Low-Dose Naltrexone

New research has brought our attention to the tremendous potential of low-dose naltrexone to help people with chronic pain. We have used this treatment in hundreds of patients with a wide range of health problems, but we recently began prescribing it for patients in our chronic pain program with very encouraging results.

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Naltrexone is a drug that was introduced in the 1960s, initially for the treatment of addiction to heroin and other substances. Researchers found that it blocks opioid receptors on cells, including the endorphins that act as the body’s natural painkillers. People on naltrexone were prevented from getting high when using the illicit drugs they were addicted to. It was used for several years for this purpose.

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In the early 1990s, naltrexone was rediscovered by a physician named Dr Bihari while treating people with HIV in New York City. Using a low dose of 4.5mg (as compared to the 100-300mg doses used to treat addiction), Dr Bihari saw major improvements in the immune systems of hundreds of patients. He described his experience in this paper. Since then, a grassroots movement has developed around the world, which has led thousands of people to use low-dose naltrexone (LDN) to treat a wide range of diseases of the immune system, including cancers and neurological disorders.

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It is known that endorphins do much more than relieve pain. These feel-good molecules, whose release can be triggered by exercise, sex and other factors, stimulate many cells of the immune system. While high doses of naltrexone block endorphins completely, low doses seem to lower them just a little bit – leading the body to increase its production of endorphins. The first published study of LDN was in patients with Crohn’s disease, followed by another in children with Crohns. Ongoing trials are evaluating LDN in multiple sclerosis and in cancer.

More recent studies have shown early positive results in treating chronic pain. Researchers at Stanford University published two clinical trials showing that LDN reduced chronic pain in women with fibromyalgia. A case series showed pain reductions in two people with complex regional pain syndrome, and many physicians are using it to treat chronic low back pain as described in this paper.

Studies suggest that LDN may heal the body in more ways than one. In addition to helping boost endorphin levels, naltrexone binds to receptor called TLR4 on cells in the brain that are called microglia. Most people think of neurons as brain cells, but glia are much more important. These are the housekeeping cells that keep the brain healthy, and microglia are specialized glia that trigger inflammation in the brain.

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Chronic pain turns on microglia, leading them to trigger inflammation in the entire nervous system. This causes pain, but also promotes sleep problems, depression, anxiety and affects memory and concentration. It seems that naltrexone turns off microglia, leading to an anti-inflammatory effect in the brain.

People using opioid medications, including morphine, codeine, Hydromorphone, oxycodone, tramadol, cannot use LDN. This interaction can cause bizarre side effects, so a two-week period is needed to flush them out of the system before starting LDN. It has no other important drug interactions.

For the first week or two, people starting LDN have more trouble sleeping. This occurs because the body is adjusting to lower endorphin levels, and it takes time for it to produce more. This can be addressed by taking melatonin, chamomile tea, Epsom salt baths and other natural sleeping aids.

The trials of LDN lasted for 12 weeks. In most cases, people will see improvements within two months. We recommend taking one week off every two months to allow the body to be maximally stimulated by this fascinating new treatment. It is not manufactured on a large scale at this very special dose, so our LDN is made by a compounding pharmacy with extensive experience making it for many leading-edge physicians across Canada.