Naltrexone was created in 1963 as an opioid receptor blocker. This means naltrexone binds to opiate receptor and neutralizes the action of opiates on the opiate receptor. Naltrexone was approved by FDA in 1984 for the treatment of opioid addiction. The typical daily dosage for opioid addiction is 50 to 100 mg daily. Low Dose Naltrexone or LDN refers to daily dosages of naltrexone that are between 1.5 is 4.5 mg. More than 20 years ago it was discovered that very small doses of this drug—3 to 4.5 mg—have profound effects on the immune system
Basic science work examining the use of opioid antagonists for treating other diseases did not appear until the late 1980s, and the first published LDN trial in humans was presented in 2007. Since that time, LDN has been studied and has been slowly gaining attention as a possible treatment for some chronic medical conditions. Currently, the best documented scientific use of LDN is in treating autoimmune conditions such as multiple sclerosis, Crohn’s disease, and Hashimoto’s thyroiditis.
What Other Conditions has LDN been used for?
ALS (Lou Gehrig’s disease)
Chronic fatigue syndrome
Inflammatory bowel disease
Multiple sclerosis (MS)
Another documented use of Naltrexone is for treating obesity. Contrave, a new medication approved to treat obesity in 2014, combines Naltrexone and bupropion in a sustained release formula. Both bupropion and Naltrexone individually have shown evidence of weight loss and the combination aims to create a synergistic effect. Contrave is a sustained release formulation of Naltrexone and bupropion. The FDA has placed a boxed warning onto Contrave stating that it may affect mood and it may increase the likelihood of suicide. This potential adverse effect is most probably due to bupropion as such adverse effects have been observed with medications designed to treat mood disorders. The Naltrexone dose in Contrave is higher than we use in Low Dose Naltrexone
What Does Treatment With LDN Involve?
LDN requires a prescription and is available only from compounding pharmacies. (Regular pharmacies typically carry only 50 mg capsules.) The suggested dose is 3–4.5 mg per day, taken orally at bedtime.
The only contraindication is narcotic drugs. Low-dose naltrexone blocks the effects of narcotics and could cause withdrawal symptoms, so it should be started only after those drugs are completely out of your system.
LDN is safe and well tolerated. You may have vivid dreams at first, but sleep disturbances are rare. To avoid this, start with a dose of 1.5 mg and build up slowly over two months.
How did you first learn about LDN?
I was familiar with Naltrexone as a treatment option for patients with cancer issues. I heard about it while I was completing my Integrative Cancer Therapy fellowship at A4M. Then it became FDA approved as a weight loss drug, and I took a look at how I could use it in my patients with sugar cravings. I then learned about its use in fertility issues from Dr. Hilgers’ approach, but he was using the “normal” dose of Naltrexone to fully block the opioid receptors in order to improve fertility for patients. Later, I encountered the NaPro website, which showed different type of approach: boosting endorphins through a low dose of Naltrexone. In this strategy, you aim for endorphin stimulation rather than blocking. So that was a completely new concept, and it didn’t occur to me at first that this would have a role for fertility. But then I started having good results in my patients who had rheumatoid arthritis and had a dramatic improvement on LDN. I thought, “The next time I see somebody with an autoimmune condition, I’m going to try them on this.”
What has been your experience using LDN with your patients?
I then started by prescribing LDN to the very obvious autoimmune patients, such as patients with active rheumatoid arthritis. In addition to improvements in their autoimmune condition, often patients would also report back to me, ‘You know what? I used to have horrible premenstrual syndrome and now that’s gone too.’ Or ‘I used to have low mood, fatigue and anxiety, and that’s no longer an issue.’ Or they had brown bleeding that has now stopped. Gradually I began to realize that these symptoms (PMS, polycystic ovaries, endometriosis, persistent fatigue, low mood, anxiety, sleep disturbance, brown menstrual bleeding, family history of autoimmune disorder) can be associated with clinical endorphin deficiency.
I was able to see over the course of about a year of prescribing LDN to the occasional autoimmune patient that not only did the endorphin deficiency symptoms improve with LDN, but it actually helped with weight as well.
It was deductive reasoning through clinical observation that led me to this conclusion.
I then decided that if we have patients who don’t have an obvious autoimmune diagnosis but have symptoms of possible clinical endorphin deficiency, we could try them on the LDN to see if the symptoms improve. Eight times out of ten symptoms like PMS and fatigue would improve. So now I use the presence of such symptoms as a guide for determining probable clinical endorphin deficiency. While other conditions can potentially cause these same symptoms, having low endorphins is a very common root cause, and therefore it’s worth a trial of LDN to see if the symptoms respond.
Given your clinical experience with LDN, what kind of patient do you think is best suited to benefit from it?
It depends on whether they need it in the first place. I try and make a clinical judgment about a patient’s probable endorphin levels. I think, ‘Does this person need LDN?’ If it looks like they probably do, we’ll try it and then we’ll listen to what their body tells us.
I look at a variety of factors that can be indicators of an underlying endorphin deficiency such as the presence of PMS, polycystic ovaries, endometriosis, persistent fatigue, low mood, anxiety, sleep disturbance, and family history of autoimmune disorder.
Do you also treat patients that do not have infertility issues with LDN?
I see a small handful of people with food addiction, smoking addiction, autoimmune conditions, and fibromyalgia; these can respond really well to treatment with LDN. I’m very quick to tell people I’m no expert in any of these kinds of conditions, but I’ve got a lot of good clinical experience with Naltrexone. I’m happy to give it a try for these patients because it’s safe. The worst case scenario is that it doesn’t work. It won’t do you any harm at least, apart from short-term transient side effects for a week or two while you get used to it.
Why do you consider LDN such an appealing treatment option?
If somebody has an autoimmune condition and they go on these super expensive, very strong immunosuppressive drugs to get relief of their symptoms but they’ve taken out their immune system by using them, while you may not see any immediate problems, you’re potentially putting yourself in harm’s way. You’re at risk of developing new additional autoimmune conditions, and you may potentially increase your risk of tuberculosis and different cancers because of the profound immune-suppression that you go through. So it’s not a great solution even if you can observe great clinical relief. LDN is so much more attractive. It’s inexpensive, has few side effects, is available in topical, sublingual and capsule forms, and it’s safe and easy to use compared to the alternatives out there.
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