Drug intelligence / Profile preview

paroxetine + oxycodone

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

A drug combination consisting of paroxetine (a selective serotonin reuptake inhibitor antidepressant) and oxycodone (an opioid analgesic). This combination has been studied due to concerns about increased respiratory depression risk. Clinical research has demonstrated that paroxetine combined with oxycodone significantly decreases the ventilatory response to hypercapnia compared to oxycodone alone, which is the primary feedback mechanism protecting against opioid-induced respiratory depression. While paroxetine affects oxycodone metabolism by inhibiting CYP2D6 (reducing conversion to oxymorphone), the respiratory effects appear to be primarily pharmacodynamic rather than pharmacokinetic in nature.

02

Targets

GRK2-DOR interface (GRK2–delta opioid receptor interface)MOR (Mu opioid receptor)SERT (Sodium-dependent serotonin transporter)

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