Drug intelligence / Profile preview

esketamine + midazolam + dexmedetomidine

Development stage
Unknown
Lead developer
Xi'an International Medical Center Hospital
Modality
Small Molecules
Administration
Intravenous
01

Overview

esketamine + midazolam + dexmedetomidine is a pharmacological combination therapy being investigated by Xi'an International Medical Center Hospital for procedural sedation, particularly in patients undergoing gastroscopy. This triple-drug regimen leverages the distinct mechanisms of its components to achieve a balanced sedative state. Esketamine, the S-enantiomer of ketamine, acts as a non-competitive NMDA receptor antagonist, providing potent analgesia and dissociative sedation while maintaining respiratory drive. Midazolam is a short-acting benzodiazepine that functions as a positive allosteric modulator of the GABA-A receptor, offering anxiolysis and anterograde amnesia. Dexmedetomidine is a highly selective alpha-2 adrenergic receptor agonist that induces a unique state of conscious sedation and provides additional analgesia without significant respiratory depression. The combination aims to improve the quality of sedation, enhance hemodynamic stability, and reduce the required doses of each individual agent, thereby minimizing potential side effects such as injection pain, respiratory depression, and post-procedural delirium.

Other names
esketamine-midazolam-dexmedetomidine
02

Targets

ADRA2A (α2A)GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)

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