Drug intelligence / Profile preview

tapentadol + oxycodone

Development stage
Preclinical
Lead developer
Grünenthal
Modality
Small Molecules
Administration
Oral
01

Overview

Tapentadol + oxycodone is a combination of two opioid analgesics used for pain management, particularly in cases where pain is severe and not adequately controlled by other treatments. Tapentadol acts as both a μ-opioid receptor agonist and a norepinephrine reuptake inhibitor, providing dual mechanisms for analgesia—opioid-mediated nociceptive pain relief and noradrenergic modulation of neuropathic pain. Oxycodone is a classical opioid that functions primarily as a μ-opioid receptor agonist, inhibiting ascending pain pathways in the central nervous system to alter the perception and response to pain. The combination may be considered in complex or refractory cases of severe chronic or cancer-related pain, especially when monotherapy with either agent does not provide sufficient relief[4]. Both drugs carry risks typical of opioids, including dependence, tolerance, constipation, nausea, somnolence, and potential for abuse.

02

Targets

NET (Norepinephrine Transporter)MOR (Mu opioid receptor)

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