Opioid antagonist

Naltrexone

ReVia (oral), Vivitrol (extended-release intramuscular injection)
FDA-Approved Indications
  • Opioid use disorder (OUD), prevention of relapse following opioid detoxification
  • Alcohol use disorder (AUD), reduction of alcohol consumption
Common Off-Label Uses
  • Impulse control disorders
  • Self-injurious behavior (limited evidence)
  • Ultra-low-dose naltrexone for various conditions (limited/controversial evidence)

Side Effects Worth Knowing

Nausea: the most common side effect

Often occurs early in treatment, particularly with oral dosing. Starting at 25mg for the first few days and titrating to 50mg may reduce initial nausea. Taking with food may help. Usually transient.

Headache: common

Often resolves within the first weeks. Not usually treatment-limiting.

Injection site reactions (Vivitrol): common

Pain, induration, nodules at the injection site. Occasionally significant enough to affect adherence. Proper injection technique (gluteal muscle, alternating sides) helps. Rarely, injection site reactions can be severe (tissue necrosis has been reported; requires monitoring).

Dizziness/fatigue: reported

Usually mild and self-limiting.

Dysphoria/mood changes: reported

Endogenous opioid blockade may diminish normal hedonic responses in some patients. Monitor for depression or mood changes, particularly in patients with co-occurring mood disorders. Clinical significance is variable, many patients tolerate naltrexone without noticeable mood effects.

Hepatotoxicity: warning in labeling

Historically observed at supratherapeutic doses (approximately 300mg/day in obesity trials). At standard 50mg/day doses, clinically significant hepatotoxicity is uncommon. Baseline and periodic LFTs recommended. Avoid in acute hepatitis or severe hepatic impairment.

Insomnia: reported

Some patients experience sleep disruption. Usually mild.

Decreased appetite: reported

Possibly related to opioid system involvement in appetite regulation.

See This Medication in Action

These case studies show how naltrexone decisions play out in real clinical scenarios:

References & Further Reading

This page synthesizes information from standard clinical references. Consult primary sources for all prescribing decisions.

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For learning and board prep — not a prescribing reference. Dosing and safety information change. Always verify against current FDA labeling and your institution’s protocols before prescribing.