The new psychoactive substances phenomenon continues to represent a considerable public health challenge. Synthetic cathinones are β-keto amphetamine analogues, also known as legal highs, research chemicals, bath salts. These drugs have surfaced as a popular alternative to other illicit drugs of abuse, such as cocaine, MDMA, and methamphetamine, due to their potent psychostimulant and empathogenic effects. Pyrovalerone cathinones (a-pyrrolidinophenones) form a distinct group of designer cathinones, such as MDPV. After being listed as an illegal product, "second generation" compounds such as α-PVP, sharing a very similar chemical structure with MDPV, were developed. Clinical effects of these compounds are individual, dose- and route of administration-dependent. Both of them have been involved in an increased number of, not only acute intoxications but also fatalities over the past few years, raising concerns in the medical field. In this paper, we will review the available data regarding the use and effects of MDPV and α-PVP in humans in order to highlight their impact on public health. Health actors and general population need to be clearly informed of potential risks and consequences of these 2 novel psychoactive substances spread and use. The literature search conducted led to the identification of potentially 83 relevant articles. All articles were screened from their abstracts to determine their relevance in the framework of the current review.