Low Dose Naltrexone is a beneficial drug used for fighting cancer and autoimmune diseases. It helps alleviate pain and inflammation caused by various conditions, and it can be beneficial for many with chronic illnesses.
Introduction to Low Dose Naltrexone (LDN)
Low Dose Naltrexone (LDN) is a drug which can help treat an array of cancers, central nervous system disorders, autoimmune diseases, and a variety of other issues.
Originally, Naltrexone was prescribed and FDA approved in much higher doses (50 mg to 300 mg) to treat drug and alcohol addiction. This article focuses on lower doses of Naltrexone (1.5 mg to 4.5 mg) and its multiple medicinal benefits.
How Does LDN Work?
LDN works by blocking the opioid growth factor and opioid growth factor receptor pathway in your body, which in turn helps to boost your body’s immune system and natural defenses.
By blocking this pathway temporarily, the body then tries to compensate by producing more beta-endorphin and met-enkephalin (your body’s natural opioids). Many body tissues have receptors for these endorphins and enkephalins, including every cell of the body’s immune system.
Cancer and autoimmune diseases are triggered by low blood levels of endorphins, contributing to the disease-associated immune deficiencies. Similarly, HIV/AIDS is accelerated by a deficiency of endorphins.
Bottom Line: LDN has the ability to correct the endorphin and enkephalin deficiencies, boost the immune system, and fight the inflammation and sickness responses to diseases.
Health Benefits of Low Dose Naltrexone
1) LDN Can Reduce Pain and Inflammation in Many Conditions
LDN Treats Fibromyalgia Symptoms
Various studies on Fibromyalgia performed at Stanford University found that the drug can significantly help with pain, fatigue, stress levels, mood, general satisfaction, and inflammation. LDN is able to fix these symptoms because it improves immune functioning and increases endorphin neurotransmitters.
LDN improved pain tolerance in cold pressor tests (CPT) and the ability for fibromyalgia patients to relate interpersonally with others and participate in human relationships.
LDN Reduces Pain and Swelling in Rheumatoid Arthritis
Ten patients with this disease have been treated with LDN. In all ten patients, the joint pain and swelling cleared. When patients stopped taking LDN for a few weeks or experienced periods of severe stress, it resulted in exacerbation of the condition.
LDN Amplifies Anticonvulsant and Anti-Pain Effects of Drugs
When low doses of naltrexone were combined with cannabinoids or opioids such as morphine or buprenorphine, their ability to reduce seizure risk and feelings of pain were amplified.
In one study with 10 patients, a buprenorphine:naltrexone ratio of 166:1 was found to have the greatest effect on pain tolerance for patients in a cold pressor pain test.
The anticonvulsant effects of opioids and cannabinoids were greatly increased when combined with low dose naltrexone in a study with mice. This means patients with diseases like epilepsy are less likely to have new seizures.
In addition, LDN was able to help patients avoid a buildup of tolerance to the anticonvulsant effects of morphine in another study done with mice.
LDN Helps with CRPS Symptoms
Complex regional pain syndrome (CRPS) is evoked/aggravated by symptoms that may be associated with local small intestinal bacterial overgrowth, obstructive sleep apnea, and potential increased microglial activity.
Since low dose naltrexone can block microglial toll-like receptors and induce production of endorphins, it is able to significantly reduce inflammation. The improvement provides relief to CRPS patients.
Low dose naltrexone can enhance the pain relieving properties of acupuncture which can also be helpful for CRPS patients.
A common symptom of patients with CRPS is dystonia. In this study, two patients were treated with low dose naltrexone in the hope that it would block the Toll-like receptor 4 (TLR4) to decrease neuroinflammation. After treatment, both patients had a decrease in pain, fixed dystonia, and dystonic spasms in their extremities.
LDN Helps with Pain in Transverse Myelitis
Transverse myelitis (TM) is characterized by inflammation of the spinal cord with varying degrees of motor, sensory and autonomic dysfunction.
This study followed one patient with TM who was unresponsive to multiple pain medications and immune-modulation therapies but noticed an improvement in neuropathic pain with low dose (3-4.5 mg) Naltrexone.
This occurred because LDN is a TLR4 antagonist and therefore stops the microglial activation and sensitization process.
In addition, low doses of Naltrexone do not inhibit other opioid receptors in the central nervous system, thereby allowing endogenous anti-pain pathways to continue operating.
2) LDN Effectively Treats Irritable Bowel Syndrome
This pre-clinical study assessed 42 Irritable Bowel Syndrome (IBS) patients. Participants received 0.5 mg per day for 4 weeks and were evaluated during baseline, treatment, and at a 4-week follow-up.
Patients initially reported degrees of abdominal pain, stool urgency, consistency, and frequency.
Treatment with LDN resulted in a number of pain-free days and overall symptom relief, evaluated by a global assessment score. Global assessment improved in 76% of 42 patients. During treatment, the mean weekly number of pain-free days increased from 0.5+/-1 to 1.25+/-2.14 (P=0.011).
There were no significant side effects.
Overall, patients noticed improvements in pain and relief from symptoms.
3) LDN Effectively Treats Inflammatory Bowel Disease
Multiple studies have shown that low dose naltrexone was able to treat patients with Irritable Bowel Disease (IBD). Crohn’s disease and Ulcerative Colitis are two common examples of this chronic relapsing bowel disorder.
In this study, Dr. Bihari followed eight patients who had Crohn’s Disease and were on LDN. In all eight cases, within 2-3 weeks the signs and symptoms of disease activity stopped. All eight remained stable anywhere from 2 months to multiple years afterward.
In a study with 14 children with Crohn’s, LDN was used to treat their condition. After an 8-week course of naltrexone therapy, twenty-five percent were considered in remission, and 67% had improved with mild disease activity. The systemic and social quality of life improved with naltrexone treatment as well.
Patients with ulcerative colitis that don’t notice improvements in symptoms from other medications may find relief with LDN. A study of 40 ulcerative colitis patients found that 30% of the severe cases responded to treatment, and 20% showed lasting benefits.
Amongst the long-term responders, many went into remission. Most of them are still in remission today, but 3 patients relapsed at 11, 12, and 21 months.
4) LDN Blocks Activation of Microglia
LDN is also known to block activation of microglia, a type of white blood cells found in the central nervous system. Activation of microglia causes common symptoms associated with sickness such as fatigue, fever, inflammation, and pain.
Blocking activation of microglial cells results in a reduction of proinflammatory cytokines as well as neurotoxic superoxides by blocking Toll-like receptor 4 (TLR4), which can control the body’s response to inflammation.
5) LDN Fights Cancer
LDN has been known to treat cancers such as bladder cancer, breast cancer, carcinoid tumors, colorectal cancer, glioblastoma, liver cancer, lung cancer (non-small cell), leukemia, lymphoma, melanoma, myeloma, neuroblastoma, ovarian cancer, pancreatic cancer, prostate cancer, renal cell carcinoma, throat cancer, thyroid cancer, and uterine cancer.
Some patients treated with LDN who were deemed terminal with little time left are still alive and doing well years later.
This study in mice found that LDN can be coupled with chemotherapy and radiotherapy; it is a unique, non-toxic, cancer therapy.
LDN increases the number and density of opiate receptors on the tumor cell membranes, making them more responsive to the growth-inhibiting effects of endorphins. It also increases the amount of cytotoxic T cells, natural killer cells, and both of their activities. All these factors cause cancer cells to die.
In a study having approximately 450 cancer patients directed by Dr. Bihari, nearly a quarter of his patients had at least a 75% reduction in tumor size, and nearly 60% of his patients demonstrated disease stability.
A study on ovarian cancer found that LDN reduced DNA synthesis, blood vessel development, and cell replication.
Exposure to LDN in combination with cancer drugs enhanced anti-cancer action.
LDN combined with a chemotherapy drug, cisplatin, alleviated the toxicity associated with cisplatin.
It increased the production of the opioid growth factor which inhibits ovarian cancer cell growth.
6) LDN Helps With Degenerative Brain Disorders
Naltrexone and Alzheimer’s Disease
In patients with degenerative illnesses like Alzheimer’s, the illness progression is slowed. People with Alzheimer’s disease do not regain already lost function, so it is crucial to begin the treatment as early as possible.
Improvements in symptoms from naltrexone (high dose) include better mood and behavior, less confusion, and stronger memory. The same may not hold true for low dose naltrexone.
LDN Alleviates Symptoms in Parkinson’s Disease
In Dr. Bihari’s study of seven Parkinson’s patients, LDN was able to stop the progression of the condition, and the signs and symptoms subsided. One patient was not seeing improvement in his condition so he discontinued LDN, but his symptoms immediately worsened. After resuming LDN, he experienced a reversal of the progression that had occurred while off of the drug. His symptoms subsided, and even his depression subsided.
In another patient, taking low dose Naltrexone resulted in the disappearance of the glabellar sign, a common symptom in PD patients.
Other symptoms which improved include tremors, sleep issues, and ability to smell, just to name a few.
LDN May Treat ALS and PLS
In patients with degenerative illnesses such as Amyotrophic Lateral Sclerosis (ALS/Lou Gehrig’s Disease) and Primary Lateral Sclerosis (PLS), the illness progression is slowed. People with ALS may even regain already lost function.
Patients notice improvements in muscle weakness, spasms, physical and speech coordination, ability to breathe, and fatigue.
In one small study, two patients showed significant improvement in their breathing, as measured by a forced vital capacity (FVC). One had a 25% improvement within two months of beginning LDN and the other an 11% improvement. A third patient had improvement in his ability to breathe and a reduction in his resting pulse from 96 to the low 80’s.
7) LDN Effectively Treats Patients with Autism
In one study of autistic children, behavioral improvements were observed as early as half an hour after dosing. LDN also increased verbal production and decreased autistic stereotypies (repetitive or ritualistic movement, posture, or utterance) (R).
Other studies found improvements in focus, mood, and behavior due to decreased anxiety and hyperactivity. LDN is unable to completely bridge the learning disadvantage for children with autism, but it is a start.
Dr. Jaquelyn McCandless has found a very positive effect of LDN in appropriately reduced dosage and applied as a transdermal cream, in children with autism.
8) LDN Improves PTSD Symptoms
In one study, 11 out of 15 patients with post-traumatic stress disorder (PTSD) who were treated with LDN felt multiple positive effects.
They reported a clearer perception of both their surroundings and their inner life. Their assessment of reality and dealing with it improved. Lastly, their perception of their own body, effects on others, and self-control got better.
9) LDN Can Improves Mood and Quality of Life
Low dose naltrexone plays a role in promoting healthy immune system control which reduces various cancerous and inflammatory autoimmune processes. This, in turn, results in less pain in patients.
In addition, LDN can increase opioid activity which promotes stress resilience, exercise, social bonding, and emotional well-being, as well as an improvement in psychiatric problems such as autism and depression. These benefits are attributed to its ability to impact both the immune system and the brain’s neurochemistries.
10) LDN Decreases Nausea in Trauma Patients
When LDN was used in conjunction with morphine in patients with trauma to their upper and lower extremities, it did not decrease pain any more than morphine alone. However, it did lower the risk of nausea in the trauma patients.
11) LDN Alleviates Itchiness and Maybe Histamine Intolerance
In this study, patients were put in a functional magnetic resonance imaging (fMRI) machine to observe the central nervous system processing of itch caused by histamine and capsaicin. Histamine and capsaicin cause itching, burning, stinging, or prickling feelings in patients. However, when the patients were treated with LDN, they noticed a reduction in the itching sensation. This was confirmed by significantly less fMRI activation.
Itchiness is also a common symptom associated with conditions like systemic sclerosis/scleroderma and psoriasis, and LDN may be able to help.
This study found that 3 female patients with systemic sclerosis all noticed significant improvements in the pruritus symptom (severe itching of the skin). It is believed that this symptom of these illnesses is increased by the inflammation from autoimmune gastrointestinal disorders which these patients often have as well.
12) LDN Enhances Maturation of Bone Marrow Dendritic Cells
This study evaluated both phenotypic and functional maturation of bone marrow dendritic cells (BMDCs). They found that LDN enhances maturation of BMDCs by increasing the expression of Costimulatory Molecules including MHC II, CD40, CD83, CD80 and CD86 molecules.
It also decreased the rates of pinocytosis and phagocytosis. This was accompanied by the results of decreased ACP, and FITC-dextran bioassay.
The study confirmed that LDN plays a role in immune system management, enhances host immunity in cancer therapy, and can be used in the design of dendritic cell-based vaccines.
13) LDN Can Help Patients Struggling with Drug Problems
LDN Can Help Treat Opioid Withdrawal and Detox Patients
LDN improved pain tolerance in cold pressor tests (CPT) and the ability for post-detoxification patients to relate interpersonally with others and participate in human relationships.
In a study of 127 patients undergoing a 6-day methadone taper, very low dose naltrexone (VLNTX) and clonidine were used to decrease withdrawal intensity and noradrenaline release.
Withdrawal symptoms and treatment completion were compared following VLNTX (.125 or .25 mg/day) and clonidine (.1-.2 mg). Both medicines used together resulted in a reduction of withdrawal symptoms such as shaking, anxiety, bone and muscle aches, restlessness, and craving, as well as lacrimation, rhinorrhea, and sweating.
Of the four groups in the study, the group that took both medications had the highest study retention at 85.3%; the average of the four was 66.9%. This shows that taking both medications had a significant effect on treatment completion and success.
LDN Reduces Craving and Drug Response in Heavy-Drinking Smokers
In one study with 130 heavy-drinking daily smokers, a combination of LDN and Varenicline was able to reduce cigarette and alcohol cravings, as well as the strength of the “high” feeling associated with both drugs (Varenicline; 1 mg twice daily, LDN; 25 mg once daily).
LDN Can Help Prevent Cocaine Relapse
This study on rats used a combination of levo-tetrahydropalmatine (l-THP) and low dose naltrexone (LDN), targeting primarily dopaminergic and endogenous opioid systems as a cocaine-relapse-prevention treatment.
The combination of the medicines reduced the drug-seeking tendencies of the rats in various scenarios. Locomotion (movement) in the rats was increased on the two drugs as well.
These effects can be attributed to the increase of beta-endorphin and increased POMC expression in the rats.
14) LDN is Effective in Treating HIV/AIDS
After Dr. Bihari had been treating hundreds of AIDS patients with LDN and accepted AIDS therapies for over 7 years, 85% of the patients had no detectable levels of the virus in their systems. This is a much higher success rate compared to most AIDS treatments, and with no side effects.
Many HIV/AIDS patients are living symptom-free for years while taking only LDN.
In patients with HIV/AIDS, low levels of beta-endorphin are found in the bloodstream. LDN is able to correct this deficiency when blocking the opioid receptors and then allowing them to open back up again.
LDN successfully treats HIV/AIDS due to its ability to stop the deterioration of Helper T cells.
The abnormal buildup of fat caused by HIV drugs usually improves significantly with LDN.
15) LDN Alleviates Symptoms in Multiple Sclerosis
People with Multiple Sclerosis (MS) may find relief from their condition by taking LDN. Some patients report up to 90% improvement in their symptoms. MS patients often note relief from spasticity, fatigue, and bladder problems.
In Dr. Bihari’s study, less than 1% of MS patients ever experienced a new attack of the disease while taking LDN.
For MS patients that experience muscle spasms at the 4.5 mg dosage, lowering the medicine to 3 mg per day may help reduce this symptom.
Consult with your physician before taking LDN to see if it is safe and the correct medication for your condition.
LDN is a prescription drug and should be taken once a day, usually at bedtime.
Depending on what your doctor prescribes for you, dosages can range from 1.5 mg to 3 mg to 4.5 mg.
Avoid slow/timed-release naltrexone and LDN capsules which contain calcium carbonate filters.
LDN is usually taken as a pill, but topical creams have successfully been developed as well.
In the clinical trials that have been done to date, most patients don’t experience any side effects, but those who do tend to find that their symptoms subside within a few days to a week. Symptoms include trouble sleeping, increased vivid dreams, nausea, gas, bloating, upset stomach, hunger pangs, and increased spasticity.
LDN shouldn’t be taken with narcotic painkillers or immunosuppressive drugs.
I have been informed that there are anecdotes on the web about some people with CFS and mold illness who don’t react well to LDN. If you’re getting side effects, you should speak to your healthcare practitioner.
- Because LDN blocks opioid receptors throughout the body, a person using medicine that is an opioid activator (narcotic medication) should not take LDN until such medicine is completely out of one’s system. Patients who have become dependent on the daily use of narcotic-containing pain medication may require 10 days to 2 weeks before being able to begin LDN safely.
- Full-dose naltrexone carries a cautionary warning against its use in those with liver disease. However, LDN will not produce impairment of liver function.
- People who have had organ transplants and are taking immunosuppressive medication permanently are cautioned against the use of LDN.