Cocaine is one of the most widely consumed psychoactive substances and has been recognized as a major public health concern for many years. While several aspects of the toxicology of cocaine have been thoroughly described in the literature, namely its effects on different target organs, other toxicological features should not be disregarded. In this perspective, the in vitro and in vivo genotoxic effects of cocaine, along with the genotoxicity data from human exposure, especially in the context of "crack" smoking, were reviewed. Some concerns regarding (1) the chronic abuse and forms of cocaine, (2) the role of metabolism and (3) the mode of action of cocaine were discussed. The major limitations of the experimental and human studies available were also addressed and some research gaps in this field identified. Overall, although the genotoxicity of cocaine is still a matter of discussion, this psychoactive substance exhibits a genotoxic potential that should be further considered.
Keywords: Cocaine biomarkers; Cytogenetic damage; Genotoxicity; Intranasal cocaine administration; “Crack” smoking.