Drug intelligence / Profile preview

ketamine

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Intranasal
01

Overview

Ketamine is a dissociative anesthetic used medically for the induction and maintenance of anesthesia in both humans and animals. It is also used off-label as a treatment for depression and as an analgesic. Ketamine acts primarily as an antagonist of the N-methyl-D-aspartate (NMDA) receptor on glutamate binding sites in the central nervous system. This NMDA receptor antagonism is responsible for its anesthetic effects (including sedation and amnesia), analgesia (pain relief), dissociation from environment and pain perception ("dissociative anesthesia"), psychotomimetic effects (hallucinations), and neuroprotection. The drug has additional mechanisms including enhancement of descending serotonergic pathways. Ketamine is available as a racemic mixture containing equal parts esketamine (S-ketamine) and arketamine (R-ketamine); esketamine has higher potency at the NMDA receptor. It can be administered intravenously or intramuscularly for medical use; it is also abused recreationally due to its hallucinogenic properties. Esketamine nasal spray has been developed specifically for treatment-resistant depression.

Brand names
Ketalar
Other names
special KKketkitkatsuper Khorse trankCat TranquilizerCat ValiumJet KPurpleSpecial La CokeSuper AcidVitamin K
02

Targets

CHRNA7 (α7 nicotinic receptor)SERT (Sodium-dependent serotonin transporter)mAChR (Muscarinic acetylcholine receptors)NMDAR (Glutamate receptor ionotropic, NMDA)

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