Drug intelligence / Profile preview

esketamine + oxycodone

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Intranasal, Oral
01

Overview

Esketamine + oxycodone is a combination of two pharmaceutical drugs, esketamine and oxycodone. Esketamine is the S-enantiomer of ketamine and acts primarily as a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, producing dissociative anesthetic and rapid-acting antidepressant effects. It is approved for use in treatment-resistant depression and major depressive disorder with acute suicidal ideation or behavior, typically as a nasal spray administered under medical supervision[1][2][7]. Oxycodone is a potent semisynthetic opioid analgesic that acts as an agonist at mu-, kappa-, and delta-type opioid receptors to provide pain relief[8]. The combination may be considered for situations where both rapid antidepressant action (esketamine) and strong analgesia (oxycodone) are required; however, co-administration increases the risk of central nervous system depression, sedation, respiratory depression, and other adverse effects due to additive pharmacodynamic interactions[1][4]. There are no known branded or approved fixed-dose combination products containing both esketamine and oxycodone.

02

Targets

KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)

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