In Western markets, the extract from the seeds of Paullinia cupana Kunth, Sapindaceae, popularly known as Guaraná, is most commonly used in high-energy foods and drinks and dietary supplements. However, a broad spectrum of medicinal activities is reported for P. cupana, ranging from stimulation of the central nervous system, in cases of physical or mental stress, to appetite suppression. It can also be used as an aphrodisiac and a treatment for impotence, as well as a medication to reduce fever, stimulate metabolism, induce antiplatelet, antioxidant and antibacterial activites. In addtition, P. cupana has been used in cosmetic preparations, and it has become a popular soft drink in Brazil. In the last two decades, Guaraná has emerged as a key ingredient in various sports and high-energy drinks. Methylxanthines, including caffeine, cathechins, theophylline and theobromine, and tannins are compounds which are reported for this plant. This article reviews the most up-to-date information on the botanical, chemical and pharmacological aspects of P. cupana extract, as well as its miscellaneous uses.