Low-dose naltrexone (LDN) is an off-label treatment for various auto-immune diseases, cancers and chronic pain syndromes. Naltrexone, having a similar chemical structure to morphine and other opiates, was developed in the 1970’s as an oral opiate blocking drug. Naltrexone was FDA approved in 1984 as a 50 mg oral tablet for treatment of drug addiction. However, the naltrexone drug failed its intended use because upon taking it, drug addicts would go into severe opiate withdrawal, and were not happy about it. However, naltrexone as a 50 mg tablet has a current day use in the treatment of alcoholism, and works quite well for that.
What are Endogenous Opiates and Endorphins?
Endorphins are endogenous opiates. Our brain makes opiates while we sleep, and the body has an entire opiate neurotransmitter system involved in our pain perception and immune regulation. In the 1990’s, A New York physician by the name of Bernard Bihari discovered that a small doses of LDN, 3 mg in oral capsule taken at bedtime, produces a rebound increase in endorphin production, thus producing health benefits for diverse conditions such as auto-immune disease, chronic pain syndromes, fibromyalgia and cancer. Let us review how LDN works, look at what conditions it may or may not help.
How Does Low-Dose Naltrexone Work?
Naltrexone is an opioid receptor blocker and comes as a 50 mg oral tablet. When Naltrexone is compounded into a smaller 3 mg capsule at bedtime, the effect is to block opiate receptors in the brain. This is a transient effect causing a rebound increase in endorphins over the next 24 hours. The transient blockade of opioid receptors results in a rebound effect. This is what provides increased endorphins that regulate pain and the immune system. Another example of endogenous endorphin production is the “runner’s high” of the marathon runner. Why are they so driven to run for miles and miles? Could it be the endogenous endorphin production of long distance running?
Anti-Inflammatory Activity, Microglial Inhibition
The anti-inflammatory effects of LDN for the brain and central nervous system are thought to be related to inhibition of microglial activation, the hallmark of inflammation in the brain. Microglia are the immune cells found in the brain involved in the inflammatory response, so microglial inhibition is a good thing. For more on this topic, see: Low Dose Naltrexone Part Four.
Fibromyalgia and Chronic Regional Pain Syndrome
A number of studies and anecdotal reports show that LDN has potent anti-inflammatory effects and is useful for fibromyalgia, neuropathic pain and chronic regional pain syndrome (reflex sympathetic dystrophy). LDN prevents activation of microglial cells in the brain and central nervous system and perhaps this is the mechanism for benefit. For more on this topic, see: Low Dose Naltrexone Part Four.
Auto-Immune Thyroid Conditions
Interest in LDN for Hashimoto’s thyroiditis has been stimulated by online message boards and popular books on the topic which suggest that since LDN has benefit for other auto-immune diseases, perhaps there may also be benefit for Hashimoto’s thyroiditis. However, reports of LDN benefit in Hashimoto’s disease are mostly anecdotal, with no published clinical trials showing efficacy. Still, because of an excellent track record for safety, we are fairly liberal with prescribing a trial LDN to evaluate response. For more on Hashimoto’s see: How to Find a Doctor for Hashimoto’s AutoImmune Disease.
What Are the Potential Benefits of Low-Dose Naltrexone?
The potential of low-dose naltrexone benefits depend on the condition being treated and the individual patient’s response.
LDN has been investigated for several conditions in which chronic pain, altered immune signaling, or neuroinflammation may play a role. Potential areas of benefit include:
- Auto-Immune Disease
- Chronic Regional Pain Syndrome, Fibromyalgia
- Cancer
- Multiple Sclerosis
- Inflammatory bowel disease, Crohn’s and Ulcerative Colitis.
Since Naltrexone is off-patent, there are no financial incentives to do large scale randomized controlled trials (RCTs). Even so, we do have a few RCTs available to establish LDN efficacy. However, available studies tend to be small in size or preliminary. Nonetheless because of its track record for safety, we are fairly liberal in prescribing LDN if the patient requests it. The decision to treat with LDN is based on the underlying diagnosis, symptoms, previous treatment response, and carefully weighing risks vs. benefits.
Who May Benefit From Low-Dose Naltrexone?
LDN may be considered for selected patients when there is a reasonable clinical indication, when a patient has:
- Auto-immune disease, Crohn’s, Ulcerative colitis, Multiple Sclerosis, Rheumatoid Arthritis, etc.
- Persistent chronic pain, chronic regional pain syndrome, fibromyalgia
- Cancer
The new patient may have a complex presentation with many seemingly unrelated symptoms of chronic fatigue, brain fog, and unexplained pain. Many of these symptoms overlap with hormonal and thyroid imbalances, in which case LDN is not particulary useful.
If there is an underlying low thyroid condition or hormone imbalance, a full medical evaluation is the best starting point.
Adverse Effects of LDN
The main adverse effect arises from the fact naltrexone is an opiate receptor blocking drug, and will block the effect of narcotic pain medications. As such, the person on long term opiate pain medication will immediately be thrown into a drug withdrawal state which can be quite uncomfortable. This is to be avoided, and includes prescription opioid pain medication as well as others such as cough medicine or other opioid containing products.
Patients should include on their medical history sheet information about current or future use of opioid pain medication, previous use of naltrexone or opiates, etc.
What Are the Side Effects of Low-Dose Naltrexone?
LDN is generally considered well tolerated, but side effects can occur. Some patients may experience:
- Headache
- Nausea
- Sleep disturbance
- Vivid dreams
- Changes in mood
LDN induced sleep-related effects, such as vivid dreams, may be noticeable when treatment is first started. This can be avoided by slowly increasing dosage over time.
Interestingly, similar complaints of disrupted sleep can be associated with chronic stress and elevated cortisol, another reason for a more complete medical evaluation before starting treatment.
What to Discuss With Your Doctor Before Starting LDN?
Before considering LDN, your physician should know about your:
- Medical History and Medical Diagnoses
- Opioid use or recent opioid treatment
- History of Liver Disease
- Current symptoms and medications
- Previous treatments and medications
- Upcoming surgeries or procedures
- Goals of Treatment
A thorough review of systems and medical history, examination and laboratory testing is particularly important when evaluating a chronic pain condition. Treating the symptoms without identifying the underlying cause is bad medicine and may delay the correct treatment. This same principle can be applied across our full range of diagnostic and lab testing services.
When Should You Seek Medical Guidance?
Medical guidance is particularly important if symptoms are severe, worsening, unexplained, or interfering with normal activities.
Low-Dose Naltrexone Treatment
At the TruemedMD Clinic, our medical director, Jeffrey Dach MD, makes treatment decisions based on the full medical history, review of symptoms, an expanded laboratory panel and careful follow up for response to treatment.
When considering LDN, we evaluate the potential benefit. We also consider whether it makes sense for the patient’s particular conditions. For a deeper dive into LDN, see our collected articles on Low Dose Naltrexone.
Questions to Ask
What are the main low-dose naltrexone benefits?
Potential low-dose naltrexone benefits include improvement in certain autoimmune and chronic pain conditions, fatigue, sleep, and inflammation in selected patients. Evidence varies depending on the underlying condition.
Can I take low-dose naltrexone with opioids?
Naltrexone blocks opioid receptors and can interfere with opioid medications. Anyone currently taking opioids should not take LDN, and should speak with a physician before considering LDN.
How long does low-dose naltrexone take to work?
LDN works for about 70 percent of the patients. Unfortunately, there is no benefit for the other 30 percent. Are you one of the 70 percent responders or one of the 30 percent non-responders? The only way to find out is to try it. Some patients may notice improvement within several weeks, while others may need longer observation before determining whether treatment is beneficial.
Is low-dose naltrexone safe for everyone?
No. Contraindications include current opioid use, liver disease, certain other medications, and medical conditions can affect whether LDN is appropriate. Medical supervision is recommended.
We Are Ready to Help
If autoimmune disease, chronic pain, fibromyalgia, or persistent inflammatory complaints continue despite conventional approaches, LDN may be worth discussing with a qualified physician.
At the TrueMedMD Clinic, Jeffrey Dach, MD, considers the potential benefits of low-dose naltrexone in the context of the patient’s diagnosis, symptoms, medications, and overall health. Rather than assuming LDN is appropriate for everyone, an individualized evaluation can help determine whether this off-label therapy has a reasonable place in your care. If interested, contact our office to schedule a consultation.
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