Drug intelligence / Profile preview

oxycodone + oxymorphone + tramadol

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

This is a combination of three opioid analgesics—oxycodone, oxymorphone, and tramadol. All three are centrally acting opioids used for the management of moderate to severe pain. Oxycodone and oxymorphone are semi-synthetic opioids that act primarily as agonists at the mu-opioid receptor, leading to analgesia by inhibiting ascending pain pathways in the central nervous system. Tramadol is a synthetic opioid with dual mechanisms; it acts as a weak mu-opioid receptor agonist and also inhibits serotonin and norepinephrine reuptake, contributing additional analgesic effects through modulation of descending inhibitory pain pathways[2][5]. This combination would theoretically provide potent multimodal pain relief but would carry significant risks for additive side effects including respiratory depression, sedation, constipation, dependence, and overdose.

02

Targets

DOR (Opioid Receptor Delta 1)SERT (Sodium-dependent serotonin transporter)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)NET (Norepinephrine Transporter)

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