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Side Effects & Dosing of Low Dose Naltrexone (LDN)
Greetings!
Most medications result in unintended reactions called side effects. LDN is no exception. Just as every marriage goes through an initial period of adjustment, so too does the taking of LDN bring about a new order of things to which the body needs to adapt. Internal chemistry changes, endorphin levels increase, and the immune system is upregulated--a generally beneficial process that can, nevertheless, take time getting used to. Fortunately, the side effects associated with LDN are usually mild and of a transitory nature--and the rewards--in terms of healing, restoration of function, and the cessation of pathology--can be wonderful, even life-saving.
Dr. M.R. Lawrence is an English physician with multiple sclerosis (MS) who treats it with LDN. He also prescribes LDN for his patients. The following are his observations and advice regarding common side effects associated with taking LDN. While they refer primarily to people with MS, they also apply (with the exception of spasticity and possibly pain) in other situations involving the administration of LDN.When starting this LDN (Low Dose Naltrexone) therapy in the treatment of MS, there may also be some initial transient, though temporary, increase in MS symptoms.
Italian researchers conducting a four month clinical trial of LDN in the treatment of MS made this statement about side effects:
Experience in using this method has demonstrated most commonly, such as disturbed sleep, occasionally with vivid, bizarre and disturbing dreams, tiredness, fatigue, spasm and pain. These increased symptoms would not normally be expected to last more than seven to ten days [but your experience may vary].
Rarely, other transient symptoms have included more severe pain and spasm, headache, diarrhea or vomiting. These additional symptoms would appear to be associated with the previous frequent use of strong analgesics, which effectively create an addiction and dependency, thus increasing the body's sensitivity to pain.[Similar symptoms can also occur in people unknowingly allergic/sensitive/intolerant to gluten and/or dairy and who take those foodstuffs concurrently with LDN.]
In addition, because LDN stimulates the immune system and many of the drugs routinely used by the NHS in the treatment of MS further suppress the immune system, LDN cannot be used in company with steroids, beta interferon, methotrexate, azathioprine or mitozantrone or any other immune suppressant drug. If there is any doubt, please submit [to your doctor] a full list of the drugs you are presently taking so that their compatibility may be assessed. In addition, because LDN will also block the analgesic effects of any opiate drugs (includes codeine, dihydrocodeine, morphine, pethidine or diamorphine) presently being taken, the use of LDN will initially greatly increase the level of pain experienced. It is therefore advisable [in cases of dependency] that any opiate-like drugs be discontinued at least two weeks before this treatment is initiated [to allow a "drying out" period].
When starting the treatment it is essential that any untoward or adverse side-effects are reported immediately [to your doctor] so that the treatment process can be further assessed and, if necessary, modified.Transitory haematological abnormalities (increase of liver enzymes, hypercholesterolemia), mild agitation and sleep disturbance were the commonest adverse events.
Because LDN tends to initially worsen MS symptoms (especially spasticity), Dr. Skip Lenz, a pharmacist who takes LDN prophylactically, recommends a nightly dose of 1.5 mg the first month, 3 mg the next month, and 4.5 mg thereafter. For life-threatening conditions such as cancer, the recommended dose is 4.5 mg from the outset. To quote Dr. Lenz:The reason we suggest a stepwise titration [for MS patients especially] is to AVOID SIDE-EFFECTS. Three years ago, we found that EVERY PATIENT WHO STOPPED TAKING LDN BECAUSE OF SIDE-EFFECTS STARTED AT 3.0 MG OR HIGHER! There was only one patient who started at 1.5 mg who stopped because of side effects. Our efforts here should be to help the greater population. Now, there are some tough guys who can go straight to 4.5 mg and have no problems, but I betcha someone with a headache would feel differently or someone whose legs are screwed up in knots or someone who has had the bejeebers scared out of them with nightmares (me).
Suggestions for reducing spasticity in cases of MS can be found here:
http://tinyurl.com/treating-ms-spasticity
Sleep aids include Chamomile tea, valerian, melatonin, calcium/magnesium capsules, Lunesta, L-Theanine, GABA, 5-HTP, and Natural Calm. My personal favorite is a dual-release melatonin tablet taken with a cup of lukewarm Chamomile tea. For best results, sleep aids should be taken about half an hour before bedtime. For additional sleep aids, visit
http://www.naturalnews.com/025065.html
I would also recommend taking an afternoon nap. Studies show that daily naps have definite health benefits, and I believe that is particularly true for people on LDN.
Some people taking LDN have reported reduced appetite, a side effect that enabled them to lose weight. If weight loss is undesirable, small frequent meals are recommended.
In cases of autoimmune-related bowel disease, LDN typically leads to weight gain as the bowel heals and begins to function normally.
Some people have reported a modest increase in blood pressure associated with taking LDN, while others have reported a decrease.
Additional side effects that some individuals taking LDN have noted include an increased sense of wellbeing, increased self-confidence, and a stronger sexual appetite.
The Mayo Clinic has extensive information on the side effects of much larger doses of Naltrexone (25 mg and up), the kind used to treat alcoholism and drug addiction. Some of these side effects (like dizziness, thirst, itching, rapid heartbeat, and urinary problems) may also apply in rare instances to LDN. To learn more, visit
http://tinyurl.com/naltrexone-side-effects
Because medications are metabolized in the liver, if that organ has been damaged by toxic chemicals, pathogenic microorganisms, previous drug therapy, or alcoholic addiction, there will be an increased likelihood of unpleasant side effects.
The optimal dose of LDN for the average adult is deemed to be 4.5 mg taken between 9 pm and 3 am. To control for the difference between Daylight Savings and Standard Time, some people take it between 10 pm and 2 am.
LDN should not be taken with food. The medication needs to be rapid release, and food prevents that. For the same reason, LDN should not be compounded with the filler calcium carbonate, as it tends to cake and prevent rapid release.
In regard to daytime dosing, of all the clinical trials of LDN conducted with humans, only one used daytime dosing--a German study with a group of MS patients. While about a third of the group did experience limited benefit, this is the comment made about the trial by Dr. David Gluck, webmaster of http://ldninfo.org:Unfortunately, because of some early complaints of sleep disturbance, the principal investigator of this trial switched all of the study group to taking LDN at 9 am in the morning, a questionable dosage time. It is generally recognized that the most effective time to take LDN is at bedtime, between 9 pm and 3 am, due to the fact that the endorphins for each day are always produced at their peak rate in the pre-dawn hours. A 9 am dosage time, as was used in this trial, might conceivably suppress—rather than boost—a patient's immune system.
In a presentation made by Dr. Bernard Bihari in 2002, he gave this perspective on LDN dosing:What we did was we measured the endorphin rises with different doses of Naltrexone. We got the same rise with 50 mg, 10 mg, 5 mg, and 3 mg. What we were looking for was the smallest dose that could produce a full naltrexone-induced endorphin rise, if taken late at night. The reason the hour is important is that 90% of the endorphins are made in the middle of the night, between 2 and 4 in the morning. If a small dose of naltrexone is taken in the late evening, generally at bedtime, generally endorphin production is boosted as much as threefold, 300%. The naltrexone itself is gone in about 3 hours, but the endorphins remain elevated all the next day. So the naltrexone doesn't significantly block the endorphins but does cause them to rise.
Because of its unique mode of action in the body (the partial and temporary blockade of opioid receptors), achieving therapeutic results with LDN is highly dose-dependent. Too much or too little of the drug can definitely be counterproductive.
Although the optimal dosage of LDN for the average adult (presumed to weigh 150 pounds) is considered to be 4.5 mg, some patients do better (i.e., have fewer side effects and a better over all response) on a lower dose, particularly if they weigh significantly less than 150 lbs. To compute one's theoretical "ideal" dose in mg based on Clark's pharmaceutical dosage rule, multiply your weight in pounds by a factor of .03 (the same formula also works in computing the dosage for children and pets). If liver functionality has been compromised, however, a dose lower than the computed dose may be necessary, and it can only be determined by trial and error.
Given the number of variables and unknowns involved, Dr. Tom Gilhooly, a Scottish physician, advises using the trial and error method at the outset, suggesting a dose of 1 mg for the first month, 2 mg the second month, 3 mg the third month, and so on until the patient's symptoms start getting worse instead of better. At that point, the dose should be reduced by 1/2 mg and kept there until the symptom picture changes.
In any event, except for brief periods during symptom exacerbations, doses of LDN higher than 4.5 mg are generally considered to be counterproductive.
In rare instances, LDN levels can build up in a person and blunt or even negate its effectiveness. Therefore, a reduction in dose, or even skipping some doses, has been suggested in cases where LDN mysteriously stops working, or bothersome side effects return for no apparent reason.
Naltrexone is an opioid receptor antagonist. It blocks narcotic painkillers from reaching their intended target, causing such painkillers to lose their effectiveness until the effect of the Naltrexone wears off. Since people appear to vary widely in their ability to metabolize LDN, Dr. Lenz currently suggests that you skip your nightly dose of Naltrexone a week before any medical or dental procedure is scheduled during or subsequent to which opioid painkillers are to be used or prescribed. Discontinuing LDN for a week might cause some loss of ground in terms of the condition for which a person is taking LDN, but apparently resuming LDN after that period at one's usual dose does not cause a significant return of unpleasant side effects. The body has already become accustomed to the drug.
In regard to taking LDN when pregnant or during breast feedng, Dr. Phil Boyle, a specialist in fertility care in Ireland, stated the following in 2008:I am confident that LDN is perfectly safe in pregnancy, and in certain cases will actually reduce the risk of miscarriage. Thomas W. Hilgers, M.D., of the U.S., who developed the fertility treatment I provide, has used high dose Naltrexone...up to 100mg throughout pregnancy and during breastfeeding safely, without ill-effect to mother or baby, since 1985. I have been prescribing LDN regularly during pregnancy [for several years] and the results have been excellent. Clinical experience has proven to me that it is safe.
If you have questions, comments, or suggestions, please feel free to contact me at
dudleydelany@webtv.net
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Hoping you find the information in this website both helpful and hopeful, I am,
Very sincerely,
Dudley Delany, R.N., M.A., D.C.
LINKS
An Introduction To Low Dose Naltrexone
Drugs To Avoid When Taking Low Dose Naltrexone
How To Obtain Low Dose Naltrexone
Why I Became An Advocate For Low Dose Naltrexone
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