Oestrogen blockers and aromatase inhibitors which are used mainly for treatment of breast cancer are considered as essential medicines in contemporary clinical practice. A current social and health problem is that many athletes abuse with these two categories of medicines to counter the side effects of anabolic steroids as part of their steroid cycle, to increase testosterone concentration by stimulation of testosterone biosynthesis and to reduce and prevent symptoms of excess oestrogen. This paper reviews the most appropriate methods for detection of these substances and their metabolites in biological samples. It also summarises the historical development of these drugs and their pharmacological aspects. We have described the difficulties and strengths of the analytical procedures that could be used for doping control of these substances. Literature search was done through Medline/PubMed, Scopus Database, Web of Knowledge search as well as an internet-based search with predefined keywords. We have also analysed many WADA’s protocols. The present review is based on a total of 69 publications.