What is LDN?
I often smile when I mention that I take Low Dose Naltrexone to conventional medicine doctors. They look at me very puzzled and they tell me that Naltrexone was developed to help people with opioid addiction and in slightly smaller dosages for people with alcohol addiction. Neither of which is even close to what I take it for. I smile because I'm happy that I've seen the benefits for myself, while knowing that unfortunately, they have not taken the time to read the large amount of literature available to learn about the many ways LDN can significantly benefit their patients.
I've been taking 3mg of Naltrexone every night for the past 2 and a half years. I have to get it from a compounding pharmacy and it unfortunately is not covered under my drug plan. My functional medicine doctor said it would benefit me because of the autoimmune conditions that I live with, but I had no idea it would help me so much with my joint pain and I've never slept better in my life! Since starting LDN, my Neuroendocrine tumors have stayed relatively the same, not increasing in size. The only contraindication is that you should not take LDN if you are planning on taking opioids or drinking heavily, the latter would make you feel ill and the former would render the opioids useless. So for example, I went off my LDN about a week before my trip to NIH just in case I needed to undergo a procedure like an endoscopy that might use opioids to sedate me. During the time off the LDN, I felt pretty run down, tired, sore and stressed out. I didn't really realize how much of a difference the LDN was making in my day to day life until that point. Now knowing what I do about it, I have no plans to go off of it!
Naltrexone: Naltrexone is a licensed, unpatented drug with no to minimal side effects, that blocks opioid receptors. Opioid receptors are located in various cells in the nervous system in the body and in the brain and are what endorphins bind to, mainly to inhibit the communication of pain signals.
Endorphins: Endorphins are endogenous opioid peptides that are created and stored in the pituitary gland and are often released during fight or flight situations. When they bind to the human opioid receptors, pain and fear are diminished, and there is also a boost to the immune system. (In fact, endorphins help regulate the immune system and that is one of the key components in the research and application of low dose naltrexone). This mechanism is also where feelings of euphoria come from such as runners high. This is the same feeling that heroin users seek. Blocking the receptors with the high 50mg-300mg dose that Naltrexone was developed for, means that those receptors are blocked all the time so that people with opioid addictions don't get the pleasure of the high.
History: A New York Neurologist and Psychiatrist named Dr. Bernard Bihari had an idea many years ago to try Naltrexone in small doses for AIDS patients and noticed that in small doses between 0.5mg to 4.5mg, the opioid receptors would only be blocked for a few hours at a time and the body would make triple the amount of endorphins [1] during that time - and they would remain elevated throughout the whole rest of the day. This has a profound affect on the immune system. He was able to do a placebo controlled trial with AIDS patients and the ones on LDN had significantly fewer deaths, fewer co-infections and noticed that the helper T cells dropped less in those patients [2].
They also found that AIDS patients have significantly lower endorphin levels, (as do patients with MS and cancer patients.)
Autoimmune Application:
LDN has also been found to bind to the TLR receptors [3], which are the first in an immune cascade and the thought is that it can also help to suppress or down-regulate the overreaction that might otherwise cause an autoimmune flare up. T helper cells are impaired in autoimmune conditions and immune system cells are unable to recognize the cells that start to attack the self. LDN can help prevent further attacks by enhancing the function of the T cells and stopping the other cells from attacking the body. There are a wide array of autoimmune conditions that have shown significant improvement with the use of LDN and there have been many studies to prove this. All one has to do is search for them. There's a couple of really amazing documentaries about the benefits of LDN for patients with Fibromyalgia and Autism on YouTube called "The LDN Story" [4] that's worth checking out. And another about MS, cancer & fibromyalgia called "Norwegian LDN Documentary, with english subtitles. [5]
Cancer Application: Mice injected with human lymphoma cells were also given B endorphin cells that bind to the endorphin receptor sites in the cancer cells, and the results were quite profound in slowing the growth of the tumor cells, promoting remission or preventing the lymphoma cells to take. [1] There have been many different animal studies since then showing similar results with all different cancers and researchers have prophesied that all cancer cells have endorphin/opioid receptors. Further studies to determine if cancer cells have these receptors (or if it was the immune system boost that was causing these dramatic effects) were done by growing colon cancer and pancreatic cancer cells in petri dishes and adding endorphins to the mix. Researchers observed programmed cancer cell death when they added endorphins, thus concluding that cancer cells do indeed have these endorphin/opioid receptor sites. Chemotherapy also has programmed cancer cell death in the nucleus of the cell, but unfortunately healthy cells are also killed with chemotherapy which is why the side effects are so great in chemotherapy. Cells that grow and divide quickly, such as hair and nail cells are damaged and hair falls out and nails stop growing. This is not the case with LDN because endorphins are naturally occurring in the body.
As I mentioned previously, cancer patients have lower endorphin levels which has a two fold effect on a person's ability to fight cancer, the first being that the endorphins are not available to directly kill the cancer cells as described above but also, lower endorphins means lowered immune system response.
There have been numerous studies [6,7,8,9] done on the effect of LDN on different types of cancer and I believe it is something that every patient with cancer or autoimmune conditions or chronic pain would benefit from!
Frustrations with acquiring LDN:
It takes millions of not billions of dollars to do these clinical trials to test it but because the patent expired many years ago, there is no one that is able to sell the drug exclusively to make a profit. There needs to be a drug company that would need to put up the money to do the trials and would not make the money back. This is why the pharmaceutical industry has opted out of promoting LDN for all of these amazing benefits!
It's very frustrating because most doctors will not formally prescribe Naltrexone in low doses for off label use, even when they actually do the research, they don't seem comfortable with prescribing it and this is also very frustrating for people who have been trying to get better by using LDN.
If you think that LDN might be something that you would like to try, talk to your doctor about it. If you become as frustrated as I did with trying to convince your conventional medicine doctor that it would be a good thing to try, it is possible that a functional medicine doctor would be able to prescribe it for you, otherwise you may have to use the resources I've provided [9,10,11] to try to educate your doctor about it.
Exciting developments:
I have recently discovered that there is a company named Cytocom, which is a subsidiary to Immune Therapeutics, Inc and is a "clinical-stage biopharmaceutical company developing its proprietary version of lower-dose naltrexone, Lodonal, as a standalone and conjunctive therapy in patients with a wide variety of conditions including HIV/AIDS, autoimmune diseases, cancer, neurodegenerative conditions and other inflammatory conditions."
This company is also re-purposing a drug called MENK that works similarly to LDN (but not exactly the same) and is showing promise for treatment of cancers such as pancreatic cancer!!! [12].
Thank you for taking the time to read this blog post and I hope I have shed some light on this underutilized medication and possibly given you some hope that there are things out there that might improve your quality of life!
List of references:
[1] Interview with Dr. Bernard Bihari: https://youtu.be/rll1A3aFhjc
[2] Bihari, B., et al., Low Dose Naltrexone in the Treatment of Acquired Immune Deficiency Syndrome, Oral Presentation at the IV International AIDS Conference in Stockholm, Jun 1988. https://scholar.google.ca/scholar?cluster=8336665520820912673&hl=en&as_sdt=0,5#d=gs_qabs&u=%23p%3DowxJhxJwuS8J
[3] Rachel Cant, Angus G. Dalgleish, and Rachel L. Allen, Naltrexone Inhibits IL-6 and TNFα Production in Human Immune Cell Subsets following Stimulation with Ligands for Intracellular Toll-Like Receptors, Institute for Infection and Immunity, St George’s University of London, London, United Kingdom, Published online July 2017. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5504148/
[4] The LDN Story, patient testimonials on fibromyalgia and autism : https://youtu.be/FDCn0JWv6Io
[5] Norwegian LDN Documentary, english subtitles, patient testimonials on MS, Fibromyalgia, cancer and lung infection and the frustration about getting a drug that has no patent.
[6] Alshimaa Aboalsouda et al.,The effect of low-dose naltrexone on solid Ehrlich carcinoma in mice: The role of OGFr, BCL2, and immune response,
Department of Pharmacology, Faculty of Medicine, Tanta University, Tanta, Egypt,
Available online 10 December 2019.
[7] Li Z.,et al, Low-dose naltrexone (LDN): A promising treatment in immune-related diseases and cancer therapy., International Immunopharmacology, August 2018:
[8] Dipak K.Sarkar, et al., Regulation of cancer progression by β-endorphin neuron,Rutgers Endocrine Program, Rutgers, The State University of New Jersey, New Brunswick, NJ 08901,published online Jan 2012
[9] Immune Therapeutics Inc Announces Publication of Peer Reviewed Scientific Paper Describing Low-Dose Naltrexone (LDN): A Promising Treatment in Immune-Related Diseases and Cancer Therapies:
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