In the early 1960’s a compound was developed to treat addicts by blocking opioid receptors on the surface of our cells (mostly brain cells). Naltrexone would block the opioid receptor sites for 24 hours stopping the high from heroin, and the addictive behavior. In 1984 the FDA approved Naltrexone for use in opioid abuse at doses of 50-150 mg per day. In 1994 the FDA approved it for alcohol abuse at a dose of 50 mg, and in 2014 the FDA approved it for use in weight loss when prescribed along with Wellbutrin (an anti-anxiety medication). These applications for Naltrexone would go on to help many suffering from addictive behaviors and this alone would qualify Naltrexone as a monumental drug in the annals of medicine. However, there is more to this story.
Dr. Bernard Bihari, a Harvard educated M.D., was working with Naltrexone and addicts in the mid 1980’s in NYC when he was suddenly inundated with AIDS patients. In an interview filmed 11 years ago, he said that “he knew the immune system was in large part controlled by the opioid system, and having sufficient endorphin levels was essential to stimulate the immune system to help these AIDS patients”. When testing AIDS patients, he found that their endorphins levels were only 30% of what they should be. Knowing that Naltrexone blocked endorphins, Bihari did a study that included fifty patients to find the lowest dose of Naltrexone hoping that it might function as an immune system modulator and increase endorphins. He discovered at a dose as low as 3 mg, he would get the same endorphin release as he would with 50 mg. Even though Low Dose Naltrexone leaves the body within 4-5 hours instead of 24 hours at the higher dose, there is an endorphin rise that lasts for 24 hours. The low dose and short-term blocking of the opioid receptors paradoxically triggers a rebound phenomenon with an overproduction of more endorphins (and enkephalins) than would have been done normally. He conducted a placebo-controlled trial, and the data was clear: those with AIDS taking the low dose Naltrexone (LDN) fared much better than those who took the placebo. In addition, those on LDN had higher levels of T Helper cells which are the cells that are most impacted by HIV infection. He also found taking it at night worked best because our bodies produce about 90% of our endorphins between 2:00-4:00 am.
With regards to cancer, Dr. Bihari knew that there had been studies showing that giving mice endorphins had arrested lymphomas, and that applying endorphins to cancer cells in petri dishes would result in those cancer cells dying by a process called apoptosis. Apoptosis is a term used to describe inducing cell death. Chemotherapy works by apoptosis too. However, chemotherapy is an unnatural chemical that attacks the nucleus and DNA of the cancer cell causing side effects whereas endorphins are a natural chemical to the body and work on the receptor surface of the cancer cell. Cancer patients similarly to AIDS patients have 30% of the endorphin levels of a normal person. Low endorphins also cause low natural killer cells (NK cells) and cytotoxic T cells which have CD8 receptors on them. NK cells rise with increased endorphins. This may explain why cancers are more likely to arise around one year after the death of a spouse or after 1-4 years of chronic stress when endorphins would be especially low.
Knowing that LDN helps with immune issues, some progressive doctors are using it to treat many chronic painful conditions and autoimmune diseases. Asthma, eczema, psoriasis, IBS, Hashimoto’s thyroiditis, rheumatoid arthritis, chronic fatigue syndrome, chronic bacterial infections such as SIBO (small intestine bacterial overgrowth), and hepatitis B and C, allergies, MCAS (mast cell activation syndrome), M.S., ALS, Lupus, Lyme disease and depression are samples of the many problems that have responded to LDN. So far LDN has been used in 174 conditions by starting with 1.5 mg and titrating up by .5-1.0 mg every two weeks up to 4.5 mg for adults. It is occasionally dosed higher than that. Some doctors prescribe it for autism with the application of a creme or drops. Additionally, LDN is used for certain eye conditions in a .1% solution eye drop made in a compounding pharmacy.
Although he has since passed away, during the interview Bihari stated he had taken LDN daily for 10 years to prevent colon cancer and his wife took it for about the same time to prevent breast cancer because both cancers were common in their family history. He said there is no risk to long term use or side effects except for possible sleep disturbances and if that occurs then just lowering the dose helps. It is also best to avoid combining it with certain drugs. He stated that two women were on it for 14 years, one for M.S. and one for metastatic melanoma and both have been in remission for the time they were on it. LDN also blocks the IL-6 cytokine from the Toll Like Receptor (TLR) on cells which is commonly associated with inflammation from infections or injuries. IL-6 increases platelets so blocking IL-6 reduces chances of blood clots. IL-6 also increases acute phase inflammatory proteins in the liver such as C-Reactive Protein, serum amyloid, hepcidin and fibrinogen.
Although there are promising applications for LDN, it is not a panacea for all problems. LDN for chronic pain, autoimmune conditions, or cancer may not be effective in all cases because a diminished endorphin level is not always present with each of these health conditions. However, it has helped in many chronic health conditions where patients had given up hope. Linda Elsegood is one of those patients. She has M.S. and her condition improved dramatically after taking LDN and she started the LDN Research Trust, where there is a lot more information to read and watch on LDN. Additionally, there are now 688 research articles on PubMed about low dose naltrexone.
Endorphins come from the words endogenous (inside the body) and morphine (a pain blocking compound) Beta endorphin and metenkephalin are the two most common endorphins. In chronic health problems that see improvement with LDN, it is occurring because the mu receptors (morphine receptors) for pain and delta receptors which play a significant role in cancer and the immune system become activated. As we age endorphins diminish. In terms of exercise, aerobic exercise can raise endorphins naturally more than weight training. In a study of two groups of AIDS patients divided between the two forms of exercise, the aerobic exercise group had better outcomes.
LDN is an off-patent drug prescribed by an M.D. The prescription filled at a compounding pharmacy costs about a dollar a pill.