Drug intelligence / Profile preview

esketamine + midazolam

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Intranasal
01

Overview

Esketamine + midazolam is a combination of two pharmaceutical agents used primarily for anesthesia and sedation. Esketamine is the S(+)-enantiomer of ketamine, acting as a dissociative anesthetic and NMDA receptor antagonist with both anesthetic and antidepressant properties. Midazolam is a benzodiazepine that acts as an agonist at gamma-aminobutyric acid (GABA) receptors, producing sedative, anxiolytic, amnestic, and muscle relaxant effects. When combined, esketamine provides rapid induction of anesthesia or sedation while midazolam attenuates the psychoactive side effects (such as agitation or hallucinations) associated with esketamine by enhancing GABAergic inhibition in the central nervous system. This combination achieves deeper sedation than either drug alone and improves patient comfort during procedures by reducing adverse psychotomimetic reactions[1]. The combination is used in both human and veterinary medicine for procedural sedation, induction of anesthesia, or to manage agitation related to esketamine administration.

Other names
s-ketamine and midazolamS(+)-ketamine + midazolamketamine + midazolam
02

Targets

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

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