While I am a fully licensed physician in Kansas, this communication does not constitute personal medical advice or establish a physician-patient relationship. See your own physician to discuss your particular diagnosis and treatment
Low-dose naltrexone treatment discussion
Naltrexone is not just for addiction.
This drug was developed in the 1960s and was approved by the FDA in the 1980s. Naltrexone is used to treat opioid and alcohol addiction. To learn more about the details of low-dose naltrexone (LDN), feel free to review my Williams Family Medicine Channel YouTube video titled: The Power of Low Dose Naltrexone at: youtu.be/0WUXNar7at8.
Compounded LDN can be used off-label in: chronic pain disorder, complex regional pain, fibromyalgia, cancer pain, prevention of cancer recurrence, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, emphysema, human immunodeficiency virus infection, depression, irritable bowel syndrome, small intestinal bacterial overgrowth, impaired bowel motility, Crohn's disease, mast cell activation syndrome, chronic fatigue syndrome, sarcoidosis, rheumatoid arthritis, multiple sclerosis, allergies, and thyroiditis. The literature suggests that multiple sclerosis, cancer pain, intestinal disorders, and fibromyalgia seem to be the conditions treated most commonly with LDN.
LDN doses of 0.05 to 6 mg orally once daily(instead of 50 mg dosage once daily for addiction) can be prepared at a compounding pharmacy. Most experts recommend starting with lower doses, then titrating up monthly. Common starting dosage is 0.5-1.5 mg daily. A common effective final dose is 4.5 mg, often taken at bedtime. Some providers use pulse dosing: 3 weeks on and 1 week off.
Some LDN side effects: Diarrhea, constipation, dizziness, nausea, insomnia, anxiety, abdominal pain, headache, joint pain, mood changes, vivid dreams. Those GI side effects seem to go away for many people when they switch fillers to something like sucrose or ginger. Avicel (and other forms of cellulose), lactose, acidophilus, etc. seem to be more likely to cause GI problems.
You can use LDN alongside other short acting opioids: Must administer the dose either 4 hours before or 4 hours after the opioid dose for optimal results.
Possible drug interactions: Cytochrome P450 medications.
LDN time of onset of action: Trial for at least 3 month
Precautions: If you have a thyroid disorder and use LDN, your thyroid function often will improve, requiring thyroid medication dosage adjustment.
Basics of opioid receptors:
Endorphin is the endogenous ligand for mu receptors. This has a significant impact on analgesia.
Enkephalin is the lambda receptors endogenous ligand and it protects myocardial tissue from ischemia.
Dynorphin is the endogenous ligand for kappa receptors. This has analgesic properties, can induce anxiety, and can weakly inhibit respiration.
LDN mechanism of action: Anti-inflammatory effects attributed to antagonist effect on toll-like receptor 4, nonopioid receptors found on macrophages and micro glial cells. Toll like receptor 4 belongs to a family of pattern recognition receptors. These receptors are key to infectious and noninfectious stimuli producing an inflammatory response in your body. These receptors are found on blood cells, endothelial cells, cardiac muscle cells, and cells in the central nervous system. Microglia are central nervous system immune cells that produce: inflammation, sensitivity to pain, fatigue, sleeplessness, mood disorders, and cognitive problems. Traditional mechanism is competitive antagonist activity at mu opioid receptors. Low-dose naltrexone promotes T regulatory cell function. T regulatory cells keep the immune system in balance and turn inflammation off.
The LDN mechanistic papers revealed that a short-term opioid receptor blockade with naltrexone (LDN), a general opioid receptor antagonist devoid of intrinsic activity, resulted in an elevation in production of endogenous opioids in response to the blockade. Interference of opioid peptide–opioid receptor interactions for a short time each day (from 4-6 hours) with LDN provided a subsequent window of time (18–20 hours) for the increased levels of endogenous opioids and opioid receptors to elicit a robust functional response and inhibit cell proliferation. In addition, many patients reported an improved sense of well-being and decrease in overall pain, as one might expect with higher levels of opioid production in the body.
Effectiveness:
About 30% of patients with inflammatory bowel disease (Crohn's and ulcerative colitis) are refractory to current medications or relapse over time. LDN boasts a 70% remission rate with mucosal healing in patients that have Crohn's disease. Consider the cost of low-dose naltrexone at $15-100 per month versus Remicade infusion at $5,000 per month. Anecdotal successes have been reported in the following: Hashimoto's disease, Graves' disease, rheumatoid arthritis, lupus, psoriasis, chronic fatigue syndrome, Parkinson's disease, and Alzheimer's disease.
Consider LDN as an alternative to opioids in some cases.
Therapeutic and chronic use of some opioids decrease optimal functioning of the immune system. Immune system effects appear to be mediated by action of opioids on target cells or indirect centrally mediated pathways. Immune cells differentially express opioid receptors. Opioids affect your innate immunity, which includes: macrophages, neutrophils, mast cells, natural killer cells, dendritic cells, and even intestinal barrier integrity. Specifically, morphine has been shown to disrupt tight junction proteins and gut epithelial cells. This disruption can allow translocation of bacteria. In addition, morphine alters the gut microbial composition, reducing bile-deconjugating strains of bacteria and expanding gram-positive pathogens. Opioids also affect adaptive immunity which includes: T cells and B cells. When these 2 aspects of immunity are affected, your body will have decreased pathogen clearance.
Important note: immune altering factors are released from tissue injury. Consider this in the case of surgery and acute injury.
Do not forget other add-on therapies for immune function. Vitamin D promotes T regulatory cell function. Adequate levels of selenium, zinc, and iodine also are important for immune function. Bacillus species probiotics also promote T regulatory cell function. Vitamin A (cod liver oil), curcumin, and omega-3 fatty acids such as EPA and DHA seem to be helpful for immune function.
I hope this information helps you and your loved ones!
Jason Williams, D.O.