John DoeGeneral Surgeon
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The LDN Research Trust Charity works to raise funds for research trials. We have helped over 100,000 people obtain LDN from a General Practitioner or Consultant, either through the National Health Service or by private prescription. We are proud to have helped people not just in the UK, but in countries throughout Europe; as well as the USA, Canada, West Indies, Australia, New Zealand, and beyond.
It reduces pain, and fights inflammation. It is used to treat cancers, autoimmune diseases, chronic pain and mental health issues, to name a few. Treatment is constantly evolving, with new conditions and methods of treatment being shared regularly.
LDN is a competitive opioid receptor antagonist. At the standard dose, naltrexone blocks the effects of both the endogenous opioids, which are in endorphins and pharmaceutical opioids. LDN is a pure antagonist, which is vital to know as a lot of people think it is a controlled medicine, narcotic or an opioid.
This is a wide range of diseases, and many clinicians will find it difficult to understand how one drug can have a positive effect on all these pathologies.
The first thing to understand is that naltrexone – the drug in LDN – comes in a 50:50 mixture of 2 different shapes (called isomers). It has been recently discovered that one particular shape binds to immune cells, whilst the other shape binds to opioid receptors.
Although consisting of exactly the same components, the two isomers appear to have different biological activity.
Summary of mechanism of action
The summary of 10 years of research is that LDN works because:
Levo-Naltrexone is an antagonist for the opiate/endorphin receptors
Blocks endorphin receptors for 4 hrs, then unlocks them thus increased endorphin release,
Increased endorphins modulate the immune response
This reduces the speed of unwanted cells growing. Dextro-Naltrexone is an antagonist for at least one, if not more immune cells
Antagonises “TLR,” suppressing cytokine modulated immune system
Antagonises TLR-mediated production of NF-kB – reducing inflammation, potentially downregulating oncogenes(Bad Genes-cause cancers)
Taking Naltrexone in larger doses of 50-300mg seems to negate the immunomodulatory effect by overwhelming the receptors, so for the effect to work, the dose must be in the range of 0.5-10mg, usually maxing at 4.5mg in clinical experience.
The Use of Low-dose Naltrexone, and the Occurrence of Side Effects
Many patients who start LDN do not experience any severe side effects.
As mentioned earlier, your symptoms may become worse – in MS, this can be characterised by increased fatigue or increased spasticity. In CFS/ME, this can be the onset of apparent flu-like symptoms. LDN can cause sleep disturbances if taken at nighttime – this is most likely because of the increase in endorphin release. These disturbances can take the form of vivid dreams or insomnia.
In various studies (and anecdotal accounts), the number of T-Lymphocytes has been shown to dramatically increase when a patient starts on LDN. This may account for some of the benefits patients feel when they are being treated for an autoimmune disease or cancer. This has not been directly evidenced in multiple sclerosis.
Clinical experience shows that in less than ten percent of cases treated, increased introductory symptoms may be more severe or more prolonged than usual, lasting sometimes for several weeks. Rarely, symptoms may persist for two or three months before the appropriate beneficial response is achieved.
If side effects are troublesome, try reducing your dose by 50% for 7 days, before increasing it again.
Some patients very rarely experience gastrointestinal side effects, such as nausea and or constipation/diarrhea. The reason for this is currently unknown, but may be due to the presence of large numbers of delta-opiate receptors in the intestines.
Patients experiencing this side effect can request LDN Sublingual Drops, which transfer the LDN directly into the bloodstream – avoiding the GI tract.
Patients who do have these side effects should increase their dose by no more than 0.5mg per week and should consult with their GP or pharmacist for appropriate treatment for the stomach upset, if necessary. (eg Omeprazole, Ranitidine, Gaviscon, Fybogel, Mucogel and Pepto Bismol are ok – but not Kaolin & Morphine or Loperamide/Imodium.)
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