THE NIACIN FLUSH: COULD IT SIGNAL A HEART PROTECTIVE PATHWAY?
The Durk Pearson & Sandy Shaw Life Extension NewsTM
Volume 12 No. 3, June 2009
One new research paper1 reports efforts to separate the mechanisms that control niacin flushing from the beneficial antilipolytic effects of niacin in order to get rid of that pesky flushing that some people find annoying or even intolerable. But, not so fast. It may be that the flushing is part of something important that niacin is doing and that you wouldn’t want to get rid of it.
Prostaglandin D2 has been identified as the molecule that naturally causes niacin flushing. Nicotinic acid-mediated stimulation of GPR109A receptors expressed on Langerhans cells in the skin leads to activation of cytosolic phospholipase A2 (cPLA2) and subsequent production and secretion of prostaglandin D (PGD2), which through activation of its own 7TMR [7 transmembrane receptors], leads to cutaneous flushing.1 The title of a new paper published subsequently2 caught our eye when it implied that prostaglandin D2 produced and released in the heart, where the enzyme responsible for its synthesis is reported to be highly expressed, could be responsible for major heart protective effects. The study reported that glucocorticoids protected rodent hearts from ischemia/reperfusion injury, the protection being a result of increased synthesis of PGD2. Moreover, the activation of L-PGDS-mediated production of PGD2 was crucial for the cardio protection against ischemia/reperfusion conferred by glucorticoid-GR [glucorticoid receptor] signaling. Indeed, L-PGDS-knockout mice are prone to develop atherosclerosis when fed a high-fat diet.2
As the authors2 explain, glucocorticoids are anti-inflammatory and generally repress prostaglandin biosynthesis in most cells. However, in rat heart cells glucocorticoids upregulated the enzyme that synthesizes PGD2 and, in fact, they report, was the most prominently induced prostaglandin in vivo in mouse hearts and in vitro in cultured rat cardiomyocytes after exposure to GR [glucocorticoid receptor]-selective agonists. Glucocorticoids are released as a natural part of the body’s protective response to a heart attack.
Although the authors of this paper2 did not mention niacin or the fact that the niacin flush is caused as a result of the release in the skin of PGD2, it is hard not to speculate that there may be a connection between the niacin flush and the very substantial (and not entirely explained) cardiovascular benefits of niacin. If PGD2 in skin is released in response to the same signals as that in heart cells, then the skin flush could be a part of a much more important process than the mere sensation of hot and itching skin. Perhaps we shouldn’t get rid of the niacin flush.
Aspirin has been reported to be a possible way to mitigate or eliminate the niacin flush. (It is a known anti-prostaglandin compound.) However, we personally have not noticed any interference between taking a daily 81 mg low dose aspirin and the occurrence of niacin flushing.
- Walters et al. Beta-arrestin 1 mediates nicotinic acid-induced flushing, but not its anti-lipolytic effect, in mice. J Clin Invest 119(5):1312-21 (2009).
- Tokudome et al. Glucocorticoid protects rodent hearts from ischemia/reperfusion injury by activating lipocalin-type prostaglandin D synthase-derived PGD2 biosynthesis. J Clin Invest 119(6):1477-88 (2009)
GET YOUR “NIACIN FLUSH” AND MUCH MORE IN THE MOST POTENT MULTI-VITAMIN ON THE MARKET TODAY!
Karl Loren MD
So, thanks for the question, giving me the chance to provide some data that can be very helpful to many people. It is well known that niacin is the safest way of reducing cholesterol counts — without any other medication. It’s also very inexpensive. However, you should know that high cholesterol readings are NOT a risk factor for heart disease. A great majority of doctors will tell you this, but it is not true. Niacin will do that very safely. The number one selling drug in America today, Lipitor, at $8 billion per year.
First, what you have experienced is the very well known “niacin flush.” It is a very healthy action of niacin, as you’ll see as you read.
You get this action from niacin, but NOT from niacinamide. Niacinamide was deliberately created to eliminate those factors in this B3 vitamin which cause the flush. While there are certain benefits from niacinamide, the real winner here is B3, the niacin.
Niacin has the property of causing the small blood vessels to increase in size. These are the capillaries. Now, capillaries are often so small that the blood cells pass through them in single file. It is the capillaries that take care of the vast majority of all the cells in the body. You have large arteries near the heart, and they get smaller and smaller as they extend from the heart. But, at the end of every well-sized artery is a very large network of capillaries.
They all start from the heart — but at the end of the line they are tiny, tiny capillaries.
Now, there are many miles of the small capillaries in your body — a vast network which gets within a small fraction of an inch of EVERY cell in the body. It is the capillaries which nourish the cells and which carry away the toxins.
Now, add into this equation the fact that most of the toxins in the body are stored in fat cells. These fat cells can hold on to toxins for years, never letting it go until some “event” (like sweating or exercise). Then, the fat cells give up their toxins and they start leaking out into the surrounding tissues. You can have a slow-leak batch of fat cells that are poisoning you constantly. Much of the disease that plagues mankind certainly comes from the constant slow leak of toxins from these fat cells.
These fat cells, like the millions of others, are all within a fraction of an inch of some capillary, but IF that capillary is clogged (as mostoften they are), and if the blood cells move through them only one cell at a time (single file), then you can see that there is not much chance for those toxins to be cleaned up by the flow of blood.
If you could find something that would increase the size of these capillaries, and not cause any harmful or adverse reaction, you can see how beneficial this would be. In fact, niacin does this — it causes these miles of tiny capillaries to increase in size. It is the INCREASE in size, partly, which causes your skin to get red.
While there are miles of these capillaries all through your body, it is near the surface of your body where the arteries are NOT! So, as all the large surface of your body, your skin, is nourished by these small capillaries, and as the capillaries get larger, you can naturally see how the skin would show that increase in blood by getting red!
There is another substance to learn a bit about — it is a hormone called “histamine.” You know of this substance when you buy “anti-histamine” medicines. Without getting into a long story on that, the “anti-histamine” substances are meant to reduce the action of histamine — this is usually not good!
What does histamine do in the body? Well, first it can be produced by EVERY cell in the body. And, it is nature’s warning signal.
Whenever a cell is in danger (as, for instance, from a mosquito bite!), the cells that are in danger emit histamine. That wonderful hormone has the ability to send a message to those places in the body which change the blood flow — to send more blood (water) to that area to provide the nutrients needed to heal the problem, and to carry away the toxins.
So, when a mosquito bites you, the area around the bite itches and swells. That is the action of histamine coming to the rescue — bringing extra blood to supply nutrients to the cells that have been poisoned by the mosquito bite, and to carry away the poison.
When a cell is completely overwhelmed (as when it is loaded with toxins) it is in such apathy that it can’t even release histamine — in other words, it is so sick that it can’t even call for help. Now, take a look at those cells near the capillaries. They are often loaded with toxins and there is never enough blood flowing near them to take the toxins away. Now, put some niacin in your body!
The capillaries increase in size. How much? I don’t know exactly, but often at least double in size. Now, you have two blood cells going through the capillary, side-by-side. The chances that this increased blood flow can take away some of those toxins is at least double what it had been. As those poor cells start coming back to life — getting rid of toxins, they rise UP to the level where they can send out calls for help. They send out small quantities of the hormone, histamine. Histamine causes an itchy feeling anywhere it goes. It also causes the body to send more water (blood) to that area, but what YOU experience is the red skin and the itchy reaction from histamine.
If you take niacin and DON’T have a flush, it could be that your capillaries are too far gone to be helped, or more likely, you don’t have a lot of toxins ready to be removed just then.
So, you should seek the niacin flush. It does a great deal of good for your body — increasing blood flow, taking nutrients to areas that are starved, and taking AWAY some of those toxins that cause illness, tiredness and disease.
More than 100 scientific studies have been published about niacin. Niacin is a vitamin that has a “getting used to” level. In other words, the first time you take niacin you may have the flush. If you keep taking the same amount each day, you will have the flush, maybe, on the second or third day, but by the fourth day you won’t have any flush.
Then is when you should deliberately increase your niacin dose. There is a critically valuable detoxification method based on this increasing dose of niacin If you start with 50 mg per day, you probably won’t have a flush — too small.
If you start with 100 mg, you will probably have that flush. If you keep taking 100 mg of niacin every day, then after one or two days, you won’t have the flush. Then, you could increase the dosage to 200 mg.
It is not always predictable. You talk of taking large doses for several days, and then taking only 500 mg and getting a dramatic flush. There are other factors besides food and exercise, but they’ll wait for another day.
I took gradually increasing amounts over a long period until I got up to 5,000 mg of niacin per day — and of course had no flush what-so-ever after a couple days at 5,000 mg!
Yes, the itch and redness can be very dramatic sometimes. And, hardly anything will reduce that experience except time. You should not jump around a lot with a large dose one day and then no niacin for a few days. If you do that, your body will lose its “tolerance” to the niacin and you’ll have a big reaction on the day when you take a large quantity.
Normally if you take, say, 100 mg and get the flush, the flush will not be very dramatic. Then increase gradually.
Also, whether or not you get the flush, and how much of a flush, depends on what food you have eaten when. It also depends on whether you’ve done some exercise before taking the niacin.
I’ll bet you’ve never found this much information about niacin anywhere!