Opioid receptor antagonist (at low doses modulates microglial activation and neuroinflammation)
At low doses, LDN transiently blocks opioid receptors, which may lead to upregulation of endogenous endorphins and modulation of microglial activity, reducing neuroinflammation
Medication-assisted treatment (MAT) for both opioid and alcohol use disorders
Augmentation in mood disorders, fibromyalgia, chronic pain syndromes
Oral tablets (typically compounded for low doses)
1.5 mg p.o. daily, titrated slowly up to 4.5 mg daily as tolerated
1.5–4.5 mg/day
Oral absorption with peak plasma concentrations within 1 hour; half-life approximately 4 hours
Vivid dreams, insomnia, gastrointestinal discomfort
Rare; generally well tolerated
Monitor for sleep disturbances and GI symptoms during initiation
None
May benefit neuroinflammatory conditions such as multiple sclerosis (MS), post-stroke syndromes, and traumatic brain injury (TBI)-related fatigue or pain, although evidence is limited and primarily anecdotal. Avoid use in patients receiving opioid therapy due to risk of opioid receptor blockade and withdrawal. Slow titration recommended to improve tolerability.