Introduction of low-dose Naltrexone (LDN)

Low-dose naltrexone (LDN) is a medication that can help in the treatment of a variety of cancers, central nervous system disorders, autoimmune diseases and several other conditions. Naltrexone was initially approved by the Food and Drug Administration (FDA) and prescribed in much higher doses to treat drug and alcohol addiction. This article focuses on the lower doses of naltrexone (1.5 to 4.5 mg) and its multiple medicinal benefits(R).

How does LDN work?

LDN works by blocking the opioid growth factor and opioid growth factor receptor pathways in the body, which boosts the body's immune system and natural defenses. The temporarily blocked pathway causes your body to try 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 in the immune system (R1,R2). Cancer and autoimmune diseases are triggered by low endorphin levels in the blood, contributing to disease-related immune deficiencies. For example, HIV/AIDS is accelerated by a lack of endorphins (R). Conclusion: LDN is able to correct endorphin and enkephalin deficiencies, boost the immune system and combat the inflammatory and disease response of disorders.

Health benefits of low-dose naltrexone


1) LDN can reduce pain and inflammation for many conditions
LDN treats symptoms of fibromyalgia

Several studies on fibromyalgia conducted at Stanford University showed that the drug is significantly effective in controlling pain, fatigue, stress levels, mood, overall satisfaction and inflammation. LDN is able to alleviate these symptoms because this drug improves immune system function, increases endorphin neurotransmitters(R), makes the receptors (OGFR) endorphins more sensitive and increases their number. LDN improves pain tolerance in cold pressor tests (CPT) and the ability of patients with fibromyalgia to interact interpersonally with others and participate in human relationships (R). LDN reduces pain and swelling in rheumatoid arthritis Ten patients with this disease were treated with LDN. In all patients, joint pain and swelling decreased. When patients stopped LDN for several weeks or experienced periods of severe stress, this led to deterioration of the condition (R). LDN enhances antiepileptic and anti-pain effects of drugs When low doses of naltrexone were combined with cannabinoids or with opioids such as morphine or buprenorphine, it reduced the risk of seizures and pain sensations. In a study of 10 patients, a buprenorphine:naltrexone ratio of 166:1 was found to have the best effect on patients' pain tolerance during a cold pressor pain test (R). In a study on mice, the antiepileptic effects of opioids and cannabinoids increased significantly when combined with low-dose naltrexone. This means that patients with conditions such as epilepsy have a lower risk of having new seizures (R). In addition, in another study on mice, LDN prevented the build-up of tolerance to the antiepileptic effects of morphine (R). LDN helps with CRPS symptoms Complex regional pain syndrome (CRPS) is induced/exacerbated by symptoms possibly related to local bacterial overgrowth in the small intestine, obstructive sleep apnea and potential increased microglial activity (R). Since low-dose naltrexone can block microglial Toll-like receptors and induce endorphin production, the drug is able to significantly inhibit inflammation. The improvement provides relief to patients with CRPS (R). Low-dose naltrexone can enhance the pain-relieving properties of acupuncture. This may also be useful for patients with CRPS. (R). A common symptom of patients with CRPS is dystonia. In this study, two patients were treated with low-dose naltrexone with the hope that it would block Toll-like receptor 4 (TLR4) to reduce neuroinflammation. After treatment, both patients experienced reduced pain, dystonia and dystonic spasms in their extremities (R). LDN helps with pain in transverse myelitis Transverse myelitis (TM) is characterized by inflammation of the spine with varying degrees of motor, sensory and automatic dysfunction (R). This study followed a patient with TM who did not respond to multiple pain medications and immune modulation therapies, but did see improvement in neuropathic pain with a low dose (3-4.5 mg) of naltrexone (R). This was because LDN is a TLR4 antagonist and therefore stops microglial activation and the sensitization process (R). Moreover, low doses of naltrexone do not disrupt other opioid receptors in the central nervous system and endogenous anti-pain pathways remain in effect (R).

2) LDN is effective in treating inflammatory (inflammatory-like) bowel diseases

This pre-clinical study evaluated 42 patients with inflammatory bowel disease (IBD). Participants received 0.5 mg daily for 4 weeks and were tested at baseline, during treatment and 4 weeks after treatment (R). Patients initially reported measures of abdominal pain and increased urgency, consistency and frequency of bowel movements (R). Treatment with LDN led to a number of pain-free days and decrease in overall symptoms, evaluated by global assessment score. The global assessment score increased in 76% of 42 patients.During treatment, the mean number of weekly pain-free days increased from 0.5+/-1 to 1.25+/-2.14 (P=0.011) (R). There were no significant side effects (R). Patients experienced improvements in pain and symptom relief (R).

3) LDN is effective in treating inflammatory bowel disease 

Multiple studies have shown that low-dose naltrexone is effective in treating patients with inflammatory bowel disease (IBD). Crohn's disease and Ulcerative Colitis are two other examples of this chronic bowel disease (R). In this study, Dr. Bihari followed eight patients with Crohn's disease who were taking LDN. In all eight cases, the signs and symptoms of disease activity stopped. All eight patients remained stable for periods between 2 months and several years after the study (R). In a study of 14 children with Crohn's disease, LDN was used to treat their condition. After an 8-week period of naltrexone therapy, 25% were in remission and showed improvement with mild disease activity in 67% of cases.Systemic and social quality of life also increased (R). Patients with ulcerative colitis who experience no improvement in symptoms with other medications may be able to find relief with LDN. A study of 40 patients with ulcerative colitis showed that 30% of severe cases responded to treatment and 20% experienced lasting benefits (R). Of the participants with a long-term response, many experienced remission. Most are still in remission today, but 3 patients relapsed after 11, 12 and 21 months (R).

4) LDN blocks the activation of microglia

LDN blocks the activation of microglia. This is a type of white blood cell in the central nervous system. Activation of microglia causes symptoms common to illness, such as fatigue, fever, inflammation and pain (R). Blocking activation of microglial cells leads to a decrease in pro-inflammatory cytokines and neurotoxic superoxides by blocking the Toll-like receptor 4 (TLR4) that can control the body's response to inflammation (R).

5) LDN supports the immune system in fighting cancer

LDN is known to have immunosuppressive effects in the treatment of cancers, including bladder cancer, breast cancer, carcinoid tumors, colorectal cancer, glioblastoma, liver cancer, lung cancer (non-small cell), leukemia, lymphoma, skin cancer, neuroblastoma, ovarian cancer, pancreatic cancer, prostate cancer, kidney cancer, throat cancer, thyroid cancer and uterine cancer (R). LDN increases the number and density of opiate receptors on the membranes of tumor cells, making them more receptive to the growth-inhibitory effects of endorphins. It also increases the number and activity of cytotoxic T cells, natural killer cells. All these factors can cause the cancer cells to die(R1,R2). In a study of about 450 cancer patients directed by Dr. Bihari, nearly a quarter of his patients showed a reduction in tumor size of at least 75%, and nearly 60% of his patients showed disease stability(R). A study of ovarian cancer showed that LDN reduced DNA synthesis, blood vessel development and cell replication (R). Exposure to LDN in combination with cancer drugs enhanced anti-cancer activity (R). LDN in combination with a chemotherapy drug (cisplatin) alleviated the toxicity associated with cisplatin (R). Another studen saw an increase in the production of opioid growth factor, which inhibits the growth of cancer cells in ovarian cancer (R).

6) LDN helps with degenerative brain disorders.

Naltrexone and Alzheimer's Disease progression in patients with degenerative diseases such as Alzheimer's is slowed. People with Alzheimer's do not regain lost functions, so it is crucial to start treatment as early as possible (R). Improvements in symptoms of naltrexone (high dose) include improved mood and behavior, less confusion and more powerful memory (R). The same may be true for low-dose naltrexone. LDN relieves symptoms of Parkinson's In a study by Dr. Bihari of seven patients with Parkinson's, LDN stopped the progression of the condition and signs and symptoms decreased. One patient noticed no benefits and stopped treatment, after which his symptoms immediately worsened. After resuming LDN, he experienced a reversal of the progression this occurred when he was not taking the drug. His symptoms decreased and his depression even disappeared(R). In another patient, a low dose of naltrexone led to the disappearance of the glabella reflex, which is a common symptom in patients with parkinson's (R). Other symptoms that improved were tremors, sleep problems and the sense of smell, to name a few (R). LDN possibly effective in treating ALS and PLS In patients with degenerative diseases such as ALS and PLS, the disease may be inhibited. People with ALS may even regain their lost functions. Patients experience improvements in muscle weakness, spasms, physical and speech coordination, breathing and fatigue (R). In a small study, two patients showed significant improvements in breathing, measured by forced vital capacity. One patient saw a 25% improvement within two months of starting LDN and the other saw an 11% improvement. A third patient could breathe better and had a lower resting heart rate (from 96 beginning 80 (R).

7) LDN effective in treating patients with autism

In a study with autistic children, behavioral improvements were observable as early as half an hour after administration of the drug. LDN also improved verbal production and reduced autistic stereotypy (repeated or ritualistic movements, posture or expression) (R). Other studies found improvements in concentration, mood and behavior caused by reduced anxiety and hyperactivity. LDN is not able to wipe out the entire learning disability of autistic children, but it is a good start (R). Dr. Jaquelyn McCandless found a very positive effect of administering an appropriately reduced dose of LDN as a transdermal cream in children with autism (R).

8) LDN improves symptoms of PTSD

In one study, 11 of 15 patients with post-traumatic stress disorder (PTSD) treated with LDN experienced multiple positive effects. They reported a clearer perception of both their environment and their inner lives. Their assessment of reality and coping improved. Finally, their perception of their own bodies, effect on others and self-control improved (R).

9) LDN can improve mood and quality of life

Low dose naltrexone plays a role in promoting healthy control of the immune system, which decreases various carcinogenic and inflammatory autoimmune processes.This in turn leads to less pain in patients. In addition, LDN can increase opioid activity which promotes stress tolerance, exercise, social bonding and emotional well-being, and leads to an improvement in psychiatric problems such as autism and depression.These benefits are attributed to LDN's ability to affect the neurochemistry of both the immune system and the brain (R).

10) LDN reduces nausea in patients with trauma

When LDN was used in combination with morphine in patients with trauma to their upper and lower extremities, it did not relieve pain more than when morphine alone was administered. However, it did reduce the risk of nausea in patients with trauma(R).

11) LDN reduces itching and possible intolerance to histamine

In this study, patients were placed in a functional magnetic resonance imaging (fMRI) machine to observe the processing of itching caused by histamine and capsaicin by the central nervous system. Histamine and capsaicin cause itching, burning, stinging or stabbing sensations in patients. However, when patients were treated with LDN, it led to a decrease in the itching sensation. This was confirmed by significantly less fMRI activation (R). Itching is also a common symptom related to conditions such as systemic sclerosis/scleroderma and psoriasis, and LDN may potentially help with this (R1,R2). This study found that three female patients with systemic sclerosis all experienced significant improvements related to severe itching. It is believed that this symptom of this disease is exacerbated by the inflammatory autoimmune gastrointestinal conditions that these patients often also have (R).

12) LDN enhances the development of bone marrow dendritic cells

This study evaluated both the phenotypic and functional development of bone marrow dendritic cells (BMDCs).They found that LDN enhances the development of BMDCs by increasing the expression of costimulatory molecules, includingMHC II, CD40, CD83, CD80 and CD86 molecules (R). It also decreased the degree of pinocytosis and phagocytosis. This was accompanied by reduced ACP and FITC-dextran bioassay (R). The study confirmed that LDN plays a role in immune system control, enhances host immunity in cancer therapy, and can be used in the development of dendritic cell-based vaccines(R).

13) LDN can help patients with drug problems

LDN may help patients with opioid withdrawal and detoxification LDN improved pain tolerance in cold pressor tests (CPT) and patients' ability after detoxification to interact interpersonally with others and participate in human relationships (R). In a study of 127 patients undergoing a six-day withdrawal from methadone, a very low dose of naltrexone (VLNTX) and clonidine was used to reduce the intensity of withdrawal and the release of norepinephrine. Withdrawal symptoms and treatment completion were compared after administration of VLNTX (0.125 or 0.25 mg/day) and clonidine (0.1-0.2 mg). The combination of both drugs led to a decrease in withdrawal symptoms such as tremor, anxiety, bone and muscle pain, restlessness and cravings, as well as tearfulness, colds and sweating (R). Of the four groups in the study, the group taking both drugs had the highest study retention of 85.3%; the average of the four groups was 66.9%. This shows that taking both medications had a significant effect on treatment completion and success (R). LDN reduces cravings and drug response in heavy-drinking smokers In a study of 130 people who smoked daily and drank heavily, a combination of LDN and varenicline was able to reduce cravings for cigarettes and alcohol, as well as the "high" related to both drugs (varenicline; 1 mg twice daily, LDN; 25 mg once daily) (R). LDN may help prevent cocaine relapse This study on rats used a combination of levo-tetrahydropalmatine (l-THP) and low-dose naltrexone (LDN), and focused primarily on dopaminergic and endogenous opioid systems as a treatment for preventing cocaine relapse (R). The combination of the drugs reduced the rats' tendency to search for the drug in different scenarios. The motor skills of the rats also increased after administration of the two drugs (R). These effects can be attributed to the increase in beta-endorphin and increased POMC expression in the rats (R).

14) LDN is an effective treatment of HIV/AIDS

Dr. Bihari has treated hundreds of AIDS patients with LDN for seven years. 85% of the patients no longer have detectable levels of the virus in their systems. This is a much higher success rate compared to most other AIDS treatments, and with no side effects (R). Many HIV/AIDS patients live for years without symptoms by using LDN alone (R). Low concentrations of beta-endorphin in the bloodstream were found in patients with HIV/AIDS. LDN is able to correct this deficiency by blocking opioid receptors and then allowing them to reopen (R). LDN offers successful treatment of HIV/AIDS by stopping the deterioration of helper t-cells (R). The abnormal buildup of fat associated with HIV medications usually improves with the use of LDN (R).

15) LDN relieves symptoms of multiple sclerosis

People with multiple sclerosis (MS) may find relief from their condition with the use of LDN. Some patients report an improvement in their symptoms of up to 90%.MS patients often see improvement in spasticity, fatigue and bladder problems (R). In a study by Dr. Biharier feed less than 1% of MS patients ever have a new attack of the disease when using LDN (R). For MS patients who experience muscle spasms at the dose of 4.5 mg, lowering the dose to 3 mg per day may help reduce this symptom (R). Other informationDosage Contact your doctor before taking LDN to see if it is safe and the right medication for your condition. LDN is a prescription medication and should be taken once a day, usually before bedtime (R). The dosage depends on what the doctor prescribes for you and ranges from 1.5 mg to 4.5 mg (R). Avoid slow/timed-release naltrexone and LDN capsules that contain calcium carbonate filters (R). LDN is usually taken as a pill. In addition, topical creams have been successfully developed. Side effects In the clinical studies conducted to date, most patients do not experience side effects. Those patients who do experience side effects often see their symptoms disappear within a few days to a week. Symptoms include difficulty falling asleep, increased lucid dreams, nausea, flatulence, bloating, upset stomach, hunger pangs and increased spasticity (R). LDN should not be combined with narcotic analgesics or immunosuppressive medications (R). There are anecdotes online about people with CFS and fungal diseases who do not respond well to LDN. If you experience side effects you should contact your health care provider. Warning

  • Since LDN blocks opioid receptors in the body, a person taking an opioid activator (narcotic medication) would not take LDN until the drug is completely out of the body. Patients who have become dependent on daily use of pain medications containing narcotics may have to wait 10 days to 2 weeks before they can safely start LDN (R).
  • Full dose of naltrexone contains a warning for users with liver disease. However, LDN will not impair liver function (R).
  • People who have undergone organ transplantation and are on permanent immunosuppressive medications are cautioned against using LDN (R).

source: selfhacked Are you wondering if LDN can do something for you make an appointment for a free informational phone consultation.