Remimazolam, a novel ultra-short acting benzodiazepine that combined the advantages of midazolam and remifentanil, has been developed for procedural sedation, induction and maintenance of general anesthesia, and sedation in the intensive care unit. In the current review, we evaluated the recent research progress on the use of remimazolam perioperatively and explored the pros and cons of remimazolam. Intravenous infusion, especially target controlled infusion may be more suitable for remimazolam administration. When given by infusion, remimazolam exhibits a faster onset and more rapid recovery than midazolam, but not faster than propofol for short procedure. However, decrease of plasma remimazolam concentration may be faster than that of propofol after long-term infusion. Oral intake has low bioavailability, and is difficult in producing sedative effects. Intranasal and inhaled intake of remimazolam is limited by unsuitable formulations. The inhibitory rate of hypotension and respiratory inhibition caused by remimazolam was low, with more advantages on patients with circulation and respiratory disorders and high-risk severe patients. The metabolism of remimazolam is affected by gene polymorphism, American Society of Anesthesiologists status and sex. The effects of remimazolam could be specifically reversed by flumazenil. However, data are still very limited concerning the safety and effectiveness of remimazolam in specific populations, suitable measurement of its sedation, potential influence on neurocognitive function, and safety after long-term use. Definitive studies will need to be performed.