Mu-opioid agonist
Mu-opioid receptor agonist
- If BBB-crossing:
- Strong analgesia and euphoria
- High abuse liability
- Respiratory depression → mechanism of opioid overdose death
- Miosis, nausea and sedation
- Nausea/emesis (especially initially)
- Cough suppression
- Sustained activation → tolerance, dependence and hyperalgesia
- Constipation
- Suppression of hypothalamic-pituitary-adrenal (HPA) axis
- decreased CRH release
- decreased ACTH secretion
- blunted cortisol response
Drugs with this mechanism (36)
Alfentanil
Beta-endorphin
Codeine
Difenoxin
Diphenoxylate
Eluxadoline
Endomorphins
Enkephalin
Hydromorphone ER
Fentanyl
Heroin
Hydrocodone
Hydromorphone
Hydrocodone ER (q24h)
Morphine ER capsules
Levorphanol
Loperamide
Morphine-6-glucuronide
Meperidine
Methadone
Morphine
Morphine ER tablets
O-desmethyltramadol
Oliceridine
Oxycodone
Oxycodone CR
Oxymorphone
R-Methadone
Remifentanil
S-Methadone
Sufentanil
Tapentadol
Tianeptine
Tramadol
Tramadol ER
Hydrocodone ER (q12h)
Self-check
- What causes opioid overdose death through central mu activation?
Respiratory depression. - What pain effect can sustained mu activation produce?
Hyperalgesia.
All mechanisms · Open Mu-opioid agonist in the interactive console ↗