Remimazolam is a recently approved benzodiazepine for procedural sedation in Taiwan. It is a new type of short-acting γ-aminobutyric acid receptor agonist with the characteristics of non-organ-dependent metabolism, no injection pain, and inactive metabolites. Remimazolam has a mild cardiopulmonary suppressive effect, showing good effectiveness and safety in clinical applications, especially in the elderly, critically ill patients, or patients with hepatic and renal insufficiency. This review aims to provide an overview of the specific basic and clinical pharmacology of remimazolam and provide scientific support for the clinical application of this novel sedative drug in procedural sedation.