Drug intelligence / Profile preview

remimazolam besylate + propofol MCT

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Remimazolam besylate + propofol MCT is a combination of two intravenous anesthetic agents used for procedural sedation and induction/maintenance of general anesthesia. Remimazolam besylate is an ultra-short-acting benzodiazepine that acts as a positive allosteric modulator at the γ-aminobutyric acid A (GABA-A) receptor, increasing chloride influx and hyperpolarizing postsynaptic neurons to produce sedative effects[3][5]. Propofol formulated with medium-chain triglycerides (MCT) is a short-acting sedative-hypnotic agent that also acts on GABA-A receptors but primarily targets the β subunit, directly opening chloride channels to induce postsynaptic inhibition[5][6]. The combination leverages the rapid onset and recovery profiles of both drugs while potentially reducing adverse events such as respiratory depression, hypotension, injection pain, and postoperative dizziness compared to either agent alone[5]. This combination has been studied in various procedural settings including endoscopy and hysteroscopy.

Other names
remimazolam besylate and propofol MCTremimazolam + propofol MCTremimazolam besylate plus propofol MCT
02

Targets

GABRR (GABA-A receptor subunit rho)

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