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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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Get Your Mag On

Mg12

Photo from the helpful Periodic Table

I’ve talked before about how I recommend using topical magnesium oil as a better method of supporting the body’s magnesium needs (see the “Start Here” link under “Home” in the menu bar). But let me break down my recommendations again:

  1. Rub an almond-sized dollop of topical MAGNESIUM OIL on yourself every night about half an hour before bedtime. Magnesium oil makes your skin a bit itchy, like how you feel after getting out of an intensely salty sea. I rub the oil on my stomach and the leftover on my legs. After half an hour, if the itchiness is still irritating me – I wipe it off. All the magnesium should have been absorbed through my skin by that time.
  2. Take epsom salt baths. There are other kinds of salt baths – like Dead Sea Salts, Brittany Fine Sea Salts, Himalayan Salts etc. All of these are great, and I love to alternate. But if it’s magnesium you are after, epsom salts have the most. Epsom salts are also by far the least expensive. I buy huge tubs of it at Whole Foods in the bulk section for about $2.
  3. Consider taking a magnesium supplement, especially if you are prone to constipation, arteriosclerosis or kidney stones. Magnesium chlorate might be best for you, possibly in powder form – but others are also good. But skip magnesium oxide – it doesn’t absorb very well at all.  This should be taken ideally in the morning and then again at bedtime. You need to pace it out. The problem with oral magnesium is that if you take too much, you can get diarrhea. So at least you always have an easy and relatively harmless way of knowing if you have taken too much. The topical magnesium oil above bypasses the digestive system, so will never give you diarrhea. Hooray for that.

A TELLING EXPERIMENT

Take an ounce of water. You know: a shot glass. Now crush up a calcium pill and try to dissolve that in the water. You will see that it doesn’t dissolve very well and leaves some chalky bits suspended in the water. Now crush up a magnesium pill and add that to the same glass. Suddenly the calcium starts disappearing. The magnesium helps keep the calcium dissolved in solution.

/END OF EXPERIMENT

When you take calcium or even just get a lot of it from your diet – without enough magnesium – this is what can happen to calcium in your body: Calcium will precipitate out of solution and form nasty things like kidney stones, stiff cell walls and arterial plaques.

So first of all, never, ever, ever take calcium supplements on their own. I don’t want you to take them at all, not for any reason. But if you absolutely must because of some deep belief or fear – then please, please take a calcium/magnesium combo. And of course make sure you are also taking Vitamin K2, which also directs calcium to your bones and teeth and away from soft tissues. Please see my book review of “K2 and the Calcium Paradox” under the “Books” tab in the “Home” menu above. (I will provide a direct link below.)

Magnesium won’t reverse arterial calcification on its own; only Vitamin K2 can do that. However to reap the full benefits of Vitamin K2 (and A and D), you will need magnesium for the maximum vitamin metabolism.

magnesium miracle

THE MAGNESIUM MIRACLE

I learned about this easy-to-visualize experiment from a book by Carolyn Dean, MD, ND called “The Magnesium Miracle”. If you want to get hot and heavy on magnesium, this is a great place to start. She promotes a very specific pico-ionic magnesium which is apparently absorbed “100% at the cellular level”! So maybe if you are not seeing profound enough effects with the above recommendations after 3 months, these crazy blue bottles are the way to go. I will link to the product at the bottom of this post, though I haven’t used it.

FOODS THAT ARE HIGH IN MAGNESIUM

  • Wild nettles
  • Almonds
  • Cashews
  • Brazil nuts
  • Pumpkin seeds
  • Sea salt

I am going to skip right over grains. That’s because although grains have incredibly high levels of magnesium, the magnesium is bound up with the grain’s high phytic acid content – so it is unavailable. Furthermore, the phytic acid can bind with the magnesium in your body and further deplete you. It is a total misunderstanding and marketing ploy to indicate that you can get magnesium from modern grain products. A caveat: if you soak your grains (at least overnight in an acidic solution), you can reduce the phytic acid content and make the magnesium more bioavailable. This is the case with traditional, whole grain sourdough bread. But come on people, we’ve come so far… Just skip the grains altogether!

Likewise legumes, which have the same phytic acid business going on.

BACK UP. REMIND ME ABOUT THIS PHYTIC ACID BUSINESS AGAIN?

Okay listen up. Phytic acid is a storage form of phosphorous which is bound up with grains, legumes, nuts and seeds to prevent them from sprouting. This is why you can store grains, legumes, nuts and seeds for so long without them growing into plants or rotting. Phytic acid does this by “locking down” these minerals: calcium, magnesium, iron, zinc (and others). Locked up means you can’t get them! Not for you!

So if you want to source fresh organic wheat berries grown on magnesium-rich soil, stone-grind them at home for freshness and to prevent oxidizing the fatty acids, then soak the ground flour overnight in a solution of water and apple cider vinegar or whey, and then pour off the phytic acid-rich water and make a sourdough with an extended rise over a couple of days – like, go for it. You can probably get a good dose of minerals from this effort.

What I do is split the difference. I buy raw, organic almonds, cashews, Brazil nuts and pumpkin seeds – which are all rich in phytic acid – and I soak them overnight with a little bit of apple cider vinegar. In the morning, I rinse them all and then put them in a dehydrator at 105F to keep the seeds “alive”. You can also use a low oven setting (ideally 140F or less) for a day or so. If you don’t dry out the nuts, they will go rancid pretty quickly.

Alternatively, you can do the super Ayurvedic thing and soak just 10 almonds overnight, and maybe 2 Brazil nuts, and then eat them “wet” the next day.

Nuts and seeds have more nutritional density and less effect on insulin than grains and legumes.

MORE BORING PROBLEMS: OXALATES

Green leafy vegetables are also rich in magnesium (and other minerals), BUT WAIT! They are also high in oxalic acid, which works just like phytic acid to bind minerals and make them unavailable to you.

Now of course there is a bit of natural buffering going on, but essentially what this means is that if you are trying to do yourself a favor by eating a lot of raw spinach, Swiss chard, and even kale to a lesser extent – you are inadvertently depleting your body of minerals. Which is pretty ironic because spinach, Swiss chard and kale are pretty packed with minerals.

SO HOW DO YOU WIN AT THIS INFURIATING GAME?

This part is easy. COOK your dark leafy greens. Swiss chard, which is particularly rich in oxalic acid, should be boiled, for a long time (!), and then drained of its oxalic acid-rich water.

I know there is a big movement afoot to eat raw vegetables for all of their fabulous enzymes. But the fact is that minerals trump enzymes. Why? Because enzyme action is driven by minerals. Not enough minerals? No enzyme action. Minerals are the chicken that comes before the enzyme egg.

So you should eat the majority of your vegetables (ALL VEGETABLES) cooked. It’s not my fault that we evolved this way.

SOME RAW IS PERFECTLY FINE!

Oxalic acid is not all bad. It’s also a fine antioxidant. So don’t freak out so much.

QUICK SAMPLE LIST OF MAGNESIUM-DEFICIENT SYMPTOMS

  • migraines, pain and insomnia
  • strokes, brain problems
  • cholesterol and hypertension, heart disease
  • obesity and diabetes
  • Alzheimer’s, Parkinson’s, dementia
  • PMS, Polycystic Ovarian Syndrome
  • infertility, pregnancy, preeclampsia, cerebral palsy
  • osteoporosis, kidney stones and tooth decay
  • anxiety and depression
  • chronic fatigue, fibromyalgia, asthma

WHY DID I EVOLVE TO NEED THIS MUCH MAGNESIUM BUT I’M NOT GETTING IT NOW?

It’s our industrialized food system, stupid! Growing food on depleted soil means no minerals. That’s why they add fertilizers like Potash, which is essentially a cheap potassium solution. Potassium is great! But it pushes out the magnesium. Now it’s not available in your crops! Those cheap crops are fed to your “protein sources” like factory-farmed cows, chickens and farmed fish. Are you getting it? What you’re not getting is magnesium.

OTHER THAN SUPPLEMENTING, WHAT CAN I DO?

Buy your vegetables from a Community Supported Agriculture (CSA) group or farmers’ market, and check in on their farming practices. You’re looking for some biodynamics going on – crops fertilized with cow and chicken manure either from the same farm or a local neighbor. You’re looking for naturally mineral-rich soils, or soils that are supplemented with balanced minerals (like Redmond Clay).

Eat pastured meats (grass-fed, grass-finished) like lamb and beef, and true free-range poultry – animals that can absorb the minerals from the soil in the grasses they eat. Use these mineral-rich bones to make stock!

Eat brains and hearts! Brains and hearts are super concentrated with magnesium. Choose young lamb brains and hearts from a butcher you trust.

THE MAGIC OF ROCKS

Did you know that having rocks in a field used to signify mineral-rich and fertile soil? But now we think rocks in a field means the farmer is too poor to remove them and buy himself a tractor. That’s because rocks mess up tractors – from tilling to seeding to harvesting, so we have developed a bias against them. Industrial farmers have to remove the rocks from their fields.  But the rocks were the sweet naturally slow-releasing mineral depositories. Now they have to replace those lost (free) minerals with purchased fertilizers and nutrients. That’s an expensive proposition, and besides, a lot of the fertilizers just get leached away when it rains… Which then accumulate in wetlands and create salty, acidic, life-averse environments. So on every front: bummer.

The CSA I buy my vegetables from uses horses to plow their fields. I’m serious! There are rocks everywhere!

THE VERY BOTTOM LINE

Magnesium is deficient in almost everyone. The Recommended Dietary Allowance is between 300 – 400 mg for adults. Any overdose is self-correcting (you will get diarrhea if you ever take too much). It improves the body’s ability to metabolize other minerals and vitamins. There’s not much magnesium doesn’t help with, and it doesn’t cause any harm.

FURTHER READING

The Magnesium Miracle” by Carolyn Dean, MD, ND

ReMag Pico-Ionic Magnesium drops

Ancient Minerals Magnesium oil, available at Smith’s Pharmacy on Yonge Street in Toronto

My book review of “K2 and the Calcium Paradox”

Arteriosclerosis linked to magnesium deficiency.

Migraines and magnesium

Diabetes and magnesium

Plowshare Organic Farm CSA outside of Toronto that uses Sally and Milly, two fine work horses to plow

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