Low-Dose Naltrexone is a prescription drug that is gaining traction for the treatment of chronic, difficult-to-manage illnesses, like cancer and autoimmune disease. With little to no side effects, clinicians are increasingly looking at it as a valuable treatment for patients suffering from several conditions.
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LDN Brief History
Naltrexone was approved by the FDA in 1994 for the treatment of opiate addiction. In high doses, between 50-100mg, naltrexone functions as an opiate antagonist, completely blocking the opioid receptors in the brain, and preventing patients from experiencing a high from the use of opioids.
After approving the drug for the treatment of opiate abuse, an HIV/AIDS researcher named Dr. Bernhard Bihari discovered that in much lower doses, about 3mg as opposed to 50-100mg, low-dose naltrexone has an immunomodulatory effect. Realizing the potential application of this drug in the treatment of many challenging conditions, patients and practitioners began advocating for more research and attention to be given to low-dose naltrexone (LDN). (1)
How Does LDN Work?
Though the research has been slow to happen, the results have been very positive. From the results of research studies, it appears that LDN functions through several different mechanisms and that the primary mechanism may differ depending on the disease that is being treated. Up till now, the research has found two primary mechanisms - 1) that LDN acts as an opioid antagonist, and 2) it acts as a potent anti-inflammatory. (1)
Elevated Natural Opioid Activity
Low-dose naltrexone, like high-dose, blocks opioid receptors in the brain. Unlike high-dose naltrexone, LDN is cleared from the body within a few hours. Researchers believe that this causes a rebound effect, that increases the body’s natural opioids, beta-endorphin, and met-enkephalin. (2) Endogenous opioids, those made naturally by the body, are known to relieve pain and stress, which could result in the alleviation of many symptoms.
In addition to providing a natural analgesic effect, research has shown that opioids play a significant role in immunomodulation, but the specifics appear to be complicated. Different opioids are immunosuppressive, immunostimulatory, or both. The exact effects of endogenous opioids on the immune system are still unknown, and both increases in immune cell activity and decreases in tumor activity have been seen in response to LDN. (3)
Recent studies have shown that LDN binds to both opioid receptors in or on cells of the immune system and tumor cells directly, creating immunoregulatory activity. (4) With the immune system playing a critical role in everything from inflammation, tumor growth, and metastasis, unpacking the specific role of opioids within the immune system is an important area of research that needs broader and wider investigation.
Decreased Inflammation of the Central Nervous System
The second mechanism of action that is independent of opiate antagonism is the suppression of microglial activity. A primary immune cell of the central nervous system (CNS), microglia create inflammation in response to injury and pathogens. Once activated, these cells produce pro-inflammatory cytokines, prostaglandins, and other factors that increase inflammation. (1)
While these are all crucial for the protection of the body in the short term, if the inflammation continues in a maladaptive way, this process contributes to a wide range of cancers and autoimmune diseases.
The research on LDN suggests that it can suppress this microglial activation, likely due to its antagonistic effect on a non-opioid receptor found in microglia known as toll-like receptor 4, or TLR4. (4) This then decreases the release of proinflammatory cytokines, including tumor necrosis factor, interleukin-6, and interleukin-12. (5) This down-regulation of the inflammatory response has been showing promising treatment in many different chronic pain conditions and autoimmune conditions, including:
- Dermatologic or skin conditions, including lichen sclerosus, lichen planopilaris, and psoriasis (5)
- Chronic pain conditions, including fibromyalgia and complex-regional pain syndrome
- Autoimmune conditions, including Crohn’s disease and rheumatoid arthritis
- Neurodegenerative conditions, including multiple sclerosis (6)
LDN in the Treatment of Cancer
While there are currently no published results from controlled clinical trials on LDN concerning cancer treatment, the published clinical observation, case studies, and lab and animal studies do show promising results.
Cancer research involves a lot more than simply searching for a cure, researchers also look to reduce the growth and spread of cancer to improve longevity markers and survival times. Research also looks to see if any treatments improve the anticancer action of other known treatments, or provide any therapeutic benefit to cancer patients overall. (7)
What is available in terms of the literature shows that LDN does have significant potential to increase disease-free status, overall survival rates, and quality of life.
Bernard Bihari, the original pioneer of LDN, continued to use LDN to treat AIDS and cancer patients. As of 2014, he has reported using LDN in 450 cancer patients and reported that 24 percent of patients showed significant tumor shrinkage of at least 75 percent reduction and that 35 percent were stabilized and moving towards remission. (7)
His research included patients with a wide variety of primary cancers, including breast, colon, liver, and lung cancer. Anecdotal evidence has shown that even more types of cancers have responded positively to LDN treatment, including colorectal, lymphomas, neuroblastomas, ovarian, pancreatic, and prostate cancers, among many others.
How Can You Get Your Hands on LDN?
That’s a great question! LDN does require a prescription from a doctor. Since it is an older drug, it is quite inexpensive, but it is not currently manufactured in low-dose form, and using LDN in low-doses is still considered off-label use. Because of this, it may be difficult to get a conventional doctor to prescribe LDN and you may need to seek out a functional medicine or naturopathic doctor for a script. LDN should be made by a compounding pharmacist. Using a professional compounder yields the best quality product and should yield better results. Though you can find online sources to purchase from, they are often created illegally and offer substandard quality. (7)
If you believe that you have a condition that would benefit from the use of LDN, don’t hesitate to talk to your physician or specialist about your interest. Because its labeled use is for the treatment of opiate addiction, it often doesn’t come up on many doctor’s radars. This doesn’t necessarily mean that they would be opposed to it as a treatment option, but rather that they are not informed or aware of its potential benefit.
The Future of LDN Looks Bright
As the research expands and the positive results continue, more research is beginning and LDN is now being registered for clinical trials, including those for metastatic melanoma, hormone-refractory metastatic breast cancer, and gliomas. (8) Researchers are also interested in very low-dose naltrexone and ultra-low-dose naltrexone, which is showing that naltrexone can potentiate other drugs and improve their efficacy and results. (6)
Since the research is showing a lot of positive results and LDN appears to hold therapeutic applications for a large number of diseases and syndromes, along with the fact that it is an inexpensive drug that is well tolerated by most people, its use will likely become more widespread and more benefits and specific mechanisms will be uncovered through further scientific investigation.
Low-Dose Naltrexone FAQs
There are few if any side effects of low-dose naltrexone. The most noted is vivid dreams.
Low-dose naltrexone has very few side-effects and is showing positive effects in treating autoimune disease, cancer, and chronic pain.
The standard dosage of low-dose naltrexone ranges from 1-4mg and larger doses are now being recommended by physicians.
Low-dose naltrexone is available by prescription only and prepared at a compounding pharmacy. You can find online sources to purchase from, they are often created illegally and offer substandard quality
Struggling with autoimmunity or chronic illness? Check out these success stories from clients who addressed the root-cause contributors of their autoimmune disease and are now thriving!
Sources
- Kresser Institute. Low-Dose Naltrexone: A Promising Drug for Hard-to-Treat Conditions. [Internet]. [cited 12th December 2019]. Available from: https://kresserinstitute.com/low-dose-naltrexone-promising-drug-hard-treat-conditions/
- Brown N, Panksepp J. Low-dose naltrexone for disease prevention and quality of life. Med Hypotheses. 2009 Mar;72(3):333-7.
- Liang X, Liu R, Chen C, Ji F, Li T. Opioid System Modulates the Immune Function: A Review. Transl Perioper Pain Med. 2016; 1(1):5–13.
- Li Z, You Y, Griffin N, Feng J, Shan F. Low-dose naltrexone (LDN): A promising treatment in immune-related diseases and cancer therapy. Int Immunopharmacol. 2018 Aug;61:178-184.
- Sikora M, Rakowska A, Olszewska M, Rudnicka L. The Use of Naltrexone in Dermatology. Current Evidence and Future Directions. Curr Drug Targets. 2019;20(10):1058-1067.
- Toljan K, Vrooman B. Low-Dose Naltrexone (LDN)-Review of Therapeutic Utilization. Med Sci (Basel). 2018 Sep 21;6(4).
- Beyond Conventional Cancer Therapies. Low-Dose Naltrexone. [Internet] [cited 12th December 2019]. Available from: https://bcct.ngo/search-therapies/search-therapy-summaries/low-dose-naltrexone
- CADTH: Canadian Agency for Drugs and Technologies in Health. CADTH Rapid Response Report: Summary Of Abstracts. Low Dose Naltrexone for the Treatment of Any Cancer Type: Clinical Effectiveness and Guidelines. [Internet]. [cited 12th December 2019]. Available from: https://www.cadth.ca/sites/default/files/pdf/htis/2019/RB1295%20Low%20Dose%20Naltrexone%20for%20Cancer%20Final.pdf
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