over 100 pharmaceuticals detected in South African waters with most studies focussing on quantitative analysis of non-steroidal anti-inflammatory drugs (NSAID), antibiotics, antiretroviral drugs and carbamazepine. Various sources of pharmaceuticals in the environment are reported, with WWTPs found as the major contributor to their occurrence in South African rivers. Notably, a NSAID, ibuprofen, with concentrations found exceeding 100 μg L-1 in selected WWTPs has also been found at high levels reaching 60 μg L-1 in river water. Mostly, pharmaceuticals detected in wastewater are also reported in corresponding rivers. The present review details pharmaceuticals that should be included in environmental monitoring studies performed in South Africa, while also identifying areas for future research through the research gap analysis.