Target-controlled Infusion of Remimazolam in Healthy Volunteers Shows Some Acute Tolerance

ConclusionsIn this study, it was shown that remimazolam-induced sedation is prone to tolerance development, which is potentially mediated by the CNS7054 concentration. The clinical consequences are, however, limited in situations where remimazolam is titrated to effect.Editor ’s PerspectiveWhat We Already Know about This TopicRemimazolam is a short-acting benzodiazepine that is administered as repeated bolus doses for procedural sedation and as a continuous infusion for general anesthesia in adultsThe pharmacokinetics of remimazolam administered as a bolus dose as well as a continuous infusion have been well-characterizedWhat This Article Tells Us That Is NewThe pharmacokinetic-pharmacodynamic relationships between remimazolam concentrations and Modified Observer ’s Assessment of Alertness and Sedation scores and bispectral index were assessed in 24 healthy volunteers using step-up and step-down target-controlled infusions to determine clinically appropriate target concentrationsTarget concentration –dependent sedation was observed with little effect on vital signsA difference in the sedative effects of remimazolam at identical target concentrations was observed between the step-up and step-down parts of the titration scheme that could not be explained by a bias in the predicted target concentrationsPharmacodynamic models for Modified Observer ’s Assessment of Alertness and Sedation scores and bispectral index that assumed tolerance development described the observed ...
Source: Anesthesiology - Category: Anesthesiology Source Type: research