Drug intelligence / Profile preview

propofol + clonidine + ketamine

Development stage
Preclinical
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination of **propofol**, **clonidine**, and **ketamine** is used in anesthesia and procedural sedation to leverage their synergistic effects for sedation, analgesia, and hemodynamic stability. - **Propofol** is a rapid-acting sedative-hypnotic agent that enhances GABAergic inhibition, resulting in sedation, amnesia, and hypnosis, but may cause hypotension and respiratory depression. - **Ketamine** is a dissociative anesthetic that acts as an NMDA receptor antagonist, providing analgesia and amnesia, while maintaining airway reflexes and sympathetic tone, thus attenuating cardiovascular depression. - **Clonidine** is an alpha-2 adrenergic agonist that produces sedation and analgesia by decreasing sympathetic outflow, enhancing the sedative effects of other agents, with minimal respiratory depression, and can reduce overall anesthetic requirements. The triple-drug combination is used primarily in perioperative and procedural sedation settings, especially in pediatric and high-risk populations, to improve induction, maintain cardiovascular stability, reduce drug-related adverse effects, and potentially lower the required doses of each component. Literature primarily describes dual regimens (propofol + ketamine or propofol + clonidine), but evidence supports hemodynamic and sedation benefits in regimens containing all three agents.

02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)I1R (Nischarin)GABRR (GABA-A receptor subunit rho)ADRA2A (α2A)

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