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Low-Dose Naltrexone Drug-Drug Interactions: The Complete Clinical Profile At a glance Standard LDN dose range / 1.5 to 4.5 mg taken once nightly Absolute contraindication / concurrent opioid agonists (risk of precipitated withdrawal) Primary metabolism / hepatic, via CYP2D6 and CYP3A4 to 6-beta-naltrexol FDA black box warning / hepatotoxicity at doses of 300 mg/day (standard naltrexone, not LDN range) Most studied indication / fibromyalgia pain reduction (Younger et al., 2009) Opioid receptor blockade duration / approximately 4 to 6 hours at LDN doses Compounding source / 503A pharmacies (not commercially available at low doses) Key monitoring parameter / liver function tests if co-prescribed with hepatotoxic agents Immunomodulatory mechanism / transient opioid blockade upregulates endorphin production and modulates glial cell activity How Low-Dose Naltrexone Works and Why Interactions Occur LDN produces its effects through a mechanism distinct from standard-dose naltrexone (50 mg)
Archives of internal medicine 168, 598608 (2008)
CMS may extend, modify, or make the coverage permanent based on results, but as currently structured the bridge is an 18-month demonstration program
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