Anesthetic drugs & techniques

Influence of Remifentanil on the Pharmacokinetics and Pharmacodynamics of Remimazolam in Healthy Volunteers

AnesthesiologyPublished Crossover dose-ranging clinical trial

Authors' conclusion

A pharmacokinetic and pharmacodynamic drug-drug interaction between remimazolam and remifentanil was quantified in this clinical trial.

Study context

Population
Healthy volunteers
Participants
24 volunteers
Comparison
Remimazolam TCI alone vs with remifentanil 0.5 ng/ml vs with remifentanil 0.1 to 4.0 ng/ml
  • Remimazolam alonen = 24reference
  • Remifentanil 0.5 ng/mln = 24
  • Remifentanil 0.1 to 4.0 ng/mln = 24
Outcome
Influence of remifentanil on remimazolam sedation (MOAAS, BIS, tolerance to laryngoscopy or tetanic stimulation) and target concentrations maximising MOAAS 2 or 3
Methodological detailsthree-period
  • Three-period

Main finding

As reported in the abstract

Remifentanil reduced apparent clearance of CNS7054; half-maximum inhibition

8.0

ng/ml; 95% CI 5.5 to 13.4

Simulated highest probability of Modified Observer's Assessment of Alertness and Sedation (MOAAS) 2 or 3: remimazolam 275 ng/ml with 0 ng/ml remifentanil

45%

Simulated highest probability of MOAAS 2 or 3: remimazolam 250 ng/ml with 0.1 ng/ml remifentanil

45%

Simulated highest probability of MOAAS 2 or 3: remimazolam 200 ng/ml with 0.5 ng/ml remifentanil

44%

Further findings

Simulated highest probability of TOTS and TOL

TOTS, at highest studied target concentrations
93.3%
TOL, at highest studied target concentrations
85.5%

Original publication

Influence of Remifentanil on the Pharmacokinetics and Pharmacodynamics of Remimazolam in Healthy Volunteers. Anesthesiology. Published 15 January 2025. doi:10.1097/aln.0000000000005348

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