Low Dose Naltrexone

Thankfully, science is evolving and a new, promising therapy for a drug called Naltrexone that is already on the market may show positive effects in those with autoimmune conditions and chronic pain.

Have you heard of Naltrexone or Low Dose Naltrexone and its use for autoimmune conditions?

Keep reading to find out more.

What Is Naltrexone?

Naltrexone can be prescribed in pill form for the treatment of alcohol use disorder and opioid use disorder and it is taken one time per day. (Source)

The pill has a brand name called ReVia.

The dosing for oral naltrexone depends on what is being treated, opioid or alcohol addiction, though it is sold in 50mg tablets.

It can also be prescribed as an intramuscular injectable to treat opioid use disorder.

A healthcare provider gives the intramuscular injection one time per month. The dosing is typically 380mg monthly.

Naltrexone was developed in 1963 and approved by the Food and Drug Administration (FDA) for opioid use disorder in 1984, and then later on approved for alcohol use disorder in 1994. (Source)

It does not “cure” alcohol or opioid use disorder, but it is used in combination with treatment programs to assist in cessation.

The pill and intramuscular injection must be started after active withdrawal from alcohol or opioids, about 7-14 days after.

A healthcare provider will determine if/when it is appropriate to start safely.

Naltrexone Mechanism Of Action

How does naltrexone assist in the treatment of alcohol and opioid addiction?

First of all, naltrexone is not an opioid or a narcotic medication.

It is not an addictive medication. It is an opioid antagonist, meaning it blocks the effects of opioids.

Naltrexone binds to opioid receptors and helps reduce cravings.

It prevents the “high,” euphoric feeling from narcotics and opioids.

Oral naltrexone is absorbed in the gastrointestinal tract and metabolized in the liver.

What Is Low Dose Naltrexone (LDN)?

Sometimes, medications are used as an “off label” meaning it has other uses in addition to what it was originally prescribed for.

That is exactly what we are seeing with Naltrexone, but given in a lower dose.

Low dose naltrexone is being explored for a variety of autoimmune conditions such as Crohn's disease, fibromyalgia, lupus, and chronic fatigue syndrome.

The dosing for low dose naltrexone is a lot lower than that of naltrexone for the treatment of alcohol and opioid use disorders which was 50mg.

One website discusses that dosing starts at 0.5-1 mg at night time, then could reach up to a max dose of 4-4.5mg nightly. (Source)

In addition, you may also be prescribed 1mg in the morning, and increase every 30 days until you reach 4mg.

My Story And Why This Is Important To Me

As you may know, I was diagnosed with Chronic Fatigue Syndrome (CFS) over 25 years ago.

If you haven’t read my story, I was a triathlete, loved training cycling, biking, and swimming, then began to feel fatigued, spaced out, and knew something was not right during my workouts.

I needed to rest for 10-12 hours per day.

I was constantly sick, and my GP provided me antibiotics to take 3-4 times in a year which provided no avail.

I also found out I had glandular fever, eventually got my tonsils removed, and started to feel better from there.

Getting my tonsils removed along with creating and drinking my Supergreen Tonik daily, I feel confident that now I am receiving adequate nutrients and adaptogens and spending fewer days feeling sick and fewer days battling with my CFS.

I have also been self-employed for most of my adult life, and the flexibility to work anywhere has made a huge positive impact as well.

Since there is a large lack of awareness and treatment for CFS, I am overjoyed with the idea that people who have been in a similar situation to me will no longer have to suffer and can be treated timely and appropriately.

That’s why the idea of LDN excites me so much!

I hope this drug, and more, can continue to be studied and provided to those with an overactive immune system and autoimmune conditions.

LDN Mechanism Of Action

Low dose naltrexone mechanism of action is similar to that above in the fact that it blocks opioid receptors in the brain.

Those with autoimmune conditions often have low levels of opioids, and by blocking the receptors, the body thinks more opioids are needed and therefore will be produced naturally. (Source)

Additionally, microglia are central nervous system immune cells that produce inflammation, pain symptoms, and fatigue which are also blocked by the opioid receptor.

LDN modulates this.

Chronic pain and chronic inflammation occur when these are inflamed constantly.

LDN Benefits For Autoimmune Conditions

LDN is not currently FDA-approved for the treatment of autoimmune conditions, but it has been used off-label.

Studies have shown the benefits of LDN on the immune system.

There are over 100 autoimmune conditions that affect 50 million Americans. That means 1 in 5 Americans are affected and live with an autoimmune disease daily. Twenty percent seem to occur in families, meaning a genetic or inherited factor is present. (Source)

One study with 34 Crohn's Disease patients provided 4.5mg of LDN over 12 weeks compared to a placebo. Thirty percent of those in the LDN group achieved remission over the 12 weeks while 18% in the placebo group received remission. (Source)

Crohn’s disease is an inflammatory disease of the GI tract, one of the two inflammatory bowel diseases, the other being ulcerative colitis.

Crohn's can affect any part of the GI tract.

Though the study discussed that it was not a statistically significant finding, it still warrants ongoing studies to assess efficacy.

They did have a statistically significant finding in such that 83% of patients in the LDN group had a 70-point clinical response while only 38% of placebo patients did.

A 70-point clinical response is the reduction of Crohn's Disease activity 70 points from baseline.

A systematic review showed that treatment with LDN had a positive association with chronic pain and sleep disturbances. (Source)

Fibromyalgia is chronic muscle pain and tenderness often coupled with fatigue and mood dysregulation.

LDN at 4.5g doses was given to 31 women in a double-blind randomized control trial. (Source)

Nearly 29% of these women in the LDN reported a reduction in baseline pain, while only 18% of those in the placebo group reported a decrease in pain.

This was a significant reduction in pain.

There was no effect between groups regarding fatigue or sleep, though there was a correlation in the LDN group that reported improved mood.

There was a pediatric case report on an 11-year-old boy with chronic regional pain syndrome, and after dosing with LDN pain severity was reduced by 70%. (Source)

He was able to stop two other medications – gabapentin and amitriptyline, which may cause unwanted side effects.

There is a clinical trial for LDN and chronic fatigue syndrome post-COVID infection, not yet recruiting.

One review notes that up to 46% of those who were diagnosed with COVID-19 suffer from long-term fatigue lasting from weeks to months.

Side Effects Or Caution?

The side effects of naltrexone for opioid and alcohol use disorder seem to be greater than that of LDN.

Some of the reported side effects of regular 50mg doses of naltrexone are headache, nausea, vomiting, abdominal pain, anxiety, dizziness, increased thirst, irritability, or fast heartbeat. (Source)

Very rarely it could cause liver problems.

Difficulty sleeping is one of the most reported side effects of LDN. (Source)

Intense dreams were another one, and very rarely, weight loss.

Low dose naltrexone side effects are minimal, around 8%, which is favorable for those wanting to try LDN for an autoimmune condition.

Debilitating the side effects of a medication when already struggling day to day is very undesirable, which is another reason why LDN appears so promising.

You should always speak with your healthcare provider before starting a new medication.

Since naltrexone can only be prescribed by a healthcare provider, you will be able to have that conversation right off the top.

LDN And Weight Loss

There is a medication on the market called Contrave, which contains 8mg of Naltrexone and 90mg of another medication called Bupripiron. (Source)

It is a prescription weight loss medication for those struggling with obesity, or individuals that are overweight and also have a medical condition such as diabetes or high blood pressure.

This dose is a bit higher, about double the dose we would see in someone using LDN for an autoimmune condition.

It is thought to target areas of the brain that regulate feelings of pleasure that help control cravings and curb hunger.

Along with behavioral modification, a study from their website showed 80% of participants taking Contrave had a >5% body weight reduction over the study period.

It doesn't seem to be known if LDN at 4.5mg or lower also has weight loss and appetite-curbing effects.

This medication does come with a few side effects, so it is important to talk with your doctor if this is something that you feel may work for you.

Someone with CFS like me or other autoimmune conditions might find it difficult to lose weight due to tiredness, poor sleep, decreased mood, or functional ability.

There are other ways to lose weight with CFS, that avoid medication.

Some of those discussed in my article are managing your diet, and cutting out alcohol and sweets.

Other Ways To Help The Immune System

Some other ways to help out the immune system and decrease inflammation, in general, is to monitor our diet.

Diet is one of the biggest modifiable factors we can control daily.

Diets, more so ways of eating or lifestyle habits, such as the Mediterranean diet and the DASH (dietary approaches to stop hypertension) diet focus on including fruits, vegetables, high fiber whole grains, mono and polyunsaturated fats, and legumes in the diet.

It focuses less on calories, and more on the quality of the food.

Foods to limit would be surgery foods like sodas, sweets, an excess of refined carbohydrates like white bread, fried foods, processed meats, and those high in saturated fats like bacon, as well as large amounts of full-fat dairy products.

There is an association with an increased risk of colon cancer in those who consume higher amounts of inflammatory foods, or foods to limit.

There are also greens powders that can help with the immune system as well.

There is an immune blend in my Super Green Tonik that provides dandelion leaf extract (500mg), Garlic Extract (250mg), Olive leaf extract (250mg).

Dandelion leaf and flower extract are thought to help the immune system and decrease inflammation in the body. (Source)

Lastly, Vitamin D has been one of the more studied vitamins in relation to autoimmunity.

A meta-analysis looked at Vitamin D intake and rheumatoid arthritis incidence, and those with a higher vitamin D intake had a 24% less likely chance of developing rheumatoid arthritis than those in the lower intake group. (Source)

Low Dose Naltrexone: Conclusion

As I have mentioned before, finding management for autoimmune conditions is near and dear to my heart and is a passion of mine.

50 million other Americans and I remain hopeful that medications like LDN will continue to be studied and eventually approved for autoimmune diseases.

We can continue to hope that more healthcare providers will be able to recognize and promptly treat these conditions.

The research is small, though promising, with manageable side effects among adults and pediatric patients.

For more information on LDN and to keep up with the ongoing research being conducted, check out the LDN Science and LDN ResearchTrust websites. (Source) (Source)