Remimazolam,　widely　used　for　procedural　sedation　and　general　anesthesia,　is　a　new　ultra　short-acting　benzodiazepine　for　intravenous　sedation　and　anesthesia.　We　aim　to　characterize　the　pharmacokinetics/pharmacodynamics　(PK/PD)　of　remimazolam　and　its　metabolite　CNS　7054　in　healthy　Chinese　volunteers　using　population　analysis　and　suggest　an　optimal　dosing　regimen　for　sedation　therapy.　Data　were　collected　from　a　single-center,　placebo-controlled,　randomized,　and　dose–escalation　clinical　pharmacology　study.　Forty-six　healthy　volunteers　received　a　single　infusion　dose　of　remimazolam,　while　nine　healthy　subjects　received　a　continuous　infusion　of　remimazolam.　A　population　PK/PD　model　was　established　and　RxODE　and　Shiny　in　R　were　used　to　design　the　remimazolam　dosing　regimens.　A　three-compartment　model　best　described　the　PK　of　remimazolam　and　a　two-compartment　model　with　one　transit　compartment　was　adopted　for　CNS　7054.　The　relationship　between　exposure　and　the　bispectral　index　was　best　described　using　an　effect　compartment　model　with　an　inhibitory　sigmoid　model.　Additionally,　a　web-based　dashboard　was　developed　to　provide　individualized　dosing　regimens,　complemented　by　a　graphical　illustration　of　the　PK/PD　profiles　of　the　proposed　dosing　regimen.　The　established　population　PK/PD　model　characterized　the　dose–exposure–response　relationship　of　remimazolam　well,　which　could　be　applied　to　optimize　individual　dosing　regimens.　©　2024　by　the　authors.