Vitamin B3 (Niacine). Pharmacological uses and Toxicity

by sydshahid

Six Principles of Physical, mental and Spiritual Health (PMSH)

Dr Shahid has summarized his six principles of health in a very simple form. Simplicity sometimes may not be politically correct. Well... What is wrong if you get the message and decide to live until 100 - 125 years and longer; without ever having to see any health care provider (MD,DO, DC, NP, PA, DP, DD, OD, psychiatrist, psychologist, spiritualist etc); during all your long and healthy life? Moreover, you will live a life that is full of vigor, enthusiasm, happiness and contentment for 100-125 years and even longer.

What else can anyone ask for? Does it sound too good to be true?

Well… IT IS "too good" and IT IS "true".

Remember! Health is what "YOU" make of it. It is "YOUR" responsibility. Not your health care provider's.

Follow these six principles of Dr Shahid’s Preventive Health. Also known as "Preventive Healthy Life Style (PHLS)", and see the result for yourself. You be the judge. The best part of it is, "it won’t cost you a penny". It is all free. And

"YOU WILL NEVER HAVE TO SEE ANY HEALTH CARE PROVIDER FOR AS LONG AS YOU LIVE."

As they say,

"One ounce of prevention is better than two pounds of cure."

So here are the six principles of holistic preventive healthy life style.

The basis of these six principles (holistic prevention) is already discussed in previous blogs. Let us discuss these principles in detail.


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The first principle of preventive health is a balanced diet. It consists of three parts:

1. Proteins, Fat & Carbohydrates in right proportion.
2. Vitamins, Minerals, fibers (VMF)
3. Water and Oxygen

We have completed an elaborate detail of the essential nutrients of balanced diet (Proteins, Fats and Carbohydrates) in previous blogs.

We have also given a brief description of #2 Vitamins, Minerals, fibers (VMF)

Let us describe vitamins in little more detail.

Very few people know what vitamins are and what is their real function in human body.

A brief history of vitamins was given in last blog. let us start with vitamins one by one in detail.

Vitamins are classified as either water-soluble or fat soluble. In humans there are 13 vitamins: 4 fat-soluble (A, D, E and K) and 9 water-soluble (8 B vitamins and vitamin C).

A. Fat-soluble vitamins

Fat-soluble vitamins are absorbed through the intestinal tract with the help of lipids (fats). Because they are more likely to accumulate in the body, they are more likely to lead to hypervitaminosis than are water-soluble vitamins. Fat-soluble vitamin regulation is of of particular significance in cystic fibrosis. Fat-soluble vitamins (vitamins A ,D, E and K), have been discussed already.

Now we discuss the Water-soluble vitamins.

B. Water-soluble vitamins

Water-soluble vitamins dissolve easily in water, and in general, are readily excreted from the body, to the degree that urinary output is a strong predictor of vitamin consumption. Because they are not readily stored, consistent daily intake is important. Many types of water-soluble vitamins are synthesized by bacteria.

The B vitamins are eight water-soluble vitamins that play important roles in cell metabolism. Historically, the B vitamins were once thought to be a single vitamin, referred to as vitamin B (much like how people refer to vitamin C or vitamin D). Later research showed that they are chemically distinct vitamins that often coexist in the same foods. Supplements containing all eight are generally referred to as a vitamin B complex. Individual B vitamin supplements are referred to by the specific name of each vitamin (e.g. B1, B2, B3 etc ).

We discussed a detailed account of Vitamin B1 (Thiamine) and Vitamin B2 (Riboflavinin), Vitamin B3 (Niacine), its history, sources and dosage in last blogs. Now we continue with its Pharmacological uses and Toxicity.
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Pharmacological uses of Vitamin B3 (Niacine)

1. Vitamin B3 has been reported to prevent Alzheimer's-like symptoms in a mouse model of the disease.

2. Niacin, prescribed in doses between 1000 and 2000 mg two to three times daily, blocks the breakdown of fats in adipose tissue, more specifically the very-low-density lipoprotein (VLDL), precursor of low-density lipoprotein (LDL) or "bad" cholesterol. Because niacin blocks breakdown of fats, it causes a decrease in free fatty acids in the blood and, as a consequence, decreased secretion of VLDL and cholesterol by the liver.

3. By lowering VLDL levels, niacin also increases the level of high-density lipoprotein (HDL) or "good" cholesterol in blood, and therefore it is sometimes prescribed for patients with low HDL, who are also at high risk of a heart attack.

4. As of August 2008, a combination of niacin with laropiprant is tested in a clinical trial. Laropiprant reduces facial flushes induced by Niacin. Niacin in cholesterol lowering doses (500-2000 mg per day) causes facial flushes by stimulating biosynthesis of prostaglandin D2, especially in the skin. PG D2 acts as a vasodilator via DP1 receptors, increasing blood flow and thus leading to flushes. Laropiprant acts as a DP1 antagonist, reducing the vasodilation.

5. Niacin and drug screening tests

Niacin is sometimes consumed in large quantities by people who wish to fool drug screening tests, particularly for lipid soluble drugs such as marijuana. It is believed to "promote metabolism" of the drug and cause it to be "flushed out". There is no scientific evidence indicating effectiveness in masking drug use, and overdose may result in arrhythmias, metabolic acidosis, hyperglycemia, and other serious problems.

Toxicity

People taking pharmacological doses of niacin (1.5 - 6 g per day) often experience side-effects that can include

1. Dermatological complaints such as dry skin, skin rashes including acanthosis nigricans (hyperpigmentation of the skin).

Skin flushing is the most commonly reported side effect. It lasts for about 15 to 30 minutes, and is sometimes accompanied by a prickly or itching sensation, particularly in areas covered by clothing. This effect is mediated by prostaglandin (and can be blocked by taking 300 mg of aspirin half an hour before taking niacin, or by taking one tablet of ibuprofen per day. Taking the niacin with meals also helps reduce this side effect. After 1 to 2 weeks of a stable dose, most patients no longer flush. Slow- or "sustained"-release forms of niacin have been developed to lessen these side-effects. One study showed the incidence of flushing was significantly lower with a sustained release formulation though doses above 2 g per day have been associated with liver damage, particularly with slow-release formulations.

2. Gastrointestinal complaints, such as dyspepsia (indigestion) and

3.Liver toxicity (severe liver failure) have also been reported.

4. Also reported include hyperglycemia (high blood sugar), thereby worsening diabetes mellitus.

5. Cardiac arrhythmias (irregular heart beats),

6. Birth defects (its use during pregnancy is contrindicated)

7. Orthostasis (also called Orthostatic hypotension or postural hypotension), is a dizzy spell when there is a sudden fall in blood pressure, typically greater than 20/10 mm Hg, that occurs when a person assumes a standing position, usually after a prolonged period of rest.

8. Hyperuricemia is another side-effect of taking high-dose niacin, and may exacerbate gout.

9. Niacin at extremely high doses can have life-threatening acute toxic reactions.

Extremely high doses of niacin can also cause niacin maculopathy, a thickening of the macula and retina which leads to blurred vision and blindness. This maculopathy is reversible after stopping niacin intake.

Inositol hexanicotinate vs regular Niacine

One popular form of dietary supplement is inositol hexanicotinate, usually sold as "flush-free" or "no-flush" niacin (although those terms are also used for regular sustained-release.) While this form of niacin does not cause the flushing associated with the nicotinic acid form, it is not pharmacologically equivalent in its positive effect. Prescription grade niacin is available and is proven to reduce cholesterol. Thus far there is not enough evidence to recommend inositol hexanicotinate to treat dyslipidemia. Niacin when taken in slowly increasing doses will cause far less flushing.


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we will continue next with Vitamin B5 (Pantothenic acid)

For comment and questions please write to :

syedshahidmd@yahoo.com.au

P.S. I must thank all of those readers who send me comments and questions. I must tell them that their inspiring comments and questions are highly appreciated. Please continue to write, preferably via email.

Thanks

Sydshahid

Posted 4/22/2009 6:58:10 PM
About the Author



Syed Shahid MD
View profile

Perth,  WA

Interests: Dr Sydney Shahid has many interests. He ejoys reading scietific magazines. He likes to keep himself busy with latest medical researches. He has special interest in Alzheimer’s illness. he has strong evidence that this tragedy can be delayed (if not prevented) for as long as 25 - 30 years and even longer, if one follows Dr Shahid’d six principles of health faithfully. He likes to make friends with those who have similar interests as his. He has few friends and they all appreciate what he is doing for humanity. He believes in positive thinking. In his opinion one must pursue those interests which make one believe in oneself. He loves to play tennis, table tennis and cricket if he can find time. Travelling is his other interest. He has travelled all over the world. He enjoys different cultures and their varied way of life. Lately world politics has become his passion. He wishes to see peace in the world but he doesn’t think it is possible because of the greed in the mind of most of the industrialised nations who are exploiting third world countries. He is also interested in writing a book about his Six Principle of Health (EUREKA). He is already in the process of making it happen. He wants the whole world to know his secret of healthy long life.

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