B3 NIACIN OR NIACINAMIDE

B3 NIACIN OR NIACINAMIDE

itamin B3 may Enhance the Function of these Substances

Amino Acids

Vitamin B3 is essential for the formation of endogenous Carnitine.

       Vitamin B3 facilitates the transport of Proline across the blood-brain barrier.

       Vitamin B3 facilitates the synthesis of endogenous Serine.

       Vitamin B3 enhances the function of Phenylalanine.  references

Vitamin B3 is a cofactor for the conversion of Tyrosine to L-Dopa.

Carbohydrates

Vitamin B3 is involved in the metabolism of Carbohydrates.

Coenzymes – Electron Transport System

Vitamin B3 is an essential component of Nicotinamide Adenine Dinucleotides (NADs) and supplemental Vitamin B3 (especially the Niacinamide form of Vitamin B3) increases the body’s level of NADs:  references

–     Approximately 33% of the body’s endogenous NADH is produced from Vitamin B3.  references

Digestive System

Vitamin B3 may stimulate the production of Hydrochloric Acid (HCl).

Enzymes

Vitamin B3 is essential for the production of Delta-5 Desaturase.

       Vitamin B3 is essential for the activity of Poly(ADP-ribose)polymerase (PARP):  references

–     PARP requires Nicotinamide Adenine Dinucleotide (NAD) as a substrate, and is very sensitive to NAD concentrations.  Vitamin B3 is required for the production of NAD.

Vitamin B3 is a cofactor for production of. Superoxide Dismutase (SOD).

Hormones

Vitamin B3 functions as a cofactor for the production of Corticosteroid Hormones (via NADs).

       Vitamin B3 stimulates the release of Human Growth Hormone (hGH):

–     hGH release peaks at four hours after ingestion of Vitamin B3.

Vitamin B3 (Niacinamide form – 100 mg per night) facilitates the production of Melatonin (this occurs from the fact that the body uses some of its Tryptophan for the production of Niacinamide function – if pre-

formed Niacinamide is provided, this “frees up” more Tryptophan for its other function, the production of Melatonin).  references

Lipids

Vitamin B3 is a cofactor for the conversion of Alpha-Linolenic Acid (LNA) into further endogenous Fatty Acids.

       Vitamin B3 is a cofactor for the production of Prostaglandin E1 (PGE1) from Dihomo-Gamma Linolenic Acid (DGLA).  references

       Vitamin B3 (Niacinamide form applied topically) increases the production of Ceramides in the Stratum Corneum layer of the Skin.  references

Vitamin B3 is a cofactor for the conversion of Polyunsaturated Fatty Acids and Superunsaturated Fatty Acids to Prostaglandins:

–     The Nicotinic Acid (Niacin) form of Vitamin B3 stimulates the release of Prostaglandin D2 in the Skin (Prostaglandin D2 is the cause of the flushing of the Skin that occurs with Nicotinic Acid consumption).  references

–     Vitamin B3 is a cofactor for the production of Prostaglandin E1 (PGE1) from Dihomo-Gamma-

Linolenic Acid (DGLA).  references

Neurotransmitters

The Niacinamide form of Vitamin B3 is a cofactor for Gamma Aminobutyric Acid’s function of filling the Benzodiazepine Receptors within the Brain.

Nucleic Compounds

Vitamin B3 (especially the Niacinamide form) may help to repair damaged Deoxyribonucleic Acid (DNA).  references

Organic Acids

Vitamin B3 may stimulate the conversion of Lactic Acid to Pyruvic Acid.

       Vitamin B3 may stimulate the conversion of Lactic Acid to Pyruvic Acid.

Proteins

Vitamin B3 may enhance the synthesis of endogenous Proteins.

Quinones

The Niacinamide form of Vitamin B3 may be an essential cofactor for the endogenous production of Coenzyme Q10.  references

Vitamins

The Niacinamide form of Vitamin B3 may increase Choline levels in the Brain.  references

       A Vitamin B3 derivative (NADPH) is a cofactor for the conversion of dietary Folic Acid to its active form – Tetrahydrofolic Acid.  references

       Vitamin B3 is synergistic with Vitamin B12.

Vitamin B3 may Counteract these Potentially Toxic Substances

Aldehydes

The Niacinamide form of Vitamin B3 may lower Acetaldehyde levels by up to 50%.  references

Neurotoxins

The Niacinamide form of Vitamin B3 may inhibit the ability of MPTP to damage the Substantia Nigra and subsequently cause Parkinson’s Disease.  references

Pharmaceutical Drugs

Vitamin B3 may alleviate the Drug Dependence (withdrawal symptoms) caused by Benzodiazepines.  references

       Vitamin B3 may inhibit the ability of the Anti-Cancer Pharmaceutical Drugs utilized in Chemotherapy to damage the Chromosomes of Bone Marrow.  references

Recreational Drugs

The Nicotinic Acid form of Vitamin B3 (500 mg per day) may reduce the craving for Alcohol (ethanol) in persons afflicted with Alcoholism and the Niacinamide form of Vitamin B3 may exert a similar effect.  references

–     The Niacinamide form of Vitamin B3 may reduce Acetaldehyde levels (Acetaldehyde is the metabolite of Alcohol that causes most of the toxic effects associated with Alcohol consumption).  references

–     Niacinamide may inhibit the ability of Alcohol (ethanol) to damage the Liver.  references

These Substances may Enhance the function of Vitamin B3

Amino Acids

Isoleucine may improve the retention of Vitamin B3.

Minerals

Phosphorus is involved in the conversion of exogenous Vitamin B3 to its active endogenous coenzyme form.

Vitamins

Biotin may enhance the function of Vitamin B3.

       Inositol may stimulate Niacinamide to bind to the Benzodiazepine Receptors in the Brain.

       Vitamin B12 may enhance the function of Vitamin B3.

These Substances may Interfere with Vitamin B3

Aldehydes

Acetaldehyde may cause Vitamin B3 deficiency.  references

Amino Acids

Leucine may increase the urinary excretion of Vitamin B3.

Pharmaceutical Drugs

Penicillins may deplete the body’s supplies of Vitamin B3.

Minor Side Effects of Vitamin B3

These cautions apply to all forms of Vitamin B3.  Problems attributable to specific forms of Vitamin B3 are described under separate entries.

Skin

Vitamin B3 may occasionally worsen some Skin Allergies.

Dietary Sources of Vitamin B3  note

(mg of Vitamin B3 per 100 grams)

Cereal Grains:            White Rice    2     Brown Rice   6

Fish:       Cod 5     Mackerel      12

Herbs:           Rosehips       Hawthorn Berries      

Licorice         Blue Cohosh

Catnip          Eyebright    

Ginger          Dandelion   

Legumes:            Miso              Peas – Green 0.3

Meats:          Liver      13    Beef      10

Kidneys  13          

Nuts:            Almonds       0.8  Hazelnuts     0.1

Pecan Nuts  0.1   Pine Nuts     0.2

Peanuts 0.1   Chestnuts     0.2

Pistachio Nuts     0.2  Macadamia Nuts 0.1

Brazil Nuts   0.1   Coconut 0.02

Cashew Nuts 0.2  Walnuts 0.1

Sea Vegetables:         Kelp                   

Seeds:           Sunflower Seeds  0.3        

Vegetables:         Broccoli        Watercress   

Yeasts:          Brewer’s Yeast     100.0           

Forms of Vitamin B3

Inositol Hexanicotinate is a specific form of the Nicotinic Acid (Niacin) form of Vitamin B3 that does not cause the flushing (from Histamine release) that is normally associated with Nicotinic Acid ingestion.

       Niacytin is a bound and unavailable form of Vitamin B3 present in some foods, especially Cereals and Grains.

Niacinamide (also known as Nicotinamide) is the main form of Vitamin B3 present in dietary sources.  Chemically, it is the Amide of Nicotinic Acid.

       Nicotinic Acid (Niacin) is the acid form of Vitamin B3.

       Xanthinol Nicotinate is a synthetic form of the Nicotinic Acid form of Vitamin B3 that can pass easily through Cell Membranes into Cells much more readily than Niacin

Dosage Recommendations

RDA vs Optimal

The official RDA for Vitamin B3 is 18 mg per day.

Therapeutic Dosages

The optimal daily allowance (ODA) for Vitamin B3 (in either its Niacinamide or Nicotinic Acid forms) (for adults) is 50 – 250 mg per day.

       The dosage of Vitamin B3 used in laboratory studies that have demonstrated the ability of Vitamin B3 to reduce Aggressiveness is 1,000 mg per day.

       The dosage of Vitamin B3 (Niacinamide form) used in clinical studies that have demonstrated the ability of Niacinamide to treat Osteoarthritis is 3,000 mg per day.

Bioavailability

The Niacinamide and Nicotinic Acid forms of Vitamin B3 are absorbed via the Small Intestines.  The Nicotinic Acid form of Vitamin B3 is also absorbed via the Stomach.

       Only 0.3% of ingested Vitamin B3 enters the Brain.

Commercial Availability of Vitamin B3 Supplements

“Singular” Oral Vitamin B3 Products

Vitamin B3 is available from health food stores and mail order supplement companies (worldwide) in the form of:

–     100 – 500 mg Niacinamide capsules

–     15 – 1,500 mg Niacinamide tablets

–     100 – 1,000 mg Nicotinic Acid capsules

–     500 mg non-flush Nicotinic Acid capsules

–     250 – 500 mg sustained-release Nicotinic Acid capsules

–     50 – 500 mg Nicotinic Acid tablets

–     loose Nicotinic Acid powder

–     250 – 600 mg Inositol Hexanicotinate capsules (mainly only sold in USA)

–     liquid Inositol Hexanicotinate (mainly only sold in USA)

–     loose Inositol Hexanicotinate powder (mainly only sold in USA)

Health Benefits of Niacinamide

The health benefits of Niacinamide are generally representative of those listed for Vitamin B3 – other health benefits of Niacinamide are listed in the topic for Vitamin B3.

Aging Process

Niacinamide (2,000 – 3,000 mg per day) may help to retard the Aging Process (at a cellular level) references and may function as a Life Extension agent.  references  The mechanism for this effect is as follows:

1.     Niacinamide increases levels of Nicotinamide Adenine Dinucleotide (NAD).

2.    NAD is a cofactor for the activity of Sir2p, an enzyme that upregulates the deacetylation (removal of Acetyl units) from Chromatin.

3.    Chromatin (when deacetylated) provides a “protective cover” to Deoxyribonucleic Acid (DNA).

4.    Extrachromasomal rDNA Circles (ERCs) (which stimulate a process known as Gene Silencing and therefore accelerate the Aging Process) are unable to issue “Cell strangulation and cellular death” messages to DNA that is protected by deacetylated Chromatin.

Cardiovascular System

Niacinamide may be an effective adjunct therapy for the early treatment of Stroke.  references

Cells

Niacinamide may help to counteract excessive Oxidation (Free Radicals)-induced Apoptosis of normal, healthy Cells.  references

Excretory System

Niacinamide may retard the development of Diabetic Nephropathy.  references

Eyes/Vision

Niacinamide may help to prevent Retinopathy.  references

Immune System

Niacinamide may inhibit the growth of Leishmania.  references

       Niacinamide (applied topically) may help to prevent Skin Cancer caused by excessive exposure to Ultraviolet Radiation (UV-B form).  references

Metabolism

Niacinamide may exert potent Antioxidant effects in the Brain.  references

       Niacinamide may lower elevated Blood Sugar levels.  references

       Niacinamide may alleviate Hypoglycemia.  references

       Niacinamide may retard the development of Diabetic Nephropathy in Diabetes Mellitus patients.  references

Niacinamide (2,000 mg per day) may help to prevent the onset of Diabetes Mellitus Type 1 (by protecting the Beta Cells of the Islets of Langerhans from destruction):  references

–     Daily administration of Niacinamide reduced the incidence of Diabetes Mellitus Type 1 by from 20% of a test population to 7.1% of the test population.

–     Note that Niacinamide does not have any effect on patients with established Diabetes Mellitus Type 1 as its primary effect is to protect the Beta Cells that have largely all been destroyed once Diabetes Mellitus Type 1 becomes evident.

Niacinamide may stabilize Blood Sugar levels in Diabetes Mellitus Type 2 patients.  references

       Niacinamide may inhibit the ability of Alcohol (ethanol) to damage the Liver.  references

Musculoskeletal System

Niacinamide (1,000 – 3,000 mg per day) may be an effective treatment for Osteoarthritis – Niacinamide therapy may improve the global impact of Osteoarthritis, may improve Joint flexibility, may reduce Inflammation and may permit Osteoarthritis patients to reduce their dosage of Anti-Inflammatory Drugs.  references

       Niacinamide may be useful for the treatment of Rheumatoid Arthritis.  references

Nervous System

Niacinamide (1,000 mg per day) may reduce Aggressiveness (by stimulating the conversion of Lactic Acid to Pyruvic Acid).  references

       Niacinamide may inhibit the damage to the Deoxyribonucleic Acid (DNA) content of Neurons that occurs during the progression of Alzheimer’s Disease.  references

Niacinamide (1,000 – 6,000 mg per day) may alleviate Anxiety (by enhancing the ability of GABA to bind to the Benzodiazepine Receptors within the Brain).  references

       Niacinamide (1,000 – 3,000 mg per day) may help to treat Autism.  references

       Niacinamide may exert potent Antioxidant effects in the Brain.  references

Niacinamide may help to prevent Parkinson’s Disease (by inhibiting the ability of MPTP to damage the Substantia Nigra).  references

       Niacinamide (500 – 800 mg per day) may reduce the symptoms of Phobias.  references

       Niacinamide (1,500 – 3,000 mg per day per day) may alleviate Schizophrenia.  references

Niacinamide (200 – 1,000 mg administered at bedtime) may improve the quality of Sleep (by binding to the Benzodiazepine Receptors of the Brain).  references

Respiratory System

Niacinamide may alleviate Asthma (it protects against Histamine-induced bronchoconstriction).  references

Skin

Niacinamide (gel containing 4% applied topically twice per day) may alleviate Acne.  references

       Niacinamide (cream applied topically) may lighten hyperpigmented areas of the Skin in Chloasma patients.  references

       Niacinamide (applied topically) may alleviate Dry Skin (by increasing the production of Ceramides in the Stratum Corneum layer of the Skin).  references

Niacinamide (3,000 mg per day) may alleviate Polymorphous Light Eruption.  references

       Niacinamide may be useful for the treatment of Psoriasis.  references

       Niacinamide (applied topically) may increase the production of Ceramides in the Stratum Corneum layer of the Skin.  references

Niacinamide (5% cream applied topically) may reduce Wrinkles.  references

Niacinamide may Enhance the Function of these Substances

Coenzymes

Supplemental Niacinamide increases the body’s production of Nicotinamide Adenine Dinucleotide (NAD):  references

–     Supplemental Niacinamide increases the body’s production of Nicotinamide Adenine Dinucleotide

 Phosphate (NADP). 

Hormones

Niacinamide (100 mg per night) may facilitate the production of Melatonin (this occurs from the fact that the body uses some of its Tryptophan for the production of Niacinamide – if pre-formed Niacinamide is provided, this “frees up” more Tryptophan for its other function, the production of Melatonin).  references

Lipids

Niacinamide (applied topically) may increase the production of Ceramides in the Skin.  references

Nucleic Compounds

Niacinamide may help to prevent damage to the body’s endogenous Deoxyribonucleic Acid (DNA).  references

Quinones

Niacinamide is an essential cofactor for the endogenous production of Coenzyme Q10.  references

Vitamins

Niacinamide may increase Brain Choline levels.  references

       Niacinamide can be converted within the body to Nicotinic Acid (however Nicotinic Acid cannot be reconverted back to Niacinamide).  references

Niacinamide may Counteract these Potentially Toxic Substances

Aldehydes

Niacinamide may lower Acetaldehyde levels by up to 50%.  references

Electromagnetic Radiation

Niacinamide (applied topically) may help to prevent Skin Cancer caused by excessive exposure to the UV-B form of Ultra-Violet Radiation.  references

Lipids

Niacinamide may counteract the toxic effects associated with Lipopolysaccharides.  references

Neurotoxins

Niacinamide may inhibit the ability of MPTP to damage the Substantia Nigra and subsequently cause Parkinson’s Disease.  references

Recreational Drugs

Niacinamide may inhibit the ability of Alcohol (ethanol) to damage the Liver.  references

       Niacinamide may reduce the craving for Alcohol in persons afflicted with Alcoholism:  references

–     Niacinamide may lower Acetaldehyde levels by up to 50%.  references

These Substances may Enhance the Function of Niacinamide

Amino Acids

Approximately 66% of the body’s Niacinamide content is derived from the metabolism of Tryptophan.

Bioavailability  references

Niacinamide is absorbed only via the Small Intestines.

       After its oral absorption, Niacinamide is present in the Blood plasma and is converted to its coenzyme form in Blood Cells, the Kidneys, the Brain and the Liver.

Commercial Availability of Niacinamide

“Singular” Oral Niacinamide Products

Niacinamide is available from health food stores and mail order supplement companies (worldwide) in the form of:

–     100 mg capsules

–     250 mg capsules

–     500 mg capsules

–     1,500 mg tablets

Topical Niacinamide Products

Topical Niacinamide is available from some internet-based suppliers in the form of:

–     cream containing 4% Niacinamide (designed for the treatment of Acne)

–     gel containing 5% Niacinamide (designed for the treatment of Acne) (Metazene)

Oral Formulas

Niacinamide is an ingredient in many multi-vitamin formulas and other specific purpose formulas.

Chemical Data

Chemically, Niacinamide is the active Amide of Nicotinic Acid.

Chemical Names

Pyridine-3-carboxamide

       3-Pyridinecarboxamide

       Pyridine-3-carboxylic acid amide

       3-pyridine carboxylic acid amide

Molecular Formula

C6H6N2O

Health Benefits of Nicotinic Acid

These beneficial actions are attributable specifically to the Nicotinic Acid form of Vitamin B3 – other beneficial actions of Nicotinic Acid are listed in the topic for “Vitamin B3”.

Aging & Life Extension

Nicotinic Acid may possess Life Extension properties.  references

Cardiovascular System

Nicotinic Acid may help to reverse Atherosclerosis.  references

       Nicotinic Acid may improve Blood Circulation.  references

       Nicotinic Acid may help to prevent abnormal Blood Clotting (by lowering elevated Fibrinogen levels).  references

Nicotinic Acid (25 mg per day) may help to treat Chilblains.  references

       Nicotinic Acid (by improving Blood Circulation to limbs) may sometimes eliminate the need for the amputation of limbs in Gangrene cases.  references

       Nicotinic Acid may reduce Blood Pressure in Hypertension patients.  references

Nicotinic Acid may help to prevent Heart Attacks and may reduce the recurrence rate for second Heart Attacks by 30%.  references

       Nicotinic Acid (especially the Inositol Hexanicotinate form – 4,000 mg per day for at least three months) may alleviate Intermittent Claudication by improving Blood Circulation to the legs.  references

Nicotinic Acid (especially the Inositol Hexanicotinate form) may alleviate Raynaud’s Disease by improving Blood Circulation to the hands and feet.  references

       Nicotinic Acid may help to prevent Stroke.  references

Digestive System

Nicotinic Acid may alleviate Hypochlorhydria.  references

Excretory System

Nicotinic Acid may inhibit the ability of Candida glabrata to cause Urinary Tract Infections (by inhibiting the ability of Candida glabrata to adhere to the epithelial cells of the Urinary Tract).  references

Hair

Nicotinic Acid (applied topically to the Scalp) may help to improve Blood Circulation to the Scalp (and may thereby help to retard Hair Loss).  Oral administration of 35 mg of Nicotinic Acid per day may also help to retard Hair Loss.  references

Immune System

Nicotinic Acid may reduce the mortality rate of Cancer patients and may help to prevent some forms of Cancer:  references

–     Nicotinic Acid may reduce the rate of recurrence of Bladder Cancer in people treated with Gamma-

Rays in Radiation Therapy.  [more info]

–     Nicotinic Acid may help to prevent Endometrial Cancer.  references

Nicotinic Acid may inhibit the ability of Candida glabrata to cause Urinary Tract Infections (by inhibiting the ability of Candida glabrata to adhere to the epithelial cells of the Urinary Tract).  references

Metabolism

Nicotinic Acid (2,000 – 3,000 mg per day) may lower serum Cholesterol:  references

–     Nicotinic Acid may increase HDL Cholesterol by 33%.  references

–     Nicotinic Acid may lower elevated LDL Cholesterol levels.  references

–     The Cholesterol lowering effect of Nicotinic Acid is achieved by interfering with a Liver enzyme that helps to produce endogenous Cholesterol.

–     Nicotinic Acid may reduce the body’s levels of VLDL Cholesterol.  references

Nicotinic Acid may inhibit Cross-Linking.  references

       Nicotinic Acid may lower elevated Lipoprotein (a) levels by up to 35%.  references

       Nicotinic Acid (1,200 – 2,000 mg per day) may lower serum levels of Triglycerides (by up to 52%).  references

Musculoskeletal System

Nicotinic Acid may alleviate Muscle Cramps that are caused by poor Blood Circulation.  references

Nervous System

Nicotinic Acid (1,000 – 3,000 mg) may terminate the Hallucinations and other symptoms of LSD “trips” within one hour of Nicotinic Acid ingestion.  references

       Nicotinic Acid may improve Memory in normal, otherwise-healthy, middle-aged adults by 10% to 40%:  references

–     Nicotinic Acid may improve Short-Term Memory.  references

Nicotinic Acid may alleviate the symptoms of Meniere’s Disease.  references

       Nicotinic Acid (administered by IV injection) may improve the condition of Multiple Sclerosis (MS) patients.  references

       Nicotinic Acid is highly beneficial for the treatment of (the Trigeminal Neuralgia form of) Neuralgia.  references

Nicotinic Acid may be useful for the treatment of Restless Legs Syndrome.  references

       Nicotinic Acid may alleviate Schizophrenia (it functions as a methyl scavenger and may therefore deactivate Adrenochrome – a compound that has been implicated in Schizophrenia).  references

Respiratory System

Nicotinic Acid may help to control Asthma attacks.  references

Sexual System

Nicotinic Acid may enhance Sexual Performance (by triggering the Histamine release that occurs during Orgasm).  references

Nicotinic Acid may Enhance the Function of these Substances

Factors

Two molecules of Nicotinic Acid are essential components of Glucose Tolerance Factor (GTF).

Hormones

Nicotinic Acid prevents the degradation of Adrenaline to Noradrenochrome (due to its role in the production of Nicotinamide Adenine Dinucleotide).

       Nicotinic Acid (taken on an empty stomach) stimulates the release of Human Growth Hormone (hGH) from the Pituitary Gland:  references

–     This effect does not occur when Nicotinic Acid is consumed with Food or on a full Stomach.

Lipids

Nicotinic Acid stimulates the release of Prostaglandin D2 in the Skin (Prostaglandin D2 is the cause of the flushing of the Skin that occurs with Nicotinic Acid consumption).  references

Nicotinic Acid may Counteract these Potentially Toxic Substances

Proteins

Nicotinic Acid may lower elevated Fibrinogen levels.  references

Recreational Drugs

Nicotinic Acid (500 mg per day) may reduce the craving for Alcohol in persons afflicted with Alcoholism.  references

       Nicotinic Acid (1,000 – 3,000 mg) may terminate the Hallucinations and other symptoms of LSD “trips” within one hour of Nicotinic Acid ingestion.  references

Nicotinic Acid may reduce the toxic effects of Nicotine.  [more info]

Neurotoxins

Nicotinic Acid may protect the body against excessive production of Adrenochrome and may reduce the toxic effects of Adrenochrome.  [more info]

These Substances may Enhance the Function of Nicotinic Acid

Amino Acids

Picolinic Acid (an isomer of Nicotinic Acid) can be manufactured within the body from Tryptophan – 60 mg of Tryptophan can generate 1 mg of Picolinic Acid).

Vitamins

Niacinamide can be converted within the body to Nicotinic Acid (however Nicotinic Acid cannot be reconverted back to Niacinamide).  references

These Substances may Counteract the Potential Side Effects of Nicotinic Acid

Alkaloids

Betaine (especially the Trimethylglycine (TMG) form of Betaine) may help to prevent the Liver damage that can occur with high-dose Nicotinic Acid therapy.  references

Side Effects of Nicotinic Acid

The cautions that apply generally to Vitamin B3 also apply to the Nicotinic Acid form of Vitamin B3.  The side effects of Nicotinic Acid do not occur with the use of the Inositol Hexanicotinate form of Nicotinic Acid.

Digestive System

Nicotinic Acid may (rarely) cause Diarrhea when supplemented at dosages above 100 mg per day.

       Nicotinic Acid may (rarely) cause Nausea when supplemented at dosages above 100 mg per day.

       If Nicotinic Acid is continually consumed on an empty Stomach, it may cause the release of excessive Hydrochloric Acid within the Stomach – which may increase the risk of Peptic Ulcers.

Metabolism

The Cholesterol-lowering effect of megadoses of Nicotinic Acid is due to its interference with a liver enzyme that helps to manufacture endogenous Cholesterol.  Excessive interference with this enzyme may cause Liver damage in  some persons.  references

Musculoskeletal System

Nicotinic Acid may (rarely) cause Muscle Cramps when supplemented at dosages above 100 mg per day.

Nervous System

Nicotinic Acid may (rarely) cause Headaches when supplemented at dosages above 100 mg per day.

Skin

Nicotinic Acid may cause Dry Skin when supplemented at dosages above 2,000 mg per day.

       Nicotinic Acid may cause Erythema (red flushing of the Skin) – especially when it is consumed on an empty Stomach (this side effect is generally harmless – it occurs as a result of dilation of the Capillaries that service the Skin and usually only persists for a period of one hour maximum).  The Erythema caused by Nicotinic Acid consumption occurs as a result of Prostaglandin D2 release stimulated by Nicotinic Acid.  references

Contraindications

Cardiovascular System

Arrhythmias patients should consult a doctor before using the Nicotinic Acid form of Vitamin B3.

Pharmaceutical Drugs

High-dose Nicotinic Acid (greater than 1,000 mg of Nicotinic Acid per day) should not be used concurrently with HMG-CoA Reductase Inhibitors (such as Lovastatin or Red Yeast Rice) as this combination increases the risk of Rhabdomyolysis.

Nicotinic Acid may Enhance these Toxic Substances

Amino Acids

Excessive consumption of Nicotinic Acid may increase Homocysteine levels.  references

Forms of Nicotinic Acid

Inositol Hexanicotinate (also known as Hexanicotinoyl Inositol, IHN, Inositol Hexaniacinate or Inositol Niacinate;  Inositol Nicotinate) consists of one molecule of Inositol bound to six molecules of Nicotinic Acid (by weight, 10% Inositol + 90% Nicotinic Acid).  Chemically, it is the hexanicotinic acid ester of Inositol.  Inositol Hexanicotinate is absorbed intact and then hydrolzyed within the body to release “free” Nicotinic Acid and Inositol.  Inositol Hexanicotinate is metabolized more slowly than “free” Nicotinic Acid – it does not reach maximum Blood Serum levels until approximately 10 hours after its oral ingestion:

–     This form of Nicotinic Acid is primarily used as a non-flushing, sustained-release form of Nicotinic Acid and is regarded by some experts as the optimal form of Nicotinic Acid.  The side effects associated with regular Nicotinic Acid do not occur with Inositol Hexanicotinate.  references

–     Inositol Hexanicotinate is regarded as the safest form of supplemental Nicotinic Acid and can be safely used in doses of up to 4,000 mg per day.

Picolinic Acid is an isomer of Nicotinic Acid (but which possesses different therapeutic properties to Nicotinic Acid).

       Xanthinol Nicotinate is a synthetic form of Nicotinic Acid consisting of Nicotinic Acid bound to Xanthinol.  It is classed as a Pharmaceutical Drug and as a Smart Drug.

Bioavailability

Inositol Hexanicotinate

The Inositol Hexanicotinate form of Nicotinic Acid is absorbed intact and then hydrolzyed within the body to release “free” Nicotinic Acid and Inositol.  Inositol Hexanicotinate is metabolized more slowly than “free” Nicotinic Acid – it does not reach maximum Blood Serum levels until approximately ten hours after its oral ingestion.  references

Nicotinic Acid

Nicotinic Acid is absorbed via the Small Intestines and the Stomach.

       Niacin is rapidly and extensively absorbed (at least 60 to 76% of dose) when administered orally.

       To maximize bioavailability and reduce the risk of gastrointestinal upset, administration of Nicotinic Acid with a low-fat meal or snack is recommended.

Nicotinic Acid and its metabolites are rapidly eliminated via the Urine.

Dosage Recommendations 

The dosage of Nicotinic Acid that has been shown in clinical trials to stimulate the release of Human Growth Hormone from the Pituitary Gland is 200 – 500 mg per day.

       The dosage of Nicotinic Acid that has been demonstrated to reduce the craving for Alcohol (ethanol) is 500 mg per day.

       The dosage of Nicotinic Acid to prevent Dementia varies according to one’s age:

–     At age 20 – 29, 100 mg may be effective.

–     At age 30 – 39, 200 mg may be effective

–     At age 40 – 49, 500 mg may be effective.

–     People over the age of 50 may require a daily dose of 1,000 mg to help prevent Dementia.

The recommended dosage of the Inositol Hexanicotinate form of Nicotinic Acid for lipid-lowering purposes and for improving conditions related to the Cardiovascular System is 1,500 mg – 4,000 mg per day, usually taken in two to three divided dosages during the day.  Doses of up to 4,000 mg per day of Inositol Hexanicotinate per day are regarded as safe.

       The dosage of Nicotinic Acid that lowers serum Cholesterol levels is 1,000 – 2,000 mg per day.  Caution:  This is a high dosage of Nicotinic Acid and should only be used on the advice of a health professional.

It is recommended that persons using supplemental Nicotinic Acid for managing their Cholesterol levels, consume their dosage at nightime (as most persons sleep during the “flushing period”;  in addition this timing is likely to produce better results as most endogenous Cholesterol is produced by the Liver during the night).

Commercial Availability of Nicotinic Acid Supplements

“Singular” Oral Nicotinic Acid Products

Niacin (Nicotinic Acid) is available from health food stores and mail order supplement companies in the form of:

–     100 – 1,000 mg capsules (in some countries the maximum potency may be less than 1,000 mg)

–     2.5 – 500 mg tablets (in some countries the maximum potency may be less than 500 mg)

The Inositol Hexanicotinate form of Nicotinic Acid is available from health food stores and mail order supplement companies (mainly only in the USA and Canada) in the form of:

–     250 mg capsules

–     500 mg capsules

–     600 mg tablets

Prescription Products

Extended-release Nicotinic Acid is available from pharmacies (prescription required) in the form of:

–     500 mg tablets (Niaspan)

–     750 mg tablets (Niaspan)

–     1,000 mg tablets (Niaspan)

Oral Formulas

Nicotinic Acid and/or Inositol Hexanicotinate are ingredients in many multi-vitamin formulas and other specific purpose formulas.

Topical Products

Nicotinic Acid is an ingredient in some topically applied Hair products designed to retard Hair Loss, for example:

–     Crinagen

–     Polysorbate 80 + Nicotinic Acid

–     Lotion containing Nicotinic Acid + 6% Minoxidil

–     Lotion containing Nicotinic Acid + 5% Minoxidil

–     Lotion containing Nicotinic Acid + 4% Minoxidil

–     Lotion containing Nicotinic Acid + 3% Minoxidil

–     Lotion containing Nicotinic Acid + 2% Minoxidil

Chemical Data

Nicotinic Acid is a white crystalline compound that is soluble in hot Water and is reasonably stable in heat, light, acids and alkalis.

Chemical Names

Carboxypyridine

       Pyridine-3-carboxylic Acid

       Pyridine Carboxylic Acid

       Pyridine-beta-carboxilic acid

       m-pyridinecarboxilic acid

       Pyridine-3-carbonic acid

Nicotine Acid

       Pyridine-beta-carboxylic acid

       3-Pyridine Carboxylic acid

Molecular Formula

C6H5NO2

       C5H4N(COOH)

Molecular Weight

123.1

Also known as:  Picolinate

Description

Picolinic Acid is an isomer of Nicotinic Acid.  It is manufactured endogenously within the human body (an average person manufactures 5 – 20 mg of Picolinic Acid per day within their Kidneys and Liver from other Amino Acids) and it is also a minor constituent of some foods.  The primary reason for the body producing its own Picolinic Acid is to enhance the absorption of dietary Minerals.

Health Benefits of Picolinic Acid

Cells

Picolinic Acid may facilitate Growth (probably by facilitating the absorption of Zinc into Cells).  [more info]

Picolinic Acid may Enhance the Function of these Substances

Growth Factors

Picolinic Acid is a precursor for the production of Skin Respiratory Factor (SRF).  [more info]

Minerals

Picolinic Acid may facilitate the absorption of Chromium.  [more info]

       Picolinic Acid may facilitate the absorption of Zinc.  references

These Substances may Enhance the Function of Picolinic Acid

Amino Acids

Tryptophan metabolizes to Picolinic Acid within the body – 60 mg of Tryptophan is required for the endogenous manufacture of 1 mg of Picolinic Acid.  references

Enzymes

Picolinic Carboxylase catalyzes the endogenous production of Picolinic Acid.

Vitamins

Vitamin B6 may enhance the body’s conversion of Tryptophan to Picolinic Acid.  [more info]

Dietary Sources of Picolinic Acid  note

Dairy Products:   Milk             

Fungi:    Yeasts                 

Picolinic Acid is also a constituent of Human Breast Milk.

Cautions

Uncomplexed Picolinic Acid should not be used as a nutritional supplement.  It should only be used in forms in which it is bound to essential Minerals.

Forms of Picolinic Acid

Chromium Picolinate consists of three molecules of Picolinic Acid chelated with one molecule of Chromium.  Chromium Picolinate is regarded as one of the best forms of supplemental Chromium as Picolinic Acid enhances the body’s absorption of Chromium.

       Boron Picolinate consists of Picolinic Acid chelated with Boron.

       Copper Picolinate consists of Picolinic Acid chelated with Copper.

Iron Picolinate consists of Picolinic Acid chelated with Iron.

       Magnesium Picolinate consists of Picolinic Acid chelated with Magnesium.

       Manganese Picolinate consists of Picolinic Acid chelated with Manganese.

       Selenium Picolinate consists of Picolinic Acid chelated with Selenium.

Vanadium Picolinate consists of Picolinic Acid chelated with Vanadium.

       Zinc Picolinate consists of Picolinic Acid chelated with Zinc.  Zinc Picolinate is regarded as one of the best forms of supplemental Zinc as Picolinic Acid enhances the body’s absorption of Zinc.

Chemical Data

Picolinic acid has a Pyridine nucleus with a carboxyl side group.  This is a particularly absorbable and biologically active chelate of essential minerals.

Chemical Names

2-Pyridinecarboxylic Acid

       Pyridine-4-carboxylic acid

lso known as:  Androgeron;  Angiomanin;  Angiomin;  Cafardil;  Circulan;  Clofamin;  Complamex;  Complamin

;  Dacilin;  Emodinamin;  Jupal;  Landrina;  Niconicol;  Sadamin;  SK 331 A;  Vasoprin;  Vedrin;  Xanidil;  Xavin

Description

Xanthinol Nicotinate is a synthetic form of the Nicotinic Acid form of Vitamin B3.  It contains 28.4% Nicotinic Acid bonded to 71.6% Xanthinol.

Health Benefits of Xanthinol Nicotinate

Cardiovascular System

Xanthinol Nicotinate may help to prevent abnormal Blood Clotting.  references

       Xanthinol Nicotinate may dilate (expand) Blood Vessels throughout the body including the Blood Vessels in Brain.  [more info]

       Xanthinol Nicotinate may alleviate Cerebral Insufficiency.  references

Metabolism

Xanthinol Nicotinate may lower serum Cholesterol levels (due to its ability to dilate Blood Vessels):  [more info]

–     Xanthinol Nicotinate may lower LDL Cholesterol levels.  references

–     Xanthinol Nicotinate may lower VLDL Cholesterol levels.  references

Nervous System

Xanthinol Nicotinate (500 mg per day) may improve Memory (in normal, healthy, elderly people).  references

–     Xanthinol Nicotinate may improve Long-Term Memory in normal, healthy humans.  references

–     Xanthinol Nicotinate may improve Short-Term Memory in normal, healthy young, middle aged and elderly people.  references

Xanthinol Nicotinate may Enhance the Function of these Substances

Carbohydrates

Xanthinol Nicotinate may enhance the body’s (especially the Brain’s) metabolism of Glucose.  references

Nucleic Compounds

Xanthinol Nicotinate may increase the body’s production of Adenosine Triphosphate (ATP).  references

Potentially Toxic Effects of Xanthinol Nicotinate

These potential side effects of Xanthinol Nicotinate usually diminish with continued usage of Xanthinol Nicotinate.

Cardiovascular System

Xanthinol Nicotinate may cause a temporary fall in Blood Pressure when standing up from a sitting position.

       Tachycardia (heart palpitations) may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

Digestive System

Diarrhea may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

       Heartburn may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

Vomiting may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

Nervous System

Blurred Vision may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

       Headache can occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

Nausea may occur as a temporary initial side effect of Xanthinol Nicotinate usage – this side effect usually disappears after continued usage of Xanthinol Nicotinate.

Skin

Xanthinol Nicotinate may cause temporary Flushing of the Skin.

Contraindications

Cardiovascular System

People who have recently experienced a Heart Attack should not use Xanthinol Nicotinate.

       Hypotension patients should not use Xanthinol Nicotinate.

Digestive System

Peptic Ulcers patients should not use Xanthinol Nicotinate.

Metabolism

People who are afflicted with Liver malfunctions should not use Xanthinol Nicotinate.

Sexual System – Female

The safety of Xanthinol Nicotinate during the Lactation period has not been established.

       The safety of Xanthinol Nicotinate during Pregnancy has not been established.

Dosage Recommendations

The usual therapeutic dosage of Xanthinol Nicotinate is 450 – 1,800 mg per day (taken in equally divided dosages).

       The maxium safe dosage of Xanthinol Nicotinate is 3,000 mg per day.

Bioavailability  references

Xanthinol Nicotinate passes through Cell Membranes into Cells much more readily than Vitamin B3.

Commercial Availability of Xanthinol Nicotinate

“Singular” Oral Xanthinol Nicotinate Products

Xanthinol Nicotinate is available from some international mail order pharmaceutical suppliers in the form of:

–     Xanthinol Nicotinate powder

–     150 mg tablets (often under the trade name Complamin)

Xanthinol Nicotinate is not approved for sale in the USA but is approved for use in Europe and Canada.