Drug intelligence / Profile preview

propofol + remifentanil + esketamine

Development stage
Preclinical
Lead developer
China-Japan Friendship Hospital
Modality
Small Molecules
Administration
Intravenous
01

Overview

The combination of **propofol**, **remifentanil**, and **esketamine** is a multi-drug regimen used for total intravenous anesthesia (TIVA). Propofol serves as the primary sedative-hypnotic agent, acting as a positive allosteric modulator of the GABA-A receptor. Remifentanil is an ultra-short-acting mu-opioid receptor agonist that provides potent intraoperative analgesia. Esketamine, the S-enantiomer of ketamine, is an NMDA receptor antagonist that contributes both to the anesthetic depth and provides additional analgesia, potentially reducing the required dose of propofol. This specific combination is being investigated by the China-Japan Friendship Hospital to determine optimal Bispectral Index (BIS) ranges and effect-site concentrations for maintaining adequate anesthesia depth during orthopedic procedures such as unilateral knee replacement surgery.

Other names
propofol + remifentanil + esketamineTIVA with esketaminepropofol-remifentanil-esketamine
02

Targets

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

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