Long Live Low Dose Naltrexone

Aging is plagued by inevitability. Marked by a gradual functional decline across body systems, some think this course cannot be corrected.  

We’re dying to believe otherwise. The older and wiser are not sitting around wallowing in their senior status but instead looking for ways to feel better. Longevity, the idea of living healthier, longer lives, is all the rage.  

Now that the World Health Organization recognizes aging as a genuine disease, longevity research is invested in understanding the mechanisms behind the systemic breakdown. And while vitality is complex, and healthy aging theories are bottomless, there’s one hypothesis that stands out:  

Increasing the human health span could depend on immune function. 

The term “immunosenescence” – the deterioration of the immune system as we get older – paints a frightening picture of what the future holds.  

A state of sustained, low-grade inflammation known as inflammaging, can lead to medical problems in our advanced age and accelerate complications: inflammatory and autoimmune conditions, infections, metabolic disease, even malignancies. Immune system dysregulation can be a driver of aging.  

Low Dose Naltrexone: Immune Modulator and Anti-Inflammatory Agent 

Naltrexone’s dose dependent nature allows the drug to have multiple pharmacological targets, eliciting different effects. Low dose naltrexone or LDN, typically compounded at doses between 1 and 5 mg daily, is a therapeutic powerhouse. LDN appears to defy gravity, with its unlimited potential to clinically benefit patients across multiple conditions.  

LDN exhibits a brief opioid receptor blockade, upregulating opioid signaling and expression. This antagonistic effect on opioid receptors can result in both endorphin upregulation and an increased immune response.  

Decreased flares, less fatigue, and improved quality of life are defining characteristics of LDN therapy; its impact on autoimmune disease is compelling. As an immune-modulator, LDN can encourage improved immune system performance, strengthening your patients’ line of defense. 

Chronic inflammatory diseases and pain conditions known to plague us as we age, may also significantly benefit from LDN. An antagonistic effect on toll-like receptor 4 (TLR4) found on macrophages, is thought to provide anti-inflammatory based relief. Patients with chronic pain conditions often find their day-to-day pain diminished, sleep improved, as well as better cognitive function and state of mind. 

Additionally, LDN can work synergistically when combined with other pain therapies, creating a multifaceted method to combat illness. 

Don’t Weight Around 

Over the course of our lifetime, millions will die from conditions related to elevated body weight. Cardiovascular disease and certain cancers are age-related diseases, with risk exacerbated by obesity. LDN is thought to impact brain areas involved in appetite regulation and cravings, helping patients take control of their calories. Coupled with its ability to upregulate endorphins and improve both metabolism and energy, LDN may help manage weight with ease. 

Pharmacist’s Corner 

Most patients experience minimal side effects, especially with dose titration. Established providers know that starting low and going slow is the key to LDN therapy. Compounded scored tablets really shine here, providing patients the flexibility of half or whole tablet dosing for therapeutic titration or divided medication delivery throughout the day. Success hinges on finding the right dose. 

Customizable LDN capsules allow for alternative fillers such as rice flour, which may be better suited for sensitive populations. Younger patients find LDN suspensions easy to swallow, and others prefer hard-pressed, fast-burst sublingual tablets because they are quick and convenient.  

Whatever the preference, personalized LDN brings meaningful convenience to the Belmar community. Ease matters most, as LDN is often a lifelong therapy. 

While sleep disturbances, mild headache and agitation are possible, they are typically transient and easily addressed with temporary dose deductions. Consider halving the dose for a few days, then reinstating the titration.  

Generally, a 3-month trial of LDN is warranted. No contraindications exist, but it is recommended to press pause on prescribing if opioid pain medications are in the mix and consider ultra-low dose naltrexone (ULDN) instead. 

While Belmar’s name may not be synonymous with biohacking just yet, compounded low dose naltrexone boasts a remarkable resume. With longevity in mind, let’s set an intention to thrive, not simply survive.  

References 

  1. Brown N, Panksepp J. Low-dose naltrexone for disease prevention and quality of life. Med Hypotheses. 2009 Mar;72(3):333-7. doi: 10.1016/j.mehy.2008.06.048. Epub 2008 Nov 28. PMID: 19041189. 
  1. Li W, McIntyre RL, Schomakers BV, Kamble R, Luesink AHG, van Weeghel M, Houtkooper RH, Gao AW, Janssens GE. Low-dose naltrexone extends healthspan and lifespan in C. elegans via SKN-1 activation. iScience. 2024 May 8;27(6):109949. doi: 10.1016/j.isci.2024.109949. PMID: 38799567; PMCID: PMC11126937. 
  1. Liu Z, Liang Q, Ren Y, Guo C, Ge X, Wang L, Cheng Q, Luo P, Zhang Y, Han X. Immunosenescence: molecular mechanisms and diseases. Signal Transduct Target Ther. 2023 May 13;8(1):200. doi: 10.1038/s41392-023-01451-2. PMID: 37179335; PMCID: PMC10182360. 
  1. Li Z, You Y, Griffin N, Feng J, Shan F. Low-dose naltrexone (LDN): A promising treatment in immune-related diseases and cancer therapy. Int Immunopharmacol. 2018 Aug;61:178-184. doi: 10.1016/j.intimp.2018.05.020. Epub 2018 Jun 7. PMID: 29885638. 
  1. Holtorf, Kent. (2021, June 4-6) Longevity: How Immune Modulation is the Key to Living Better Longer {Webinar} LDN Research Trust 2021 Virtual Conference. https://ldnresearchtrust.org/longevity-kent-holtorf-md-2021-conference-ldn-low-dose-naltrexone 
  1. Toljan K, Vrooman B. Low-Dose Naltrexone (LDN)-Review of Therapeutic Utilization. Med Sci (Basel). 2018 Sep 21;6(4):82. doi: 10.3390/medsci6040082. PMID: 30248938; PMCID: PMC6313374. 
  1. Younger J, Parkitny L, McLain D. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clin Rheumatol. 2014 Apr;33(4):451-9. doi: 10.1007/s10067-014-2517-2. Epub 2014 Feb 15. PMID: 24526250; PMCID: PMC3962576. 

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