One of the main causes of maternal mortality is obstetric bleeding, among which 2/3 of cases are bleeding in the early postpartum period. The existing methods of preventing and stopping uterine bleeding in the postpartum period do not always allow achieving the desired result due to the ineffectiveness of the measures taken. The aim of this study was to assess the effectiveness of existing uterotonic drugs in the obstetric bleeding prevention and treatment. We performed a detailed systematic analysis of modern domestic and foreign literature on uterotonic drugs being used to prevent and stop obstetric bleeding, with their main parameters considered. The study used such information databases as eLIBRARY.RU, Scopus, PubMed, MEDLINE, ScienceDirect, and Cochrane Library from inception to December 2020. Despite a significant number of studies devoted to exploring the possibilities of uterotonic drugs, currently there are no methods with absolute therapeutic efficacy, which requires research to develop new drugs based on their synthetic analogues.