Naltrexone® has been classically used as an FDA-approved drug since 1980s in a 50mg dose for the purpose of helping heroin, tobacco and opium addicts, by blocking the effect of such drugs. By blocking opioid receptors, Naltrexone® also blocks the reception of the opioid hormones that our brain and adrenal glands produce.

In 1985, Bernard Bihari, MD, a physician with a clinical practice in New York City, discovered the effects of a much smaller dose of Naltrexone® (3 to 4.5 mg once a day) on the body’s immune system. Naltrexone®, blocking endorphins, sends a false signal to the hypothalamus that “there are no endorphins” and in response the hypothalamus increases their production. Endorphins are a natural defense of the body against viruses and infections. In people with HIV, their quantity was less than 30% of the norm of healthy people. Therefore, Bihari then began to experiment with Naltrexone® doses, which, on the one hand, would increase the number of endorphins, and on the other, would not block them for a long time. The effect began with a 1.5 mg dose and ceased to increase from doses above 4.5 mg. He found that this low dose Naltrexone (LDN) was able to enhance a patient’s response to infection by HIV, the virus that causes AIDS. The brief blockade of opioid receptors between 2 a.m. and 4 a.m. that is caused by taking LDN at bedtime is believed to produce a prolonged up-regulation of vital elements of the immune system by causing an increase in endorphin and enkephalin production.

In the mid-1990’s, Dr.Bihari found in his practice that patients with cancer (such as lymphoma or pancreatic cancer) could benefit, in some cases dramatically, from LDN. In addition, people who had an autoimmune disease (such as lupus) often showed prompt control of the disease activity while taking LDN.

In human cancer, research by Professor Ian S. Zagon of the Pennsylvania State University over many years has demonstrated inhibition of a number of different human tumors in laboratory studies by using endorphins and LDN. It is suggested that the increased endorphin and enkephalin levels, induced by LDN, work directly on the tumors’ opioid receptors and, perhaps, induce cancer cell death (apoptosis). In addition, it is believed that they act to increase natural killer cells and other healthy immune defenses against cancer.

In general, in people with diseases that are partially or largely triggered by a deficiency of endorphins (including cancer and autoimmune diseases), or are accelerated by a deficiency of endorphins (such as HIV/AIDS), restoration of the body’s normal production of endorphins is the major therapeutic action of LDN. In general, LDN has shown promise for the treatment of the following diseases: Cancer; Hepatitis C; Lupus; Ulcerative colitis; Autism; Chronic fatigue syndrome; HIV/AIDS; Irritable bowel syndrome (IBS); Diabetic neuropathies; Dermatomyositis (an inflammatory muscle disease); Multiple sclerosis; Crohn’s disease; Alzheimer’s disease; Hasimoto’s thyroiditis; Parkinson’s disease etc.

* https://www.youtube.com/watch?v=rBd2gv8UGU0 – in 2012 the Norwegian documentary program, called “Our Small Country”, aired this documentary about LDN that has helped many patients with a large number of autoimmune diseases and some cancers. By 2015, LDN users in Norway had increased from a mere 300 to about 15,000 people. It has also changed many doctors’ attitude towards LDN, turning a widespread skepticism towards this unfamiliar drug into a willingness to prescribe LDN at a patient’s requests.