Drug intelligence / Profile preview

ketamine + xylazine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intraperitoneal, Intramuscular, Intravenous
01

Overview

Ketamine + xylazine is a widely used **injectable veterinary anesthetic combination** that pairs the dissociative anesthetic ketamine with the alpha-2 adrenergic agonist sedative xylazine to produce balanced anesthesia, analgesia, and muscle relaxation, particularly in small laboratory animals and other veterinary species.[1][2][3][6][9] Ketamine acts primarily as a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist to induce dissociative anesthesia and potent analgesia with relative preservation of respiratory drive, while also interacting with opioid, serotonin, GABA, sigma, and dopamine receptors.[2][6] Xylazine is an α2-adrenergic receptor agonist that provides sedation, analgesia, amnesia, and muscle relaxation and serves as an adjunct to ketamine to counteract ketamine-induced muscle hypertonicity, improve immobilization, and reduce the dose of ketamine required.[1][2][6][9] The combination is recommended for short-term, well-balanced anesthesia in many animal protocols, but can cause bradycardia, hypotension, respiratory depression, and hypothermia, and xylazine’s effects can be reversed with α2-adrenergic antagonists such as atipamezole or yohimbine.[1][6][9] It is not approved for human medical use as a fixed combination, and its use is largely restricted to veterinary anesthesia and research animal procedures.

Other names
ketamine/xylazineketamine-xylazineKX
02

Targets

KOR (Kappa opioid receptor)SIGMAR1 (Sigma non-opioid intracellular receptor 1)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))HTR7 (5-hydroxytryptamine receptor 7)NMDAR (Glutamate receptor ionotropic, NMDA)ADRA2A (α2A)

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