Apexion Health Low-Dose Naltrexone oral tablets
IMMUNELDN

MONTHLY SUPPLY · ORAL TABLET

LOW-DOSE NALTREXONE

TREATMENT

Immune modulation at sub-therapeutic opioid-blocking doses

SUPPORT

Low-dose naltrexone (LDN) uses transient opioid receptor blockade at sub-therapeutic doses (1.5–4.5 mg) to upregulate endogenous opioid production, reduce neuroinflammation, and modulate immune function — distinct from naltrexone's therapeutic opioid-blocking dose.

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Lab-Tested · Physician-Supervised · Discreet Delivery

Apexion Health — IMMUNE

SUB-THERAPEUTIC DOSING. SIGNIFICANT IMMUNE MODULATION.

Naltrexone at standard doses (50 mg) is an opioid receptor antagonist used to treat addiction. At 1.5–4.5 mg — roughly 1/10th the therapeutic dose — it transiently blocks opioid receptors for 4–6 hours, triggering a compensatory rebound: the body upregulates its own endorphin and enkephalin production. The short blockade also attenuates microglial activation and reduces pro-inflammatory cytokine output, producing an immune-modulatory effect that has been studied in autoimmune conditions, chronic pain, and inflammatory disease.

Clinical Benefits

LOW-DOSE NALTREXONE SUPPORTS YOUR HEALTH AT THE CELLULAR LEVEL

  1. 01.

    TRANSIENTLY BLOCKS OPIOID RECEPTORS TO TRIGGER ENDORPHIN REBOUND

  2. 02.

    UPREGULATES ENDOGENOUS BETA-ENDORPHIN AND MET-ENKEPHALIN PRODUCTION

  3. 03.

    REDUCES MICROGLIAL ACTIVATION AND NEUROINFLAMMATION

  4. 04.

    MODULATES PRO-INFLAMMATORY CYTOKINE SIGNALING

  5. 05.

    STUDIED IN AUTOIMMUNE, CHRONIC PAIN, AND INFLAMMATORY CONDITIONS

  6. 06.

    PHYSICIAN-PRESCRIBED ORAL TABLET AT SUB-THERAPEUTIC DOSE

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Clinical Evidence

How It Works in the Body

01 — Dose & Efficacy

Immune Modulation & Pain Relief

Fibromyalgia ≥30% pain reduction in ~50%50%
Crohn’s Disease Response at 12 weeks67%
Fatigue Patient-reported improvement40%

Younger et al., Arthritis Rheum 2013; Raknes et al., Clin J Pain 2017

02 — Hormone Panel

Inflammatory & Symptom Markers

MarkerWithoutWith Treatment
VAS Pain (Fibro)0–100
65
45−20
ESR (Crohn’s)mm/hr
28
16−12
TNF-α—
Elevated
Modestly ↓↓ (est.)
Daily Function (FIQ)Score
60
45−15

Biphasic mechanism: transient blockade → receptor upregulation

At 1.5–4.5 mg, naltrexone transiently blocks opioid receptors 3–4 hrs, triggering compensatory endogenous opioid upregulation. Also antagonizes TLR4 on microglia, reducing TNF-α and IL-6.

Younger et al., Arthritis Rheum 2013; Patten et al., Mult Scler 2018

03 — Protocol

LDN Dose Titration

InitiationWeeks 1–4
  • ›Start 1.5 mg at bedtime
  • ›Sleep quality diary
  • ›Pain & symptom log
  • ›Assess vivid dreams
TitrationWeeks 5–12
  • ›Increase 3.0 → 4.5 mg
  • ›Symptom response weekly
  • ›Find optimal dose (1.5–4.5 mg)
MaintenanceMonth 4+
  • ›Continue optimal dose nightly
  • ›Symptom & QOL q3 months
  • ›Annual safety labs (CBC, LFTs)

Requires compounding — no commercial LDN product

Compounded from 50 mg naltrexone to 1.5–4.5 mg capsules. Vivid dreams common initially (transient). Contraindicated with concurrent opioids. Well tolerated at low doses.

All protocols physician-supervised and adjusted per individual labs.