Definition

A short-acting benzodiazepine derivative that is structurally related to midazolam, with sedative-hypnotic activity. Upon administration, remimazolam targets and binds to a specific site on the gamma-aminobutyric acid (GABA)-A-chloride ionophore receptor complex located on the neuronal membrane. Binding causes an allosteric modification of the receptor thereby enhancing the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events, which leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability.