Vitamin B3 (Niacin)

Written by Slawomir (“Swavak”) Gromadzki, MPH

We know that B vitamins work together and all are essential for preserving our mental health and mood, normal metabolism and energy levels. But, what if one of them, alone, held astonishing health benefits? This exceptional B vitamin is called Vitamin B3 or Niacin. It is a water-soluble vitamin which is involved in more than 50 metabolic processes. It helps in the release of energy from food, the maintenance of a normal body weight, healthy nervous system, proper blood circulation, cholesterol levels, brain function, strong joints, along with a healthy skin and proper digestion. Niacin also supports hormone production (especially in the adrenal glands), liver, DNA repair, cell signalling, and genetic stability. Chronic Vitamin B3 deficiency leads to pellagra and its symptoms which include dementia, low mood or depression, skin problems, and diarrhoea.

Boosts energy & metabolism promoting normal body weight

Of all the B vitamins, the deficiency of Vitamin B3 can cause most serious problems, not the least of which is chronic fatigue. Vitamin B3 is fundamental to feeling full of pep. It is known to be beneficial in improving mental energy, memory, focus and alertness. Your body needs Vitamin B3 to convert fats, proteins and carbohydrates to energy to function properly. In this way it also helps to burn more calories and maintain normal body weight.

Helps improve mental health and brain function

Niacin contributes to normal functioning of the nervous system and promotes healthy psychological function. There are studies which seem to suggest that no other vitamin or mineral seem to be able to impose more positive influence on mood and emotional well-being than Vitamin B3, especially among individuals with an underlying deficiency. This beneficial effect of Vitamin B3 is associated with its stimulating and balancing effect on brain-derived neurotrophic factor, hormones, and serotonin (the good mood hormone).

Promotes healthy skin and hair

Research shows that Vitamin B3 can help keep ageing skin firm and glowing. It also helps protect skin cells from sun damage. A 2015 study found that taking Vitamin B3 supplement in the form of Nicotinamide significantly increased the level of skin protection. Since Vitamin B3 helps to maintain the structure of the blood vessels and improves blood circulation it brings more blood flow to the skin and hair follicles, providing them with more oxygen and nutrients, thus stimulating hair growth and skin health.

Promotes healthy joints & protects insulin-producing pancreas cells

According to the National Institute of Health Vitamin B3 in the form of Niacinamide can be very beneficial in improving joint health as taking supplements with this vitamin seems to improve joint flexibility and functionality. According to a study published in The British Journal of Clinical Practice, Nicotinamide type of Vitamin B3 may protect insulin-producing pancreas cells from damage and improve insulin secretion. In this way Vitamin B3 delays the need for insulin.

Non Flush Vitamin B3

Since Vitamin B3 in the form of nicotinic acid often causes hot flushes, tingling and itching the HealthAid Vitamin B3 is in the Non Flush form of Niacin called Nicotinamide.

 

TYPES OF VITAMIN B3 (NIACIN)

Niacin (Vitamin B3) (nicotinic acid) is one of the B vitamins that help to break down proteins and fats converting them into energy.

Niacin raises good cholesterol HDL, lowers triglycerides and bad cholesterols LDL and VLDL. Being a vasodilator Niacin causes blood vessels to widen thus lowering blood pressure and preventing heart attacks or strokes.

Unfortunately, since niacin is a vasodilator it also causes the skin blood vessels to dilate leading to a redness of the skin called hot flushes as well as other sensations such as tingling and itching. Fortunately, this effect usually lasts for only about 20 to 30 minutes and is not dangerous. In addition, if larger doses of niacin are taken regularly, the body gradually builds up a tolerance and minimizes this effect. It’s the nicotinic acid that causes this flushing effect and usually this effect is triggered by doses over 500mg but more sensitive individuals can develop flashes with doses as low as 50mg. The flushing effect can be minimized by taking niacin immediately after meals.

The no-flush vitamin B3 generally doesn’t contain the nicotinic acid but other forms of this vitamin. They still can increase energy, metabolism and are beneficial for the nervous system but are not very effective in lowering cholesterol and high blood pressure. To lower cholesterol I would suggest taking pure nicotinic acid staring from lower doses of 2 times 50 to 100mg after meals and slowly increasing the dose while controlling symptoms.

According to Abram Hoffer, M.D., Ph.D., “Niacin is one of the best substances for elevating high density lipoprotein cholesterol (the “good cholesterol) and so decreases the ratio of the total cholesterol over high density cholesterol.”

There are 3 types of Vitamin B3 (Niacin):

Nicotinic acid (flush), lowers cholesterol.

Nicotinamide (or Niacinamide) “no-flush”, no effect on cholesterol levels. Dr. Hoffer: “In my opinion, it is less effective in inducing relaxation and calming effects.”

Inositol hexanicotinate “no-flush”, some say no effect on cholesterol levels. Others (Dr Hoffer) say it does (but even if it does it looks like it is not as effective as Nicotinic acid).

Nicotinic acid is known to lower two types of “bad” cholesterol (LDL and VLDL) as well as increase levels of “good” cholesterol (HDL). In fact, it is able to increase HDL more than any other medication.

The nicotinic acid is the substance that causes the flushing side effect of niacin. The flush normally begins as a deep red in the face and then spreads to the rest of the body. Intense warmth and itching usually accompany the flush and this lasts for about 30 minutes. Other side effects of niacin include increased blood sugar levels, increased uric acid levels (which can affect people with gout), dry skin, stomach irritation, or heartburn.

How can “flushing” be avoided?

Flushing may also be reduced if niacin is taken after meals.

Avoid hot drinks or alcohol for 1 to 2 hours after taking niacin, as this can add to the flushing.

If you are just starting to take niacin, begin at a low dose and gradually increase the dose. The good news is that the flushing effect often decreases over time as you get used to taking niacin. In fact, many patients find that the flushing stops after 1 to 2 weeks of being on a stable dose of niacin.

There are some people who should not take niacin, such as those who have a history of stomach ulcers.

Dr A Hoffer:

Niacin and niacinamide are equally effective for schizophrenia, but higher doses of niacin can be tolerated without nausea.

Inositol hexaniacinate (a no-flush form of niacin) works, too, but not quite as well.

Only niacin or inositol hexaniacinate can lower cholesterol; niacinamide does not.

There is nothing wrong with niacinAMIDE, by the way. That form of vitamin B-3 is frequently found in multiple vitamins and B-complex preparations. Niacinamide does not cause a flush at all. In my opinion, it is less effective in inducing relaxation and calming effects. 

 

Dr Andrew Soul

HOW TO DETERMINE A SATURATION LEVEL OF NIACIN

Niacin is vitamin B-3, one of the water soluble B-complex vitamins. One of niacin’s unique properties is its ability to help you naturally relax and get to sleep more rapidly at night. And it is well established that niacin helps reduce harmful cholesterol levels in the bloodstream. Abram Hoffer, M.D., Ph.D. explains: “Niacin is one of the best substances for elevating high density lipoprotein cholesterol (the “good cholesterol) and so decreases the ratio of the total cholesterol over  high density cholesterol.”

Another niacin feature is its ability to greatly reduce anxiety and depression. Yet another feature of niacin is that it dilates blood vessels and creates a sensation of warmth, called a “niacin flush.”

The idea is to initially take just enough niacin to have a slight flush.  This means a pinkness about the cheeks, ears, neck, forearms and perhaps elsewhere. A slight niacin flush should end in about fifteen minutes or so. If you take too much niacin, the flush may be more pronounced and longer lasting.  If you flush beet red for half an hour and feel weird, well, you took too much. And a large dose of niacin on an empty stomach is certain to cause profound flushing. Niacin should always be taken immediately after finishing ones meal.

I have found that the best way for me to accurately control the flushing sensation is to start with very small amounts of niacin and gradually increase until the first flush is noticed. One method is to start with a mere 25 milligrams (25 mg) three times a day, say with each meal. The next day, try 50 mg at breakfast, 25 mg at lunch and 25 mg at supper. The following day, one might try 50 mg at breakfast, 50 mg at lunch, and 25 mg at supper. And, the next day, 50 mg at each of the three meals. The next day, 75 mg, 50 mg and 50 mg.  Then, 75. 75 and 50, and so on. In this way you have increased at the easy rate of only 25 mg per day. One would continue to increase the dosage by 25 mg per day until the flush occurs.

It is difficult to predict a saturation level for niacin because each person is different. As a general rule, the more you hold, the more you need.  If you flush early, you don’t need much niacin. If flushing doesn’t happen until a high level, then your body is obviously using the higher amount of the vitamin.

Since a flush indicates saturation of niacin, it is desirable to continue to repeat the flushing, just very slightly, to continue the saturation. This could be done three or more times a day. To get to sleep sooner at night, niacin can be taken to saturation at bedtime, too. You might be asleep before you even notice the flush.

An important point here is that niacin is a vitamin, not a drug. It is not habit forming. Niacin does not require a prescription because it is that safe.  It is a nutrient that everyone needs each day. Different people in different circumstances require different amounts of niacin.

Says Dr. Hoffer: “A person’s “upper limit is that amount which causes nausea, and, if not reduced, vomitingThe dose should never be allowed to remain at this upper limit. The usual dose range is 3,000 to 9,000 milligrams daily divided into three doses, but occasionally some patients may need more. The toxic dose for dogs is about 5,000 milligrams per 2.2 pounds (1 kilogram) body weight. We do not know the toxic dose for humans since niacin has never killed anyone.”

Persons with a history of heavy alcohol use, liver disorders, diabetes, or experiencing pregnancy will especially want to have their physician monitor their use of niacin in quantity. 

If a niacin tablet is taken on an empty stomach, a flush will occur (if it is going to occur at all) within about 20 minutes. If niacin is taken right after a meal, a flush may be delayed. In fact, the flush may occur long enough afterwards that you forgot that you took the niacin! Don’t let the flush surprise you.

If you want a flush right away, you can powder the niacin tablet. This is easily done by crushing it between two spoons. Powdered niacin on an empty stomach can result in a flush within minutes. Sustained release niacin is often advertised as not causing a flush at all. This claim may not be completely true; sometimes the flush is just postponed. It would probably be difficult to determine your saturation level with a sustained- or time-released product.  They are also more costly. But the biggest reason to avoid sustained-release niacin is that most reports of side effects stem from use of that form.

There is nothing wrong with niacinAMIDE, by the way. That form of vitamin B-3 is frequently found in multiple vitamins and B-complex preparations. Niacinamide does not cause a flush at all. In my opinion, it is less effective in inducing relaxation and calming effects. Niacinamide also does not lower serum cholesterol. This is an important distinction to make when purchasing.

It is a good idea to take all the other B-complex vitamins in a separate supplement in addition to the niacin. The B-vitamins, like professional baseball players, work best as a team. Still, the body seems to need proportionally more niacin than the other B vitamins. Even the U.S. Recommended Daily Allowance (RDA) for niacin is much more than for any other B-vitamin.  Many physicians consider the current RDA for niacin of only 20 mg to be way too low for optimum health. While the government continues to discuss this, it is possible to decide for yourself based on the success of doctors that use niacin for their patients every day.

QUESTION: Dr. Hoffer. He had written that the niacin flush is normal with many people and will diminish or go away as the patient continues to use niacin at his recommended level of 3,000 milligrams per day. You, however, state that the flush is an indication of no niacin deficiency. Who is correct or am I misinterpreting one of you?”

Andrew Saul’s Response: This is how I look at it: Generally speaking, people in fairly good health usually choose to increase their doses gradually in order to minimize flushing. If they do increase the dose slowly, what I describe is pretty accurate. For instance, I’ve been taking niacin for years, in daily but varying doses depending on my stress level or dietary intake. I know by the flush when I’ve had enough for the moment. It is like turning off the hot water when the tub is full enough for a nice bath. Dr Hoffer is highly experienced with serious psychiatric cases. Such patients have a niacin dependency, not a mere deficiency. Let’s let him speak for himself:

Abram Hoffer, MD, writes: “We are both correct. Most people flush at the beginning and gradually get adapted to it unless they stop for a few days and then resume it. A few cannot ever get used to it, and they take the no-flush preparations. But the intensity of the flush is very variable. Generally people who need it the most flush the least. That includes arthritics, schizophrenics, and elderly people with cardiovascular problems. Some schizophrenics do not flush until they get well and then they do. But the presence of the flush or its intensity cannot be uniquely used measure the need as there are too many variables such as food in the stomach, whether the drink with it is hot or cold, the kind of food, other medication.”

The standard dose for treating cholesterol is one to three grams daily.

There are three categories based on the rate of release of the niacin:

Immediate-release niacin is effective and least expensive, but causes more flushing. It has to be taken two or three times a day.

Sustained-release/extended-release niacin causes less flushing. However, some over-the-counter formulations may be less effective and increase the risk of liver toxicity. The extended-release form sold by prescription (Niaspan is the best-known brand) is effective, least likely to cause in­­tense flushing and safer for the liver—but it costs even more than brand-name statins. An over-the-counter sustained-release preparation called Slo-Niacin is similar to Niaspan but much less expensive.

 Niacin can be used to treat high cholesterol levels thanks to its role in fat metabolism, but niacinamide does not work for this purpose.

Niacinamide may be useful for treating osteoarthritis, according to the National Institutes of Health.

Either niacin or niacinamide can be used to treat mental disorders such as depression and anxiety.

Niacin is taken by mouth for high cholesterol. It is also used along with other treatments for circulation problems, migraine headache, Meniere’s syndrome and other causes of dizziness. Niacin is taken by mouth for preventing vitamin B3 deficiency and related conditions such as pellagra. It is also taken by mouth for schizophrenia, hallucinations due to drugs, Alzheimer’s disease and age-related loss of thinking skills, chronic brain syndrome, muscle spasms, depression, motion sickness, alcohol dependence, blood vessel swelling linked with skin lesions, and fluid collection (edema).

Some people taken niacin by mouth for acne, attention deficit-hyperactivity disorder (ADHD), preventing premenstrual headache, lowering blood pressure, improving circulation, improving orgasms, and preventing cataracts.

Osteoarthritis. Taking niacinamide seems to improve joint flexibility and reduce pain and swelling. Some people who take niacinamide might be able to cut down on standard painkilling medications.

Diabetes, types 1 and 2.

Erectile dysfunction. Taking extended-release niacin seems to improve penetration frequency and the duration of an erection after penetration in men with erectile dysfunction.

Pregnancy and breast-feeding: Niacin is LIKELY SAFE for pregnant and breast-feeding women when taken in the recommended amounts. The recommended amount of niacin for pregnant or breast-feeding women is 30 mg per day for women under 18 years of age, and 35 mg for women over 18.

Allergies: Niacin can make allergies more severe because they cause histamine, the chemical responsible for allergic symptoms, to be released.

Diabetes: Niacin might increase blood sugar. People with diabetes who take niacin or niacinamide should check their blood sugar carefully.

Gallbladder disease: Niacin might make gallbladder disease worse.

Gout: Large amounts of niacin might bring on gout.

Kidney disease: Niacin might accumulate in people with kidney disease. This might cause harm.

Liver disease: Niacin might increase liver damage. Don’t use large amounts if you have liver disease.

Stomach or intestinal ulcers: Niacin might make ulcers worse. Don’t use them if you have ulcers.

Very low blood pressure: Niacin might lower blood pressure and worsen this condition.

Thyroid disorders: Thyroxine is a hormone produced by the thyroid gland. Niacin might lower blood levels of thyroxine. This might worsen symptoms of certain thyroid disorders.

Are there interactions with medications?

Alcohol (Ethanol) Niacin can cause flushing and itchiness. Consuming alcohol along with niacin might make the flushing and itching worse. There is also some concern that consuming alcohol with niacin might increase the chance of having liver damage.

Allopurinol (Zyloprim), Clonidine (Catapres), Medications for diabetes (Antidiabetes drugs), Medications used for lowering cholesterol (Bile acid sequestrants), Medications used for lowering cholesterol (Statins), Probenecid, Sulfinpyrazone (Anturane), GEMFIBROZIL (Lopid)

Are there interactions with herbs and supplements?

Beta-carotene

A combination of niacin and the prescription drug simvastatin (Zocor) raises HDL (high density lipoprotein) cholesterol (“good cholesterol”) in people with coronary heart disease and low HDL levels. However, taking niacin along with combinations of antioxidants, including beta-carotene, seems to blunt this rise in HDL. It is not known whether this effect happens in people who don’t have coronary heart disease.

Chromium

Taking niacin and chromium together might lower blood sugar. If you have diabetes and take chromium and niacin supplements together, monitor your blood sugar to make sure it doesn’t get too low.

Herbs and supplements that lower blood pressure (hypotensive herbs and supplements)

Niacin might lower blood pressure. Taking niacin with other herbs and supplements that also lower blood pressure might cause blood pressure to drop too much. Other herbs and supplements that can lower blood pressure include andrographis, casein peptides, cat’s claw, coenzyme Q10, L-arginine, lycium, stinging nettle, theanine, and others.

Herbs and supplements that might harm the liver

Niacin, especially in higher doses can cause liver damage. Taking niacin along with other herbs or supplements that might harm the liver could increase this risk. Some of these products include androstenedione, borage leaf, chaparral, comfrey, dehydroepiandrosterone (DHEA), germander, kava, pennyroyal oil, red yeast, and others.

Herbs and supplements that might slow blood clotting

Niacin might slow blood clotting. Using niacin along with other herbs and supplements that also slow blood clotting might increase the risk of bleeding in some people. Some other herbs of this type include angelica, clove, danshen, garlic, ginger, Panax ginseng, and others.

Kombucha tea

There is some concern that kombucha tea might decrease niacin absorption. However, this needs to be studied more.

Selenium

A combination of niacin and the prescription drug simvastatin (Zocor) raises HDL (high density lipoprotein) cholesterol (“good cholesterol”) in people with coronary heart disease and low HDL levels. However, taking niacin along with combinations of antioxidants, including selenium, seems to blunt this rise in HDL. It is not known whether this effect happens in people who don’t have coronary heart disease.

Tryptophan

Some tryptophan from the diet can be converted into niacin in the body. Taking niacin and tryptophan together might increase levels and side effects of niacin.

Vitamin C

A combination of niacin and the prescription drug simvastatin (Zocor) raises HDL (high density lipoprotein) cholesterol (“good cholesterol”) in people with coronary heart disease and low HDL levels. However, taking niacin along with combinations of antioxidants, including vitamin C, seems to blunt this rise in HDL. It is not known whether this effect happens in people who don’t have coronary heart disease.

Vitamin E

A combination of niacin and the prescription drug simvastatin (Zocor) raises HDL (high density lipoprotein) cholesterol (“good cholesterol”) in people with coronary heart disease and low HDL levels. However, taking niacin along with combinations of antioxidants, including vitamin E, seems to blunt this rise in HDL. It is not known whether this effect happens in people who don’t have coronary heart disease.

Zinc

The body can make niacin. People who are malnourished and have niacin deficiency, such as chronic alcoholics, make extra niacin if they take zinc. There might be an increased risk of niacin-related side effects such as flushing and itching if niacin and zinc are taken together.

 

Vitamin B-3: Niacin and Its Amide

by A. Hoffer, M.D., Ph.D.

The term vitamin B-3 was reintroduced by my friend Bill W., co-founder of Alcoholics Anonymous, (Bill Wilson). We met in New York in 1960. Humphry Osmond and I introduced him to the concept of mega vitamin therapy. We described the results we had seen with our schizophrenic patients, some of whom were also alcoholic. We also told him about its many other properties. It was therapeutic for arthritis, for some cases of senility and it lowered cholesterol levels.

Bill was very curious about it and began to take niacin, 3 g daily. Within a few weeks fatigue and depression which had plagued him for years were gone.

He gave it to 30 of his close friends in AA and persuaded them to try it. Within 6 months he was convinced that it would be very helpful to alcoholics. Of the thirty, 10 were free of anxiety, tension and depression in one month. Another 10 were well in two months.

Vitamin B-3 is made from nicotine, a poison produced in the tobacco plant to protect itself against its predators, but in the wonderful economy of nature which does not waste any structures, when the nicotine is simplified by cracking open one of the rings, it becomes the immensely valuable vitamin B-3.

Vitamin B-3 is made in the body from the amino acid tryptophan. On the average 1 mg of vitamin B-3 is made from 60 mg of tryptophan, about 1.5%.

The best-known vitamin deficiency disease is pellagra. More accurately it is a tryptophan deficiency disease since tryptophan alone can cure the early stages.

The dementia is a late stage phenomenon. In the early stages it resembles much more the schizophrenias, and can only with difficulty be distinguished from it. The only certain method used by early pellagrologists was to give their patients in the mental hospitals small amounts of nicotinic acid. If they recovered they diagnosed them pellagra, if they did not they diagnosed them schizophrenia. This was good for some of their patients but was not good for psychiatry since it prevented any continuing interest in working with the vitamin for their patients who did not recover fast, but who might have done so had they given them a lot more for a much longer period of time, the way we started doing this in Saskatchewan. I consider it one of the schizophrenic syndromes.

Indications

These are psychiatric disorders including children with learning and behavioral disorders, the addictions including alcoholism and drug addiction, the schizophrenias, some of the senile states. Its efficacy for a large number of both mental and physical conditions is an advantage to patients and to their doctors who use the vitamin, but is difficult to accept by the medical profession raised on the belief that there must be one drug for each disease, and that when any substance appears to be too effective for many conditions, it must be due entirely to its placebo effect, something like the old snake oils.

I have thought about this for a long time and have within the past year become convinced that this vitamin is so versatile because it moderates or relieves the body of the pernicious effect of chronic stress. It therefore frees the body to carry on its routine function of repairing itself more efficiently. The current excitement in medicine is the recognition that hyperoxidation, the formation of free radicals, is one of the basic damaging processes in the body. These hyperexcited molecules destroy molecules and damage tissues at the cellular level and at the tissue level.

All living tissue which depends on oxygen for respiration has to protect itself against these free radicals. Plants use one type of antioxidants and animals use another type. Fortunately there is a wide overlap and the same antioxidants such as vitamin C are used by both plants and animals. There is growing recognition that the system adrenaline -> adrenochrome plays a major role in the reactions to stress. I have elaborated this in a further report for this journal. [4]

The catecholamines, of which adrenalin is the best known example, and the aminochromes, of which adrenochrome is the best known example, are intimately involved in stress reactions. Therefore to moderate the influence of stress or to negate it, one must use compounds which prevent these substances from damaging the body. Vitamin B-3 is a specific antidote to adrenalin, and the antioxidants such as vitamin C, Vitamin E, beta carotene, selenium and others protect the body against the effect of the free radicals by removing them more rapidly from the body. Any disease or condition which is stress related ought therefore to respond to the combined use of vitamin B-3 and these antioxidants provided they are all given in optimum doses, whether small or large as in orthomolecular therapy. I will therefore list briefly the many indications for the use of vitamin B-3.

For each condition I will describe one case to illustrate the therapeutic response. For each condition I can refer to hundreds and thousands of case histories and have already in the literature described many of them in detail. [5]

Psychiatric
1) The Schizophrenias. I have reviewed this for this journal. [6]

2) Children with Learning and/or Behavioral Disorders.

In 1960 seven year-old Bruce came to see me with his father. Bruce had been diagnosed as mentally retarded. He could not read, could not concentrate, and was developing serious behavioral problems such as cutting school without his parents’ knowledge. He was being prepared for special classes for the retarded. He excreted large amounts of kryptopyrrole, the first child to be tested. I started him on nicotinamide, one gram tid. Within four months he was well. He graduated from high school, is now married, has been fully employed and has been paying income tax. He is one case out of about 1500 I have seen since 1960.

Current treatment is more complicated as described in this Journal. [7]

3) Organic Confusional States, non-Alzheimers forms of dementia, electroconvulsive therapy-induced memory disturbances. 

In 1954 I observed how nicotinic acid relieved a severe case of post ECT amnesia in one month. Since then I have routinely given it in conjunction with ECT to markedly decrease the memory disturbance that may occur during and after this treatment. I would never give any patient ECT without the concomitant use of nicotinic acid. It is very helpful, especially in cardiovascular-induced forms of dementia as it reverses sludging of the red blood cell and permits proper oxygenation of the cells of the body. For further information see Niacin Therapy in Psychiatry. [8]

In September 1992, Mr. C., 76 years-old, requested help with his memory. He was terribly absentminded. If he decided to do something, by the time he arrived where he wanted to do it he had forgotten what it was he wanted to do. His short-term memory was very poor and his long-term memory was beginning to be affected. I started him on a comprehensive vitamin program including niacinamide 1.5 G daily. Within a month he began to improve. I added niacin to his program. By February 1993 he was normal. April 26, 1993, he told me he had been so well he had concluded he no longer needed any niacin and decreased the dose from 3.0 G to 1.5 G daily. He remained on the rest of the program. Soon he noted that his short term memory was failing him again. I advised him to stay on the full dose the rest of his life.

4) An antidote against d-LSD,9,10 and against adrenochrome. [5]

5) Alcoholism.

Bill W. conducted the first clinical trial of the use of nicotinic for treating members of Alcoholics Anonymous. [11] He found that 20 out of thirty subjects were relieved of their anxiety, tension and fatigue in two months of taking this vitamin, 1 G tid. I found it very useful in treating patients who were both alcoholic and schizophrenic. The first large trial was conducted by David Hawkins who reported a better than 90% recovery rate on about
90 patients. Since then it has been used by many physicians who treat alcoholics. Dr. Russell Smith in Detroit has reported the largest series of patients. [12]

Physical

  1. Cardiovascular

Of the two major findings made by my research group in Saskatchewan, the  nicotinic acid-cholesterol connection is well known and nicotinic acid is used worldwide as an economical, effective and safe compound for lowering cholesterol and elevating high density cholesterol. As a result of my interest in nicotinic acid, Altschul, Hoffer and Stephen [3] discovered that this vitamin, given in gram doses per day, lowered cholesterol levels. Since then it was found it also elevates high density lipoprotein cholesterol thus bringing the ratio of total over HDL to below 5.

In the National Coronary Study, Canner [2] showed that nicotinic acid decreased mortality and prolonged life. Between 1966 and 1975, five drugs used to lower cholesterol levels were compared to placebo in 8341 men, ages 30 to 64, who had suffered a myocardial infarction at least three months before entering the study. About 6000 were alive at the end of the study. Nine years later, only niacin had decreased the death rate significantly from all causes. Mortality decreased 11% and longevity increased by two years. The death rate from cancer was also decreased.

This was a very fortunate finding because it led to the approval by the FDA of this vitamin in mega doses for cholesterol problems and opened up the use of this vitamin in large doses for other conditions as well. This occurred at a time when the FDA was doing its best not to recognize the value of megavitamin therapy. Its position has not altered over the past four decades.

Our finding opened up the second major wave of interest in vitamins. The first wave started around 1900 when it was shown that these compounds were very effective in small doses in curing vitamin deficiency diseases and in preventing their occurrence. This was the preventive phase of vitamin use. The second wave recognized that they have therapeutic properties not directly related to vitamin deficiency diseases but may have to be used in large doses. This was the second or present wave wherein vitamins are used in therapy for more than deficiency diseases. Our discovery that nicotinic acid was an hypocholesterolemic compound is credited as the first paper to initiate the second wave and paved the way for orthomolecular medicine which came along several years later.

  1. Arthritis

I first observed the beneficial effects of vitamin B-3 in 1953 and 1954. I was then exploring the potential benefits and side effects from this vitamin. Several of the patients who were given this vitamin would report after several months that their arthritis was better. At first this was a surprise since in the psychiatric history I had taken I had not asked about joint pain. This report of improvement happened so often I could not ignore it. A few years later I discovered that Prof. W. Kaufman had studied the use of this vitamin for the arthritides before 1950 and had published two books describing his remarkable results. [13] Since that time this vitamin has been a very important component of the orthomolecular regimen for treating arthritis.

The following case illustrates both the response which can occur and the complexity of the orthomolecular regimen. Patients who are early into their arthritis respond much more effectively and are not left with residual disability.

K.V. came to my office April 15, 1982. She was in a wheelchair pushed by her husband. He was exhausted, depressed, and she was one of the sickest patients I have ever seen. She weighed under 90 pounds. She sat in the chair on her ankles which were crossed beneath her body because she was not able to straighten them out. Her arms were held in front of her, close to her body, and her fingers were permanently deformed and claw-like. She told me she had been deeply depressed for many years because of the severe pain and her major impairment. As she was being wheeled into my office I saw how ill she was and immediately concluded there was nothing I could do for her, and had to decide how I could let her know without sending her even deeper into despair. However I changed my mind when she suddenly said, “Dr. Hoffer, I know no one can ever cure me but if you could only help me with my pain. The pain in my back is unbearable. I just want to get rid of the pain in my back.” I realized then she had a lot of determination and inner strength and that it was worthwhile to try and help her.

She began to suffer from severe pain in her joints in 1952. In 1957 it was diagnosed as arthritis. Until 1962 her condition fluctuated and then she had to go into a wheelchair some part of the day. She was still able to walk although not for long until 1967. In 1969 she depended on the wheelchair most of the time, and by 1973 she was there permanently. For awhile she was able to propel herself with her feet. After that she was permanently dependent on help. For the three years before she saw me she had gotten some home care but most of the care was provided by her husband. He had retired from his job when I first saw them. He provided the nursing care equivalent to four nurses on 8 hour shifts including holiday time. He had to carry her to the bathroom, bathe her, cook and feed her. He was as exhausted as she was but he was able to carry on.

She was severely deformed, especially her hands, suffered continuous pain, worse in her arms, and hips and her back. Her ankles were badly swollen and she had to wear pressure bandages. Her muscles also were very painful most of the day. She was able to feed herself and to crochet with her few useful fingers, but it must have been extremely difficult. She was not able to write nor type which she used to do with a pencil. A few months earlier she had been suicidal. On top of this severe pain and discomfort she had no appetite, was not hungry and a full meal would nauseate her. Her skin was dry, she had patches of eczema, and she had white areas in her nails.

I advised her to eliminate sugar, potatoes, tomatoes and peppers, (about 10% of arthritics have allergic reactions to the solanine family of plants). She was to add niacinamide 500 mg four times daily (following the work of W. Kaufman), ascorbic acid 500 mg four times daily (as an anti-stress nutrient and for subclinical scurvy), pyridoxine 250 mg per day (found to have anti-arthritic properties by Dr. J. Ellis), zinc sulfate 220 mg per day (the white areas in her nails indicated she was deficient in zinc), flaxseed oil 2 tablespoons and cod liver oil 1 tablespoon per day (her skin condition indicated she had a deficiency of omega 3 essential fatty acids). The detailed treatment of arthritis and the references are described in my book. [14]

One month later a new couple came into my room. Her husband was smiling, relaxed and cheerful as he pushed his wife in in her chair. She was sitting with her legs dangling down, smiling as well. I immediately knew that she was a lot better. I began to ask her about her various symptoms she had had previously. After a few minutes she impatiently broke in to say, “Dr. Hoffer, the pain in my back is all gone.” She no longer bled from her bowel, she no longer bruised all over her body, she was more comfortable, the pain in her back was easily controlled with aspirin and was gone from her hips, (it had not helped before). She was cheerful and laughed in my office. Her heart was regular at last. I added inositol niacinate 500 mg four times daily to her program.

She came back June 17, 1982, and had improved even more. She was able to pull herself up from the prone position on her bed for the first time in 15 years, and she was free of depression. I increased her ascorbic acid to 1 gram four times daily and added vitamin E 800 IU. Because she had shown such dramatic improvement I advised her she need no longer come to see me.

September 1, 1982, she called me on the telephone. I asked her how she was getting along. She said she was making even more progress. I then asked her how had she been able to get to the phone. She replied she was able to get around alone in her chair. Then she added she had not called for herself but for her husband. He had been suffering from a cold for a few days, she was nursing him, and she wanted some advice for him.

After another visit October 28, 1983, I wrote to her doctor “Today Mrs. K.V. reported she had stayed on the whole vitamin program very rigorously for 18 months, but since that time had slacked off somewhat. She is regaining a lot of her muscle strength, can now sit in her wheelchair without difficulty, can also wheel herself around in her wheelchair but, of course, can not do anything useful with her hands because her fingers are so awful. She would like to become more independent and perhaps could do so if something could be done about her fingers and also about her hip. I am delighted she has arranged to see a plastic surgeon to see if something can be done to get her hand mobilized once more. I have asked her to continue with the vitamins but because she had difficulty taking so many pills she will take a preparation called Multijet which is available from Portland and contains all the vitamins and minerals and can be dissolved in juice. She will also take inositol niacinate 3 grams daily.”

I saw her again March 24, 1988. About 4 of her vertebra had collapsed and she was suffering more pain which was alleviated by Darvon. It had not been possible to treat her hands surgically. She had been able to eat by herself until six months before this last visit. She had been taking small amounts of vitamins. She was able to use a motorized chair. She had been depressed. I wrote to her doctor, “She had gone off the total vitamin program about two or three years ago. It is very difficult for her to swallow and I can understand her reluctance to carry on with this. I have therefore suggested that she take a minimal program which would include inositol niacinate 3 grams daily, ascorbic acid 1 gram three times, linseed oil 2 capsules and cod liver oil 2 capsules. Her spirits are good and I think she is coming along considering the severe deterioration of her body as a result of the arthritis over the past few decades.” She was last seen by her doctor in the fall of 1989.

Her husband was referred. I saw him May 18, 1982. He complained of headaches and a sense of pressure about his head present for three years. This followed a series of light strokes. I advised him to take niacin 3 grams daily plus other vitamins including vitamin C. By September 1983 he was well and when seen last March 24, 1988 was still normal.

  1. Juvenile Diabetes

Dr. Robert Elliot, Professor of Child Health Research at University of Auckland Medical School is testing 40,000 five-year old children for the presence of specific antibodies that indicate diabetes will develop. Those who have the antibodies will be given nicotinamide. This will prevent the development of diabetes in most the children who are vulnerable. According to the Rotarian for March 1993 this project began 8 years ago and has 3200 relatives in the study. Of these, 182 had antibodies and 76 were given nicotinamide. Only 5 have become diabetic compared to 37 that would have been expected. Since 1988 over 20,100 school children have been tested. None have become diabetic compared to 47 from the untested comparable group. A similar study is underway in London, Ontario.

  1. Cancer

Recent findings have shown that vitamin B-3 does have anti-cancer properties. This was discussed at a meeting in Texas in 1987, Jacobson and Jacobson. [15] The topic of this international conference was “Niacin, Nutrition, ADP-Ribosylation and Cancer,” and was the 8th conference of this series.

Niacin, niacinamide and nicotinamide adenine dinucleotide (NAD) are interconvertable via a pyridine nucleotide cycle. NAD, the coenzyme, is hydrolyzed or split into niacinamide and adenosine dinucleotide phosphate (ADP-ribose). Niacinamide is converted into niacin, which in turn is once more built into NAD. The enzyme which splits ADP is known as poly (ADP-ribose) polymerase, or poly (ADP) synthetase, or poly (ADP-ribose) transferase. Poly (ADP-ribose) polymerase is activated when strands of deoxyribonucleic acid (DNA) are broken. The enzyme transfers NAD to the ADP-ribose polymer, binding it onto a number of proteins. The poly (ADP-ribose) activated by DNA breaks helps repair the breaks by unwinding the nucleosomal structure of damaged chromatids. It also may increase the activity of DNA ligase. This enzyme cuts damaged ends off strands of DNA and increases the cell’s capacity to repair itself. Damage caused by any carcinogenic factor, radiation, chemicals, is thus to a degree neutralized or counteracted.

Jacobson and Jacobson, conference organizers, hypothesized that niacin prevents cancer. They treated two groups of human cells with carcinogens. The group given adequate niacin developed tumors at a rate only 10% of the rate in the group deficient in niacin. Dr. M. Jacobson is quoted as saying, “We know that diet is a major risk factor, that diet has both beneficial and detrimental components. What we cannot assess at this point is the optimal amount of niacin in the diet… The fact that we don’t have pellagra does not mean we are getting enough niacin to confer resistance to cancer.” About 20 mg per day of niacin will prevent pellagra in people who are not chronic pellagrins. The latter may require 25 times as much niacin to remain free of pellagra.

Vitamin B-3 may increase the therapeutic efficacy of anti-cancer treatment. In mice, niacinamide increased the toxicity of irradiation against tumors. The combination of normobaric carbogen with nicotinamide could be an effective method of enhancing tumor radiosensitivity in clinical radiotherapy where hypoxia limits the outcome of treatment. Chaplin, Horsman and Aoki16 found that nicotinamide was the best drug for increasing radiosensitivity compared to a series of analogues. The vitamin worked because it enhanced blood flow to the tumor. Nicotinamide also enhanced the effect of chemotherapy. They suggested that niacin may offer some cardioprotection during long-term adriamycin chemotherapy.

Further evidence that vitamin B-3 is involved in cancer is the report by Nakagawa, Miyazaki, Okui, Kato, Moriyama and Fujimura [17] that in animals there is a direct relationship between the activity of nicotinamide methyl transferase and the presence of cancer. Measuring the amount of N-methyl nicotinamide was used to measure the activity of the enzyme. In other words, in animals with cancer there is increased destruction of nicotinamide, thus making less available for the pyridine nucleotide cycle. This finding applied to all tumors except the solid tumors, Lewis lung carcinoma and melanoma B-16.

Gerson [18] treated a series of cancer patients with special diets and with some nutrients including niacin 50 mg 8 to 10 times per day, dicalcium phosphate with vitamin D, vitamins A and D, and liver injections. He found that all the cancer cases were benefited in that they became healthier and in many cases the tumors regressed. In a subsequent report Gerson elaborated on his diet. He now emphasized a high potassium over sodium diet, ascorbic acid, niacin, brewers yeast and lugols iodine. Right after the war there was no ready supply of vitamins as there is today. I would consider the use of these nutrients in combination very original and enterprising. Dr. Gerson was the first physician to emphasize the use of multivitamins and some multiminerals. More details are
in Hoffer. [19]

Additional evidence that vitamin B-3 is therapeutic for cancer arises from the National Coronary Study, Canner. [2]

  1. Concentration Camp Survivors

In 1960 I planned to study the effect of nicotinic acid on a large number of aging people living in a sheltered home. A new one had been built. I approached the director of this home, Mr. George Porteous. I arranged to meet him and told him what I would like to do and why. I gave him an outline of its properties, its side effects and why I thought it might be helpful. Mr. Porteous agreed and we started this investigation. A short while after my first contact Mr. Porteous came to my office at University Hospital. He wanted to take nicotinic acid himself, he told me, so that he could discuss the reaction more intelligently with people living in his institution. He wanted to know if it would be safe to do so.

That fall he came again to talk to me and this time he said he wanted to tell me what had happened to him. Then I discovered he had been with the Canadian troops who had sailed to Hong Kong in 1940, had been promptly captured by the Japanese and had survived 44 months in one of their notorious prisoner of war camps.

Twenty-five percent of the Canadian soldiers died in these camps. They suffered from severe malnutrition from starvation and nutrient deficiency. They suffered from beri beri, pellagra, scurvy, infectious diseases, and brutality from the guards.

Porteous, a physical education instructor, had been fit weighing about 190 pounds when he got there. When he returned home he weighed only 2/3rds of that. On the way home in a hospital ship the soldiers were fed and given extra vitamins in the form of rice polishings. There were few vitamins available then in tablets or capsules. He seemingly recovered but had remained very ill. He suffered from both psychological and physical symptoms. He was anxious, fearful and slightly paranoid. Thus, he could never be comfortable sitting in a room unless he sat facing the door. This must have arisen from the fear of the guards. Physically he had severe arthritis. He could not raise his arms above his shoulders. He suffered from heat and cold sensitivity. In the morning he needed his wife’s help in getting out of bed and to get started for the day. He had severe insomina. For this he was given barbiturates in the evening and to help awaken him in the morning, he was given amphetamines.

Later I read the growing literature on the Hong Kong veterans and there is no doubt they were severely and permanently damaged. They suffered from a high death rate due to heart disease, crippling arthritis, blindness and a host of other conditions.

Having outlined his background he then told me that two weeks after he started to take nicotinic acid, 1 gram after each meal, he was normal. He was able to raise his arms to their full extension, and he was free of all the symptoms which had plagued him for so long. When I began to prepare my report [20] I obtained his Veterans Administration Chart. It came to me in two cardboard boxes and weighed over ten pounds, but over 95% of it was accumulated before he started on the vitamin. For the ten years after he started on the vitamin there was very little additional material. One could judge the efficacy of the vitamin by weighing the chart paper before and after he started on it. Porteous remained well as long as he stayed on the vitamin until his death when he was Lieutenant Governor of Saskatchewan. In 1962, after having been well for two years, he went on a holiday to the mountains with his son and he forgot to take his nicotinic acid with him. By the time he returned home almost the entire symptomatology had returned.

Porteous was enthusiastic about nicotinic acid and began to tell all his friends about it. He told his doctor. His doctor cautioned him that he might damage his liver. Porteous replied that if it meant he could stay as well as he was until he died from a liver ailment he would still not go off it. His doctor became an enthusiast as well and within a few years had started over 300 of his patients on the vitamin. He never saw any examples of liver disease from nicotinic acid.

I have treated over 20 prisoners from Japanese camps and from European concentration camps since then with equally good results. I estimated that one year in these camps was equivalent to 4 years of aging, i.e. four years in camp would age a prisoner the equivalent of 16 years of normal living.

George Porteous wanted every prisoner of war from the eastern camps treated as he had been. He was not successful in persuading the Government of Canada that nicotinic acid would be very helpful so he turned to fellow prisoners, both in Canada (Hong Kong Veterans) and to American Ex-Prisoners of War. These American veterans suffered just as much as had the Canadian soldiers since they were treated in exactly the same abysmal way. The ones who started on the vitamin showed the same response. Recently one of these soldiers, a retired officer, wrote to me after being on nicotinic acid 20 years that he felt great, owed it to the vitamin and that when his arteries were examined during a simple operation they were completely normal. He wrote, “About two years ago, I was hit, was bleeding down the neck. The MDs took the opportunity to repair me. They said the arteries under the ears look like they had never been used.”

There is an important lesson from the experiences of these veterans and their response to megadoses of nicotinic acid. This is that every human exposed to severe stress and malnutrition for a long enough period of time will develop a permanent need for large amounts of this vitamin and perhaps for several others.

This is happening on a large scale in Africa where the combination of starvation, malnutrition and brutality is reproducing the conditions suffered by the veterans. Those who survive will be permanently damaged biochemically, and will remain a burden to themselves and to the community where they live. Will society have the good sense to help them recover by making this vitamin available to them in optimum doses?

Doses

The optimum dose range is not as wide as it is for ascorbic acid, but it is wide enough to require different recommendations for different classes of diseases. As is always the case with nutrients, each individual must determine their own optimum level. With nicotinic acid this is done by increasing the dose until the flush (vasodilation) is gone, or is so slight it is not a problem.

One can start with as low a dose as 100 mg taken three times each day after meals and gradually increase it. I usually start with 500 mg each dose and often will start with 1 gram per dose especially for cases of arthritis, for schizophrenics, for alcoholics and for a few elderly patients. However, with elderly patients it is better to start small and work it up slowly.

No person should be given nicotinic acid without explaining to them that they will have a flush which will vary in intensity from none to very severe. If this is explained carefully, and if they are told that in time the flush will not be a problem, they will not mind. The flush may remain too intense for a few patients and the nicotinic acid may have to be replaced by a slow release preparation or by some of the esters, for example, inositol niacinate. The latter is a very good preparation with very little flush and most find it very acceptable even when they were not able to accept the nicotinic acid itself. It is rather expensive but with quantity production the price might come down.

The flush starts in the forehead with a warning tingle. Then it intensifies. The rate of the development of the flush depends upon so many factors it is impossible to predict what course it will follow.

The following factors decrease the intensity of the flush: a cold meal, taking it after a meal, taking aspirin before, using an antihistamine in advance.

The following factors make the flush more intense: a hot meal, a hot drink, an empty stomach, chewing the tablets and the rate at which the tablets break down in liquid.

From the forehead and face the flush travels down the rest of the body, usually stopping somewhere in the chest but may extend to the toes. With continued use the flush gradually recedes and eventually may be only a tingling sensation in the forehead. If the person stops taking the vitamin for a day or more the sequence of flushing will be re-experienced. Some people never do flush and a few only begin to flush after several years of taking the vitamin. With nicotinamide there should be no flushing but I have found that about 2% will flush. This may be due to rapid conversion of the nicotinamide to nicotinic acid in the body.

When the dose is too high for both forms of the vitamin the patients will suffer from nausea at first, and then if the dose is not reduced it will lead to vomiting. These side effects may be used to determine what is the optimum dose. When they do occur the dose is reduced until it is just below the nausea level. With children the first indication may be loss of appetite. If this does occur the vitamin must be stopped for a few days and then may be resumed at a lower level. Very few can take more than 6 grams per day of the nicotinamide. With nicotinic acid it is possible to go much higher. Many schizophrenics have taken up to 30 grams per day with no difficulty. The dose will alter over time and if on a dose where there were no problems, they may develop in time. Usually this indicates that the patient is getting better and does not need as much. I have divided all patients who might benefit from vitamin B-3 into the following categories.

Category 1. These are people who are well or nearly well, and have no obvious disease. They are interested in maintaining their good health or in improving it. They may be under increased stress. The optimum dose range varies between 0.5 to 3 grams daily. The same doses apply to nicotinamide.

Category 2. Everyone under physiological stress, such as pregnancy and lactation, suffering from acute illness such as the common cold or flu, or other diseases that do not threaten death. All the psychiatric syndromes are included in this group including the schizophrenias and the senile states. It also includes the very large group of people with high blood cholesterol levels or low HDL when it is desired to restore these blood values to normal. The dose range is 1 gram to 10 grams daily. For nicotinamide the range is 1 1/2 g to 6 g.

Nicotinamide does not affect cholesterol levels.

Side Effects

Here are Dr. John Marks’ conclusions. [21]

“A tingling or flushing sensation in the skin after relatively large doses (in excess of 75 mg) of nicotinic acid is a rather common phenomenon. It is the result of dilation of the blood vessels that is one of the natural actions of nicotinic acid and one for which it is used therapeutically. Whether this should therefore be regarded as a true adverse reaction is a moot point. The reaction clears regularly after about 20 minutes and is not harmful to the individual. It is very rare for this reaction to occur at less than three times the RDA, even in very sensitive individuals. In most people much larger quantities are required. The related substance nicotinamide only very rarely produces this reaction and in consequence this is the form generally used for vitamin supplementation.

“Doses of 200 mg to 10 g daily of the acid have been used therapeutically to lower blood cholesterol levels under medical control for periods of up to 10 years or more and though some reactions have occurred at these very high dosages, they have rapidly responded to cessation of therapy, and have often cleared even when therapy has been continued.

“In isolated cases, transient liver disorders, rashes, dry skin and excessive pigmentation have been seen. The tolerance to glucose has been reduced in diabetics and patients with peptic ulcers have experienced increased pain. No serious reaction have been reported however even in these high doses. The available evidence suggests that 10 times the RDA is safe (about 100 mg).”

Dr. Marks is cautious about recommending that doses of 100 mg are safe. In my opinion, based upon 40 years of experience with this vitamin the dose ranges I have recommended above are safe. However with the higher doses medical supervision is necessary.

Jaundice is very rare. Fewer that ten cases have been reported in the medical literature. I have seen none in ten years. When jaundice dose occur it is usually an obstructive type and clears when the vitamin is discontinued. I have been able to get schizophrenic patients back on nicotinic acid after the jaundice cleared and it did not recur.

Four serious cases have been reported, all involving a sustained release preparation. Mullin, Greenson & Mitchell (1989) [22] reported that a 44 year-old man was treated with crystalline nicotinic acid, 6 grams daily, and after 16 months was normal. He then began to take a sustained-release preparation, same dose. Within three days he developed nausea, vomiting, abdominal pain, dark urine. He had severe hepatic failure and required a liver transplant. Henkin, Johnson & Segrest found three patients who developed hepatitis with sustained release nicotinic acid. When this was replaced with crystalline nicotinic acid there was no recurrent liver damage. [23]

Since jaundice in people who have not been taking nicotinic acid is fairly common it is possible there is a random association. The liver function tests may indicate there is a problem when in fact there is not. Nicotinic acid should be stopped for five days before the liver function tests are given. One patient who had no problem with nicotinic acid for lowering cholesterol switched to the slow release preparations and became ill. When he resumed the original nicotinic acid he was well again with no further evidence of liver dysfunction. I have not seen any cases reported anywhere else. I have described much more fully the side effects of this vitamin elsewhere. [24]

Inositol hexaniacinate is an ester of inositol and nicotinic acid. Each inositol molecule contains six nicotinic acid molecules. This ester is broken down slowly in the body. It is as effective as nicotinic acid and is almost free of side effects. There is very little flushing, gastrointestinal distress and other uncommon side effects. Inositol, considered one of the lesser important B vitamins, does have a function in the body as a messenger molecule and may add something to the therapeutic properties of the nicotinic acid.

Conclusion

Vitamin B-3 is a very effective nutrient in treating a large number of psychiatric and medical diseases but its beneficial effect is enhanced when the rest of the orthomolecular program is included. The combination of vitamin B-3 and the antioxidant nutrients is a great anti-stress program.

Reprinted with the permission of the author:

Abram Hoffer, M.D., Ph.D.

References

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Hoffer A: Safety, Side Effects and Relative Lack of Toxicity of Nicotinic acid and Nicotinamide. Schizophrenia 1:78-87, 1969.

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