Low Dose Naltrexone

Naltrexone was discovered in 1963 by Endo Laboratories and FDA approved the 50 mg tablet for the treatment of additions to opioids in 1984 and alcohol use disorder in 1994. 

Naltrexone is a medication that helps to manage alcohol and opioid addiction by preventing the “high” caused by these substances.  However, providers also use low-dose naltrexone (LDN) to treat a variety of conditions, including multiple sclerosis.  

Low Dose Naltrexone (LDN) was developed in 1985 by Dr. Bernard Bihari, a Doctor of Internal Medicine, Psychiatry and Neurology.  During the AIDS epidemic Dr. Bihari changed his research interest from addictions to AIDS after he discovered that AIDS patients had only 20% of the normal endorphin levels.  His pivotal discovery was that 1% of the typical dose of Naltrexone caused a 300% increase in endorphins. 

Endorphin comes from the words “endogenous,” which means within the body, and “morphine,” an opiate pain reliever.  This means that endorphins are the body’s natural pain relievers.  Endorphins are also the body’s natural “feel-good” chemicals because they lift our mood and put us in a positive state of mind.  So, in essence, Dr. Bihari discovered that LDN is able to modulate the immune system and brain neurochemistry to produce positive effects and lift mood.  

How Low Dose Naltrexone Works

High dose Naltrexone blocks opioid receptors completely, so if someone had a craving for and illicit drug, it would not work as naltrexone blocks the receptors. However, when naltrexone is given as low dose, it temporarily blocks some of the opioid receptors and thereby stimulates the body’s production of endorphins.  

Another benefit of LDN is that it disrupts the body’s signaling so that less inflammatory cytokines are produced (TNF-alpha, IF-beta).  These inflammatory cytokines are those signal messengers we all produce, but hopefully in small levels.  Inflammatory cytokines could be made from eating a processed food, a stressful argument, poor night’s sleep, and any number of the daily toxins/stressors we face. 

Then, when a virus comes along your body is already taxed and doesn’t have the reserves to ward off the virus for example.  So LDN produces and anti-inflammatory response without decreasing your body’s innate immune response. Not turning everything off, your body is still able to fight and use other aspects of your immune system for other challenges such as warding off bacteria and viruses.  

Low Dose Naltrexone Dosage

LDN is taken in doses that are about a tenth of the size of a traditional dose, usually less than 5 milligrams (mg) per day.  The dose is typically started 1.5 mg by mouth at bedtime for 7 days, then 2 capsules (3mg) at bedtime for 7 days, then 3 capsules (4.5 mg) at bedtime thereafter.  

Everyone has an individual response to the dosing and finding the appropriate dose is truly individualized medicine.   For certain specific conditions the dosing and response will vary. 

As was mentioned it releases hormones called endorphins over an extended period of time.  Endorphins help to reduce inflammation, the root cause of diseases and disorders.  As a result, LDN has shown beneficial use in many conditions and has been shown to ameliorate and modify the course of various diseases including: 

• Multiple Sclerosis
• Insomnia
• Polycystic Ovarian Syndrome 
• Hashimoto’s Thyroiditis
• Ulcerative Colitis
• Crohn’s Disease
• Fibromyalgia
• Rheumatoid Arthritis
• Cancer
• Psoriasis
• Lupus
• Osteoarthritis
• Eczema
• Chronic Pain 
• Mental Health and Mood Disorders 

LDN has shown encouraging promise as a potential treatment for Multiple Sclerosis symptoms with relatively few side effects compared to other treatments. However, experts are still trying to figure out exactly how it affects Multiple Sclerosis symptoms. 

LDN has a reputation for helping desperate patients, even when many other treatments have failed.  In order to increase the efficacy of LDN treatment it is important to consider nutritional factors that may influence your body’s response to LDN. 

For example, several LDN prescribers report that their patients see better results from LDN when they correct deficiencies in vitamin D.  While there is some debate about what serum levels of vitamin D are “normal” versus “optimal”, there is increasing evidence that levels between 40-60ng/mL are associated with more health benefits than the previous goal of >30ng/mL. 

Side Effects of LDN may include: 

• Anxiety
• Dizziness
• Vivid Dreams and insomnia 
• Nausea
• Headache

Conducted clinical trials indicate that most side-effects resolve on their own with ongoing therapy and that LDN is well tolerated according to present studies in humans. 

Contraindications for LDN would be anyone who is legitimately being treated for pain with opioids. 

You should not take LDN if you: 

• Take opioid pain medications
• Are in an opioid maintenance program
• Are in acute opiate withdrawal
• Have liver problems 

Research is ongoing and showing increasing promise for the effectiveness of LDN in treating and reduce the symptomatology of various health challenges and enhance the quality of life. 

Based on the current state of research and reports on the numerous benefits and excellent safety profile, the clinical use of LDN will most likely be increasingly seen as a positive novel treatment modality for a variety of health conditions. 

RESOURCES:

• Conditions Where Low Dose Naltrexone (LDN) Could be of Benefit
• Low-Dose Naltrexone (LDN)-Review of Therapeutic Utilization
• Preclinical and clinical studies into the bioactivity of low-dose naltrexone (LDN) for oncotherapy
• Low Dose Naltrexone: The Potential Benefit Effects for its Use in Patients with Cancer
• Low-dose naltrexone therapy improves active Crohn’s disease
• A pilot trial of low-dose naltrexone in primary progressive multiple sclerosis
• Low Dose Naltrexone for Chronic Pain: Update and Systemic Review
• The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain