Low Dose Naltrexone: A “non-Pharma” Pharmaceutical

More sensitive OGFr

Look at all the new, beefed up Opioid Growth Factor receptors formed on the cell as a result of LDN… So fluorescent!

I’m definitely into low-tech solutions in life: food over synthetic vitamins, fecal transplants over antibiotics (ew gross, right? I talk a big game but it’s not like I’ve ever tried it). However when I started reading about Low Dose Naltrexone last summer, I just couldn’t get it out of my head. Low Dose Naltrexone, known as “LDN”, is safe, cheap, essentially free of side-effects, and remarkably effective at treating a ridiculously long list of ailments, particularly auto-immune disorders, cancer, AIDs and chronic pain.

Most patients with auto-immune disorders (such as Crohn’s Disease, Multiple sclerosis, Hashimoto’s, Rheumatoid Arthritis, Grave’s disease, Lupus, Psoriasis, Alopecia etc.) are put on a regimen of immunosuppressant drugs. Logically this makes sense, because the patient’s immune system is attacking itself – so if you suppress the immune system it loses ammunition for attack. This usually works pretty well at keeping auto-immune disorders at bay. However, and this is a very big however, when you suppress a patient’s immune system she takes on a higher risk for everything from the common cold to Cancer. This is what I call treating the disease at the expense of the patient.

However if you are living with an autoimmune disease, you are probably in chronic pain of one sort or another, and would rather live with a shorter amount of good years than a longer life in pain. There are a million really good reasons to take immunosuppressive drugs, and not a lot of alternatives.

There are many, many different kinds of immunosuppressive drugs at this point, and they all invariably have some acute side effects. But on the positive side, they usually work by a two-fold mechanism: first they act by suppressing the immune system, either by inhibiting the genes that code for T cell proliferation, or by inhibiting B cell and various antibody production; secondly immunosuppressive drugs are usually also strong antioxidants, so that they work by reducing inflammation in the body which tends to reduce immune system reaction (or over-reaction in the case of auto-immune disorders).

I think we can agree that the while the T/B cell reduction is a dicey move if you’re playing a long game, at least the antioxidant part of the drugs is probably very helpful. After all, inflammation seems to be the cause of just about every problem, so curbing it is pretty useful. (Inflammation has its purpose when you have a physical trauma or infection that needs to be sealed off from the rest of the body and healed – but is overkill as a reaction to food choices, stress, and small environmental inputs. More on inflammation another time!).

HERE’S WHY “LDN” IS DIFFERENT

Rather than suppressing the immune system, Low Dose Naltrexone works on another level “upstream” in the healing cascade and appears to regulate the immune system. Some of the doctors (Dr. Ian Zagan et al) who are developing LDN for autoimmune issues claim that it is immunosuppressive, but while this is technically true – LDN is actually concurrently immunostimulating. It seems to be able to curb inappropriate immune responses while simultaneously increasing immune function. In other words, it helps auto-immune diseases without compromising the patient’s immune system. So it’s basically a miracle. People who take LDN only get sick very rarely, if at all, and do not suffer from prolonged infections the way they would if taking proper immunosuppressant drugs.

FIRST, WHAT IS NALTREXONE? SOUNDS INTENSE

Naltrexone is a drug that was first synthesized in the 1960s in America, and determined as an opiate agonist, meaning it could block opiates so that the subject taking naltrexone would not feel the effects of opium and heroin. There was little market value for naltrexone, however the US Governement stepped in and paid for extensive clinical trials hoping it could be used to cure heroin addiction and other drug ills of society. Naltrexone was determined to be completely safe, to have no negative side effects, and to be useful even during pregnancy and breastfeeding – which is very rare for any drug. By the time the trials were completed, the drug was already off patent – though the government extended the patent to DuPont for another seven years. In the ’80s, DuPont started marketing naltrexone as a treatment for alcoholism as it causes drinkers to feel none of the pleasant effects of alcohol yet all of the unpleasant effects. As you can imagine, the biggest issue was patient compliance. Naltrexone never really took off as a treatment for anything, and as of now is off patent, of little value to manufacturers and available pretty freely on the internet without a prescription (!).

One of the main things naltrexone does is bind with Opioid Growth Factor Receptors (OGFr), which are on every cell in the body, and blocks them so that Opioid Growth Factor (OGF) molecules cannot bind to them. When OGF binds with OGFr, cell growth and division is regulated. When OGFr’s are blocked, the cells respond in three ways: by spontaneously creating new OGFr’s on the surface of every cell, by making those new OGFr’s more sensitive, and by increasing the amount of Opioid Growth Factor released in the body. The terms are often used interchangeably, but when I am talking here about “opioids” I mean the natural endorphins created by the body; when I talk about opiates I am using a blanket term for the various natural and synthetic external drugs that act on the central nervous system like morphine, codeine, heroin, oxycodone, alcohol and even sugar and dairy.

In normal naltrexone therapy (full dose), the patient doesn’t get to benefit from the increased amount of more sensitive OGF receptors nor the surplus of circulating OGF caused by the naltrexone because the patient takes another dose and all the OGF receptors, including the new ones, continue to be blocked. And in fact if the patient has other problems, like AIDs or cancer, those problems will get worse. So it was determined by Dr. Bernard Bihari in the 1980s that OGF and OGFr play a tremendous role in healing, and that by blocking them healing is grossly impaired.

HERE’S HOW THE “LOW DOSE” WORKS INSTEAD

A regular dose of naltrexone is between 50mg and 200mg per day. A “low dose”, however, is between 1mg – 5mg per day – much less than 10%. It is available online at 4.5mg compounded doses, which is usually where people start when they are experimenting on their own because they can’t get their doctor to take an interest in it and prescribe it for them.

When you take a “low dose” of 4.5mg, the suggestion is to take it at 10pm. By 2am, the dose is fully working and manages to block your OGF receptors for about two hours, until 4am. What happens during these two sleeping hours is that the body panics and makes more OGF, more OGF receptors and makes these new receptors more sensitive. However when the drug wears off at 4am, you are left with the benefit of all these extra sensitive receptors and a surplus of OGF. You experience a rebound effect which supercharges healing.

It isn’t all about the OGF and OGFr. There are many other endorphins which are blocked and then subsequently rebound to become more effective. Some of them have been studied. Some are still unknown. A pubmed search for LDN comes up with some fifty-four thousand hits on its efficacy for fibromyalgia, multiple sclerosis, Crohn’s disease etc. It is also being used in at least three different fertility clinics around the world, which suggests it is not only safe for pregnancy but also effective for women trying to get pregnant.

SOME TIPS

If you are going to bother to try this out, you might as well go for the best experience. As LDN is an opiate agonist, it works best when there aren’t any opiates in your system! It may be easy enough for you to avoid heroin and oxycodone, but it is more difficult to avoid everyday minor opiates like sugar, dairy and any excess of carbohydrates. If you are going to go out and drink alcohol one night, skip the LDN at bedtime and start again the next night. (If you drink alcohol on a full dose of naltrexone, it can actually make you really sick).

If you want to try this because you have auto-immune disease, you should know that people don’t have the best response when they continue to take their immunosuppressant drugs at the same time. It has been described as trying to drive (taking LDN) with the brakes on (immunosuppressant drugs). However that’s a pretty big decision that you shouldn’t make impulsively just from reading a blog post.

WARNINGS

This isn’t just some natural herb that has always been around and tested by thousands of years of civilization. Natrexone is a synthesized drug – serious business. Even though LDN is in an incredibly small dose, it still makes meaningful changes to your body. Fortunately, just about all of the meaningful changes are positive. However there remains one common side effect:

The side effect is that in the first three to seven days, people who take LDN at night tend to experience vivid dreams that seem to last forever, and sometimes experience nightmares. After a week at most, the body becomes conditioned and the potential for bad dreams is gone.

That is the only negative side effect.

A positive side effect is that people tend to sleep more restfully, their auto immune disease stops progressing or regresses, their chronic pain is lessened, etc. This is being used to reverse both AIDs and cancer, and the doctors doing these trials not only take LDN themselves as a preventative, but have their spouses take LDN as preventatives. It seems to have powerful inhibitory effects on tumor cell proliferation.

MY STORY

I don’t have any auto immune diseases, though I continue to be very interested in them. However I have some special friends who I thought could benefit from Low Dose Naltrexone. I gave them some reading, which they brought along to their doctors. But since their doctors had never heard of it, they all thought it was dangerous and wouldn’t read about it. So I found a way to order LDN online without a prescription, and then proceeded to “test” the product to see if the lack of side effects story was true. I am generally very healthy and thought I would be able to notice anything negative fairly quickly.

In my first three nights taking 4.5mg of LDN, I experienced extremely vivid dreams which momentarily turned dark. These dreams felt like they were days and days long. Having been an insomniac my entire life, and having tried every sedative and sleeping pill on the market, I was very surprised that within half an hour of taking LDN I felt pleasantly tired and fell asleep. Although I normally wake up a couple times during the night, sometimes for hours, instead I slept through until the morning. The vivid dreams remained for three nights and then stopped. However I continued to have an easy time falling asleep and staying asleep. My entire quality of life has changed for the better.

Usually sleeping pills (such as Trazadone, Atavan, Seconal, Neo Citran, NyQuil etc) would give me a feeling of intense physical drowsiness that would drug me to sleep but not help me stay asleep; also the effect would wear off after a week unless the dose was raised. This was never a good solution for me, so I stuck with natural remedies like intermittent melatonin, valerian, magnesium, meditation and elaborate bedtime rituals. But mostly I had just come to accept that I was never going to have an easy time falling asleep and getting the rest I needed.

There is no literature linking LDN with curing insomnia. In fact, most patients report the opposite effect – that LDN initially gives them vivid dreams and restless nights. However for some reason this has worked for me, and I am deeply grateful for the sleep that now forms a regular part of my life.

MY RAT FRIENDS

My one friend who tried LDN to deal with chronic pain went from taking 6 Aleve pain pills a day to taking none. However she found the 4.5mg/day dose made her sleep too much, so she reduced her dose to 3mg yet has maintained the same reduction in chronic pain.

My other friend with auto immune disease could not risk stopping her immunosuppressant prescriptions so tried LDN at the same time. She did not have any noticeable benefit except good quality sleep; if anything, she experienced some of the worst flare ups she had ever had, requiring her to increase her doses of immunosuppressants. Putting the car in drive while the parking brake was on didn’t work for her.

BUT IS IT REALLY SAFE?

I started going to a fancy private doctor so that I could get every blood test ordered and every hormone level checked. I wanted to be able to say without a doubt that eating LCHF (Low Carbohydrate High Fat) and doing all my weird things isn’t just making me “feel” healthier, but is actually making me healthier. So I came clean to my new doctor about taking LDN without a prescription. She was not excited, and urged me to stop taking it, and offered me some good alternatives for sleep aids (holy basil tea etc)…

However three months later, my doctor got back to me after having done her own research on LDN. She said not only did she think it was extremely safe, and probably a great prophylactic against cancer and the diseases of aging, but that she would write me a prescription herself.

I have settled on a dose of 3mg/night at 10pm. When I travel, I take it at 10pm in whatever time zone I am in. I skip it whenever I drink more than a single glass of wine.

NOW GO DO YOUR OWN RESEARCH

Fortunately there is a lot of research available on Low Dose Naltrexone. Right now (July 2014) there are dozens and dozens of clinical trials taking place for myriad auto immune diseases, AIDs, cancer etc. There is a non-profit website devoted to organizing resources for LDN. There are thousands of users online sharing their stories of successes and failures. And there is a small window where LDN is still under the radar and so loosely monitored that you can order it for yourself without too much fuss.

WHY DID I CALL THIS A “NON-PHARMA” PHARMACEUTICAL?

LDN is a “People’s Medicine” because it is extremely safe, non-toxic, inexpensive, off-patent, easy to get, and incredibly effective. This is a “non-pharma” pharmaceutical because there is barely any profit to be made off of it. A single 50mg generic naltrexone pill can be bought off the internet for less than $6. Dissolved in 50ml of distilled water, a regular person can use a calibrated medicine dropper to administer 3ml at a time for less than $0.40/dose. If LDN cures your cancer, it’s a great bargain. If it doesn’t, you only risked $135 for a year’s supply.

FURTHER READING

The Low Dose Naltrexone Homepage is a non-profit website devoted to the latest news and information about LDN

LDN SCIENCE: A group of researchers pooling their clinical trials and information

LDN Research Trust: resources, videos and conferences in the UK. THEIR DOCTORS CAN ARRANGE TO GET YOU A PRESCRIPTION, REGARDLESS OF YOUR COUNTRY, IF YOUR DOCTOR WILL NOT.

This book, The Promise of Low Dose Naltrexone Therapy, from Amazon is useful but already over six years old – you have to go online to find more recent updates and news. However this is a good start if you want a solid book in your hand to take to a doctor.

LDN for chronic pain sufferers, a citation from Clinical Rheumatology publication

A presentation about LDN used to boost fertility in cases with low ovarian reserve (low AMH)

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3 thoughts on “Low Dose Naltrexone: A “non-Pharma” Pharmaceutical

  1. michael horowitz says:

    Thanks S. Very enlightening. Passing it along to a cancer patient.

  2. Jessica Wolfe says:

    I have suffered from Fibromyalgia since 2000, along with ulcerative colitis caused from medicine given to me for my degenerative bone disease (literally deteriorating from skull to toes). I’m very interested in learning more about LDN because I live my life right now with MsContin and it doesn’t always work! I go days without sleep and catch every virus I get near. I would love a better quality of life ! Thank you for sharing!

    • Jessica I hope this helps you. If you can’t find a dr to prescribe, I’ve had luck ordering from “anti aging system” search naltrexone. They sell a 4.5mg dose. Later, when you’re more comfortable with it, you can just dissolve your own dose from 50mg tablets, also readily available.

      Also, this is a longer shot and totally off the radar, but you seem to have a lot of issues. Why don’t you look up c60oo (carbon-60 in olive oil). I haven’t written about it because it’s really such a long shot and I try to stick with the facts. However I take it myself, ordered from the Swiss supplier. Best of luck with your healing journey.

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