Naltrexone: How It Works, What It's Studied For & Safety
Naltrexone is an opioid receptor antagonist FDA-approved for opioid and alcohol use disorders; used off-label at much lower doses (LDN, 1.5–4.5 mg) for pain, autoimmune, and inflammation research. Clinicians consider it for opioid and alcohol use disorders (FDA-approved). Compounded variants are dispensed by Wells Pharmacy Network only after a clinician evaluation.
Also known as: Vivitrol, ReVia, Low-Dose Naltrexone (LDN)
How does Naltrexone work?
At full doses, naltrexone competitively blocks mu-opioid receptors. At low doses, transient receptor blockade is studied for upregulation of endorphin signaling and modulation of microglial Toll-like receptor 4 - the proposed mechanism behind anti-inflammatory low-dose naltrexone effects.
What is Naltrexone studied for?
- Opioid and alcohol use disorders (FDA-approved)
- Off-label low-dose naltrexone (LDN) in fibromyalgia, chronic pain, and autoimmune research
- Off-label adjunct in inflammation-axis protocols
How is Naltrexone taken?
FDA-approved as 50-mg oral tablets and an extended-release IM injection (Vivitrol). Compounded low-dose oral capsules and topical preparations exist for off-label clinician-directed protocols.
Is Naltrexone FDA-approved? Is it safe?
FDA-approved as a finished drug product when prescribed under its labeled indications. Compounded variants on this site are separate from the branded product and are dispensed only when a clinician determines a compounded preparation is appropriate. Hepatotoxicity boxed warning at high doses. Concurrent opioid use is contraindicated. LDN dosing has a more modest safety profile. Compounded prescription-only preparations are dispensed by Wells Pharmacy Network. Eligibility is decided by a licensed clinician based on intake and labs, not by checkout. Compounded products on this site are not FDA-approved and are not generic equivalents of any branded medication.
In the Regen Therapy catalog
This compound does not currently appear in an active Regen Therapy protocol. Browse the full catalog for adjacent options.
What does the research say about Naltrexone?
Strong evidence for the labeled indications; LDN literature includes small RCTs in fibromyalgia and Crohn's research.
Citations & further reading
Considering Naltrexone as part of a protocol?
Browse Regen Therapy's catalog or start a clinician evaluation. Every prescription is reviewed by a licensed clinician and dispensed by Wells Pharmacy Network.
Browse the catalog →