UMEM Educational Pearls

Category: Pharmacology & Therapeutics

Title: Naltrexone vs. Methylnaltrexone

Keywords: naltrexone, methylnaltrexone, constipation, opioid dependence (PubMed Search)

Posted: 6/1/2012 by Bryan Hayes, PharmD (Emailed: 6/2/2012) (Updated: 6/15/2012)
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Naltrexone and methylnaltrexone are both mu-receptor antagonists that look similar and have similar names. But, they have very different uses.

  • Naltrexone (ReVia, Vivitrol)
    • Used to treat opioid/alcohol dependence or to prevent relapse following opioid detoxifcation
    • Dose: 25 to 100 mg PO daily or 380 IM every 4 weeks
    • Crosses blood-brain-barrier and can precipitate withdrawal
  • Methylnaltrexone (Relistor)
    • Used to treat opioid-induced constipation
    • Dose (weight-based): 8 to 12 mg (or 0.15 mg/kg) subcutaneously once daily
    • Peripherally acting, does not cross blood brain barrier


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