Wednesday, January 05, 2011

LDN links I want to keep in one place

  • LDN is rapidly metabolized and excreted from the body, within a few hours at most. Its beneficial effect in autoimmune disease is as result of it tricking the body into producing large amounts of OGF - which act as an immune suppressant/modulator. However, if the dose of LDN being used is too high, this making it naltrexone treatment rather than low dose naltrexone, it could definitely exacerbate the symptoms of autoimmune diseases. This is because the continuous presence of naltrexone will block production of OGF on a continuous basis. OGF is needed to keep the immune system in order.
  • I dissolve naltrexone in 50ml of water to make LDN, is a filler involved in this process?

    A filler is a substance that is mixed with an active ingredient in order to enable tabletting or encapsulation of consistent quantities of active ingredient. If you are dissolving pure naltrexone, there would be no filler involved. However if you are dissolving naltrexone tablets or capsules, those may well contain fillers or binders. You should check the manufacturer's product insert.
  • Should LDN be stopped before surgery?

    This question must be discussed with the anesthetist who will be aware of how much time before the surgery LDN should be stopped. You should ensure you make the anesthetist aware that you are using a low dose, and the exact dose being used.
  • Will LDN interfere with Lomotil (an anti-diarrhea medication).

    Lomotil contains Diphenoxylate which is an opiate agonist. LDN will therefore prevent it from working for a short period of time which could last up to several hours, until the LDN is metabolized and excreted from the body.
  • Can your body become accustomed to LDN's rebound effect?

    In theory the answer is yes, and therefore it may make sense if LDN is losing its effectiveness to take a break from using it every so often. This question has not yet been addressed in clinical trials.
  • How soon after taking LDN can you take an opiate painkiller?

    It will take a few hours (with individual variation) for the LDN to be metabolized, and therefore enable the opiate to relieve pain. There is no harm in taking the painkiller sooner, except that it may not work. 
  • Is LDN compatible with melatonin?

    At this time there is no known contraindication concerning LDN and melatonin. LDN can be taken at any time of the day, so if it disturbs sleep it would be wise to take in the morning.
  • Is LDN compatible with Natalizumab?

    Is there a preference for the filler used when preparing LDN?

    Yes, for two reasons. Certain fillers may interfere with rapid absorption of LDN. Additionally, some patients are intolerant of certain fillers. It has been reported that microcrystalline cellulose and dextrose are both compatible with LDN. However individual tolerance to these may vary in very sensitive individuals.
  • Can LDN be taken twice a day?

    As mentioned elsewhere on this site, according to Dr. Zagon's studies the optimal daily dose of LDN is between 2.5 and 10mg. It is conceivable that some individuals, depending on their metabolism, would benefit from taking two doses daily of 3mg or 4.5mg, 12 hours apart, and in fact this has been reported by some people.
  • Are there any contraindications for combining LDN with Tricyclic or SSRI, SNRI Antidepressants?

    At this time there are no known contraindications for this combination.
  • How quickly can one expect to see benefit from LDN?

    Most users typically experience benefit within days. If no benefit has been seen by the end of one month, it may be necessary to modify the dose being taken. If the dose adjustment does not help, it is unlikely that benefit will be seen from LDN in such cases.
  • Is it possible for LDN to raise blood pressure?

    This has not been reported previously. In fact endorphins are known to lower blood pressure and since LDN raises certain endorphin levels, one would if anything a regulation of blood pressure. If LDN does cause raised blood pressure, one should question whether the correct form of naltrexone has been used. It could be that a slow release form has been incorrectly used instead of an immediate release form. 
  • Has LDN been used for diabetes?

    No studies have been carried out yet in diabetes, whether type 1 or type 2. However there have been physician reports of LDN's help in regulating blood sugar levels in diabetes.

  •  Is LDN an immuno-suppressive drug?LDN is best classified as an immuno-regulator. It causes an increase in OGF levels - and OGF regulates proliferation of all cells, including immune cells (T-cells and B-cells). When immune cells are being produced in excess (leading to autoimmune conditions), OGF acts to slow down their proliferation. Whilst this can be construed as immune-suppression, it is most accurately described as immune-regulation.
  • Can LDN be used together with OGF?

    Research at present does not support taking the two together. Since LDN neutralizes the effect of OGF, it would not make sense to combine the two. However there are physicians who prescribe the two together, whilst advising a long distance (like 10 - 12 hours) between the two. Whether the results are better than taking OGF on its own remains to be clarified in a trial.

  •  Please discuss taking LDN and alcohol usage, wine, in particular.

    If wine is consumed at night, should LDN be taken in the morning?
    LDN does not interact with alcohol in any negative way. Whilst naltrexone is used to treat alcohol craving, there is no problem taking LDN after alcohol. LDN can be taken in the night or in the day as desired.
  •  If a person takes LDN for 2-4 months and then stops, will the newly-formed opioid receptors remain, or will they go back to pre-LDN levels?

    The newly formed receptors will last a short time, probably days at most.

  • The benefit from LDN in MS has been reported to be cumulative, and the time it takes to achieve maximal benefit varies amongst individuals.
  • Would LDN be indicated for other auto-immune disorders, such as lupus?

    Based on its mechanism of action, LDN could in theory work for any autoimmune disorder. There have been favorable reports of its usage in lupus, although no formal studies have been conducted.
  • Can you take Prednisone (cortisone) while on LDN?

    At this time there is no research showing any problem in combining these medications.
  • When will LDN be approved by the FDA to treat Multiple Sclerosis?

    Obtaining FDA approval is a costly process, often running into hundreds of millions of dollars. Where a drug's patent has expired, no incentive exists for a drug company to invest the funds needed to gain FDA approval. It is unlikely that LDN will ever gain FDA approval for multiple sclerosis unless charitable sponsorship is found to finance the process.  

    How Does LDN Work?

    In order to understand how LDN works, it is crucial to briefly introduce the workings of the ‘natural opioid’ (endorphin) system.
    Endorphins are opiate-like molecules produced naturally in the body. The term ‘endorphin’ comes from ‘endogenous morphine’, meaning that it is created within the body, and differentiating it from opioids that are administered from external sources.
    Endorphins are produced in most cells in the body, and are important regulators of cell growth and therefore the immune system. Disorders of the immune system can occur with unusually low levels of these endorphins.  The particular endorphin that has been found to influence cell growth as well as immunity is called Opioid Growth Factor (OGF) or Met-Enkephalin.
    For an endorphin such as OGF to exert its beneficial effects, it must interact with the body’s cells. It does this by binding to a receptor on the surface of the cells. The receptor to which OGF binds is the ‘Opioid Growth Factor Receptor’ (OGFr) – previously known as the Zeta (ΞΆ) receptor.
    Thus, for the endorphin system to be fully functional, two elements are required: opioid production and cell interaction.
    Naltrexone is an externally administered drug that binds to opioid receptors.  In doing so, it displaces the endorphins which were previously bound to the receptors. Specifically, by binding to the OGF receptor, it displaces the body’s naturally produced OGF.
    As a consequence of this displacement, the affected cells become deficient in OGF and three things happen:
  • Receptor production is increased, in order to try to capture more OGF.
  • Receptor sensitivity is increased, also to try to capture more OGF.
  • Production of OGF is increased, in order to compensate for the perceived shortage of OGF.
Since LDN blocks the OGF receptors only for a few hours before it is naturally excreted, what results is a rebound effect; in which both the production and utilization of OGF is greatly increased. Once the LDN has been metabolized, the elevated endorphins produced as a result of the rebound effect can now interact with the more-sensitive and more-plentiful receptors and assist in regulating cell growth and immunity.
The duration of the rebound effect varies from individual to individual, but generally persists for about one day.

The benefits of the rebound effect can only be utilized by taking a low dose of regular naltrexone. Taking a high dose of naltrexone or using a timed-release formulation will result in continuous blockade of OGF receptors, and the rebound effect will not serve any useful purpose.
In scientific terminology, the use of regular-dose naltrexone results in ‘continuous opioid receptor blockade’ whilst the use of LDN results in ‘intermittent opioid receptor blockade’. In order to benefit from the rebound effect and achieve the therapeutic benefit of LDN, it is essential to avoid timed-release versions of naltrexone.
Individuals vary in their metabolic speed and this will result in inter-patient variation in the speed at which LDN is eliminated from the body, as well as the length of the rebound effect. Whilst a single daily dose of between 3mg and 5mg will be suitable for most patients, individual modification of dose or frequency is sometimes needed. Pty Ltd
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