“Flakka” is the street name for the synthetic cathinone α-pyrrolidinopentiophenone (α-PVP). Although it was developed by Boehringer Ingelheim as a central nervous system stimulant and pressor agent in the 1960s, it entered in the drug arena at an accelerated rate during the last 4 years causing intoxications, fatal or not. α-PVP is abused in Europe, as well as in the United States and Japan, as a substituent of 3, 4-methylenedioxypyrovalerone, and recently scheduled by the United States Drug Enforcement Administration, possessing similar pharmacological action to that of the latter. It can be easily manufactured and purchased through the Internet or in retail shops and is usually sold as “bath salts”. The aim of this review is to summarize the current knowledge of this drug concerning its chemistry, synthesis, metabolism, pharmacology, and toxicology. “Flakka” related cases, published or reported, including fatalities or intoxications, as well as seizures are reviewed. The existing analytical methodologies for the determination of α-PVP in biological and postmortem samples are summarized, and its current legal status is reported.