Mu-opioid antagonist
Mu-opioid receptor antagonist
- If BBB-crossing:
- Reverses analgesia, euphoria and respiratory depression
- Opioid-overdose rescue and dependence treatment
- Precipitates withdrawal in the opioid-dependent
- Reverses opioid constipation
- ➔ naltrexone in CONTRAVE
Drugs with this mechanism (11)
- Alvimopan — Peripheral mu antagonist speeding gut recovery after bowel surgery.
- Methylnaltrexone — Peripheral mu antagonist for opioid-induced constipation.
- Nalbuphine — Mixed opioid agonist-antagonist analgesic with a ceiling on respiratory depression.
- Naldemedine — Peripheral mu-opioid antagonist for opioid-induced constipation; no food restriction.
- Nalmefene — Long-acting intranasal opioid antagonist for overdose reversal.
- Naloxegol — Oral peripheral mu antagonist for opioid-induced constipation.
- Naloxone — Short-acting opioid antagonist; the overdose-reversal agent.
- Naloxone nasal spray — OTC intranasal mu-opioid antagonist for community overdose reversal; repeat doses may be needed.
- Naltrexone — Opioid antagonist for alcohol and opioid use disorder; monthly injectable option.
- Samidorphan — Mu antagonist added to olanzapine to blunt weight gain.
- Naltrexone ER injection — Extended-release injectable naltrexone for alcohol and opioid use disorders.
All mechanisms · Open Mu-opioid antagonist in the interactive console ↗