Naltrexone was first made in 1963 as an orally active competitive opioid receptor antagonist. It is structurally and functionally similar to the opioid antagonist naloxone, but it has greater oral bioavailability and a longer biologic half-life.
Low-dose naltrexone (LDN) is an off-label use of the drug naltrexone, which is traditionally used in much higher doses to treat opioid and alcohol dependence. When used in low doses (typically 0.5 to 4.5 mg), it has been found to have paradoxical properties in various autoimmune diseases, chronic pain conditions, including fibromyalgia, and other inflammatory disorders.
Here are some key points about LDN:
Mechanism of Action:
- Endorphin Modulation: LDN is believed to work by temporarily blocking opioid receptors, which leads to an increase in the production of endorphins and enkephalins. These are natural painkillers and immune modulators in the body.
- Immune System Regulation: It modulates the immune system, potentially reducing inflammatory responses and offering relief in autoimmune conditions.
Uses:
- Autoimmune Diseases: LDN has been studied for conditions like multiple sclerosis (MS), Crohn's disease, and lupus.
- Chronic Pain: It may help with fibromyalgia, complex regional pain syndrome (CRPS), and other chronic pain conditions.
- Mental Health: Some research suggests it may benefit conditions like depression and anxiety, potentially due to its effects on endorphins.
- Other Conditions: LDN is also explored for its benefits in conditions like cancer, HIV/AIDS, and Parkinson’s disease.
Benefits:
- Reduced Inflammation: LDN can help reduce inflammation, which is beneficial for various chronic inflammatory conditions.
- Pain Relief: By increasing endorphin levels, LDN can help manage chronic pain.
- Immune Modulation: It can potentially normalize immune function, helping in autoimmune diseases.
Side Effects:
- Mild and Transient: Side effects are generally mild and can include sleep disturbances, vivid dreams, headaches, and digestive issues. These often subside with continued use.
- Tolerance: Most users tolerate LDN well, especially at low doses.
Dosage and Administration:
- Low Dose: Typically, the dose ranges from 0.5 to 4.5 mg per day, taken at bedtime.
- Gradual Increase: Starting with a low dose and gradually increasing can help minimize side effects.
- Prescription: LDN requires a prescription and should be used under medical supervision.
Research and Evidence:
- Clinical Trials: There is a growing body of research supporting the efficacy of LDN for various conditions, though more large-scale, randomized controlled trials are needed.
- Anecdotal Evidence: Many patients report significant benefits, contributing to its popularity despite the need for more comprehensive clinical studies.
Considerations:
- Not licensed for Low Dose: While naltrexone is approved for addiction treatment, LDN is not specifically approved for the conditions mentioned and is considered off-label use.
Buccal Film
APC Labs has compounded low-dose naltrexone into a transmucosal buccal film for an easy and superior drug delivery. The transmucosal film uses an advanced drug delivery technology that allows the active ingredients to be delivered across the buccal mucosa of the mouth. The mucoadhesive properties of the film keep it firmly in place while it dissolves, releasing the active ingredient, which then diffuse across the mucosa straight into the bloodstream. Since the active ingredients are not swallowed but rather are allowed to diffuse across the buccal mucosa, they enter the bloodstream directly without having to pass through the acidic environment of the stomach and the liver. This means that the active ingredient bypasses the degradative effects of the stomach and the first-pass metabolism of the liver, meaning more of the drug reaches the circulation.
This formulation is utilised in the treatment of a wide range of diseases, including Multiple Sclerosis (MS), various autoimmune diseases, Fibromyalgia, Ulcerative Colitis, Irritable Bowel Syndrome (IBS), and Pain. When naltrexone is administered in the low dose of 4.5mg, it has been proven to be an effective and safe treatment option for these conditions and can be prescribed by a healthcare provider.
