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Opioid Antagonist

Naltrexone | Revia

Clinical Overview

Naltrexone is an opioid receptor antagonist indicated for alcohol dependence and opioid dependence as part of a comprehensive treatment program. It blocks the euphoric and sedating effects of opioids and reduces alcohol cravings, making it a valuable tool in addiction treatment when combined with psychosocial support.

Primary Clinical Applications

Naltrexone is indicated for alcohol use disorder to reduce heavy drinking and maintain abstinence, and for opioid use disorder to prevent relapse after detoxification. It is available as oral tablets (Revia) and extended-release injection (Vivitrol) for improved compliance.

Mechanism and Clinical Benefits

As a competitive opioid receptor antagonist, naltrexone blocks the rewarding effects of alcohol and opioids. For alcohol dependence, it reduces craving and the reinforcing effects of drinking. For opioid dependence, it prevents euphoria and respiratory depression from opioid use.

Treatment Considerations

Patients must be opioid-free for 7-10 days before starting naltrexone to avoid precipitating withdrawal. The medication is most effective when combined with psychosocial interventions and requires ongoing monitoring and support for optimal outcomes.

Prescribing Information

Dosing & Administration

Alcohol Dependence:

  • Oral: 50 mg once daily
  • Alternative: 100 mg every other day or 150 mg every 3 days
  • Injectable (Vivitrol): 380 mg IM monthly

Opioid Dependence:

  • Initial: 25 mg daily for 1-2 days (if no withdrawal)
  • Maintenance: 50 mg daily
  • Alternative: 100 mg every other day or 150 mg every 3 days
  • Injectable (Vivitrol): 380 mg IM monthly

Pre-treatment Requirements:

  • Opioid-free for 7-10 days minimum
  • Negative urine drug screen
  • Naloxone challenge test if indicated

Indications

  • Alcohol dependence (as part of comprehensive treatment)
  • Opioid dependence (prevention of relapse after detoxification)

Contraindications

  • Current opioid use or physiological dependence
  • Acute opioid withdrawal
  • Positive urine screen for opioids
  • Acute hepatitis or liver failure
  • Hypersensitivity to naltrexone

Warnings & Precautions

  • Hepatotoxicity: Monitor liver function tests
  • Precipitated withdrawal: Ensure opioid-free status
  • Increased opioid sensitivity: Risk of overdose if opioids used
  • Depression and suicidality: Monitor mood, especially early treatment
  • Injection site reactions: With Vivitrol injections

Drug Interactions

  • Opioid analgesics: Blocks therapeutic effects
  • Opioid-containing medications: Antidiarrheals, cough suppressants
  • Disulfiram: Potential hepatotoxicity (oral naltrexone)

Adverse Reactions

Common:

  • Nausea, headache, dizziness, fatigue, insomnia, anxiety

Injection Site (Vivitrol):

  • Pain, tenderness, induration, swelling

Serious:

  • Hepatotoxicity, depression, injection site necrosis

Special Populations

  • Hepatic Impairment: Contraindicated in acute hepatitis or liver failure
  • Renal Impairment: Use with caution, monitor closely
  • Pregnancy: Category C – use only if benefits outweigh risks
  • Emergency Medical Situations: Larger opioid doses may be needed
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.