Pharmacodynamics and pharmacokinetics
Nicotinamide - what is it?
Vitamin remedy Nicotinamide has a structure close to nicotinic acid . Its synonyms also include vitamin PP .
This substance is an important component necessary for the full course of redox processes occurring in the cell. The vitamin also takes part in the metabolism of fats, amino acids, purines, proteins, tissue respiration and glycogenolysis . At the same time, there is no pronounced vasodilating effect, redness and irritation on the skin, or “flushes” of blood. In addition, the drug has an antipellagritic effect. Nicotinamide is characterized by rapid absorption and metabolism.
Vitamin PP (nicotinic acid, niacin; nicotinamide (nicotinamidum)
Niacin is the only vitamin that traditional medicine considers a cure. It may actually be the most effective cholesterol-lowering 'cure' that exists.Vitamin PP is a component of the B-complex and is critical for energy production and well-being on many levels, especially for heart health and optimal circulation. It is involved in more than fifty reactions during which sugar and fat are converted into energy. It is also essential for amino acid metabolism and is involved in the conversion of fats into substances called eicosanoids, hormone-like agents that control our body's metabolic pathways.
Niacin is a vitamin that has no equal in cholesterol control. In people who have already experienced a myocardial infarction, niacin increases the chances of survival to a greater extent than pharmaceutical drugs. That was the conclusion of a study called Project Coronary Medicine, which compared niacin with two anti-cholesterol drugs to see which best curbed non-fatal heart attack and prolonged life after a heart attack. Even several years after stopping treatment, the death rate was lower only among those taking niacin.
Niacin simultaneously combats four major risk factors for cardiovascular disease:
- High LDL cholesterol. This 'bad' form of cholesterol accumulates on the inside of artery walls, restricting blood flow and leading to hardening of the arteries (atherosclerosis). Niacin supplements cause a decrease in LDL cholesterol levels.
- Low HDL cholesterol. Low cholesterol is one of the surest predictors of cardiovascular disease, since HDL helps clear LDL from the circulatory system.
- Increased levels of lipoprotein (a). A sticky byproduct of LDL, lipoprotein(a), has emerged in the past few years as an independent risk factor for heart disease—as dangerous as high blood pressure, smoking, obesity and total cholesterol. It contributes to clogged arteries and increases the likelihood of blood clots. The higher its level, the greater the risk. No known drugs have any effect on high amounts of lipoprotein(a). However, niacin along with vitamin C reduces the risk associated with it.
High triglyceride content. Recently recognized as an independent risk factor of critical importance, these blood fats signal the presence of insulin disorder type II diabetes and hypertension. The best way to manage high triglycerides is to sharply reduce your intake of sugar and other carbohydrates, but niacin supplements can provide strong support by lowering triglyceride levels.
Indications for use
Nicotinamide is prescribed for hypo- and avitaminosis of the RR and a high need for it associated with:
- inadequate and unbalanced nutrition;
- malabsorption;
- rapid weight loss;
- diabetes mellitus;
- prolonged fever ;
- gastrectomy;
- diseases of the hepatobiliary region - hepatitis, cirrhosis;
- hyperthyroidism;
- chronic infections;
- gastrointestinal diseases;
- malignant tumors;
- diseases of the oropharyngeal region;
- prolonged stress;
- lactation, pregnancy.
In addition, this drug is actively used in the treatment of acute alcohol conditions and addiction.
Contraindications for use
It is recommended to refrain from consuming this vitamin if:
- hypersensitivity;
- peptic ulcer of the stomach and duodenum.
Caution in treatment requires such disorders as:
- hemorrhages;
- diabetes;
- gout;
- glaucoma;
- hyperuricemia;
- arterial hypotension;
- liver diseases;
- hyperacid gastritis.
special instructions
In addition to taking a vitamin supplement to prevent hypovitaminosis RR , it is necessary to adhere to a balanced diet, including foods rich in this vitamin in the diet. These include: yeast, liver, egg yolk, nuts, milk, fish, meat, legumes, buckwheat, chicken, unrefined grains, ground nuts, green vegetables, protein products and so on.
As a result of heat treatment, vitamin PP is retained in milk.
Taking the vitamin requires monitoring liver function. To prevent the development of fatty liver disease, you need to supplement your diet with foods saturated with methionine , take a drug with methionine or other lipotropic drugs.
The drug is not used as a lipid-lowering agent. You can reduce the irritating effect on the mucous membranes of the gastrointestinal tract if you take the tablets with milk.
Vitamin B3 (niacin, nicotinamide, nicotinic acid)
Vitamin B3
(
niacin, nicotinamide, nicotinic acid, vitamin PP
*) is a water-soluble vitamin from the group of B vitamins.
Basic functions and intakes of niacin (vitamin B3)
According to Methodological Recommendations MP 2.3.1.2432-08 “Norms of physiological needs for energy and nutrients for various groups of the population of the Russian Federation”, approved by Rospotrebnadzor on December 18, 2008, vitamin B3 (niacin) as a coenzyme is involved in the redox reactions of energy metabolism .
Insufficient vitamin intake is accompanied by disruption of the normal condition of the skin, gastrointestinal tract and nervous system. The average consumption in different countries is 12-40 mg/day, in the Russian Federation - 13-15 mg/day. Niacin can be synthesized from tryptophan (60 mg of tryptophan produces 1 mg of niacin). The established level of requirement in different countries is 11-25 mg/day. The upper tolerable level of niacin intake is 60 mg/day. The physiological requirement for adults is 20 mg/day. The physiological need for children is from 5 to 20 mg/day. The 2015–2020 Dietary Guidelines for Americans (official publication of the US Department of Health) recommend the following daily intakes of niacin (vitamin B3):
- children under 3 years old - 6 mg
- children from 4 to 8 years old - 8 mg
- children from 9 to 13 years old - 12 mg
- girls and women aged 14 years and older - 14 mg
- boys and men aged 14 years and older - 16 mg
With insufficient intake of vitamin B3 in the body, lethargy, apathy, fatigue, dizziness, insomnia, palpitations, pale and dry skin, and reduced resistance to infections are observed. With a severe deficiency of vitamin B3, pellagra develops - a serious disease affecting the gastrointestinal tract, skin, central and peripheral nervous system.
Nicotinamide is the international nonproprietary name of the drug
In ATC, nicotinamide is included in the “A11 Vitamins” group, the “A11HA Other pure vitamins” subgroup.
Nicotinamide code is A11HA01. Pharmacological group “Vitamins and vitamin-like products”. Nicotinamide is part of the B vitamin group (vitamin B3, or PP). It is a source of niacin, as well as nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which are coenzymes for many enzymes that catalyze redox reactions. Nicotinamide is involved in the metabolism of carbohydrates, normalizes intestinal motility, and is necessary for the functioning of normal intestinal microflora. Nicotinamide does not cause adverse reactions characteristic of nicotinic acid: it does not cause redness of the skin, tingling or burning sensation, hypotension, dizziness, heart rhythm disturbances, or dyspeptic symptoms. There was no connection between the use of nicotinamide and exacerbation of gastric and duodenal ulcers, or decreased glucose tolerance (Serebrova S.Yu.).
Nicotinic acid is the international nonproprietary name of the drug
In the ATC, nicotinic acid and its derivatives are included in section “C.
Drugs for the treatment of diseases of the cardiovascular system": in group "C04. Peripheral vasodilators" and have the following codes:
C04AC Nicotinic acid and its derivatives C04AC01 Nicotinic acid C04AC02 Nicotinyl alcohol (pyridylcarbinol) C04AC03 Inositol nicotinate C04AC07 Cyclonicate
to group “C10. Lipid-lowering drugs" and have the following codes:
Nicotinamide |
Nicotinic acid (niacin) |
C10AD Nicotinic acid and its derivatives C10AD01 Niceritrol C10AD02 Nicotinic acid C10AD03 Nicofuranose C10AD04 Aluminum nicotinate C10AD05 Nikonitic alcohol (pyridylcarbinol) C10AD06 Acipimox C10AD52 Nicotinic acid in combination with other drugs
Nicotinamide and nicotinic acid (niacin) as chemicals
Nicotinamide (eng. nicotinamide
) - amide of nicotinic acid, 3-pyridine carboxamide. White crystalline powder. Easily soluble in water and alcohol. Its structure and action are similar to nicotinic acid. Gross formula: C6H6N2O.
Nicotinic acid
or
niacin
). 3-Pyridinecarboxylic acid. White crystalline powder, odorless, slightly acidic taste. Slightly soluble in cold water (1:70), better in hot water (1:15), slightly soluble in ethanol, very slightly soluble in ether. Gross formula: C6NH5O2.
Indications for use of vitamin B3
Patient with pellagra (vitaminosis B3) |
Taking vitamin B3 in any form is indicated:
- in the prevention and treatment of pellagra (vitaminosis B3, vitamin deficiency PP)
- slow-healing wounds and ulcers
- gastritis with low acidity
- colitis
Nicotinamide is also recommended for:
- peptic ulcer of the stomach and duodenum (not in the acute stage)
- diabetes mellitus
- atherosclerosis
Nicotinic acid is also indicated for:
- Crohn's disease
- tropical sprue
- spasm of peripheral vessels
- Hartnup's disease
- Raynaud's disease
- migraine
- cerebrovascular disorders
- angina pectoris
- hypercoagulability
- neuritis of the facial nerve
Nicotinic acid (niacin) as a means of preventing heart attack and stroke?
Extended-release niacin (niacin) in men who have had a myocardial infarction increases high-density lipoprotein (HDL) cholesterol levels and reduces lipoprotein (a) concentrations, reducing the risk of recurrent myocardial infarction. Nicotinic acid preparations can be used in patients with low HDL cholesterol values or increased lipoprotein (a) levels, but the benefit of this therapy in reducing the risk of ischemic stroke is not shown (Fonyakin A.V., Geraskina L.A.).
Sources of vitamin B3
Many foods are rich in vitamin B3: yeast, liver, nuts, egg yolk, milk, fish, chicken, meat, legumes, buckwheat, unrefined grains, green vegetables, ground nuts, flaxseed oil.
Vitamin B3 (nicotinamide or nicotinic acid) can be sold as a medicine or dietary supplement in the form of a single drug, it is also included in complex preparations, for example, Enzymtal (fungal amylase + papain + simethicone + activated carbon + nicotinamide), Cytoflavin (inosine + nicotinamide + riboflavin + succinic acid), eye drops Oftan Katahrom (adenosine + nicotinamide + cytochrome C).
Vitamin B3 is part of the vitamin and mineral complexes: Bio-Max, Complivit, Selmevit, Vitrum, Hexavit, Multi-Tabs, Vitamin and mineral complex from A to Zn (“Vitamins for adults”) and many others.
Vitamin B3 is usually included in infant formula (Kozhevnikova E.N.).
Vitamin B3 is synthesized by human intestinal bacteria, in particular Escherichia coli
.
Vitamin B3 (niacin, nicotinamide) has contraindications, side effects and application features; consultation with a specialist is necessary.
* By “vitamin B3” we mean not one substance, but several different substances that are very similar in their biochemical effects on the human body and physiology. Please note that different authors do not have 100% terminological unity. For example, in the articles of Serebrova S.Yu., Kovaleva K.A. and a number of others, the terms “vitamin B3”, “vitamin PP” and “nicotinamide” are used as synonyms. And in the article by Kivaeva I.V. and others, on the one hand, “nicotinic acid” and “vitamin PP” are considered synonyms, and on the other, “niacin” and “vitamin B3”. We do not set out to arbitrate these differences and try to avoid them as far as possible.
Nicotinamide - a means of preventing skin cancer (?)
Non-melanocytic skin cancers, such as basal cell and squamous cell carcinomas, are common cancers caused primarily by ultraviolet radiation.
Nicotinamide has been shown** to have a protective effect against damage caused by ultraviolet healing and also to reduce the incidence of new cases of precancerous photochemically active keratoses. Nitotinamide, when taken orally, is safe and effective in reducing the incidence of new cases of non-melanocytic skin cancer and photoactive keratoses in high-risk patients.** It is emphasized that the trials were conducted specifically with nicotinamide .
and not with nicotinic acid or other similar substances.***
** Andrew C. Chen AC et al. A Phase 3 Randomized Trial of Nicotinamide for Skin-Cancer Chemoprevention. N Engl J Med 2015;373:1618-26 | DOI: 10.1056/NEJMoa1506197. *** Damian DL et al. Nicotinamide for Skin Cancer Chemoprevention / The Melanoma Letter, A Publication of The Skin Cancer Foundation. Vol. 34, Spring 2016.
Nicotinic acid - food supplement
Nicotinic acid, as a food additive, has code E375 and is defined by SanPiN 2.3.2.1293-03 as a color stabilizer. In 2008, it was excluded from the list of permitted food additives in Russia. The reason is a lack of research data. Also, nicotinic acid does not have permission for use as a food additive in Ukraine. Back to section
Overdose
Taking high doses of the vitamin can lead to the development of: arrhythmia, dizziness, diarrhea , dry skin and mucous membranes of the eyes, hyperglycemia, glucosuria, thirst, hyperuricemia, myalgia, nausea, vomiting , and so on.
Long-term use of vitamin PP sometimes causes fatty liver degeneration and cholestasis .
Niacin (nicotinic acid) is a water-soluble vitamin, the deficiency of which leads to pellagra, a disease primarily affecting the skin, gastrointestinal tract and nervous system.
Synonyms Russian
Nicotinic acid, vitamin PP, antipellagric factor, 3-pyridinecarboxylic acid.
English synonyms
Niacin, vitamin B3, nicotinicacid, vitamin PP, Pyridine-3-carboxylicacid, 3-pyridinecarboxylicacid, Apelagrin, Pellagrin, Akotin, Daskil, Pelonin, Acidumnicotinicum.
Research method
High performance liquid chromatography with tandem mass spectrometry.
Units
ng/ml (nanograms per milliliter).
What biomaterial can be used for research?
Venous blood.
How to properly prepare for research?
- Do not eat for 2-3 hours before the test; you can drink clean still water.
- Do not smoke for 30 minutes before the test.
General information about the study
Niacin (vitamin B3) is a water-soluble vitamin that is converted into nicotinamide in the human body. It is part of the coenzymes of some dehydrogenases: nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP). In these molecular structures, nicotinamide acts as an electron donor and acceptor and participates in vital redox reactions that are catalyzed by dozens of different enzymes. As a cofactor of enzymes, nicotinamide is involved in the metabolism of proteins, fats and carbohydrates, purine metabolism, tissue respiration, and glycogen breakdown.
Niacin has a hypolipidemic effect, dilates small blood vessels and improves microcirculation. It reduces the concentration of total cholesterol, apolipoprotein A, triglycerides, low-density lipids and increases the level of high-density lipids, which have anti-atherogenic properties (prevent the formation of atherosclerotic plaques in blood vessels). It also increases the fibrinolytic activity of the blood and prevents thrombus formation, reducing platelet aggregation.
Niacin is primarily supplied to the body through food. It is found in rye bread, buckwheat, beans, nuts, unrefined grains, yeast, egg yolk, milk, meat, liver, kidneys, mushrooms, pineapple. In the food industry it is used as a food additive E375. Satisfying the body's need for niacin is also ensured by its synthesis from the essential amino acid tryptophan in the presence of vitamin B6, riboflavin and iron by the intestinal bacterial flora.
If there is insufficient intake of niacin, the skin, digestive organs and nervous system are affected. A deficiency of this vitamin leads to pellagra, a disease that manifests itself with diarrhea, dermatitis, dementia and is life-threatening without treatment. Skin lesions with pellagra are erythema resembling sunburn, especially pronounced on parts of the body exposed to sunlight; Pigmentation gradually increases and the skin thickens. Nausea, constipation or diarrhea occurs, the tongue becomes bright red, apathy, fatigue, depression, headache, disorientation appear, and sometimes the patient even loses memory. The development of dementia with delirium is preceded by increased irritability, depression and anorexia.
When consuming high doses of vitamin B3, hyperemia of the skin of the face and upper half of the body, dizziness, paresthesia, arrhythmia, diarrhea, dry skin and mucous membrane of the eyes, and itching occur. Long-term use of niacin can lead to fatty liver, decreased glucose tolerance, papilledema, asthenia, increased blood concentrations of uric acid, ALT, LDH,. During treatment with nicotinic acid preparations, it is recommended to monitor liver function.
What is the research used for?
- To diagnose vitamin B3 deficiency in the body.
When is the study scheduled?
- With clinical signs of pellagra (dermatitis, diarrhea, dementia, glossitis);
- with malabsorption syndrome due to diseases of the gastrointestinal tract;
- with Hartnup syndrome (hereditary pathology of the absorption of tryptophan and some other amino acids from the intestine).
What do the results mean?
Reference values
Vitamin B3 (niacin) | 3.00 - 36.00 ng/ml |
Vitamin B3 (nicotinamide) | 5.20 - 72.10 ng/ml |
Reasons for increased vitamin B3 levels:
- oral or parenteral administration of nicotinic acid preparations.
Reasons for low vitamin B3 levels:
- Insufficient intake of vitamin B3 into the body: Hartnup disease (a hereditary disease accompanied by impaired absorption of certain amino acids, including tryptophan);
- inadequate and unbalanced nutrition (including parenteral);
- gastrointestinal diseases accompanied by malabsorption syndrome (pancreatic pathology, celiac disease, persistent diarrhea, Crohn's disease);
- condition after surgical treatment of gastrointestinal diseases (for example, gastrectomy).
- prolonged fever;
What can influence the result?
The level of niacin in the body is reduced by: isoniazid, phenytoin, valproic acid, azathioprine, chloramphenicol, cycloserine, fluorouracil, levodopa, mercaptopurine.
Analogs
Level 4 ATC code matches:
Medobiotin
Calcium Pantothenate
Volvit
Alpha Tocopherol Acetate
Riboflavin
Pyridoxine Hydrochloride
Pyridoxine
Vitrum Vitamin E
Analogs are represented by the following drugs: Aminicotin, Benikot, Endobion, Niacevit, Bepella, Niacinamide, Nicofort, Nicotol, Nicotinic acid, Nikamide and Pelmin.
Also have a similar effect: Neurovitan, Folic acid and Bepanten.
Reviews about Nicotinamide
In most cases, reviews of Nicotinamide are left by people who take it during pregnancy or to prevent vitamin deficiency . Pregnant women note that this drug is well tolerated and highly effective. It is also often reported that taking this vitamin improves the condition, appearance and quality of hair and nails.
Nicotinamide is often included in the diet of athletes, bodybuilders and athletes. At the same time, it is described as an excellent anabolic steroid that helps quickly and effectively build muscle mass.
Thus, there are only positive opinions about this vitamin product. However, experts remind that taking the drug without indications and without consulting a doctor is not recommended.
Nicotinamide (niacinamide, vitamin B3)
INCI: Nicotinamide
Appearance: White crystalline powder
Solubility: soluble in water; also soluble in ethanol and glycerol
Input rate: 2–5%
pH of solution: 6,0-7,5
Recommended pH range: 5.5-7 (optimally 6). At a pH below 5, it can turn into nicotinic acid (which causes redness of the skin, while maintaining all the beneficial properties of the asset).
Features: not afraid of heating, but easily disintegrates in light, therefore it is recommended to store the asset itself and products with it in a dark container.
Niacinamide is a water-soluble form of vitamin B3, also called vitamin PP. Nicotinamide and Nicotinic acid are often interpreted as synonyms in cosmetics, but in fact these components are different forms of vitamin B3. The transformation of one component into another served as the basis for conditionally combining them. In cosmetics, these components play different roles - as a vitamin antioxidant, an anti-irritant substance, a protective agent and a regulator of cellular metabolism. Nicotinamide, unlike nicotinic acid, does not have a pronounced warming and vasodilating effect, and no redness of the skin is observed when it is used. Therefore, it can be used for rosacea or rosacea. However, temporary skin redness, tingling and warmth are possible when used on irritated skin or following acidic products. Niacin is a great ingredient for those struggling with wrinkles, inflammation, uneven skin and pigmentation. This component is able to even out skin tone and soften post-acne scars. Nicotinic acid, in turn, dilates blood vessels and improves blood circulation, resulting in the skin looking elastic and healthy. It removes excess fluid from cells, relieving swelling. By adjusting the pH of the finished product, you can start the process of degeneration of Niacinamide into Nicotinic acid and thus select the desired properties.
Basic properties:
Increases collagen synthesis;
Improves barrier function, increases skin hydration, reduces trans-epidermal water loss by 24%;
Reduces dryness and sensitivity of the skin;
Reduces wrinkles, reduces pores, makes skin smoother;
Brightens and evens out the skin surface;
Regulates sebum production by the skin and has a powerful anti-inflammatory effect;
Protects cells from immunosuppression caused by UV radiation.
Application:
Anti-aging products (to improve skin structure and elasticity);
Acne remedies;
Moisturizers;
Whitening serums;
Sunscreens and after-sun products;
Aftershave products.
Cosmetic raw materials.
All information presented on the site is for reference only; before use, it is recommended to test for individual reaction.