Low-dose naltrexone (LDN) is compounded naltrexone at 1.5–4.5mg — a prescribed off-label use of the FDA-approved 50mg naltrexone molecule. Compounded LDN is not FDA-approved. It is prepared by a licensed compounding pharmacy and requires a prescription from a licensed provider. Prescription required.

Immune Modulation · Compounded

A 35-year-old molecule. A new mechanism. Low dose naltrexone works by briefly blocking opioid receptors to trigger a powerful endorphin rebound.

Low-dose naltrexone (LDN) uses the FDA-approved naltrexone molecule at 1/10th the standard dose — unlocking a completely different biological mechanism. At these micro-doses (1.5–4.5mg), naltrexone briefly blocks opioid receptors during sleep, triggering compensatory upregulation of endorphins and enkephalins, while simultaneously modulating microglial activity and reducing neuroinflammation.

At Obsidian Genetics, we offer physician-supervised compounded LDN — one flat monthly price, bedtime dosing protocol guidance, and ongoing provider support built in.

Prescription required · Free shipping
vial

Low Dose Naltrexone

Compounded naltrexone at 1.5–4.5mg. Bedtime dosing protocol with provider support.
Starting at
$99.00
Billed monthly
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Treatment Timeline

What to expect over the first 3+ months.

Most patients experience the most significant benefits between weeks 4 and 12. Cumulative improvements continue through month 3 and beyond.

Week 1–2
Initiation

Low dose initiation (typically 1.5mg). Vivid dreams possible as endorphins calibrate and rebound upregulation begins.

Week 2–4
Titration

Dose titration upward toward target (3–4.5mg). Sleep normalizes. First signs of energy and mood improvement may emerge.

Month 1–2
Adjustment

Inflammation markers improving, pain threshold rising. Energy and mood shifts becoming more noticeable. GI side effects resolve.

Month 3+
Full Effect

Full therapeutic benefit — most patients notice cumulative improvement in fatigue, pain, and immune function over 3–6 months.

What the Research Shows

The mechanism, quantified.

Published research on LDN's unique immunomodulatory and neuroinflammatory pathways.

1/10th
Micro-dose vs. standard naltrexone
1.5–4.5mg LDN vs. 50mg (FDA-approved dosage)
TLR4
Microglial receptor target
LDN acts as a toll-like receptor 4 antagonist on microglia, reducing pro-inflammatory cytokine release — the proposed mechanism for LDN's effects on chronic pain and neuroinflammation
30+
Studied conditions
Fibromyalgia, MS, Crohn's, long COVID, chronic fatigue, and more
2–4am
Peak receptor blockade window
Timing coincides with natural endorphin release during sleep
Fibromyalgia pain reductionYounger J et al., Arthritis Rheum. 2013;65(2):529-538; PMID 23359310; randomized controlled crossover trial showed daily pain reduction with LDN vs. placebo in fibromyalgia
Anti-inflammatory mechanismYounger J et al., Clin Rheumatol. 2014;33(4):451-459; PMID 24526250; review of LDN as a novel anti-inflammatory treatment for chronic pain via microglial TLR4 modulation

Research citations reflect published work on low-dose naltrexone mechanisms. Individual clinical outcomes vary. Compounded LDN is not FDA-approved. Prescription required.

How It Works

Dual mechanism of action.

Part 1

Transient Opioid Receptor Blockade & Endorphin Rebound

At bedtime, LDN briefly occupies opioid receptors for 4–6 hours, triggering the brain to compensate by upregulating endogenous endorphins and enkephalins. This rebound effect persists for hours after the drug is metabolized, supporting mood, pain threshold elevation, and improved immune tone during waking hours. The timing is critical — bedtime dosing aligns with your body's natural endorphin circadian rhythm.

Part 2

Microglial Modulation & Neuroinflammation Reduction

LDN acts as a toll-like receptor 4 (TLR4) antagonist on microglial cells, reducing pro-inflammatory cytokine release (IL-6, TNF-α, IL-1β). This dampens the neuroinflammatory cascade implicated in chronic pain, autoimmunity, post-viral fatigue, and mood dysregulation. The anti-inflammatory effect compounds over weeks, making LDN effective for chronic inflammatory and autoimmune conditions.

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Clinical Applications

Prescribed For

Chronic inflammation & immune modulationResearch Supported
Fibromyalgia & chronic painResearch Supported
Autoimmune condition supportResearch Supported
Long COVID & post-viral fatigueEmerging Research
Mood & neuroinflammation supportEmerging Research
Longevity & healthspan (as adjunct)Emerging Research
Multiple sclerosis symptom supportEmerging Research
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Pricing

LDN Protocol Pricing

One flat rate. Physician supervision, compounded medication, and ongoing support included.

Includes: physician consultation · compounded medication · ongoing provider support · free shipping

What You Get

A complete program. One flat price.

01

Physician consultation & dosing

Licensed provider evaluates your health history and prescribes a custom LDN dose (typically 1.5–4.5mg) based on your condition and response.

02

Compounded LDN capsules

Custom-dosed compounded naltrexone capsules, taken at bedtime. Prepared by a licensed compounding pharmacy and shipped directly to you.

03

Bedtime protocol guidance

Detailed guidance on optimal timing, what to expect in the first weeks (vivid dreams, GI adjustments), and how the mechanism works to maximize benefit.

04

Dose titration support

Ongoing provider support for dose adjustments as you progress through weeks 1–4. Check-ins and guidance throughout your first 3 months.

05

Free, discreet shipping

Fast, confidential delivery — right to your door. No surprises. No hidden subscription terms.

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Important Information

Safety & Considerations

Compounded naltrexone is a prescription medication. Your Obsidian Genetics provider will review your full health history before prescribing.

⚠ Important Safety Information

Do NOT use LDN if you are currently taking opioid medications or are opioid-dependent. LDN will precipitate acute opioid withdrawal. Do NOT use in chronic opioid therapy or opioid use disorder. LDN is contraindicated in opioid dependence. Your Obsidian provider must confirm opioid-free status before prescribing.

Common side effects (first 2 weeks): Vivid dreams or sleep disturbance (transient, usually resolves by week 3), mild nausea, GI changes (constipation or diarrhea). These effects are typically dose-dependent and resolve quickly. Why vivid dreams? The endorphin rebound during sleep can produce hyperarousal — a sign the mechanism is working. Most patients report this as a favorable signal. Contraindications: Do not combine with opioid medications, do not use if currently on chronic opioid therapy, do not use in opioid dependence disorder. LDN is generally very well tolerated outside these contraindications and has an excellent long-term safety profile.

Frequently asked question

No. High-dose naltrexone (50mg) is FDA-approved for opioid and alcohol dependence — it blocks opioid receptors to prevent intoxication. Low-dose naltrexone (1.5–4.5mg) works via a completely different mechanism: it briefly blocks receptors during sleep, triggering a rebound upregulation of endogenous endorphins. The dose, timing, and biological mechanism are entirely different. LDN is not used for addiction.

LDN has few drug-drug interactions. The critical exception: do NOT combine with opioid medications (will precipitate withdrawal). If you take immune-modulating drugs (biologics, DMARDs, immunosuppressants), inform your Obsidian provider — they will monitor your response and adjust as needed. Most medications are compatible with LDN. Your provider will review your full med list during your consultation.

Bedtime dosing is critical to LDN’s mechanism. You take it at night because: (1) the 4–6 hour window of opioid receptor blockade aligns with your natural sleep cycle, (2) peak receptor blockade (2–4am) coincides with your body’s peak endorphin release window, (3) the endorphin rebound persists throughout the day after the drug is metabolized, (4) bedtime avoids side effects (vivid dreams, nausea) during waking hours. Timing is everything for LDN.

Low-dose naltrexone is 1.5–4.5mg per day — roughly 1/10th the FDA-approved dose of 50mg used for addiction treatment. This micro-dose is compounded by a licensed pharmacy. The low dose is essential: it’s only at these micro-doses that the opioid receptor rebounds and endorphin upregulation occur. Higher doses (50mg) block receptors completely and work via opioid antagonism, not rebound. Your provider will titrate your dose starting at 1.5mg, increasing gradually to find your optimal therapeutic dose.

Week 1–2: You may notice vivid dreams or initial sleep changes — these are transient signs the mechanism is activating. Week 2–4: During dose titration, you’ll likely notice the first shifts in energy, mood, or pain perception. Month 1–2: Inflammation markers improve, pain threshold rises, sleep normalizes. Month 3+: Most patients report cumulative improvements in fatigue, pain, and immune function. Full therapeutic benefit typically emerges over 3–6 months. Patience is rewarded.

LDN is well-compatible with most longevity and biohacking compounds — rapamycin, NAD+ precursors, resveratrol, metformin, and others. In fact, the immune-modulating and anti-inflammatory effects of LDN complement many longevity protocols. Always disclose your full supplement and medication list to your Obsidian provider. They will review potential synergies and any adjustments needed.

Important: Naltrexone is FDA-approved at 50mg for opioid and alcohol dependence. Low-dose naltrexone (LDN, 1.5–4.5mg) is an off-label use prescribed by a licensed healthcare provider. Compounded LDN is not FDA-approved; its safety and effectiveness have not been verified by the FDA. Compounded LDN is prepared by a licensed 503B or 503A compounding pharmacy and requires a prescription. A licensed Obsidian Genetics physician will evaluate your health history and determine if LDN is appropriate for you. Research statistics and mechanism references reflect published literature on LDN and opioid receptor biology — individual outcomes vary. Do NOT use LDN if currently taking opioid medications or if opioid-dependent; it will precipitate acute withdrawal. LDN is contraindicated in opioid dependence and chronic opioid therapy. Always disclose all medications and health conditions to your provider. Results vary widely; this product is not a guarantee of therapeutic benefit.