The use of illegal performance-enhancing drugs (PEDs) in sports, and other tactics by athletes to gain an unfair competitive advantage is becoming a global concern since it negatively impacts the athlete, participants, and the integrity of sports. Annually, a list of drugs and techniques that are prohibited from being used in sports is published by the World Anti-Doping Agency (WADA). The WADA list consists of different classes, namely, non-approved substances, anabolic androgenic steroids (AAS), peptide hormones, growth factors, related substances and mimetics, beta-2 agonists, hormone and metabolic modulators, diuretics and masking agents, stimulants, narcotics, cannabinoids, glucocorticoids, and beta blockers. Moreover, athletes tend to use other cheating techniques, such as blood doping, urine adulteration, and gene doping, to increase their chances of winning. This review encompasses the various classes of PEDs and methods that are most widely used to enhance the performance of athletes. In addition, herein we discuss some of the most commonly used methods that are implemented in the detection of doping.