naltrexone
Naltrexone is an opioid antagonist used for alcohol use disorder and opioid use disorder relapse prevention. Low-dose naltrexone (4.5mg, LDN) is used off-label for chronic pain, fibromyalgia, and inflammatory conditions — different mechanism, different evidence base.
50mg tablets (oral); 380mg IM monthly (Vivitrol); 4.5mg compounded (low-dose naltrexone, off-label)
Tablets: 50mg; IM (Vivitrol): 380mg/month; Compounded LDN: 1.5-4.5mg (off-label)
Category C
Competitive antagonist at mu, kappa, and delta opioid receptors. At low doses, paradoxical effects may involve transient receptor blockade and endogenous opioid upregulation.
For oral naltrexone, most patients can stop without taper. For depot, the long half-life provides a natural taper. Plan for return of cravings.
Naltrexone is not dependence-forming; the main risk on discontinuation is loss of the medication-supported buffer against the underlying disorder, not pharmacological withdrawal.
Days (oral) or weeks (depot wear-off)
1-2 weeks
Usually 2-4 weeks
Rare for the medication itself; the underlying condition is the main long-term consideration
Toxicity
Hepatotoxicity (dose-dependent — uncommon at standard doses), nausea, headache, dizziness, anxiety, insomnia, depression. Will precipitate severe withdrawal in opioid-dependent patients.
Pharmacokinetics
Hepatic via dihydrodiol dehydrogenase.
Browse our map of deprescribing-informed providers worldwide.