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← Compounds

Low-Dose Naltrexone

off-label Rx · co-headlineFDA-approved · off-label

Transient opioid blockade → endorphin rebound; TLR4/microglial modulation

Summary

Low-dose naltrexone — the opioid antagonist naltrexone at ~1/10th its addiction dose. Transient nightly receptor blockade is thought to trigger an endorphin rebound and modulate microglial/immune (TLR4) activity. Cheap, off-label, cross-condition; a co-headline agent alongside peptides.

How it works

  • Transient mu-opioid blockade → endorphin rebound
  • TLR4 antagonism / microglial modulation
  • Immune & inflammatory downregulation

Dosing

  • unit: mg
    frequency: nightly (titrate from 1.5)
    standard dose: 4.5
    administration route: Oral

Cycling

  • Continuous; titrate slowly over weeks

Side effects

common: ["Vivid dreams / early sleep disturbance","Headache","Transient GI upset"]
warnings: ["Contraindicated with concurrent opioid therapy — precipitates withdrawal"]

Verified citations

3 · PubMed-checked
  • Low-Dose Naltrexone for Chronic Pain: Update and Systemic Review.reviewPMID 32845365 ↗
  • Low-Dose Naltrexone in MS, Fibromyalgia, Crohn's Disease, and Other Chronic Pain Disorders.reviewPMID 29377216 ↗
  • Fibromyalgia symptoms are reduced by low-dose naltrexone: a pilot study.clinicalPMID 19453963 ↗

Used for

Legal / compounding

FDA-approved · off-label

Legal status is a hard gate: non-compoundable or delisted agents cannot be filled and are blocked from protocol export. Keep 503A status current.