Introduction In societies that place a great emphasis on physical appearance and body aestheticism, the use of image enhancing drugs (IEDs) has become increasingly widespread. Of particular concern is the use of skin lightening drugs, which might contain undisclosed and harmful ingredients of potential adulterated nature. These products are frequently advertised on social media platforms and elsewhere and used without medical consultation. Methods An explorative literature search was carried out in PubMed, Scopus, CINHAL, and ProQuest to better understand the motivational risk factors associated with skin lightening and assess their relation to body image, self-esteem, and other psychological disorders. All studies published until December 2020 were included in the review. Results A number of non-psychological factors can be associated with this practice. These include: (a) sociocultural i.e., achieve different social and cultural benefits, and (b) skin conditions such as hyperpigmentation lesions. Conversely, psychological factors can be correlated to (a) low self-esteem, (b) body image disturbances, and (c) other psychological factors like history of trauma and depressive symptoms. Conclusion Skin lightening remains a poorly studied and understood multifactorial phenomenon. More extensive research is needed to improve current clinical practice and raise public awareness on this dangerous practice.