Waking up to yet another day of painful, achy joints, sore muscles, and brain fog is not the good morning greeting you were hoping for. Yet it seems to be the new normal these days.

Your immune system is designed to protect you, so the mere thought of it turning against you feels like nothing short of a betrayal. 

Autoimmune disease is on the rise these days.(1) I bet right now you can think of someone you know who is struggling with an autoimmune condition. Or perhaps that someone is you. 

Low-dose naltrexone (LDN) has been gaining traction recently as a potential treatment for autoimmune illness – including multiple sclerosis, fibromyalgia, Hashimoto’s thyroiditis, and Crohn’s disease.

But what is it? How does it work? And is it effective?

Let’s take a closer look at LDN and how it may be helpful for autoimmune patients – as well as those with chronic pain and inflammatory conditions. 

What is Low-Dose Naltrexone?

Naltrexone is an opioid receptor antagonist, meaning it blocks the opiate/endorphin receptors in your brain. 

Regular strength naltrexone (50-100 mg) has been used as a treatment for opioid addiction since the 1980s. It was effective for addiction since it blocks endorphins, preventing patients from feeling the “high” of opioid drugs. If patients can’t feel the “high”, then the drugs are powerless, decreasing the chance of relapse. 

But in the mid-1980s, Dr. Bernard Bihari, a Harvard-trained neurologist, began using Naltrexone at a very low dose. He was treating many HIV patients who were taking Naltrexone for their opioid addictions. 

As he weaned them off Naltrexone, the patients noticed a marked improvement in their physical and mental symptoms when they reached very low doses. Dr. Bihari also observed beneficial results using LDN in patients with autoimmunity and even cancer.(2) 

How Does Low-Dose Naltrexone Work?

Like full-strength Naltrexone, low-dose Naltrexone’s mechanism of action is through the role of endorphins.

Endorphins are naturally occurring proteins produced by the central nervous system. They act on the opioid receptors in our brains, promoting a feeling of well-being – just like the “runner’s high” produced after exercise. 

Endorphins play an important role in reducing pain and inflammation, and also are a key factor in modulating the immune system.(3)

The term “modulating” refers to bringing balance to the immune system. If it’s deficient, an immune-modulating therapy will stimulate it. If it’s overactive, as is the case in autoimmune disease, an immune-modulating therapy will calm it down.

Although the cause is unclear, most people with autoimmunity have lower levels of endorphins than those without autoimmunity.

When Naltrexone is taken at very low doses (0.5-4.5 mg), it blocks the opioid receptors for just a few hours. Then a rebound effect occurs, resulting in increased endorphin production. It’s this rebound effect that is believed to cause the modulation of the immune system, as well as reductions in pain and inflammation seen with LDN.

On the other hand, taking full-strength Naltrexone cancels out the immunomodulatory effect by completely overwhelming the opioid receptors. So to have an immune-modulating effect, the dose must be kept between 0.5 and 4.5 mg per day.(4) 

Benefits of Low-Dose Naltrexone

Although its use is still considered experimental, research has discovered the following benefits of LDN:

• Immune modulatory

• Anti-inflammatory

• Analgesic (alleviates pain)

• May improve symptoms of anxiety and depression

• Inexpensive

• Well tolerated

• Few drug interactions (5)
  
  

What Conditions Can Low-Dose Naltrexone Help?

Because of its immune-modulating effects, LDN has the potential to improve symptoms in any autoimmune disease. This includes:

• Ankylosing spondylitis

• Autism

• Chronic fatigue syndrome (CFS)

• Crohn’s disease

• Ehlers-Danlos Syndrome

• Fibromyalgia

• Hashimoto’s

• Lupus

• Multiple sclerosis

• PANS/PANDAS

• Psoriatic arthritis

• Rheumatoid arthritis

• Sjögren's syndrome

• Ulcerative colitis

LDN has been shown to be particularly helpful in painful autoimmune conditions, such as fibromyalgia, multiple sclerosis, Crohn’s disease, and complex regional pain syndrome.

In particular, two studies suggested that LDN was superior to placebo in reducing the pain associated with fibromyalgia.  In Crohn’s disease, LDN has been found to reduce not only self-reported pain but also laboratory measures of inflammation and disease severity.(6)  

 Its benefits in pain reduction are particularly important since most prescription pain relievers have a high risk of dependence. 

How To Safely Use Low-Dose Naltrexone

LDN is generally prescribed for autoimmune conditions at doses of 1.5-4.5 mg. Some doctors prefer to start patients at a very low dose of 1-1.5 mg and then slowly increase the dose so the body has time to adjust to it.  

It’s best to take LDN around 9 pm because of the rhythm of the body’s natural production of endorphins. So most patients take it just before bed. However, if the increased endorphins keep you up at night, you may want to take it in the morning instead.

Since it’s an opioid antagonist, LDN can interfere with opioid medications you may be taking for pain. So you’d need to take LDN away from those medications to ensure proper absorption.(7)

LDN is considered an off-label treatment, meaning it hasn’t been approved by the FDA for autoimmune illness. Because of this, it’s not available in low doses from regular commercial pharmacies. Instead, it must be formulated at a compounding pharmacy. 

If you’re interested in trying LDN for your autoimmune condition, be sure to consult your doctor first so your dose can be carefully monitored. If you’re searching for a doctor familiar with LDN use, the LDN Research Trust has a searchable feature on its website to locate a prescribing physician. 

Side Effects of Low-Dose Naltrexone

Studies suggest that the side effects of LDN are relatively rare and mild. Some patients report more vivid dreams or difficulty sleeping, particularly when first starting LDN. This is likely related to the increase in endorphins. 

Some patients with multiple sclerosis have reported an increase in muscle spasms when beginning treatment with LDN. If any side effects are observed, it may be helpful to lower the dose temporarily and then slowly work back up.(8)

How Long Does It Take Low-Dose Naltrexone to Work?

LDN does not work immediately. For most conditions, it seems to “kick in” within the first month of use. Most benefits are seen within 6 months and full benefits should be seen within 9-12 months.(9) 

What Have You Got to Lose?

If you’ve been struggling with an autoimmune or inflammatory condition, talk to your doctor today about giving LDN a try. With a great safety profile, low cost, and potential for big improvements – what have you got to lose – except your chronic pain? 

ALWAYS consult your physician before starting any supplements or drugs.

*These statements have not been evaluated by the Food and Drug Administration. The information in this article is not intended to replace any recommendations or relationship with your physician. Please review references cited at the end of the article for scientific support of any claims made.

Reference:

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3114837/ 

2. https://ldnresearchtrust.org/what-is-low-dose-naltrexone-ldn

3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3104618/

4. https://ldnresearchtrust.org/what-is-low-dose-naltrexone-ldn

5. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3962576/

6. https://pubmed.ncbi.nlm.nih.gov/24526250/

7. https://pubmed.ncbi.nlm.nih.gov/29377216/

8. https://ldnresearchtrust.org/how-naltrexone-works

9. https://ldnresearchtrust.org/content/low-dose-naltrexone-and-chronic-pain-pradeep-chopra-md