LOW DOSE NALTREXONE
Low Dose Naltrexone
Naltrexone was approved by the FDA in 1984 in a 50mg dose for the purpose of helping heroin or 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: beta-endorphin and metenkephalin. Many body tissues have receptors for these endorphins and enkephalins, including virtually every cell of the body’s immune system.
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 (3mg taken at night) on the body’s immune system. He found that this low dose naltrexone (LDN), taken at bedtime, was able to enhance a patient’s response to infection by HIV, the virus that causes AIDS. [Note: Since then the optimal adult dosage of LDN has been found to be 4.5mg.]
In the mid-1990’s, Dr. Bihari found that patients in his practice 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 disease activity while taking LDN.
The brief blockade of opioid receptors between 2 a.m. and 4 a.m. that is caused by taking LDN at bedtime each night is believed to produce a prolonged up-regulation of vital elements of the immune system by causing an increase in endorphin and enkephalin production. Normal volunteers who have taken LDN in this fashion have been found to have much higher levels of beta-endorphins circulating in their blood in the following days. Animal research by I. Zagon, PhD, and his colleagues has shown a marked increase in metenkephalin levels as well. A body of research over the past two decades has pointed repeatedly to one’s own endorphin secretions (our endogenous opioids) as playing the central role in the beneficial orchestration of the immune system, and recognition of the facts is now growing.
In the November 13, 2003 issue of the prestigious New England Journal of Medicine: “Opioid-Induced Immune Modulation: …. Preclinical evidence indicates overwhelmingly that opioids alter the development, differentiation, and function of immune cells, and that both innate and adaptive systems are affected. Bone marrow progenitor cells, macrophages, natural killer cells, immature thymocytes and T cells, and B cells are all involved. The relatively recent identification of opioid-related receptors on immune cells makes it even more likely that opioids have direct effects on the immune system.”
“Low Dose Naltrexone (LDN) may well be the most important therapeutic breakthrough in over fifty years. It provides a new, safe and inexpensive method of medical treatment by mobilizing the natural defenses of one’s own immune system.
LDN substantially reduces health care costs and improves treatment of a wide array of diseases. Unfortunately, because naltrexone has been without patent protection for many years, no pharmaceutical company will bear the expense of the large clinical trials necessary for FDA approval of LDN’s new special uses. It is now up to public institutions to seize the opportunity that LDN offers.”
— David Gluck, MD
Bernard Bihari, MD, as well as other physicians and researchers, have described beneficial effects of LDN on a variety of diseases: various cancers, ALS (Lou Gehrig’s Disease), Alzheimer’s Disease, Ankylosing Spondylitis, Autism Spectrum Disorders, Behcet’s Disease, Celiac Disease, Chronic Fatigue Syndrome, Crohn’s Disease, Fibromyalgia, HIV/AIDS, Irritable Bowel Syndrome (IBS), Multiple Sclerosis (MS), Parkinson’s Disease, Systemic Lupus (SLE), Ulcerative Colitis.
Side effects: LDN has virtually no side effects. Occasionally, during the first week’s use of LDN, patients may complain of some difficulty sleeping. This rarely persists after the first week. Should it do so, dosage can be reduced from 4.5mg to 3mg nightly.
Cautionary warnings: Because LDN blocks opioid receptors throughout the body for three or four hours, people using medicine that is an opioid agonist should not take LDN until such medicine is completely out of one’s system.
Those patients who are taking thyroid hormone replacement for a diagnosis of Hashimoto’s thyroiditis with hypothyroidism ought to begin LDN at the lowest range (1.5mg for an adult). Be aware that LDN may lead to a prompt decrease in the autoimmune disorder, which then may require a rapid reduction in the dose of thyroid hormone replacement in order to avoid symptoms of hyperthyroidism.
Full-dose naltrexone (50mg) carries a cautionary warning against its use in those with liver disease. This warning was placed because of adverse liver effects that were found in experiments involving 300mg daily. The 50mg dose does not apparently produce impairment of liver function nor, of course, do the much smaller 3mg and 4.5mg doses. People who have received organ transplants and who therefore are taking immunosuppressive medication on a permanent basis are cautioned against the use of LDN because it may act to counter the effect of those medications.
We produce immediate release (NOT SLOW RELEASE) capsules in a variety of strengths using pharmaceutical grade naltrexone powder with pure dextrose monohydrate as the filler. It is very important that immediate release capsules are used and not any modified, slow release or enteric coated capsules. Due to the low doses involved it is also very important that you use a compounding pharmacy experienced in producing low dose capsules such as ourselves which require multiple triturations and extensive powder mixing using proven powder mixers to achieve uniform and accurate capsules.