Naltrexone

FDA-approved Naltrexone®, in a low dose, can normalize the immune system — helping those with HIV/AIDS, cancer, autoimmune diseases, and central nervous system disorders.

 

Dosage and Administration:

The therapeutic dosage range for LDN is from 1.5mg to 4.5mg every night. The course is usually started with 1.5 mg at bedtime. After one week the dosage is increased to 3mg, and after another week or two – to 4.5 mg. Because of the rhythms of the body's production of master hormones, LDN is best taken between 9pm and 3am. Most patients take it at bedtime.

 

The drug comes in a dosage of 50mg per a pill. To make a solution with the right concentration one pill is dissolved in 50 ml of distilled water (i.e. 1 part of water and 1 part of medication). The solution is kept in a refrigerator. Shake it up prior to use. Then pull up the necessary amount of a solution using a measuring device and plunge it into the back of your mouth. Take a small glass of water after an intake.

Interaction with other drugs:

Naltrexone® blocks the action of opioid drugs.

 

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, the dosage can be reduced from 4.5mg to 3mg nightly.

 

Storage

Store the pills in a dry place, at a temperature not exceeding 25°C (77°F). The solution should be kept in a refrigerator. Keep out of the reach of children.

 

Note:

  1. LDN users who are planning to have a surgery performed generally discontinue taking LDN for one or two days prior to the scheduled procedure. They then are able to restart it promptly after the surgery, when they no longer need to take narcotics regularly.
  2. 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.
  3. Full-dose Naltrexone (50mg) carries a cautionary warning against its use in those with liver disease.
  4. People who have received organ transplants and who therefore are taking immunosuppressive medication on a permanent basis are cautioned against the use of LDN.

It is important to note that full-dose Naltrexone® can potentiate the course of a disease rather than inhibit it!

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.

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  12. Bronfenbrener R (2019). Inexpensive compounding of low dose naltrexone (LDN) with orange juice. https://www.ncbi.nlm.nih.gov/pubmed/ 30930087
  13. Wang R et al (2019). Interaction of opioid growth factor (OGF) and opioid antagonist and their significance in cancer therapy. https://www.ncbi.nlm.nih.gov/pubmed/ 31404891
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  15. Bolton MJ et al (2020). Low-dose naltrexone as a treatment for chronic fatigue syndrome. https://www.ncbi.nlm.nih.gov/pubmed/31911410


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