Low-dose naltrexone (LDN) is an off-label pharmaceutical that has been used with great success by many doctors for a myriad of health concerns. LDN is unique in the fact that, unlike many drugs, it actually has a restorative effect on the body. As you will understand after reading this post, LDN allows the immune system to function optimally.

Many clinicians have found LDN to be an effect treatment or adjunct treatment for a wide-range of conditions from autoimmune disease to chronic pain to cancer. Because LDN is incredibly safe and has minimal side effects, it should be a consideration for many struggling with chronic conditions. We think LDN is an important tool for health restoration and should be the focus of further research.  

  

The History of Low-Dose Naltrexone

After WW2, researchers were looking for more comprehensive opioid medications to treat wounded soldiers. By accident, a scientist found a compound-Naltrexone- an opiate antagonist that actually blocks opiate receptors. While they were looking for morphine analogs to treat soldier’s pain, they in fact found the exact opposite! Later, in the 1960’s, naltrexone was synthesized and approved as a medication. In the 1980’s, Naltrexone was used to help patients overcome opioid addiction using a dose of 50-100mg. In the 1990’s it was then used for alcohol addiction. Today, naloxine (Narcan) is used to rapidly reverse opioid overdose as it is an opioid antagonist.

Throughout the 1970’s and 1980’s, Dr. Bihari, a Harvard Medical School Graduate, was the first to use naltrexone in lower doses. He found that his HIV-infected patient population had less than 20% of the normal levels of endorphins and that these low levels of endorphins contributed to a weakened immune system. Dr. Bihari sought to find a drug that would raise endorphins in his sick patients and found that a few milligrams of naltrexone to be an effective treatment for HIV patients. Since Dr. Bihari’s initial findings and success with using naltrexone at lower doses, many clinicians have been using it for diseases that involve the immune system as LDN has a restorative effect on immune function.

 

How Does Low-Dose Naltrexone Work Within the Body?

Researchers at The Pennsylvania State University College of Medicine, Hershey, Pennsylvania have discovered the mechanism the makes LDN a powerful therapeutic agent. LDN exerts a profound inhibitory effect on cell proliferation. It is believed that the brief opioid receptor blockade by LDN provokes a compensatory elevation in endogenous opioids and opioid receptors that can function after LDN is no longer available.  

As we discussed earlier, Naltrexone is an opioid antagonist, meaning it blocks opiate/endorphin receptors within the body. Used low doses and compounded in a clean way, naltrexone can have a profound impact on physiology. Research shows that briefly blocking the opioid receptors in the central nervous system can cause a “rebound effect” and increase the body’s ability to create its own endogenous opioids including beta-endorphin and met-enkephalin, as well as increased expression of opioid receptors. This in turn increases the body’s own immune function. 

When LDN is taken at bedtime, opioid receptors are blocked for a short time during the night, usually between 2 and 4 am. As a result of this temporary opiate blockade, the body thinks it needs more opioids and produces more. At this point, LDN is out of the system and receptors are free to receive the opioids. This is where a major therapeutic action of LDN occurs by increasing the body’s endogenous opioid production.

In addition to LDN’s ability to increase endogenous opioids and immune function, it also reduces inflammation within the central nervous system by suppressing microglial activity. Microglia are the primary immune cells in the central nervous system and initiate an inflammatory response to injury or pathogens. When microglia become activated, they secrete pro-inflammatory cytokines, prostaglandins, nitric oxide, and excitatory amino acids. The activation of microglia and subsequent inflammatory response can initiate various symptoms such as fatigue, pain, sleep problems, mood disturbances, reduced cognitive function, and general malaise. LDN suppresses microglial activation because of its effect on toll-like receptor 4 (TLR4) which are found on microglia.

 

What Conditions Can LDN Help With?

 As stated earlier, LDN has been used to treat or as an adjunct treatment for a myriad of health conditions with outstanding results. For a full list, please visit LDN Research Trust.

 

Chronic pain

Chronic Fatigue Syndrome (CFS)

Fibromyalgia

Hashimoto’s thyroiditis

Grave’s disease

Addison’s disease

Cushing’s syndrome

Diabetes mellitus type 1

Celiac disease

Crohn’s disease

Small Intestinal Bacterial Overgrowth (SIBO)

Ulcerative colitis 

Epstein Barr Virus

Mast Cell Activation Syndrome (MCAS)

PANDAS/PANS

Lyme disease

Cancer, many kinds

Ankylosing spondylitis (ALS)

Parkinson’s disease

Autism

Rheumatoid arthritis

Multiple Sclerosis (MS)

Lupus

Scleroderma

Anxiety

Depression

Post Traumatic Stress Disorder (PTSD)

Endometriosis

Infertility

Premenstrual syndrome (PMS)

Polycystic Ovary Syndrome (PCOS)

Vulvodynia

Interstitial cystitis

Ehler’s Danlos Syndrome

Raynaud phenomenon 

Alopecia

Sleep disorders

Eczema

Psoriasis

Lichen sclerosis

Meniere’s disease

Vitiligo

Restless Leg Syndrome

Traumatic Brain Injury

Transitioning off of opiate pain medications

 

Are There Any Downsides to LDN?

LDN is usually very well tolerated by patients. However some people can experience headaches, insomnia, or unusually vivid dreams when first starting this treatment. Additionally, some patients may experience a brief exasperation of their symptoms as their immune system adapts to the medication. These side effects are minor and often go away after a few days or weeks of starting this medication and can be mitigated by starting LDN at lower doses.

There is no standard dose for LDN, so it usually takes some additional discussion between the patient and doctor as well as adjusting doses to find what is most effective. Usually the best dose is between 1.5-4.5 milligrams a day. Usually we start patients at 1.5 milligrams and gradually increase to 4.5 milligrams and monitor symptoms with each increase. It is important to note that patients with thyroid conditions may experience a change in their thyroid function and their thyroid medications and supplements are suddenly too much. This is because LDN has the ability to improve thyroid function. 

Based on research and anecdotal evidence, LDN is an effective treatment for about 70- 80% of patients dealing with chronic illness. While LDN has proven to be a useful therapy for many, it is not a sure fire fix for everyone. Nevertheless, it is definitely worth considering. 

 

Next Steps

 If you find yourself with chronic symptoms and think that LDN might be helpful for you, please reach out to our office and schedule an appointment with our MD, Dr. Mike to discuss whether or not this medication would be a good fit!

 

 

Sources

https://ldnresearchtrust.org

https://journals.sagepub.com/doi/full/10.1258/ebm.2011.011f08

http://www.gidoctor.net/client_files/file/Naltrexone-Side-Effects-and-Efficacy-in-GI-Disorders.pdf

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

https://onlinelibrary.wiley.com/doi/full/10.1002/art.37734

https://link.springer.com/article/10.1007%2Fs10067-014-2517-2

https://www.cochranelibrary.com/cdsr/doi/10.1002/14651858.CD010410.pub2/full

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3586944/

https://link.springer.com/article/10.1007/s11481-013-9451-y