Naltrexone is a pharmaceutical drug that doctors first began prescribing nearly 30 years ago to treat opioid addiction. At a dose of 50 – 100 mg, Naltrexone prevents people from experiencing the ‘high’ associated with opioid drugs by blocking the opioid receptors. This decreases the response of endorphins, your body’s natural feel-good chemicals, which is thought to be a major player in why pain medicine addiction happens.
Knowing that, imagine my surprise when about five years ago, I started hearing the craze surrounding Low Dose Naltrexone (LDN) – touting it as a little known generic drug that could be used for autoimmune conditions and pain. Since I work in functional medicine, I see a lot of patients with autoimmune conditions. After researching more, I decided it was something that could have a great benefit to many of my patients with very little risk.
Since then, I have used it in many patients and often people come asking about it because they have researched it and have read about its benefits. I want to give you a quick look at the history, mechanism of action, precautions, and use of LDN. My hope is that if you are suffering from chronic pain or an autoimmune condition, this will be of help to you.
History and mechanism of action
When being used for opioid abuse treatement, the levels of Naltrexone prescribed prevent an endorphin rush, however, Dr. Bernard Bihara discovered that when Naltrexone is taken at much lower doses (1.5-4.5 mg), it actually increases the levels of endorphins in the body. It does this due to the short partial blockade of the receptors, in turn, causing an increase in endorphin release. His initial research was for its possible use for HIV, AIDS, and cancer. However, low dose naltrexone’s role has expanded significantly in helping those with autoimmune conditions and research has spread significantly in this area. The reason is that increased endorphin response is beneficial for autoimmune patients, due to the fact that endorphins play a role in immune system modulation. It has also been shown to balance the immune system by diminishing the release of inflammatory and neurotoxic chemicals in the brain.
Although LDN can be used for most autoimmune conditions, it is especially helpful in those with painful conditions due to its role in increasing endorphins. It has been used in those with Hashimoto’s, Multiple Sclerosis, Rheumatoid Arthritis, Crohn’s, Ulcerative Colitis, Fibromyalgia, Psoriasis, and Chronic Fatigue Syndrome.
Dosing and when to take LDN
As mentioned previously, the dose for autoimmune conditions is 1.5-4.5 mg, although some start as low as 0.5 mg when initially starting a sensitive patient. LDN is best taken around 9 pm to allow maximum effect at 4 am when endorphins are highest. LDN provides a short term partial blockade of opioid receptors, which then causes the endorphins to increase their response and modulate the immune system after the blockade is released.
For most patients, it is best tapered up every couple of weeks to let the body adjust. Side effects are usually minimal and include transient difficulty falling asleep and/or vivid dreams. These side effects normally go away after several weeks, however, a small percentage of people have more long term issues. Although not settled, recent research has shown that LDN may be just as effective taken in the morning as at night. If this is true, it would be very helpful for those whose only side effect is insomnia but more research is needed in this area. It is also important for patients to know that it can take months to notice the full benefit of LDN.
Where to get LDN
While Naltrexone is FDA approved, low dose Naltrexone is not. However, it is available at compounding pharmacies. Be sure to work with a provider to guide you to a reputable pharmacy because the ingredients used to compound make a big difference in how well LDN will work. It also is important that it is compounded in an immediate-release form, and not a sustained-release, as you only want to block the receptors for a short time.
Important precautions:
As LDN does interfere with pain medications, please talk with your doctor if you have to be on opioid medications and want to consider LDN. Also, LDN can potentiate a change in thyroid medication dose as less medicine may be needed as a result of being on LDN. For this reason, dosing should be lower and slower and thyroid labs followed carefully. Also, for those with MS, at doses above 3 mg, it can cause an increase in spasticity, so the most therapeutic dose seems to be 3 mg. More is not always better, and that is certainly the case here.
My thoughts and take aways from patient responses
As a clinician, I like LDN and have seen it work very well in many patients. I will say it does not work in every patient and finding the root cause in each individual’s case is still foremost in my mind. LDN is not a wonder or miracle drug by itself, but it can be a good part of a well-rounded treated approach in many patients and can provide them relief while looking for the underlying cause of their issue. I consider LDN another tool in my toolbox to help my patient get relief as we work to restore vibrant health. If you have any questions as to whether LDN might be an option for you, feel free to contact us and we can help you determine if it’s right for you.