Low-Dose Naltrexone to Quell Chronic Pain & Cut Dementia Risk

Image: GrAI/Shutterstock

If naltrexone was still patentable, you can be certain that the pharmaceutical industry would make sure that every physician was using it to treat patients experiencing chronic pain. It would also probably cost around $24,000 a year.

But this drug is 60 years old, and available for about 75 cents per day. Since it is not under patent and therefore not profitable for Big Pharma, most physicians outside of holistic and functional medicine, or addiction medicine, are unfamiliar with its uses.

Naltrexone blocks opioid receptors. Because of this, it is able to reverse the effect of narcotics, and is used for treating opioid overdoses.

But naltrexone is a very unusual drug in that different doses have completely different effects.

Dose-Dependent Effects

At doses of 50 mg/day or more, it will block the ability of addicted people to get high from opiates. It also blocks an opiate’s pain-relieving benefits. For reasons unknown, this dose taken one hour before drinking alcohol also decreases craving in alcoholics, and can be helpful in moderating alcohol intake among those unwilling or unable to stop drinking completely. This has been called the Sinclair Method for treating alcoholism.

But at low doses between 3 to 5 mg, taken at night, naltrexone has a completely different set of actions: it turns off microglial activation, which we can consider to be a form of brain inflammation, and it balances immune system function. LDN also decreases a form of pain called central sensitization, or “brain pain,” which occurs in numerous chronic pain conditions. These effects are lost at much higher or much lower doses.

If LDN, and other nutritional and botanical pain remedies are used more widely, we can avert the twin disasters of chronic pain and cognitive impairment that we’re now facing.

When to Consider LDN

Consider a 2-3 month course of LDN (3-5 mg, taken at night) in any patient with:

Standard pharmacies do not supply LDN. It needs to be obtained from a compounding pharmacy. Almost every compounding pharmacy can do an excellent job of making it. My recommendation? Call your local compounding pharmacist and ask if she or he would be willing to guide your patients in adjusting the dosage as needed. If the answer is yes, then use that pharmacy and leave the fine-tuning to the pharmacist.

Things to Know About LDN

Before starting a course of LDN, there are a few important things that you and your patients should know:

1. It won’t work if the person is concurrently taking narcotics.

2. Doses over 4.5 mg at night usually lose effectiveness. This is a general rule, although we do see exceptions, and sometimes doses even up to 8 mg might still work. A study of veterans with chronic pain found the 3 mg dose to be more effective than 4.5 mg. The standard dose used by most physicians (to block the narcotic high in addicts) is 50 mg/day, but this high dose won’t likely be effective for treating chronic pain.

3. Some people find that LDN disrupts sleep, especially at the beginning of treatment. But this only happens in a small percentage of people, and usually resolves with time. Still, it is a concern, which is why many compounding pharmacies offer a “starting pack” of LDN that begins with doses below 3 mg. Overall, it’s very good idea to start low, followed by 3 mg capsules for patients weighing under 150 pounds, and 4.5 mg for those over 150. If sleep disruption is a persistent problem, I have patients take the naltrexone in the morning instead of at bedtime.

4. It takes two full months at the full dose for LDN to start working. When I first started using LDN about 35 years ago, I only gave it 3-4 weeks to work, so I didn’t see the effect. This is not a rapid-relief therapy. Give it time!

5. LDN is only available from compounding pharmacies, and therefore not generally covered by insurance. Most insurers won’t cover compounded LDN, but they will cover standard naltrexone 50 mg tablets. For cash-strapped patients, I recommend that they use the compounded LDN for two months at full dose, to see if it will be effective. If it is working, switch to the standard 50 mg tablets obtained from a regular pharmacy, so it will be covered by insurance.  Grind a tablet up very finely with a mortar and pestle, and then mix it with about three 3 ounces of water (83 cc), and shake it well. One teaspoon (5 cc) of the solution per night will supply the 3 mg dose. For the 4.5 mg dose, mix a ground 50 mg tablet in with just under 2 ounces (55 cc) of water and take 1 teaspoon of the solution a night. This will give 11 doses.

The good news is that not only is LDN cheap, it is also extremely safe. A recent systematic review of 9 LDN trials indicated that there were no severe adverse events reported in any of the trials that tracked safety measures.

I’ve seen first-hand that when it works, LDN not only dramatically decreases pain, but also improves overall energy and cognition. My sincere hope is that if LDN, and other nutritional and botanical pain remedies are used more widely, we can avert the twin disasters of chronic pain and cognitive impairment that we’re now facing.

For information on how to implement LDN, and strategies for treating CFS, Fibromyalgia, and Long Covid, feel free to email me at FatigueDoc@gmail.com and ask for my free information sheets. Please let me know that you are a practitioner, so I can include the free treatment questionnaires and checklists.


Jacob Teitelbaum, MD, is one of the most frequently quoted integrative medical authorities in the world. He is the author of several best-sellers, including From Fatigued to Fantastic!, the Beat Sugar Addiction Now! series, The Fatigue and Fibromyalgia Solution, and the popular free smartphone app Cures A-Z. He is the lead author of 4 studies on effective treatment for fibromyalgia and chronic fatigue syndrome. He earned his MD degree from Ohio State University, and recently celebrated his 50th year as a physician. Learn more at Vitality101.com.

Subscribe to Holistic Primary Care