ApothéCure, Inc. - Immune Products

Low Dose Naltrexone (LDN)

What is it?

Naltrexone is a medication that blocks the effects of drugs known as opioids (a class that includes morphine, heroin or codeine). It competes with these drugs for opioid receptors in the brain. It was originally used to treat dependence on opioid drugs but has recently been approved by the FDA as treatment for alcoholism. In clinical trials evaluating the effectiveness of naltrexone, patients who received naltrexone were twice as successful in remaining abstinent and in avoiding relapse as patients who received placebo (an inactive pill).

Why is everyone talking about it?

Low Dose Naltrexone (LDN), where naltrexone is used in doses approximately one-tenth those used for drug/alcohol rehabilitation purposes, is being used as an "off-label" treatment for certain immunologically-related disorders. The use of LDN for such diseases as cancer was discovered and developed by Ian Zagon, PhD in animal and in vitro research, and the broader clinical effects of LDN in humans were discovered by Bernard Bihari, MD. ApothéCure was one of the first compounders that Dr. Bihari asked to make Naltrexone 4.5mg. Since that time, we have compounded thousands more in a variety of doses.

What does it do and how?

Some of the many conditions for which LDN has been reported as beneficial include multiple sclerosis (in particular, the primary progressive variant), Crohn's disease, HIV/AIDS, chronic fatigue syndrome, irritable bowel syndrome, psoriasis, fibromyalgia, ALS, autism in children, and cancer. Several clinical trials have been planned and a few are currently taking place. LDN has been theorized to work in multiple modalities. Without formal studies, there is no formal conclusion as of yet, but the generally accepted theory posited originally by Dr. Bihari is as follows:

Beta-endorphins are important regulators of the immune system. Naltrexone, which is a pure antagonist to narcotics, causes an artificial blockade of the endorphin/opioid receptors in the brain. However, unlike the normal (~50mg) dose of naltrexone used to treat drug addiction, which maintains this blockade continuously for 24 hours (preventing any derived pleasure from taking the forbidden drugs), low dose naltrexone (~3mg to 5mg) blocks the endorphin receptors for only a few hours. During that time, endorphins fail to attach to the receptors and the body apparently compensates by creating more. (Note that Dr. Bihari prescribes LDN to be taken at bedtime to take advantage of the body's pre-dawn boost in endorphin production.) Once the low dose naltrexone dose has been metabolized, the body is left with a "normal" amount of endorphins as compared to healthy controls, which consequently normalizes the immune function.

This theory of LDN's mechanism contradicts the widely-held belief that autoimmune diseases are caused by an overactive immune system. However, since 2005, at least 3 separate scientific reports have described an underlying immunodeficiency as being characteristic of four different autoimmune diseases, including multiple sclerosis, rheumatoid arthritis, Crohn's disease and chronic fatigue syndrome. In addition, recent scientific research has demonstrated abnormally low beta-endorphins in all forms of multiple sclerosis.

In April 2006 an LDN conference was held at the National Cancer Institute. Several lecturers were present discussing the use of LDN in Crohn's disease, multiple sclerosis, general autoimmune disease, and cancer. One participant, Burton M. Berkson, MD, PhD of Las Cruces, New Mexico discussed his successful experience treating metastatic pancreatic cancer and B cell lymphoma with LDN at bedtime.

Dr. Berkson described one patient who was diagnosed with "terminal" and metastatic pancreatic cancer at a well-respected oncology center. After treatment with a healthy life style program and LDN at bedtime he is alive, well, and back at work almost 5 years after diagnosis. Today, he is described as free of symptoms.

Another patient with greatly enlarged lymph nodes in his neck, axillae, and groin and diagnosed with a B cell lymphoma was found to be free of signs and symptoms after 6 months of LDN therapy. In his presentation, Dr. Berkson used before and after CT and Pet scans to show improvement, or reversal, of the disease process in four patients.

The most recent (now annual) LDN Conference was held on October 11, 2008 at the USC Health Sciences Campus, Los Angeles, California, USA.

Controversy:

LDN is a low-cost drug that is unlikely to enjoy ironclad patent protection. Many patients, who have benefitted substantially from the medication, suspect that clinical trials of LDN have been discouraged by the pharmaceutical companies, which prefer selling high-margin, patent-protected drugs. These claims are unsubstantiated at this time. Critics however point out that the drug companies, and doctors refuse to test LDN on multiple sclerosis patients, as LDN boosts the immune system, and since multiple sclerosis patients tend to have over-active immune systems, many do not feel that LDN is a safe drug for those with multiple sclerosis, even though many sufferers of the disease have had first hand experience with it, claiming substantial improvements to their symptoms, and even remissions. Critics also point to the fact that doctors who prescribe LDN to multiple sclerosis patients tend to do it via a telephone conversation, without even seeing the patients, or their medical records, for which they receive a payment from the person that they prescribed to. Many who use LDN for multiple sclerosis can also suffer from side effects, including stiffness, and the long term effects of using the drug are still unknown.

Side Effects and Cautionary Warnings:

So far, the only adverse events reported in clinical studies have been temporary insomnia and vivid dreaming in some patients. However, there are a few cautionary warnings with this drug, as with most others. According to LowDoseNaltrexone.org, if you fall in any of the categories below, you need to take special precautions:

If you use opioid agonists, i.e. narcotic medications such as Ultram (tramadol), morphine, Percocet, Duragesic patch or codeine-containing medication, should not take LDN until such medicine is completely out of your system. Patients taking thyroid hormone replacement for a diagnosis of Hashimoto's thyroiditis with hypothyroidism need to begin LDN at the very lowest range (1.5mg for an adult), as 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. 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.

Additional Resources:

Some excellent web sites for additional information and research include:

LDNers.org LowDoseNaltrexone.org

Ordering Information:

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