Evidence is mounting that low doses of naltrexone can treat conditions like lupus and multiple sclerosis effectively and with few side effects.
A slew of drugs, both new and old, are used to treat autoimmune disorders like multiple sclerosis (MS), lupus and Crohn’s disease. Most of them come with side effects, some of them serious. But research and experience from patients and doctors are mounting that a drug used to treat substance abuse, when used in lower doses, can effectively treat autoimmune conditions with few side effects.
The drug is naltrexone, which was first approved in the 1980s to treat heroin addiction. In recent years, it has been prescribed more and more at a low dose for patients with autoimmune disorders. But is this off-label use (yet to be approved by the FDA) safe and effective?
Proponents say low-dose naltrexone (LDN) is a treatment with few side effects that, for autoimmune patients, can regulate the immune system (keeping it from behaving abnormally), provide pain relief and stop the body from attacking itself further.
How It Works
Naltrexone is an opioid antagonist, meaning it blocks the brain’s opioid receptors. Opioid receptors interact with endorphins, the body’s “feel good” chemicals, and give us a sense of calm. Drugs like heroin or opioid painkillers can also attach to these receptors, and they produce that same calming effect.
Naltrexone keeps a substance like heroin from attaching to the brain’s opioid receptors, preventing users from getting high. That’s why it’s used to keep drug users in recovery from relapsing, and even to save the life of a patient who’s overdosed. LDN is thought to treat autoimmune diseases because it helps to trigger the body’s production of endorphins, and a lack of these chemicals is thought to contribute to the diseases.
It’s also been prescribed for alcohol addiction. The typical addiction treatment dose is 50 mg a day, a dose that’s been associated with nausea and vomiting, headache, fatigue and joint pain.
While some autoimmune patients who’ve taken LDN report no change at all in their health, and others note side effects like insomnia, vivid dreams or night sweats, others, like Darlene Nichols from St. Louis, report successes. Nichols was diagnosed with lupus in 1989, and later, myasthenia gravis.
She tried prednisone and other drugs typically prescribed for autoimmune conditions, “but they didn’t really work for me,” she said. “I had days where my legs would be so weak I couldn’t walk.” In 2009, she started taking 3.5 mg a day of LDN and then 4.5 mg.
“After two weeks, I was feeling great,” she said. “I had energy and strength, my fatigue disappeared. It’s like a miracle for me.” As for side effects, Nichols said initially her quality of sleep declined slightly, but soon returned to normal.
Other autoimmune patients who’ve taken LDN point to decreased autoantibodies — the cause of many autoimmune conditions — and an improvement in their pain.
No Significant Side Effects For Most
Physicians prescribing LDN for autoimmune conditions typically give between 1.5 to 4.5 mg to be taken before bed for peak effectiveness. Patients having vivid dreams, insomnia or night sweats, however, can take their dose in the morning instead.
The medication is popular with functional medicine doctors. Functional medicine aims to restore health by getting to the root cause of patients’ symptoms.
Ann Shippy, an Austin, Texas, doctor board certified in internal medicine and functional medicine, has prescribed LDN for patients with a variety of autoimmune conditions for the last 10 years. “It can be so helpful for a person’s general sense of well-being while we’re working on the root cause of getting the body repaired,” she said.
Some of her patients have found the medication to be “a game changer,” she said, while some report no change in symptoms. Others have been very sensitive to it, she said, reporting vivid dreams. Intense dreams typically subside though, Shippy added, or improve on a lower dose. “I haven’t seen any significant side effects,” she said.
Since LDN is not approved by the FDA for autoimmune diseases, it’s not commercially available. Patients must obtain the medication from a compounding pharmacy. Doctors advise finding a pharmacy familiar with making LDN to ensure they don’t compound a slow-release formula or add calcium carbonate as a filler, which can slow absorption.
An Immune System Regulator
In the mid-1980s — when naltrexone was approved for addiction treatment — New York City physician Bernard Bihari found it could help patients with autoimmunity, cancer, HIV and AIDS when taken at low doses of around 4 mg.
Low doses only partly block opioid receptors at times when our endorphin levels are high, at around 3 or 4 am. That tells the brain our endorphin levels are low, prompting our brain to make more. It’s a mechanism that can theoretically help autoimmune patients, who typically have lower levels of endorphins, which play a key role in regulating the immune system.
In treating HIV patients in the 1980s, “it wasn’t a home run,” said Ronald Hoffman, a physician and medical nutritionist in private practice in Manhattan.
However, decades later, Hoffman has seen his patients with ulcerative colitis, Crohn’s disease and itchy skin conditions improve on LDN. He uses it in conjunction with lifestyle changes, including diet modifications and adding supplements. He now also prescribes LDN routinely for cancer patients.
Seemingly Safe, But More Research Needed on Efficacy
Research has shown LDN can reduce symptom severity in autoimmune conditions marked by chronic pain, especially Crohn’s.
A study in Digestive Diseases and Sciences found more than 80% of participants with Crohn’s taking LDN saw an improvement in symptoms. Another study, however, in the Multiple Sclerosis Journal, showed no difference between MS participants taking LDN and those taking a placebo in terms of quality of life.
Researchers from the MS study concluded that LDN is a “relatively safe therapeutic option” for MS patients. However, “its efficacy is under question and probably a long duration trial is needed in the future.”
Research supports LDN for other major autoimmune conditions. A March study in the Journal of Translational Medicine showed that 74.5% of patients with inflammatory bowel disease treated with LDN showed an improvement in symptoms, and 25.5% went into remission.
Meanwhile, pharmaceutical company Immune Therapeutics is in talks with the FDA about a clinical trial for its LDN-based drug Lodonal, which is currently being used abroad for various indications.
New York-based internist David Gluck, MD, writes about LDN at www.lowdosenaltrexone.org, where physicians and patients report they’ve seen success in autoimmune conditions including Hashimoto’s disease, rheumatoid arthritis, ulcerative colitis, celiac, Sjogren’s syndrome and scleroderma.
LDN “provides a new, safe and inexpensive… medical treatment by mobilizing the natural defenses of one’s own immune system,” he writes.