What is Low Dose Naltrexone?

Low-Dose Naltrexone (LDN) is one of the most requested compounds that we see on a day to day basis within the pharmacy. With dosing ranging from 0.5mg to upwards of 6mg, there are a plethora of uses to specialize patient therapy.

Originally prescribed for patients with alcohol and opioid dependence at the 50mg dose, recent studies over the years have shown that much smaller doses can provide beneficial results in patients with chronic conditions. But what exactly is LDN, how does it work, and why is compounding such an important part of its story?

What is LDN?

With its smaller dosing range, the drug acts differently compared to its 50mg high dose. While the 50mg completely blocks the opioid receptors long term, LDN briefly occupies opioid receptors and triggers a rebound effect in the body’s immune pathways and natural endorphins.

How does LDN Work?

Research is still currently ongoing, but LDN is believed to work through 2 primary pathways.

• Modulation of Endorphins:

  • With LDN temporarily blocks opioid receptors, which in turn tells the body to produce more endorphins (i.le. Dopamine, serotonin) and upregulate the immune system.
    • Endorphins Support:
      1. Pain control
      2. Mood Regulation
      3. Immune balance
• Anti-inflammatory benefits

  • LDN has been shown to reduce the activation of microglial cells. These cells are the primary immune cells of the brain and linked to being a cause of inflammation. Since LDN is helping calm these cells, it could reduce inflammatory symptoms in certain chronic conditions.

Both of these mechanisms allow LDN to be considered an option in patients experiencing pain, inflammation or immune dysfunction.

What conditions is LDN being studied in?

LDN is not an FDA-approved treatment for the following conditions listed below and used as an off-label option for:

• Fibromyalgia

• Chronic Pain syndrome

• Multiple sclerosis

• Hashimoto’s (autoimmune thyroid disorder)

• Chronic fatigue syndrome

• Dermatological autoimmune conditions (i.e. psoriasis)

There are many other conditions that are currently being studied to see if LDN would be a good treatment option for patients.

Compound LDN, but why?

Since LDN is not commercially available at such lower doses, that's where we step in and bring the gap to provide personalized prescriptions depending on patient need:

Common preparations included but are not limited to:

• Capsules

• Liquid Suspensions (preferable for patients who cannot swallow tablets/capsules

• Topical cream / gels

Dosing and How to Titrate?

There is unfortunately no universal dosing regimen for starting LDN. Depending on patient age and if they have sensitivities to medications, patients can start at:

• Starting at 1.5mg and increasing by the same dose every 2 weeks

• Starting at 0.5mg and increasing by 0.5mg every week

Patients can stop along the protocol depending on if they are achieving desired effects and/or experienced side effects at a higher dose. Patients may not see full benefit until being on the medication for 6-8 weeks. You may begin to see little improvements in between that time frame

Side Effects:

LDN is generally well tolerated, but potential side effects include:

• Headaches

• Vivid dreams - if this occurs can take in the morning to bypass vivid dreams

• Stomach upset

LDN should not be used with any opioid medication, due to it potentially blocking the effectiveness of opioids. You should let your providers know especially if there are any upcoming surgeries if you are currently taking LDN.

What’re Potential Benefits?

Patients have reportedly seen improvements in:

• Overall quality of life

• Inflammation

• Fatigue

• Pain

How Do We Support LDN Therapy?

For us as a compounding pharmacy, we have a special role in aiding our patients well-being from LDN:

• Changeable delivery routes

• Guideable titration protocols

• Collaboration with local providers

• Appropriate low-dose preparations

• Hypoallergenic options for patients with sensitivities.

Being able to make LDN patient specific is key in providing care in complex or chronic conditions.

Final Thoughts:

Low Dose Naltrexone is continuing to show itself as a versatile treatment option for chronic conditions, pain and immune dysfunction. There is more research being conducted on other disease states or issues such as infertility, PCOS, ulcerative colitis, inflammatory bowel disease among many other conditions. The LDN Trust website has a list of conditions where LDN could potentially be a treatment option. The feedback from our patients and providers has been motivating and we are happy to answer any questions anyone has about the medication itself.

If you are interested in getting started or have additional inquiries, please don’t hesitate to reach out and one of our pharmacists would be happy to answer any questions you may have.

By: Amanda Beliveau CPhT, Lab Manager