Opioid antagonists block opioid receptors to reverse overdose, treat addiction, or at very low doses (LDN), modulate the immune system and reduce neuroinflammation. Low Dose Naltrexone (LDN) at 1.5–4.5mg is one of the most commonly prescribed compounded medications.
Naltrexone binds to opioid receptors (μ, δ, κ). At standard 50mg doses it blocks opioid effects. At ultra-low doses (LDN), the brief receptor blockade triggers an endorphin rebound and modulates microglial activity and TLR4 receptors, reducing neuroinflammation.
FDA-approved naltrexone is only available at 50mg tablets. LDN doses of 0.5–4.5mg, pediatric liquid formulations, and topical LDN preparations all require compounding from a specialized pharmacy.
LDN is an off-label use of naltrexone — FDA-approved at 50mg for addiction, but not approved at low doses. Compounding LDN is legal under 503A for individual patient prescriptions. Multiple clinical trials support its use for autoimmune and inflammatory conditions. It has no addiction potential and minimal side effects.
These compounded medications belong to this drug class. Click any medication to learn more and compare pharmacy prices.
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