Several studies have reported the ethnobotany characteristics and pharmacological properties of ayahuasca, beverage prepared from decoction of two Amazon forest native species, the vine Banisteriopsis caapi and the bush Psychotria viridis. This beverage, in which its use date from pre-Columbian period, has been employed in religious cults by many south-American populations situated in the Brazilian Amazon and in the region comprised between Panamá and Peru. Considered the keystone of Amazon medicine, its composition presents a series of psychoactive substances capable to generate visionary experiences in healers, shamans and followers. In this review, it will be addressed the main aspects related to aims and ways of using ayahuasca, its chemical compounds and action mechanisms. Besides, it will be briefly discussed the regulatory aspects involved in its use and the approach that this beverage have been taken by international scientific community during the last years.