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Current Drug Metabolism

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ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

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Research Article

Drug-Drug Interaction Potential of Remimazolam: CYP 450, Transporters, and Protein Binding

Author(s): Karl-Uwe Petersen*, Wolfgang Schmalix, Marija Pesic and Thomas Stöhr

Volume 25, Issue 4, 2024

Published on: 30 May, 2024

Page: [266 - 275] Pages: 10

DOI: 10.2174/0113892002300657240521094732

Price: $65

Abstract

Background: The ultra-short-acting benzodiazepine, remimazolam, is a new treatment modality for procedural sedation and general anesthesia. Its activity is terminated by carboxylesterase 1 (CES1).

Objective: The objective of this study was to determine the drug-drug interaction (DDI) potential of remi-mazolam through mechanisms unrelated to its metabolizing enzyme, CES1.

Methods: Conventional in vitro co-exposure experiments were conducted to study possible interactions of remimazolam and its primary metabolite, CNS7054, mediated by competitive binding to plasma protein or reactions with cytochrome P450 isoforms or drug transporters

Results: No relevant interactions of remimazolam or its metabolite with cytochrome P450 (CYP) isoforms at clinically relevant concentrations were identified. Likewise, standard experiments revealed no clinically relevant interactions with drug transporters and plasma proteins.

Conclusion: The present data and analyses suggest a very low potential of remimazolam for pharmacokinetic DDIs mediated by CYP isoforms, drug transporters, and protein binding.

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