Drug intelligence / Profile preview

esketamine + remimazolam

Development stage
Preclinical
Lead developer
OMJ Pharmaceuticals
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Esketamine + remimazolam is a combination of two intravenous anesthetic agents used primarily for procedural sedation and anesthesia. Esketamine is the S-enantiomer of ketamine, acting as a non-competitive antagonist at the N-methyl-D-aspartic acid (NMDA) receptor, providing analgesic, sedative, and dissociative effects. Remimazolam is an ultra-short-acting benzodiazepine that acts as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA\(A\)) receptor, producing rapid-onset sedation with minimal cardiovascular and respiratory depression. The combination leverages esketamine’s analgesia and hemodynamic stability with remimazolam’s rapid onset/offset sedation profile. Clinical studies have shown this regimen to be effective for procedures such as painless gastroenteroscopy, outpatient colonoscopy, tracheal intubation in pediatric patients without muscle relaxants, and ICU sedation[1][2][3][5]. The combination offers advantages including stable hemodynamics, reduced adverse events compared to propofol-based regimens, less injection pain/fatigue than propofol alone[5], fewer circulatory/respiratory side effects[1], rapid recovery times[1][9], and potential reduction in opioid requirements when used for analgesia[3].

Other names
remimazolam tosilate + esketamine
02

Targets

GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)

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