Background: Some ergogenic medicinal plants are used in exercise and sport in Africa in order to increase sport performance. However, data on their composition and their possible impacts on health are limited. This study was initiated to provide ethnobotanical data on plants traditionally used to optimize physical performance and to perform a qualitative characterization of their main chemical groups. Methods: Ethnobotanical surveys in two communes (Dedougou and Nouna), of the region of Boucle du Mouhoun, Burkina Faso and phytochemical analyses of the most interesting plants were conducted. Results: A total of 50 respondents including traditional hunters dozo, farmers, healers, herbalists, marabouts, etc., were interviewed. Fifty-two species used in the optimization of exercise and sports have been identified. The most cited species were Cassia sieberiana, Tamarindus indica, Annona senegalensis, Gardenia sokotensis, Securidaca longepedunculata, and Ficus tonningii. These plants are known to prevent muscle and skeletal disorders, aches and pains, and mental disorders. The study identified several types of plants including those displaying stimulation, anxiolytic, sedative, adaptogenic, or erythropoietic activities. Phytochemical screening revealed the presence of phenolic compounds, alkaloids, terpenes, and steroids, which are similar molecules families of those of doping molecules. Additionally, TLC screening allowed the characterization of numerous terpene and flavonoid compounds including rutin. Conclusions: The possible structural similarity of the characterized chemical groups of these species with those of doping families raise concerns about the consequences of their consumption. However, the identification of the active molecules of these species remains to be performed in order to predict the real risks associated with their consumption.