This literature review addresses the pharmacology of main doping agents in details, mainly focused on the three most frequently used doping classes according to AAFs in 2018. Notably, anabolic steroids are first synthesized several decades ago, yet still fight for antidoping action. WADA and other antidoping organizations have raised awareness of doping agents significantly, thus provide a proper education for many of the altheletes including adolescents. Pharmacology of doping agents is an ongoing challenge for deep understanding due to a clandestine manner and supraphysiological doses in use.