Low-Dose Naltrexone

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

Transient opioid blockade → endorphin rebound; TLR4/microglial modulation

Overview

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

1.5–4.5 mg PO at bedtime; titrate up from 1.5 mg.

Oral4.5 mg standard· nightly (titrate from 1.5)

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 ↗

Reconstitution

Not applicable — this compound is oral. No vial reconstitution needed.

Used for

Legal / compounding

FDA-approved · off-label

FDA: Approved (naltrexone); low-dose is off-label / compounded

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