Low Dose Naltrexone
A promising immunomodulatory agent for many immune-related diseases.
- Immune Modulation
- Anti-Inflammatory Effects
- Mental health benefits
Low Dose Naltrexone (LDN) operates by binding to and temporarily blocking opioid receptors, a mechanism typically associated with higher doses of the medication. At lower doses, approximately ranging from 1 to 5 mg, LDN is believed to stimulate the production of endorphins, the body's natural opioids. This unique modulation of endorphin levels contributes to its potential in immune modulation, anti-inflammatory effects, and influencing cellular processes for overall well-being.
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The science of Low Dose Naltrexone
Active ingredients
The active ingredient in low dose naltrexone (LDN) is naltrexone hydrochloride, typically administered in very low doses ranging from 1.5 to 4.5 milligrams. In addition to the active ingredient, LDN formulations may contain inactive ingredients such as fillers, binders, and coating agents to facilitate proper dosage form and administration.
Mechanism
Low Dose Naltrexone (LDN) is typically administered orally, and the recommended dosage often falls within the range of 1 to 5 mg. It is crucial to follow the prescribed dosage and administration guidelines provided by healthcare professionals. LDN is commonly taken at night before bedtime to minimize potential side effects, and it is advisable to avoid consuming opioid-containing medications during the LDN regimen to prevent interference with its effects.
History
Low Dose Naltrexone (LDN) has a rich history of over 40 years of prescription use, primarily known for its exceptional safety record. Originally FDA-approved for treating opioid dependencies and obesity at higher doses, LDN gained prominence for its alternative use at lower dosages, with 4.5mg/day being the most common. Beyond its conventional applications, LDN has exhibited novel and paradoxical effects, garnering attention for potential therapeutic benefits across various conditions. Since 1985, LDN has been explored in the treatment of autoimmune diseases and viral infections, sparking ongoing research and discussions within the medical community.
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Frequently Asked Questions
A good candidate for low dose naltrexone (LDN) typically has a chronic condition such as autoimmune disease, chronic pain, or inflammation. They may also be seeking alternatives to traditional treatments or have had limited success with conventional therapies.
LDN has shown promise in managing various conditions such as autoimmune diseases like multiple sclerosis, rheumatoid arthritis, and Crohn's disease, as well as chronic pain conditions like fibromyalgia and neuropathic pain. Research also suggests potential benefits for mood disorders, neurodegenerative diseases, and immune system dysregulation.
LDN works by temporarily blocking opioid receptors in the brain, which leads to a rebound increase in endorphin production. This increase in endorphins is believed to modulate immune function, reduce inflammation, and potentially alleviate symptoms associated with various conditions.
Naltrexone administration can lead to a variety of side effects across multiple body systems. Gastrointestinal effects are common, with nausea occurring in 33% of patients, and other symptoms like abdominal pain, decreased appetite, diarrhea, and vomiting also reported. The nervous system can be affected, with notable side effects including anxiety, asthenia, headaches, insomnia, and dizziness. Liver enzyme levels may increase, indicating potential hepatic side effects, and neuromuscular & skeletal complaints such as arthralgia, arthritis, and increased creatine phosphokinase levels are observed. Less common and postmarketing side effects span a wide range, including dermatologic, respiratory, cardiovascular, and hypersensitivity reactions, highlighting the broad impact naltrexone can have on patients.
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Important Safety Information
While Low Dose Naltrexone (LDN) is generally well-tolerated, some individuals can experience side effects across multiple body systems. Gastrointestinal effects are common, with nausea occurring in 33% of patients, and other symptoms like abdominal pain, decreased appetite, diarrhea, and vomiting also reported. The nervous system can be affected, with notable side effects including anxiety, asthenia, headaches, insomnia, and dizziness. Liver enzyme levels may increase, indicating potential hepatic side effects, and neuromuscular & skeletal complaints such as arthralgia, arthritis, and increased creatine phosphokinase levels are observed. Less common and postmarketing side effects span a wide range, including dermatologic, respiratory, cardiovascular, and hypersensitivity reactions, highlighting the broad impact naltrexone can have on patients.
Any of the following are contraindications to taking the medication:
- People with hypersensitivity to any component of the medication
- Current physiological opioid dependence or current use of opioid analgesics (including partial opioid agonists)
- Acute opioid withdrawal
- People with alcohol use disorder
- Moderate-Severe Liver Disease
- Moderate-Severe Kidney Disease
- History of Depression
- History of Suicide Ideation or Attempt
- Pregnant women, women attempting to conceive, and women at high risk of pregnancy
- Women who are breast-feeding
Interacting drugs include, but not limited to:
Bremelanotide
May decrease the serum concentration of Naltrexone.
Risk X: Avoid combination
Lofexidine
May decrease the serum concentration of Naltrexone.
Risk C: Monitor therapy
Methylnaltrexone
May enhance the adverse/toxic effect of Opioid Antagonists. Specifically, the risk for opioid withdrawal may be increased.
Risk X: Avoid combination
Naldemedine
Opioid Antagonists may enhance the adverse/toxic effect of Naldemedine. Specifically, the risk for opioid withdrawal may be increased.
Risk X: Avoid combination
Naloxegol
Opioid Antagonists may enhance the adverse/toxic effect of Naloxegol. Specifically, the risk for opioid withdrawal may be increased.
Risk X: Avoid combination
Opioid Agonists
Naltrexone may diminish the therapeutic effect of Opioid Agonists.
Management: Seek therapeutic alternatives to opioids. See full drug interaction monograph for detailed recommendations.
Risk X: Avoid combination
Sibutramine
May enhance the adverse/toxic effect of Centrally Acting Weight Loss Agents.
Risk X: Avoid combination
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