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
- naltrexone in CONTRAVE
- Reverses opioid constipation
Drugs with this mechanism (12)
- 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 nasal — Long-acting opioid antagonist nasal spray for opioid overdose; outlasts naloxone, prolonging precipitated withdrawal.
- Nalmefene auto-injector — Long-acting opioid antagonist auto-injector for intramuscular or subcutaneous use in opioid overdose.
- 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.
Self-check
- What can a BBB-crossing mu antagonist precipitate in an opioid-dependent person?
Withdrawal. - Which bowel effect of opioids can mu antagonism reverse?
Constipation.
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