Low Dose Naltrexone (LDN) 101

A quick guide to low dose naltrexone (LDN)

Low dose naltrexone (LDN) refers to using a dose one-tenth of the normal dose of Naltrexone HCL – an opioid antagonist developed in the early 1960s for treating opioid addiction at a dosage range of 50 to 100mg per day.

Low dose naltrexone is usually prescribed at 1.5mg to 4.5mg daily. This dosage is not commercially available. Instead, LDN and LDN prescriptions are only available at a compounding pharmacy.

Let’s take a look at LDN in more depth, from the benefits to how it works and the potential risks of using it.

The uses and benefits of low dose naltrexone

LDN causes different pharmacological effects than higher doses of naltrexone used to treat addiction.

When taken at very low doses, LDN triggers natural endorphin production. This can boost immune function and help the immune system malfunction.

New studies continue to support the benefits of using low dose naltrexone (LDN) to treat the following:

  • Chronic pain
  • Dermatological conditions
  • Autoimmune disorders, such as Crohn’s disease and multiple sclerosis
  • Autism
  • Fibromyalgia
  • Gastrointestinal disorders

How low dose naltrexone works

LDN works by blocking the natural opiate receptors. The body then responds by regulating the synthesis of its endogenous opiates, known as endorphins.

This means the body ends up with a hundred or a thousand times more endorphins and a better-functioning immune system.

Essentially, when using a very low dose, about one-tenth to one-fifteenth of the amount you’d use for opioid addiction, or less, naltrexone works like a form of hormesis. This is when a compound that’s toxic at high doses ends up having the opposite effect in small or minute doses.

LDN is thought to work independently from its action on opioid receptors by blocking glial cells, which are a type of central immune cell. When activated, the glial cells are thought to cause pro-inflammatory effects that result in pain sensitivity, fatigue, cognitive disruptions, and sleep disorders.

Blocking this action of glial cells is believed to provide neuroprotective and analgesic effects. Most research suggests that LDN takes about one month to start reducing pain. Therefore, a 3-6 month trial is recommended.

Low dose naltrexone dosing recommendations

The normal range for LDN is between 1.5 and 4.5 mg per day, taken about an hour before bedtime (not in the morning).

When taking LDN at bedtime, LDN boosts the immune system by producing a brief blockade of opioid receptors between 2 am and 4 am. This block increases endorphin and encephalin production, which are vital for activating the body’s natural defences.

Potential risks and side effects of low dose naltrexone

All pain-relieving opiate medications must be avoided while taking Naltrexone. Non-opioid analgesics, such as simple analgesics or anti-inflammatory drugs, can be used.

Reported side effects of LDN include:

  • Headache
  • Drowsiness
  • Vivid or unusual dreams

LDN is contraindicated in patients taking Interferon, pregnancy, lactation and allergy to the ingredient itself.

Because dose titration is often necessary (adjusting the dose of the drug for the maximum benefit without adverse effects), our pharmacy formulates LDN in the following dosage forms:

  • Oral capsules
  • Transdermal creams
  • Sublingual troches

Sublingual solutions (vanilla, mint or strawberry flavour)

If you would like to know more about low dose naltrexone (LDN) as a treatment in your clinic, get in touch with our friendly team of compounding pharmacists today.

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