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Low Dose Naltrexone: could this help your chronic pain or autoimmune disease?

April 25, 2022

What is Low Dose Naltrexone?

Naltrexone is a medication approved as a treatment for opioid addiction and alcoholism. In 1985, while working at addiction clinics in New York, Harvard-educated internist Bernard Bihari, MD, discovered many novel benefits of using low doses of naltrexone (about 4.5 mg., or 1/10th of the typical dose of 50 mg. that is used to treat addiction). Ongoing research has shown that Low Dose Naltrexone (LDN) has potential benefits for patients with chronic pain, autoimmune diseases, and central nervous system disorders.

The Science Behind LDN:

Naltrexone is a mu-opioid antagonist that is a mixture of two distinct shapes known as isomers. Research suggests that the L isomer binds to opioid receptors, while the D isomer binds to immune cells. As an opioid antagonist, naltrexone binds to and blocks opioid receptors on cells. Because the opioid receptors are blocked only intermittently by Low Dose Naltrexone, the receptor sites rebound with increased and persistent production of endorphins (endogenous opioids best known for relieving pain and enhancing your sense of well-being). These natural opioids are also powerful regulators of the immune system.

What does this Increased endorphin release from LDN do?

  • May lessen pain
  • Downregulates inflammatory cytokines, while increasing T cells and Natural Killer Cells
  • Stimulates mucosal and tissue healing
  • Directly inhibits tumor growth
  • Reduces death of oligodendrocytes that produce myelin in the brain, thereby increasing the production of myelin (a protective covering for nerves)

LDN also blocks some non-opioid receptors (e.g. Toll-like receptor 4; TLR4). This is thought to be how LDN produces its anti-infammatory effects. LDN has demonstrated the ability to reduce the severity of symptoms in certain inflammatory conditions such as Fybromyalgia, Crohn’s disease, multiple sclerosis and complex regional pain syndrome (CRPS).

Are there side effects from LDN?

LDN is well tolerated in most patients and side effects are usually transient. However, care should be taken to slowly titrate/increase the dose to avoid side effects.

Common Side Effects:

  • Sleep disturbances/Vivid dreams
  • Gastrointestinal upset, nausea
  • Mild headache
  • Mild agitation

Uncommon Side Effects:

  • Flu-like symptoms
  • Rash
  • High temperature
  • Dizziness
  • Increased fatigue or spasticity

The following may require dosage adjustments:

  • Thyroid sensitivity in Hashimoto’s patients may require a supervised decrease in the dose of thyroid medication.
  • Agitation/extrapyramidal symptoms in patients with Parkinson’s disease may require supervised adjustment of dopamine dose.
  • Liver enzyme elevation may respond to dose reductions. Patients with kidney disease should be monitored for any decline in renal function.

Caution: LDN should not be taken by patients who are also taking opioids such as morphine, oxycodone, or hydrocodone. It is possible that even a low dose of naltrexone could cause blockade of opioid receptors and reduce the effectiveness of opioid analgesics or induce withdrawal symptoms.

What forms does LDN come in and where do I get it?

LDN is not commercially available but can be compounded in various dosage forms by prescription. You will need your doctor to send a prescription to a compounding pharmacy, like Person Street Pharmacy, where they can make your medication in the best format for you.

  • Liquids - allows for slow titration to optimal dose
  • Capsules – in appropriate dose
  • Sublingual Drops - for patients with swallowing diffculties or GI side effects from the liquid or capsules. SL drops facilitate more rapid absorption through the oral mucosa
  • Topical Creams – can be helpful when administering to children

LDN is WILDLY underutilized!

For various reasons, many doctors do not know about LDN and/or don't prescribe it. If you have any of the conditions previously mentioned and are not finding relief from your symptoms with your current protocol, talk to your doctor to find out if LDN is right for you.

If you would like to learn more about LDN, please fill out a form at PersonStreetRX.com and a pharmacist can reach out to you with more information and can even speak to your doctor and discuss this as an option for you.


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