Naltrexone is an opioid antagonist that was originally developed in the 1960s and approved for medical use by the FDA in the 1980s. It has been used clinically to treat opioid and alcohol addictions. More recently, low-dose naltrexone (LDN) has been promoted for off-label use as a safe and inexpensive option to treat myriad conditions including pain, inflammation, immune dysfunction, gastrointestinal, neurological, and psychological conditions.
Low dose naltrexone works in the opposite way to high dose naltrexone. This is called a paradoxical effect. At low dosages, naltrexone appears to “trick” the brain into producing more natural opioids (these are called endogenous opioids). It does this by binding briefly to opioid receptors, blocking our naturally occurring opioids from binding. Our body counteracts this by producing more naturally occurring opioids to “wash off” the low dose naltrexone. This increases the levels of naturally occurring opioids in our body which makes us feel good and provides pain relief.
Low dose naltrexone has a very short half-life – around 4 to 6 hours – which means its binding effects wear off quickly, but this is long enough to boost levels of naturally occurring opioids for 18 to 24 hours. Endogenous opioids are natural pain relievers and having more of these around in the body is one of the ways low dose naltrexone is thought to work.
Low dose naltrexone also appears to have anti-inflammatory effects by regulating microglial cells which have a key role in general and nerve inflammation. When microglial cells are activated, they produce pro-inflammatory cytokines, free radicals (reactive oxygen species), and nitric oxide – all of these substances have been associated with pain, inflammation, fatigue, feeling rundown or like you have come down with something. Low dose naltrexone is thought to stop microglial cells from being activated by blocking the TLR-4 receptor.
Low dose naltrexone is thought to relieve symptoms such as pain, fatigue, stress, and inflammation by increasing the production of endogenous opioids and dampening down the effect of microglial cells.
It may take up to 8 to 10 weeks for low dose naltrexone to work. It is important to keep taking it until at least then to know if it works for you.
Side effects with low dose naltrexone are uncommon because the dose is so low and have been reported by less than 8% of people. Low dose naltrexone is unlikely to cause the same side effects as high dose naltrexone. Side effects of low dose naltrexone may include:
Contraindications associated with standard doses of naltrexone include:
Most studies investigating low dose naltrexone have been small with most reporting a favorable effect for conditions such as fibromyalgia, Crohn’s disease, and pain. Research has shown low dose naltrexone is safe, well tolerated, inexpensive, and has minimal side effects.
Titrating the LDN dose is very important to success. This allows the patient to achieve their individual specific therapeutic dose
LDN STARTER PACK 1
TAKE 0.5MG DAILY DAY 1-7
TAKE 1.5MG DAILY DAYS 8-14
TAKE 3.5MG DAILY DAYS 15-21
TAKE 4.5MG DAILY DAYS 22-28
LDN MAINTENANCE
TAKE 4.5MG DAILY
Monday — Friday 9:00am — 5:00pm
Saturday — Sunday Closed
A prescription from a licensed practitioner is required for compounded medications.
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