Small molecule
PubChem CID 5284603
Oxycodone
Roxicodone
- Mechanism of action
- Full opioid agonist, binds mu-opioid receptors to block pain signaling
- In plain language
- Attaches to opioid receptors in the brain and spinal cord that the body normally uses for its own natural pain-relief signals, blocking pain messages and producing a sense of relief and calm — the same activity responsible for its risk of slowed breathing and its potential for dependence.
- How it works
- Oxycodone (Roxicodone) is a full opioid agonist. Per the FDA label, it is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses; analgesia is its principal therapeutic action, and like all full opioid agonists there is no ceiling effect for analgesia -- clinically, dosage is titrated to provide adequate pain relief and may be limited by adverse reactions, including respiratory and CNS depression. The precise mechanism of the analgesic action is unknown, though specific CNS opioid receptors for endogenous opioid-like compounds have been identified throughout the brain and spinal cord and are thought to mediate its analgesic effects.
- Therapeutic applications
- Oxycodone (Roxicodone) is FDA-indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. It carries a boxed warning for the serious and life-threatening risks of addiction, abuse, and misuse; life-threatening respiratory depression, especially during initiation or dosage increases; accidental pediatric ingestion, which can cause a fatal overdose; and profound sedation, respiratory depression, coma, and death when used concomitantly with benzodiazepines or other CNS depressants, including alcohol. Because these risks can occur at any dosage or duration, the label directs that opioid analgesics be reserved for patients for whom alternative treatment options are ineffective, not tolerated, or otherwise inadequate.
- Class
- Small molecule
- Therapeutic area
- Analgesic / Pain
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