Do you need to taper Naltrexone (opioid receptor antagonist)?

Naltrexone Does Not Require Tapering When Discontinuing

Naltrexone does not require tapering when discontinuing treatment as it is an opioid receptor antagonist that does not cause physical dependence. 1

Understanding Naltrexone's Mechanism

• Naltrexone functions as a competitive antagonist at mu opioid receptors, blocking the euphoric effects of opioids and reducing alcohol cravings 1
• Unlike opioid agonists which can cause physical dependence, naltrexone does not produce physical dependence requiring tapering 1
• Naltrexone is available as 50-mg oral tablets or as a 380-mg monthly injection (Vivitrol) 1

Clinical Considerations When Discontinuing Naltrexone

• Abrupt discontinuation of naltrexone does not cause withdrawal symptoms like those seen with opioid agonists 1
• The primary concern when discontinuing naltrexone is not withdrawal but rather increased risk of opioid overdose due to decreased opioid tolerance if patients return to opioid use 1
• Patients who discontinue naltrexone treatment have increased risk of opioid overdose and death if they resume opioid use, as their tolerance has been reduced 1

Special Considerations

• For patients discontinuing naltrexone who have a history of opioid use disorder:

  • Provide opioid overdose education and consider offering naloxone 2
  • Schedule follow-up appointments to monitor for potential relapse 2
  • Consider alternative treatments such as buprenorphine/naloxone if appropriate 1

• For surgical patients on naltrexone who may need opioid pain management:

  • Oral naltrexone should be held for 3-4 days prior to elective procedures 1, 3
  • Extended-release naltrexone should be held for 24-30 days after the last injection before elective procedures 1, 3

Common Pitfalls to Avoid

• Failing to warn patients about the increased risk of overdose if they return to previous opioid use after naltrexone discontinuation 2
• Confusing naltrexone (an opioid antagonist) with opioid agonists that do require tapering 1
• Not providing adequate follow-up care after naltrexone discontinuation, particularly for patients with opioid use disorder 2

Important Distinctions from Opioid Tapering

• Unlike opioids, which require careful tapering to minimize withdrawal symptoms (anxiety, insomnia, abdominal pain, vomiting, diarrhea, diaphoresis, tremor, tachycardia) 2, naltrexone does not produce these withdrawal symptoms upon discontinuation 1
• Opioid tapers typically recommend a 10% reduction per month for long-term users 2, but this approach is unnecessary for naltrexone 1

Remember that while naltrexone itself doesn't require tapering, patients should still receive appropriate monitoring and support when discontinuing treatment, particularly if they have a history of substance use disorder.