What is the recommended protocol for increasing the naltrexone (opioid receptor antagonist) dose over 7 days?

Naltrexone Dose Titration Protocol Over 7 Days

For opioid dependence treatment, naltrexone should be initiated at 25 mg on the first day, then increased to 50 mg daily thereafter if no withdrawal signs occur. 1

Initial Requirements Before Starting Naltrexone

• Ensure patient is completely detoxified from opioids with a drug-free period of 7-10 days prior to first dose 2
• Verify opioid-free status through either:
  • Urine drug screening 2
  • Naloxone challenge test to confirm absence of physical dependence 1

Naloxone Challenge Test Protocol

• Intravenous method:

  • Inject 0.2 mg naloxone and observe for 30 seconds for withdrawal signs
  • If no withdrawal signs appear, inject 0.6 mg naloxone and observe for 20 additional minutes 1

• Subcutaneous method:

  • Administer 0.8 mg naloxone and observe for 20 minutes for withdrawal signs 1

7-Day Naltrexone Titration Schedule

1. Day 1: Start with 25 mg oral naltrexone (half the standard dose) 1, 2
2. Day 2-7: If no withdrawal signs occur, increase to the standard dose of 50 mg daily 1

Monitoring During Titration

• Monitor for signs of opioid withdrawal which may include:

  • Nausea, vomiting, dysphoria, yawning, sweating
  • Tearing, rhinorrhea, stuffy nose, craving for opioids
  • Abdominal cramps, sense of fear, skin erythema
  • Anxiety, irritability, muscle aches or cramps 1

• Perform liver enzyme tests before and during treatment 2

Special Considerations

• Do not administer naltrexone to:

  • Pregnant women or women who are breastfeeding
  • Children under 18 years of age
  • Patients with renal failure 2
  • Patients showing clinical signs of opioid withdrawal 1

• For patients requiring supervised administration, alternative dosing schedules may be considered:

  • 50 mg every weekday with 100 mg on Saturday
  • 100 mg every other day
  • 150 mg every third day 1

Important Cautions

• Higher risk of hepatocellular injury may occur with single doses above 50 mg 1
• Naltrexone should be considered only one component of a comprehensive treatment program 1, 3
• Patients most likely to benefit from naltrexone therapy are those who are:
  • Employed, married, stabilized on low-dose methadone prior to detoxification
  • Highly motivated to maintain a non-opioid treatment regimen 3

This protocol provides a safe and effective method for initiating naltrexone therapy while minimizing the risk of precipitating withdrawal symptoms in patients transitioning from opioid dependence to abstinence.