LDN – Could it be a “magic pill”?

LDN is a little known, life-changing & very affordable medication with more and more success stories in the integrative and Functional Medicine world. It may just be the ‘magic’ pill many with chronic pain, Chronic Fatigue, Autoimmune conditions/symptoms and cancer therapy, and supporting weight loss.

LDN is an abbreviation for “Low Dose Naltrexone”.

You may know its (full dose) brother Naltrexone as the ‘anti-overdose’ drug used for reversing accidental overdose with opiates such as morphine, heroin, oxycontin, etc.   Full dose Naltrexone is typically administered in doses up to 50mg, however about 20 years ago it was found that in very low doses (1.5 -4.5mg), it has profound effects on modulating the immune system and reducing chronic, miserable and deteriorating conditions.

Bear with this moment of science class…

LDN boosts the levels of a naturally occurring chemical in our body called endorphins.

Endorphins got their name because they are “Endogenous (made in the body) Morphines” and totally different than the synthetic opioids (such as those mentioned above).

Most chronic conditions are “too much or too little” cellular behavior.  Endorphins known as Opioid Growth Factors (OGF) are produced naturally in our body. They bind to every cell in our body through an Opioid Growth Factor “receptor” or OGFR (think of this action like Velcro).  This Velcro action helps to control cellular growth (not too much, not too little).  For this binding action to work properly we must appropriately produce OGF and then it must bind to the OGFR (the ‘Velcro’).

Naltrexone is an OGFR blocker.

Have you ever had the experience when a toddler’s Velcro sneaker fails to fasten because the Velcro no longer ‘sticks’.  As it always does so well, the body’s response to this lack of OGF binding is to compensate and rebound by supercharging the signal and pushes more and more OGFR and more and more OGF.  The cells make more OGFR (more sticky Velcro) to try to get the higher amounts of OGF in as well as increasing the sensitivity to the OGF (now the Velcro is longer, thicker and stickier).

To help visualize this, the picture to the right shows the cell covered in pink receptors (OGFR- the Velcro).  The yellow and green represent the OGF binding to the receptors. With Naltrexone (and LDN), this cell would be covered with many more pink, green and yellow molecules. Any dose of Naltrexone will produce this increase in receptors and growth factors. For any of this to occur, the body must first metabolize the medication; however, the higher the dose, the longer it takes to occur and experience the benefits.

Low dose Naltrexone works exactly the same way, however, the ‘blocking’ of the OGFR lasts only a couple of hours as the lower dose is quickly metabolized and excreted from the body. In this case, it’s a good thing as the short term blockade allows for a higher level of natural opioid (feel good) hormones for the following 18-20 hours.

LDN also prevents the immune system from working overtime.

Our bodies have an amazing ability to overcompensate for balance. By increasing the number of pinks, green and yellow, the immune system now works at a more appropriate rate. (Not too much as in AutoImmunity and not too little as in poor immune system not fighting appropriately).
The body working ‘overtime’ (or attacking what it shouldn’t) is something many sufferings from. Autoimmunity is known too well as the culprit for many miserable and life-altering symptoms. As explained above; when taken at bedtime, LDN attaches to opioid receptors in the brain. This occurs in all types of immune cells, temporarily blocking endorphins’ ability to attach to the immune cells.

OGF & OGFR are joined by the immune system guys – specifically the T-regulatory cells (aka T-regs).  Think about T-regs as the police in our body. They are there to keep peace and help out when needed, but also enforce the law to ensure balance in our community. T-regs keep the immune system in balance in our body by turning inflammation on and off, depending on the body’s needs.  They also prevent the immune system from getting stuck or “freaking out” in patients with overactive immune systems, such as those with allergies or asthma or Autoimmune conditions (ie: attacking things it shouldn’t such as the thyroid in Hashimoto’s Hypothyroid or myelin sheath on the brain in Multiple Sclerosis).

What is the connection between the OGF, OGFR and the Immune system?

People with Autoimmune conditions often have low levels of the OGF and OGFR. White blood cells (our ‘fighting’ immune cells) drive the immune response and they have receptors for these opioids. LDN also blocks a receptor on white blood cells called Microglia which is responsible for inflammation in the body. If the Microglia are constantly on alert, we have symptoms of inflammation such as pain, fatigue, insomnia, mood disorders and cognitive disorders (such as brain fog, dementia, etc).  LDN blocks the receptors on the Microglia cells and in turn reducing Central Nervous System inflammation. This reduced inflammation has been shown to reduce ESR (erythrocyte sedimentation rate), which is an inflammatory marker that’s elevated in many AutoImmune conditions.

Ok – enough science! What does this mean and who might benefit from LDN?

Who might benefit from LDN? 

• AutoImmune disorders– Patients with Auto-Immune disorders; especially Multiple Sclerosis, Hashimoto’s Thyroiditis, and Colitis and Crohn’s.
  * Hashimoto’s patients: It is important to remember to have your Thyroid levels watched more closely as LDN may reverse the autoimmunity closely requiring less thyroid hormone replacement.
• Chronic conditions- Patients with chronic or deteriorating syndromes such as Chronic Fatigue and Fibromyalgia, Agitated Autism, Parkinson’s, HIV/AIDs, Lou Gehrig’s, chronic pain and Lyme.

Where can I get LDN? 
LDN is not available from most traditional medical providers or at chain pharmacies because it is a Compounded medication (ie: made in a compounding pharmacy). Most Functional Medicine providers (like 4 Better Health) are prescribing LDN when appropriate for their patients. We do not recommend you purchase these from overseas pharmacies.  There are no safety standards and not knowing what you are really getting and should you be not getting LDN, health issues could increase dramatically.

What is the dose?

The suggested dose is 1.5–4.5 mg per day in a capsule or liquid, taken orally at bedtime. The medication should not be in a ‘slow release’ formula. As mentioned above, we want fast metabolism for the best response.  Some people have found that the best formula is those made without Calcium Carbonate (a filler for many pharmacies).

Is LDN addictive? LDN does not have any known abuse potential. It’s not an addictive medication.

Are there Contraindications?

LDN blocks the Opioid receptor = Narcotics will not be effective. Anyone who needs a Narcotic medication (whether it be for injury, surgery, or chronically) would not be a candidate. As their narcotics will not offer the pain relief they require. LDN may interfere with the efficacy of immunosuppression medications (such as those who’ve had an organ transplant).

LDN does not effect NSAIDs (ibuprofen, Aleve, Naproxen, etc) or Tylenol & acetaminophen and is well tolerated. The biggest side effect is sleep disturbance and vivid dreams at first, but these typically go away after time. To avoid this, start with a dose of 1.5 mg and build up slowly over two months. Some patients have complained of nausea.

For more information we recommend you visit here or lowdosenaltrexone.org.