Biology:Low-dose naltrexone

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Short description: Off-label, experimental use of the drug

Low-dose naltrexone (LDN) refers to daily naltrexone dosages that are roughly one-tenth or less of the standard opioid addiction treatment dosage. Most published research suggests a daily dosage of 4.5 mg, but this can vary by a few milligrams.[1] Low-dose naltrexone has been studied for the treatment of multiple chronic pain disorders including fibromyalgia, multiple sclerosis, Crohn's disease, Long COVID, and complex regional pain syndrome.[2]

Naltrexone is approved by the Food and Drug Administration (FDA) for medication-assisted treatment of alcoholism and opioid use disorders.[3] Bernard Bihari's initial off-label usage of naltrexone in doses ranging from 1.5 mg to 3 mg as an adjuvant therapy for acquired immune deficiency syndrome (AIDS) in the 1980s led to the introduction of LDN into clinical practice.[4] Due to a lack of large-scale clinical trials and standardized research aimed at determining appropriate indications for LDN, it has remained an off-label option.[5]

Mechanism of action

Naltrexone and its active metabolite 6-β-naltrexol are competitive antagonists at μ-opioid and κ-opioid receptors, and to a lesser extent at δ-opioid receptors.[6] Standard therapeutic doses of naltrexone block these receptors, which does two things; it prevents inhibition of GABA receptors (normally, signaling through the GABA receptors inhibits the activity of neurons; many recreational drugs inhibit GABA and thus "free up" neuronal activation; preventing inhibition of GABA allows GABA's normal inhibition activity to take place) and it blocks dopamine release (many recreational drugs stimulate dopamine release, which is part of the brain's reward system that creates pleasure).[6] As Naltrexone is a competitive antagonist at the identical sites of action of many opioid agonists, such as morphine, care must be taken to ensure that Low-dose naltrexone is not taken near the same time as these medications, as they will not be as efficacious in relieving pain.[7]

Research

Multiple studies have shown that low-dose naltrexone has promise as a treatment for chronic pain, some autoimmune disorders and cancers.[8][9][10] Studies on the efficacy of low-dose naltrexone for multiple sclerosis (MS) have been inconclusive.[11][12] Clinical trials for treatment of fibromyalgia were initiated in 2021.[13]

Low-dose naltrexone is also being studied in long COVID.[14][15]

A 2018 therapeutic utilization review concluded that low-dose naltrexone may be an appropriate option for treatment of fibromyalgia and irritable bowel disease, but that "Proper clinical trials are needed in order to establish evidence that could lead to correct indications, mode of administration, and other aspects necessary for effective clinical pharmacology of [low-dose naltrexone]."[16] The UK's National Health Service echoed this sentiment in 2020.[17]

Younger et al. (2014) found reduced pro‑inflammatory cytokines and self‑reported pain in fibromyalgia patients using LDN.[18] A 2018 review summarized mixed trial outcomes and emphasized methodological limitations.[19]

A 2023 systematic review published in the Australian Journal of General Practice found that preliminary research into the use of low-dose naltrexone as a treatment for fibromyalgia is promising. All clinical studies examined showed statistically significant improvements in pain and pain tolerance with mild side effects, however, sample sizes were small and the evidence is inconclusive.[20]

A 2025 scoping review article recommended larger, placebo‑controlled Randomized controlled trials with standardized dosing and long‑term follow‑up to establish efficacy and appropriate clinical indications.[21]

References

  1. ↑ Younger, Jarred; Parkitny, Luke; McLain, David (2014-02-15). "The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain". Clinical Rheumatology (Springer Science and Business Media LLC) 33 (4): 451–459. doi:10.1007/s10067-014-2517-2. ISSN 0770-3198. PMID 24526250. 
  2. ↑ Kim, Phillip S.; Fishman, Michael A. (2020). "Low-Dose Naltrexone for Chronic Pain: Update and Systemic Review". Current Pain and Headache Reports 24 (10): 64. doi:10.1007/s11916-020-00898-0. ISSN 1531-3433. PMID 32845365. 
  3. ↑ Sudakin, Daniel (2015-11-06). "Naltrexone: Not Just for Opioids Anymore". Journal of Medical Toxicology (Springer Science and Business Media LLC) 12 (1): 71–75. doi:10.1007/s13181-015-0512-x. ISSN 1556-9039. PMID 26546222. 
  4. ↑ Bihari, Bernard (2013). "Bernard Bihari, MD: low-dose naltrexone for normalizing immune system function". Alternative Therapies in Health and Medicine 19 (2): 56–65. ISSN 1078-6791. PMID 23594453. 
  5. ↑ Toljan, Karlo; Vrooman, Bruce (2018-09-21). "Low-Dose Naltrexone (LDN)—Review of Therapeutic Utilization". Medical Sciences (MDPI AG) 6 (4): 82. doi:10.3390/medsci6040082. ISSN 2076-3271. PMID 30248938. 
  6. ↑ 6.0 6.1 Niciu, Mark J.; Arias, Albert J. (24 July 2013). "Targeted Opioid Receptor Antagonists in the Treatment of Alcohol Use Disorders". CNS Drugs 27 (10): 777–787. doi:10.1007/s40263-013-0096-4. PMID 23881605. 
  7. ↑ Papantoniou, E (2024-04-17). "What to Avoid When Taking Low Dose Naltrexone - Trinova Health" (in en-US). https://www.trinovahealth.com/what-to-avoid-low-dose-naltrexone/. 
  8. ↑ Kim, Phillip S; Fishman, Michael A (26 August 2020). "Low-Dose Naltrexone for Chronic Pain: Update and Systemic Review". Current Pain and Headache Reports 24 (10): 64. doi:10.1007/s11916-020-00898-0. PMID 32845365. 
  9. ↑ Younger, Jarred; Parkitny, Luke; McLain, David (April 2014). "The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain". Clinical Rheumatology 33 (4): 451–9. doi:10.1007/s10067-014-2517-2. PMID 24526250. 
  10. ↑ Zijian Li; Yue You; Noreen Griffin; Juan Feng; Fengping Shan (August 2018). "Low-dose naltrexone (LDN): A promising treatment in immune-related diseases and cancer therapy". International Immunopharmacology 61: 178–184. doi:10.1016/j.intimp.2018.05.020. PMID 29885638. 
  11. ↑ Raknes, Guttorm; Småbrekke, Lars (2017). "Low dose naltrexone in multiple sclerosis: Effects on medication use. A quasi-experimental study". PLOS ONE 12 (11). doi:10.1371/journal.pone.0187423. ISSN 1932-6203. PMID 29099849. Bibcode: 2017PLoSO..1287423R. 
  12. ↑ Ludwig, Michael D.; Turel, Anthony P.; Zagon, Ian S.; McLaughlin, Patricia J. (2016). "Long-term treatment with low dose naltrexone maintains stable health in patients with multiple sclerosis". Multiple Sclerosis Journal - Experimental, Translational and Clinical 2. doi:10.1177/2055217316672242. ISSN 2055-2173. PMID 28607740. 
  13. ↑ Bruun, Karin Due; Amris, Kirstine; Vaegter, Henrik Bjarke; Blichfeldt-Eckhardt, Morten Rune; Holsgaard-Larsen, Anders; Christensen, Robin; Toft, Palle (December 2021). "Low-dose naltrexone for the treatment of fibromyalgia: protocol for a double-blind, randomized, placebo-controlled trial" (in en). Trials 22 (1): 804. doi:10.1186/s13063-021-05776-7. ISSN 1745-6215. PMID 34781989. 
  14. ↑ Steenhuysen, Julie (18 October 2022). "Addiction drug shows promise lifting long COVID brain fog, fatigue". Reuters. https://www.reuters.com/business/healthcare-pharmaceuticals/addiction-drug-shows-promise-lifting-long-covid-brain-fog-fatigue-2022-10-18/. 
  15. ↑ "Safety and efficacy of low dose naltrexone in a long covid cohort; an interventional pre-post study". Brain, Behavior, & Immunity — Health 24. October 2022. doi:10.1016/j.bbih.2022.100485. PMID 35814187. 
  16. ↑ Toljan, Karlo; Vrooman, Bruce (2018). "Low-Dose Naltrexone (LDN)—Review of Therapeutic Utilization". Medical Sciences 6 (4): 82. doi:10.3390/medsci6040082. PMID 30248938. 
  17. ↑ Eve, Marianne (5 February 2020). "What is the evidence for low dose naltrexone for treatment of multiple sclerosis?". Specialist Pharmacy Service. National Health Service. https://www.sps.nhs.uk/wp-content/uploads/2020/02/UKMI_QA_LDNfor-MS_Feb_2020.pdf. 
  18. ↑ Younger, Jarred; Mackey, Sean (2013). "Fibromyalgia symptoms are reduced by low-dose naltrexone: a pilot study". Arthritis & Rheumatology 65 (2): 529–538. doi:10.1002/art.37734. PMID 23359310. 
  19. ↑ Toljan, Kristina; Vrooman, Brigitte (2018). "Low-dose naltrexone (LDN)—review of therapeutic utilization". Medical Sciences 6 (4): 82. doi:10.3390/medsci6040082. PMID 30513713. 
  20. ↑ Aitcheson, Nicholas; Lin, Zhen; Tynan, Kristin (2023). "Low-dose naltrexone in the treatment of fibromyalgia: A systematic review and narrative synthesis". Australian Journal of General Practice (Royal Australian College of General Practitioners) 52 (4): 189–195. doi:10.31128/AJGP-09-22-6564. PMID 37021443. 
  21. ↑ Leiber, Kayla K. (2025). "Therapeutic Uses and Efficacy of Low-Dose Naltrexone: A Scoping Review of Human Clinical Trials". Cureus 17 (3). doi:10.7759/cureus.42291. PMID 40271304. 

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