Vitamin drugs
01 Dec 2016
Vitamin drugs are drugs of natural vitamins (from vegetable and animal raw materials), their synthetic analogs, or isomers (vitamer), and also ready cofactors which are a part of ferment systems. Vitamin drugs regulate processes of a fabric metabolism along with trace substances, hormonal and ferment medicines. At the vitamin deficiency arising at high exercise stresses the body weight and power supply of the working athlete's muscles changes. In sports medicine the need for vitamins is enlarged several times depending on intensity and duration of exercise stresses, and also from imbalance of a delivery therefore vitamin drugs are used, most often, is combined for prophylaxis of hypovitaminosis during the whole year of sports preparation, when changing klimato-cingular zones, in a heat and cold, during aftertreatment after extreme exercise stresses.
Classification of vitamin drugs by solubility and chemical structure
Drugs of liposoluble vitamins
- Retinolum acetate, Retinolum
- Ergocalciferol (Videinum, akvadetry).
- Tocopherol acetate.
- Vicasolum, phytomenadionum.
Drugs of water-soluble vitamins
1. Thiamini chloridum, cocarboxylase.
2. Riboflavinum.
3. Pyridoxine Sodium chloridum.
4. Nicotinic acid, Nicotinamidum.
5. Cyancobalamine.
6. Folic acid.
7. Ascorbic acid.
8. Bioflavonoids (Rutinum, Quercetinum).
9. Pantothenic acid.
10. Calcium
Medicines of oil-soluble vitamins
Retinoida (Vit. A) — it is group of derivatives beta (Retinolum, retinoyevy acid, Retinolum air, etc.) which have biological activity of transretinolum. Retinolum (trans-9,13-dimetil-7-(1,1,5-trimetiltsiklogeksen-5-silt-6) - nonatetrayen-7,9,11,13-ol) is a nonsaturated alcohol with five double communications — one in beta enonovom a cycle and four in an aliphatic side chain.
Carotinoids which have pharmacological activity of beta carotene belong to pro-vitamins of Retinolum and can turn in an organism into Retinolum.
Retinolum in the form of air contains in animal products — cod-liver oil (cods, a grouper, a halibut), a liver, butter, milk and dairy products. The main source of carotene — products of plant origin — carrots, parsley, a sorrel, a sea-buckthorn, a krasnoplodny mountain ash, dogrose, apricots.
Pharmacokinetics. Retinolum in the form of medicines (Retinolum acetate and Retinolum) and carotinoids are well soaked up in the food channel. They arrive in a small intestine where in the presence of bilious acids there is an emulsification and formation of micelles. Hydrolysis of air of Retinolum and free fatty acids is performed by not specific pancreatic lipase.
Free Retinolum and (3 carotene is created in micelle guts which part bilious acids, cholesterol, fatty acids, etc. are. Formation of micelles in a certain measure increases efficiency of absorption of Retinolum and carotene. Digestion of Retinolum in guts constitutes 80 — 90% of vitamin which arrives with food. Digestion of carotene is much lower — on average than 50 — 60%. The compulsory provision of its absorption is availability in a diet of fat and sufficient concentration of bilious acids in intestines.
Retinolum which came to microvillis of intestines eterifitsirutsya again by fatty acids. These Aethers get to lymphatic ways and as a part of chylomicrons come to a liver. It is the main depot of Retinolum which on requirement comes to the blood circulatory system. In a blood Retinolum is in the connected state with proteins of plasma. Transfer from a blood in a cell happens owing to immediate interaction of a complex Retinolum — Retinolum the binding protein to specific receptors of membranes then free Retinolum comes to a cell, and reprotein comes back to system of a circulation.
In a liver 30 — 50% of Retinolum arriving with a nutrition are deposited. Other its part which is soaked up in intestines is bound and removed with a feces (20 — 30%) or oxidized and removed with urine (10 — 20%). Removal of Retinolum is carried out slowly: in 21 days — 34% of the entered quantity.
There are three main hypotheses concerning the mechanism of action of Retinolum: 1) genetic, 2) membranous, 3) glycoprotein. A large amount of the different physiological effects inherent in Retinolum, give the chance to understand plurality of biochemical mechanisms of effect of vitamin. According to this concept biochemical effects of Retinolum considerably are implemented at the level of cellular membranes and are bound as to its immediate interaction with albuminous and lipide complexes of membranes, and with influence on a metabolism of membranous phospholipids and glycoproteins. An important role is played by antioxidatic properties (participation of Retinolum in a regulation of peroksidny oxidation of lipids). Retinoida influence functions of an organism which can be divided into two groups: visual and systemic as which understand the functions bound to requirement of Retinolum for body height, a reproduction, differentiations of an epithelium, maintenance of an immunologic state.
Influence of Retinolum on processes of photoreception is bound to its participation in creation of a photosensitive pigment of a rhodopsin (visual purple) which contains in bacillary (photosensitive) cells of a retina and immediately perceives visual borings. The rhodopsin is formed mainly in the (an aldegidny form of vitamin) and a squirrel of opsin that increases visual acuity at bad lighting. On light the rhodopsin breaks up to protein
At deficiency of Retinolum formation of a rhodopsin and a perception of light is broken, the hemeralopia ("night blindness") develops. One of early and classical symptoms of deficiency of Retinolum is the growth inhibition as it exerts the expressed impact on a bone tissue, a metabolism of proteins and nucleic acids. Retinolum increases contents and promotes bracing of a glycogen in muscles, heart and a liver, and also to transformation of regulates exchange of phospholipids. Do not forget take Mildronate for better results.
Retinolum stimulates a proliferation of cells, cuticularization and prevents an excess of an epithelium. At its failure the skin becomes dry, there are papular eruption, ecdysis, dryness of a cornea (xerophthalmia) develops, the lesion of the top respiratory tracts, the digestive channel, genitourinary system is observed.
Characteristic sign of deficiency of Retinolum — dropping of immunologic resistance of an organism to an infection in this connection vitamin was called "anti-infectious". Dropping of resistance of an organism to infectious diseases is caused by three major factors: disturbance of a condition of a barrier epithelium of a skin, top respiratory tracts, urinary ways, etc.; a loss of appetite that promotes an excavation of a failure of Retinolum; decrease in immunity. Retinolum takes part in realization of all forms of an immune response. Its deficiency at experimental animals is followed by an atrophy of immunocompetent organs — a thymus and a lien, depression of quantity of cells in them, the maintenance of lymphocytes in a blood, oppression of synthesis of antibodies.
Retinolum takes part in maintenance of genesial function. A failure at animals leads it to the termination of a spermatogenesis, atrophy of spermaries, to a keratinization of an epithelium of a vagina, uterine tubes and uteri, resorptions of a placenta and to spontaneous abortions.
Indications to use: ophthalmologic practice (a keratitis, a xerophthalmia, disturbance of dark adaptation), diseases of a skin (dyskeratosis), inflammation of respiratory tracts, the digestive channel, combustions, a freezing injury, trophic ulcers and other wounds which don't epitelizirutsya. Therapeutic doses — from 10 to 100 LLC ED.
Side effect is shown by acute or chronic intoxication. In case of excess introduction of Retinolum the anoksichny syndrome, i.e. a hypervitaminosis develops And. The clinical picture of acute intoxication is characterized by temperature increase, appetite loss, emergence of nausea, vomiting, deterioration in vision (photophobia), a headache.
Chronic intoxication: disturbances from a nervous system (irritability, a headache, sleeplessness, apathy, paresthesia); osteal system (pain in the field of bones and joints, a hyperostosis); skins (dryness, cracks on palms and soles, a pigmentation), a hair loss, fragility of fingernails. The augmentation of a liver and a lien is characteristic.
Calciferolums (Vit. D) unite to group of bonds which render antirachitic effect. The most active are ergo-(Vit. D) also care for Calciferolum (Vit. D3). Drug of D2 vitamin wears the name an ergocalciferol, drugs of D3 vitamin are known as Videinum. Calciferolum has steroid structure, in its molecule it is possible to allocate two parts: carbon skeleton and aliphatic side chain. The structure of ring system is identical to all Calciferolums which differ among themselves only in a structure of a carbon chain.
Ergocalciferol — substance of a plant origin.
Holekaltsiferol contains in a skin of the person and animals, in a large number — in a liver of a tuna, cod, halibut, whale, in insignificant — in cow's milk, eggs.
Pharmakokinetics. Like other liposoluble vitamins, Calciferolum is soaked up by means of bile acids, comes to a lymphatic stream as a part of chylomicrons and is quickly absorbed by a liver where there is its enzymatic hydroxylation. At the same time of a holekaltsiferol it is formed 25-gidroksikholekaltsiferol, and of an ergocalciferol — a 25-oxy-ergocalciferol. These metabolites in a small amount are formed also in intestines, kidneys, lungs. Biological activity to a 25-gidroksikhola Calciferolum and is 2 — 5 times higher, than a holekaltsiferola, it is the main form of Calciferolum which circulates in the blood circulatory system and has the period of semi-life of 20 — 30 days; 25-gidroksikholekaltsiferol comes to kidneys where active metabolites.
The calciferol and its metabolites are transported in blood plasma in the connected condition by means of special kaltsiferolsvyazyvayushchy protein — a transkaltsiferin. The calciferol accumulates in bones, a liver, blood, a mucous membrane of a small intestine. In the form of polar metabolites it is localized mainly in membranes of cages, mitochondrions, microsomes and kernels.
The calciferol and its metabolites are allocated in intestines with bile (30% of the entered dose for 24 — 48 h) where again are partially soaked up that creates system of enterogepatichesky circulation. The most part of products of exchange of a calciferol is removed from an organism with a stake, smaller — with urine.
Exchange of calcium and phosphorus is regulated not only by a calciferol, and also hormones of steam-tireoidinom and a calcitonin.
Paratireoidin stimulates synthesis of a 1,25-digidroksikholekaltsiferol in kidneys thanks to influence on enzymes a 1a-hydroxylase and 24 hydroxylase. Action of a paratireoidin on absorption of calcium in intestines completely mediately effect of a 1,25-digidroksikholekaltsiferol. The calcitonin doesn't influence directly activity 1 and - hydroxylases, its impact on products of a 1,25-digidroksikholekaltsiferol is caused by decrease in level of calcium in blood and strengthening of secretion of a paratireoidin.
Along with classical target organs (intestines, bones, kidneys) receptors of a 1,25-digidroksikholekaltsiferol are revealed also in the keratinotsitakh and the fibroblastakh whose growth and differentiation are regulated by a calciferol. Thus, skin is not only the place of formation of a holekaltsiferol, and and fabric which development is controlled by it.
Pharmakodinamika. The calciferol is considered not only as vitamin, but also as hormone which regulates exchange of calcium and phosphorus in an organism, providing their proper concentration in blood.
The most important effect of a calciferol is a stimulation of absorption of calcium in intestines. It increases permeability of an intestinal epithelium for calcium ions. Process of absorption consists of two stages: passive diffusion from intestines content in enterotsita (a cell of a mucous membrane of a small intestine) and active transport from enterotsit in blood plasma against a concentration gradient in which 1,25 dihydroxycalciferol take part. Respectively one of the most developed modern hypotheses a calciferol in the form of an active metabolite of a 1,25-digidroksikholekaltsiferol is realized by the stimulating action on transport of Sa2 + through biological membranes by induction at the genetic level of synthesis of proteins which perform this transport.
The mechanism of action of a calciferol on transport of Sa2" from blood plasma in a bone tissue isn't established. In bones the calciferol regulates a mineralization, influences proliferation and differentiation of bone and cartilaginous cages; 1,25-di-gidroksikholekaltsiferol gets into cells of intestines, bones and kidneys where interacts with specific receptors, forming with them a complex which gets into a kernel of a cage and initiates protein synthesis there (specific which connects calcium, and nonspecific — collagen, alkaline phosphatase, etc.). Thereof synthesis of a proteinaceous stroma of bones is activated, cartilaginous cages in zones of growth of bones normally develop, there is an extraction of calcium from plasma of blood and its adjournment in bones.
Insufficiency of a calciferol is shown mainly in violation of a mineralization of a skeleton and development of a cartilage that leads to rickets at children and to an osteomalyation at adults.
Under control of Calciferolum there is also a process of mobilization of a calcium of a bone tissue which happens slowly to parallel restoration of osteal cells.
Special value for maintenance of appropriate concentration of Natrii phosphases in an organism has property of Calciferolum to raise their reabsorption in a canaliculus of kidneys. The absorption of phosphatic anion is considered as the secondary process bound to a calcium absorption. The mechanism of action of Calciferolum on exchange of a calcium and phosphorus in an organism is shown in the figure 2.8.
Indications to use: prophylaxis of a rachitis, treatment of the children sick with a rachitis, osteomalacy, osteoporosis, fractures of bones (acceleration of consolidation of an osteal callositas), spasmophilia, tetany, caries (calcareous infiltration of firm tissues of tooth), systemic lupus erythematosus, tuberculosis cutis and bones, psoriasis.
Side effects: intoxication (in case of an over dosage), acute (a headache, a sleepiness, nausea, vomiting, a photophobia, sudorg) or chronic.
Chronic intoxication: at the use throughout long time of excessive quantity of Calciferolum, in case of a hypersensibility to vitamin under usual conditions of dosage, the hypervitaminosis of D develops. Implications of a hypervitaminosis are identical at children and adults: general flaccidity of muscles, constant nausea, loss of appetite or its loss (anorexia); abdominal pain, diarrhea, thirst, polyuria, heartburn; tachycardia, arterial hypertension, weakening of cardiac sounds, systolic hum, fever. In urine the content of calcium increases, are defined protein, leucocytes, erythrocytes, single hyaline cylinders. There is a demineralization of bones (insignificant injuries can lead to fractures). In blood serum concentration of a calcium and phosphorus considerably increases that leads to adjournment of a calcium in soft tissues (vessels, heart, lungs, intestines, kidneys) and to formation of stones in kidneys, and then — to a secondary hydronephrosis (often the patient sees a doctor for a cause of illness of kidneys), the polyuria, a proteinuria, a cylindruria, a leukocyturia become perceptible. Assume that ability of Calciferolum to bystry oxidation with education of free radicals, and also products of the peroksidny nature which are strong oxidizers is the cornerstone of these disturbances. They damage structure of a lipoproteinovy complex of membranes and the active centers of proteins.
Tocopherols (Vit. Å, tocopherol drug an acetate) is a group of derivatives of a tokol and tokotriyenol. Tocopherols (and - beta, at--) differ from each other in quantity and situation the metilnykh of deputies in an aromatic 6 ring of an oksikhromon. The most active of them — and - a tocopherol which has three CH3-groups in all free provisions of an aromatic ring: 5, 7 and 8.
In medical practice stabler synthetic drug — a tocopherol an acetate which in a human body isn't synthesized is used, it is formed only in plants and gets to an organism with natural foodstuff. The richest source of a tocopherol is vegetable oil.
Pharmakokinetics. A tocopherol after acceptance is inside soaked up mainly in a proximal part of a small bowel by means of bile acids. Transport passes slowly on the mechanism of passive diffusion. Vitamin gets mainly to a lymph, and also to a blood. About 90% of a tocopherol in a blood plasma are bound to lipoproteins. Vitamin comes to all body tissues where it is localized mainly in membranes of cells and subcells of organellas, mainly mitochondrions and microsomas. The highest content of a tocopherol is defined in adrenals and fatty tissue (90% of the entered dose). The organism of the woman contains 4 times more tocopherol in comparison with the man's organism.
The main part of drug (70 — 80%) which arrives per os is removed in not changed view with a feces. At parenteral administration of drug 20 — 30% of the entered dose are removed with urine in the form of water-soluble glucuronides and products of oxidation of a tocopherol — tokoferoniyevy acid and its lactone.
Like other liposoluble vitamins a tocopherol is subject to an enterogepatichesky recycling: secretions with bile in a cavity of intestines and repeated absorption.
Pharmacodynamics. A tocopherol is the main natural antioxidant. In tissues of plants, animals, people together with processes of enzymatic biological oxidation of feedstuffs which provide an organism with necessary energy non-enzymatic free radical reactions are possible. Intensifying of processes of free radical oxidation is observed during a stress, in the period of a hypodynamia, at excess entering in an organism of the refined products with high energy value, at some diseases (a radial illness, an atherosclerosis, a diabetes mellitus, a cataract, a periodontal disease, etc.). On modern representations, non-enzymatic oxidation is the main factor in the course of aging.
Products of free radical oxidation are free radicals, oxides, aldehydes — are very reactive. They damage cellular membranes, enzymes and structural proteins. Substances which oppress reactions of non-enzymatic free radical oxidation of lipids and biopolmers (proteins, glikozaminogli-kan, mucopolysaccharides and nucleic acids) are called antioksidantama.
Tocopherol, Retinolum, ascorbic acid, bioflavonoids belong to vitamins of antioxidatic action (Vit. Ð). Owing to cyclic transformations a tocopherol — òîêîôåðèëõèíîí — tokoferit a hydroquinone — a tocopherol is formed oxidation-reduction system which is capable to transfer electrons and to provide antioxidatic effect.
According to the antioxidatic theory of biological effect a tocopherol is "trap" for free radicals.
Tocopherol stabilizes biological membranes, normalizing their microviscosity, carries out protective influence on peroksidny mechanisms of an atherogenesis: slows down development of atherosclerotic changes in an aorta (a destruction of elastic fibers, calcification, a lipide infiltration of a vascular wall), reduces the level of cholesterol in a blood and cholesterol / ipida reduces coefficient.
At administration of tocopherol contents and activity of glutathione, myofibrillar transport Na+, K*-Atfaza, cytochrome - With - oxidases, and also dehydrogenases of degidrolipoyevy acid increase. A tocopherol has high specificity of action on exchange and function of an ubikhinon — an important component of processes of phosphorylation. Thereof stimulates tissue respiration, increases membranous activity and intracellular oxidation-reduction processes, takes part in exchange of proteins and lipids.
Classical implication of a failure of a tocopherol at rats is a sterility: resorption of a fetus and degeneration of spermaries. Signs of deficiency of a tocopherol are also the dystrophia of muscles, a hypersensibility of erythrocytes to peroksidny hemolysis, accumulation in fatty tissue and sceletal muscles of a brown pigment of a lipofuscin, a creatinuria.
Indications to use: hypo - avitaminoses, for conservation of pregnancy in cases of the menacing abortion, the slowed-down period of puberty, disturbance of a menstrual cycle, juvenile bleedings, a complex pharmacotherapy of cardiovascular diseases, sterility at men and women, myocardial dystrophies, prophylaxis and treatment of an atherosclerosis and coronary failure, before - and postinfarction states, a chronic heart failure, a climacteric at women, a radial illness.
Side effects: long use of high doses of drug can cause oppression of activity of vitamin K, emergence of hemorrhages in the digestive channel, pro-oxidatic effect.
Naphthoquinone. To group of naphthoquinone (Vit. J) carry phyloquinone (Vit. To.) — - the natural vitamin synthesized by some plants and its synthetic analogs (for example, drug ôèòîìåòàíäèîí); vitamin which is synthesized mainly by saprophytic bacteria of a small bowel and also liver of animals is a form of naphthoquinone, K2 vitamin.
Vicasolum (Vit. K3) — synthetic drug of naphthoquinone, unlike natural drugs is water-soluble.
Drugs of water-soluble vitamins
Thiamini chloridum (Vit. In) is a heterocyclic compound which consists of pirimidi-new and tiazolovy cycles.
Thiamin in a large number contains in yeast, a cover and a germ of seeds of cereals. An important source of Thiamin for the person is intestinal microflora.
In medicine use synthetic drugs: Thiamini chloridum and Thiamini bromidum.
Pharmakokinetics. At introduction inside Thiaminum and its Aethers are quickly soaked up throughout a small bowel: in 15 min. they are found in a blood, and through 30 — in other tissues. A half of total of the entered Thiaminum contains in a myocardium and sceletal muscles, about 40% — in internals.
Thiaminum with urine is allocated.
Pharmacodynamics. Thiaminum shows such main effects in an organism: cardiotrophic, neurotropic and hypoglycemic. The most active of phosphoric Aethers is òèàìèíäèôîñôàò, having kofermentny properties (cocarboxylase). In this form Thiaminum is a coenzyme of decarboxylases which take part in oxidation, decarboxylation pyrogrape and other ketoacids, and also a transketolase — the main enzyme of a pentozny cycle.
Important kofermentny effect of thiamine — cardiotrophic. The cocarboxylase controls process of aerobic oxidation of carbohydrates and a catabolism of a glucose through a cycle of citric acid, improves energy balance, dilates coronal vessels. Rising of blood supply of a myocardium causes improvement of oxidation-reduction processes in a cardiac muscle. Owing to improvement of a trophicity of a myocardium under the influence of a cocarboxylase its sokratitelny activity amplifies — the cardiotonic effect is shown. The cocarboxylase exponentiates effect of cardiac glycosides and weakens poisoning symptoms in cases of their over dosage.
The neurotropic properties of Thiaminum influencing both on central and on a peripheric nervous system are known. Has the most expressed neurotropic effects òèàìèíòðèôîñôàò. Thiaminum exerts impact on mental (highest) nervous activity. It is necessary for normal activity of a serotonin, aminobutyric acid, Acetylcholinum. After its introduction the latent period decreases and force of positive conditioned reflexes increases, however there are more weak differentiated reactions. Thus, Thiaminum strengthens exaltation process, reducing at the same time internal inhibition.
Effect of thiamine on a peripheric nervous system is especially expressed. At inflammatory processes (a neuritis, a radiculitis, etc.) and injuries in axons of peripheric nerves exchange of carbohydrates amplifies and products of their oxidation (a pyruvate, an acetaldehyde) collect, exaltation processes decrease. It promotes development of a pain syndrome and dysfunction of nerves. Thiaminum reduces quantity of products of carbohydrate metabolism, activity of a cholinesterase oppresses that facilitates transfer of nervous impulse on an effector tissue. Thanks to existence in a molecule of a quarternary nitrogen atom Thiaminum shows ganglioblokiruyushchy and curariform properties.
Thiaminum regulates carbohydrate metabolism not only in a myocardium and in nervous tissue, it also reduces the level of a glucose and lactic acid in a blood. This effect is pronounced at patients with a diabetes mellitus.
Also Thiamin drugs — Benphothiaminum, phosphothiaminum which are characterized by the best absorption are known. Salbutiamin (ýíåðèîí) possesses a specific neyrotropnost, antigipoksantny effect, takes out a fatigue.
Indications to use: prophylaxis hypo-and B1 avitaminosis, a heart failure, disturbance of a cordial rhythm (like ekstrasistoliya), coronary heart disease, a peripheric neuritis of a different etiology, a radiculitis, neuralgia, a diabetes mellitus, dermatoses of a neurogenic parentage, an eczema, a psoriasis. The cocarboxylase is applied in complex treatment of a renal, liver failure, an acidosis at a diabetes mellitus and diseases of cardiovascular system, a hepatic diabetic coma, mild forms of multiple sclerosis.
Side effects: allergic reactions, an urticaria, Quincke's edema, an attack of bronchial asthma, in hard cases — anaphylactic shock. Bystry intravenous administration of Thiaminum is followed by falling of arterial pressure, disturbance of reduction of sceletal muscles, respiratory depression (curariform action). Side effects of a cocarboxylase are shown in the form of allergic reactions, and at intramuscular introduction — in the form of an itch, an edema, a hyperemia.
Riboflavinum. At the heart of a chemical structure of Riboflavinum (Vit. B2) lies system of an izoalloksazin. As a side chain its molecule contains the rest of pentatomic alcohol of a ribitol owing to what vitamin was called Riboflavinum.
Riboflavinum comes to a human body mainly with meat and dairy products, it contains also in fish, yeast, peas, germs and covers of cereal cultures.
Drugs: Riboflavinum and Riboflavinum mononucleotide.
Pharmakokinetics. Riboflavinum is absorbed in an intestine and is subject to phosphorylation in a mucosa of intestines, cells of a liver and a blood. At the same time two kofermentny forms.
Riboflavin collects mainly in a liver, kidneys and adrenals. In tissues Riboflavinum can be in a free state, however its nucleotides (FMN and FAD) are reliably bound to proteins of an apoenzyme. Riboflavinum from an organism is allocated with kidneys, painting urine in light yellow color.
Pharmacodynamics. Riboflavinum as prosthetic group the flavinovykh (yellow) enzymes performs function of the conveyor of Hydrogenium in the course of tissue respiration and regulates oxidation-reduction reactions. Coenzymes of biological oxidation are intermediate carriers of Hydrogenium from OVER to cytochromes, are a part glutathione reductase — enzyme which translates the oxidized glutathione in got into condition.
As a part of an oxidase of amino acids Riboflavin takes part in synthesis and exchange of amino acids. In general he normalizes exchange of fats and proteins, plays an important role in maintenance of normal visual function of eyes (synthesis of flasks and rods), participates in function of mucosas, skins and in hemoglobin synthesis. Enzymes which incorporate Riboflavin participate in exchange of other vitamins: pantothenic acid, pyridoxine and folic acid. Riboflavinum is necessary for colibacillus vital activity, and also facilitates an iron absorption, increases fastness of an organism to a hypoxia and other adverse factors.
Precursory symptoms of a failure of Riboflavinum in an organism — dysfunctions of a CNS (a hypochondria, hysteria, a depression), decrease further secretion of a gastric juice and activity of enzymes of intestines, appetite worsens, body weight decreases, the feeling of fever in a body appears, there are cracks in angles of a mouth and on labiums (an angular stomatitis), tongue becomes dry, bright red color (glossitis), there is an acute pain in eyes, a photophobia, develop a keratitis, konyyuktivit, a phacoscotasmus (cataract).
Indications to use: hypo - and an ariboflavinosis, diseases of eyes (the keratitis, konyyuktivit, helcomas, a cataract) and skins (a seborrheal eczema, a systemic lupus erythematosus), combustions, a frostbite, a myocardial dystrophy, a chronic enteritis, a radial illness, a failure albuminous and excessive carbohydrate deliveries.
Riboflavin the mononucleotide is used in ophthalmology, dermatology, a neurology.
Side effects are observed at an overdosage. Riboflavinum the mononucleotide causes morbidity in an injection site. Treatment by high doses of vitamin owing to its bad solubility can cause an occlusion of a canaliculus of a nephron.
Pyridoxines (Vit. B6) is a group of bonds of derivatives of a pyridine which have activity of a pyridoxine. Is issued in the form of hydrochloride pyridoxine drug. Natural derivatives of a pyridoxine — ïèðèäîêñàëü and a pyridoxamine. Biological activity is shown by phosphoric Aethers of these bonds — piridoksal-5-Natrii phosphas and pyridoxamine-5-Natrii phosphas.
The pyridoxine arrives in an organism with products vegetable (cereals, vegetables) and an animal (a liver, heart, kidneys) of an origin, and also is partially synthesized by microflora of guts.
Pharmacokinetics. The pyridoxine gets to an organism in the connected condition. Under the influence of food juice the pyridoxine, its derivatives (ïèðèäîêñàëü and ïèðèäîêñàìèí) are released and soaked up in intestines. The pyridoxine is distributed unevenly. In the greatest numbers it contains in a liver and in heart, in fabrics by phosphorylation turns into biologically active forms: pyridoxal phosphate and which have kofermentny functions. About 90% of the pyridoxine entered to the person are oxidized to 4-piridiksovy acid and in this form is removed with urine.
Pharmakodinamika. The pyridoxine in an organism renders generally kardiotropny and hepatotrophic effect and influences a krovoobrazovaniye. Cardiotonic action is shown in improvement of sokratitelny function of a myocardium, especially in the conditions of chronic heart failure. Medicine also strengthens action of warm glycosides.
Under the influence of a pyridoxine carbohydrate, proteinaceous and dezintoksikatsionny functions of a liver improve (release of bile increases).
The pyridoxine is a hematopoiesis stimulator, it raises ýðèòðîïîýç in case of toxic defeat of a red blood sprout, nevertheless, in case of iron deficiency and malignant anemia this means inefficiently. Influences on more actively, it is effective, radiation sickness, X-ray radiation.
The mechanism of action of a pyridoxine is caused by its participation in exchange of amino acids. Its active form — pyridoxal phosphate — as a coenzyme of the corresponding enzymes provides decarboxylation, reamination and deamination of the amino acids necessary for synthesis of nucleinic acids and proteins, including a myoglobin and hemoglobin. The pyridoxine intensifies absorption of amino acids in guts, their penetration from the blood course into cages and reabsorption in kidneys.
Piridoksalzavisimy enzymes exert the regulating impact on fatty exchange: promote intensive transformation of linolic acid to unsaturated arachidonic acid, at an atherosclerosis reduce the level of cholesterol and lipids in tissues, and also take part in process of carbohydrate metabolism, causing rising of maintenance of a glycogen in a liver.
Together with it the pyridoxine takes part in exchange of glutaminic acid, DIN To and a serotonin, in synthesis of catecholamins, exerts immediate impact on the course of exaltation and inhibition in a brain.
Implications of a failure of B6 vitamin (seborrheal dermatitis, glossitis, stomatitis, polyneuritis) can arise in cases of long treatment by antituberculous remedies — derivatives of Hydrazidum of isonicotinic acid (Isoniazidum, etc.). Formation of a gidrazon ïèðèäîêñàëÿ and its phosphoric Aether is the reason of it.
Indications to use: myocardial dystrophy, myocardiosclerosis, hepatitis, toxic and aplastic anemia, agranulocytosis, radial illness, chorea, parkinsonism, diseases of a peripheric nervous system (neuritis, radiculitis, etc.), intoxication, infectious diseases, prevention of toxiferous effect of remedies (antituberculous, sulfanylamide, Methyluracilum, etc.).
Side effects: allergic reactions, and also rising of acidity of a gastric juice.
Nicotinic acid (PP, B3 vitamins, Niacinum) and Nicotinamidum which is also considered as RR vitamin are pyridine derivatives, drugs nicotinic acid and Nicotinamidum respectively are produced.
Rich source of nicotinic acid are seedings of cereals, yeast, buckwheat, animal products — a liver, meat, milk. The human body is provided with this vitamin not only at the expense of products, but also by endogenic synthesis from irreplaceable amino acid of a tryptophan. Besides, nicotinic acid is synthesized by normal intestinal microflora.
Pharmakokinetics. After intake nicotinic acid and Nicotinamidum are intensively soaked up in a stomach and is limited in an intestine. This process can be broken at patients with a peptic ulcer of a stomach and duodenum, an enteritis, a colitis, a lambliasis. The biotransformation of nicotinic acid (amidation, formation of pyridine nucleotides — NMN, NAD, NADF) occurs mainly in a liver, and also in kidneys, adrenals and other organs with the participation of ATP. Pyridine nucleotides are distributed in an organism unevenly: a liver (the depositing organ)> a brain> a cardiac muscle> kidneys> sceletal muscles> erythrocytes. The period of semi-life of nicotinic acid — 45 min. The main final product of a metabolism of pyridine nucleotides is N-metilnikotinamid. All derivatives of nicotinic acid are removed with urine.
Pharmacodynamics. Nicotinic acid influences functions of a brain, cardiovascular system and digestive organs, system of a blood, and also a ratio of processes of exaltation and inhibition in a brain. Promotes the accelerated development of negative brake conditioned reflexes or their fixing if they were unstable. Under the influence of nicotinic acid processes of internal inhibition it is more expressed amplify in the conditions of pathological delicacy of brake process (neurosis, hysteria, psychotic states). The selativnykh, tranquilizing and neuroleptics exponentiates action.
Effects of nicotinic acid of rather cardiovascular system are important. In 3 — 5 min. after reception the dermahemia of the person, neck, the top part of a trunk (an inflammation phenomenon) develops. This reaction is caused by a trichangiectasia and is followed sometimes by feeling of a pricking and an itch. Nicotinic acid makes vasodilating impact at vasospasms of extremities, kidneys and a brain.
The cardiotrophic effect is implemented at two levels: on the one hand, this immediate participation the nikotinamidnykh of coenzymes in exchange of carbohydrates and in energy balance — decreases the content of pyrogrape and milk acids, the maintenance of a glycogen and ATP increases. On the other hand, microcirculation at the expense of a trichangiectasia which creates favorable conditions for supply of a myocardium with oxygen and nutrients improves. Improvement of a trophicity promotes rising of sokratitelny function of a myocardium.
Influence of drug on function of a liver predetermines rising of secretion and biliation owing to what improve digestion in an intestine, a glikogenobrazovaniye and beloksinteziruyushy function of a liver. Also property of nicotinic acid to strengthen lezintoksikatsionny function of a liver is important: processes of a conjugation and methylation of toxiferous bonds are activated.
In high rods nicotinic acid oppresses to an alenilatniklaz in fatty cells, and it leads to depression in them of tsAMF, oppression of processes of a lipolysis and decrease of entering of fatty acids in a liver. In high doses (3 — 4 g a day) vitamin reduces also the maintenance of trianilglitserol and atherogenous lipoproteins in a blood that is the cornerstone of its antiatherosclerotic action.
Nicotinic acid stimulates an erythrogenesis (especially in the conditions of pathology); before rising of a gemoglobinoobrazovaniye there is a mobilization of the iron deposited in an organism and augmentation of its contents in tissues of a red bloody sprout. Nicotinic acid has anticoagulating effect, under its influence production of anticoagulative factors in a blood raises and the fibrinolysis is activated. Purpose of this vitamin B a complex of medical actions gives the chance to reduce doses of anticoagulants at patients with a myocardial infarction, a stroke, a clottage of cerebral veins.
Pharmakodinamichesky effect of nicotinic acid is caused by its role in a metabolism. In an organism it turns into Nicotinamidum which participates in formation of NAD and NADF, and also is partially formed of a tryptophan. Nikotinamidny coenzymes (NAD and NADF) are necessary for vital activity of all living cells. Nitrogen of a pyridinic ring can turn from tetravalent (positively charged) into trivalent. Change of placement of double communications in a ring gives the chance of the return accession or return of a hydrogen atom (electron). Activity of constantly functioning oxidation-reduction system is so shown.
Participation the nikotinamidnykh of coenzymes in reaction of transferring of Hydrogenium does them universal almost for all types of exchange.
Important function of NAD and NADF is their participation in tissue respiration (the first link of a respiratory chain). Besides, direct participation the nikotinamidnykh of coenzymes in energy balance of a cell is established: at interconversions of NAD and NADF 151 kJ of mol "1 is released (36 Ltd companies a feces mol" 1).
Along with the kofermentny (specific) mechanism of adjustment of a metabolism there is a nekofermentny (mediated) mechanism of effect of nicotinic acid which is implemented through endocrine glands. It stimulates production of a thyroxine and strengthens function of cortical substance of epinephral glands, and also has hypoglycemic effect.
At a failure of nicotinic acid the pellagra develops: the CNS function (there is a dementia — mental retardation), systems of digestion (oppression of activity of enzymes, a diarrhea) are broken, the dermatitis appears.
The indication to use: a pellagra, neurotic states, mental diseases, a heart failure, stenocardia, a myocardial infarction (in the postinfarction period), a clottage of vessels of a retina and brain, an obliterating endarteritis, a Raynaud's disease, diseases of a liver, hypo - and anacid gastritis, a peptic ulcer of a stomach and duodenum, an enteritis, a coloenteritis, poisoning with industrial poisons and medicines (antituberculous drugs, barbiturates, Sulfanilamidums, etc.).
Side effects: feeling of fever, itch, giddiness, sharp erubescence of the person, neck and top third of a trunk. For prevention of these phenomena drug needs to be accepted right after food or to prescribe Nicotinamidum which doesn't cause the mentioned undesirable effects. In case of long the use of nicotinic acid in high doses can develop a fatty dystrophia of a liver. To prevent this complication, it is necessary to enrich a diet with the products rich with a methionine (cheese) or to prescribe drug a methionine and other lipotropic agents.
Acid pantothenic (Vit. B5) is issued in the form of pantothenate calcium medicine. It is widespread in the nature. A large number it is revealed in yeast, a liver, eggs, fish roe, grain crops, a cauliflower. Acid pantothenic is synthesized by intestinal microflora. Its dextrorotatory isomer is physiologically active.
Pharmacokinetics. Calcium pantothenate is well soaked up in a digestive tract, collects in heart, a liver, kidneys, adrenal glands. It is allocated in not changed view with urine (60%) and excrements (30%).
Firmakodinamika. In an organism acid pantothenic is a part of coenzyme A which plays an important role in processes of acetylation and oxidation (the atsilnykh of the remains is an acceptor and a carrier), formations of lemon acid (joining in a cycle the trikarbonovykh of acids), corticosteroids, acetylcholine, AGF, takes part in oxidation and biosynthesis of fatty acids, oxidizing decarboxylation of ketoacids (pyrogrape and-ketoglutarovoy, etc.), in absorption of potassium, tocopherol and other connections. Optimizes power ensuring reduction of a myocardium, improves regeneration processes. Insufficiency of acid pantothenic practically doesn't happen, at special modeling observed fatigue, a sleep disorder. headache, dispepsichesky frustration, parasteziya, muscular pains and other violations.
Indications to application: neuritis, neuralgia, some allergic reactions, diseases of respiratory organs, ulcers, burns, a postoperative atoniya of intestines, for elimination of toxic effects of streptomycin, compounds of arsenic.
Side effects: dispepsichesky phenomena, hypersensitivity reactions.
Acid pangamovy (Vit. B15) is issued in the form of a calcium of a pangamat.
Pharmakokinetics, pharmacodynamics. It is well soaked up in a digestive tube, delivers active metilny groups, calcium ions for biosynthetic processes, promotes formation of a creatine phosphate in muscles and a glycogen in muscles and a liver, eliminates the dystrophia phenomena. Participates in formation of a fosfatidinkholin, improves lipide exchange, digestion of oxygen of liver tissues.
Indications to use: atherosclerosis, pneumosclerosis, emphysema of lungs, chronic hepatitises, chronic drunkenness, skin and venereal diseases (pruritic dermatoses, syphilitic aortites), bad acceptability of Sulfanilamidums, corticosteroids and other drugs.
Side effects: allergic reactions.
Cyancobalamine (Vit. B12), and also folic acid (Vit. Su) — see the section "The Agents Influencing Blood Formation and Processes of a Blood Coagulation".
Ascorbic acid (Vit. Ñ). Most characteristics — the active restoring property (it is caused by Hydrogenium of enolny group at - the DREAM = the DREAM-) and mild oxidation in degidroaskorbinovy acid (fig. 2.9) which is easily restored by Cysteinum and glutathione.
Ascorbic acid belongs to irreplaceable components of a nutrition of the person, important sources of this vitamin are fresh vegetables and fruit. Hips, needles are very rich with ascorbic acid of berry of blackcurrant, mountain ash, sea-buckthorn.
Pharmacokinetics. In case of intake ascorbic acid is soaked up in intestines in the form of degidroaskorbinovy acid which gets through an intestinal membrane without energy costs and in cages the tiolovykh and disulfide groups is recovered in ascorbic acid due to oxidation of NADFN with participation.
The maximum concentration of medicine in blood plasma when entering per os is determined in 4 h. From plasma ascorbic acid arrives in all bodies, accumulating mainly in fabrics with intensive exchange, in particular, in adrenal glands, it is less in tissues of eyes, a brain, heart, lungs, kidneys, a liver. In fabrics ascorbic acid is both in a free condition, and in connections. From an organism it is allocated with urine in not changed condition (20%), and also in the form of degidroaskorbinovy (2%), diketogulonovy (20%) and oxalic (44%) acids. Smoking and abuse of alcohol accelerate transformation of ascorbic acid to inactive metabolites.
Pharmakodinamika. Ascorbic acid is necessary for various biological oxidizing processes. She promotes optimum fabric exchange, actively participates in oxidation-reduction reactions, creating system of transfer of atoms of hydrogen with degidroaskorbinovy acid. At the same time a number of enzymes which have to the tiolo-Vyya and disulfide groups is activated, the valency of metals changes.
Ascorbic acid plays an important role in an oxidizing vostanovitelnykh processes in system hemoglobin — a methemoglobin — hemoglobin. Availability it in erythrocytes protects hemoglobin, interfering with its oxidation. Ascorbic acid is capable to recover directly a methemoglobin, itself at the same time is oxidized in degidroaskorbinovy acid which is recovered under the influence of glutathione subsequently. Thanks to this system the methemoglobin doesn't accumulate in cages.
Along with a tocopherol ascorbic acid is a bioantioxidant that provides stability of cellular membranes. This action is bound to its recovery properties: a) restores the oxidized tocopherol which is a trap for free radicals (as a result they get a neutral molecular form); b) blasts peroxides, oppressing processes of free radical oxidation. Ascorbic acid is the factor necessary for a mitosis. As an antioxidant it provides the restored condition of SH-group, stimulates RNA exchange, provides formation of dihydrofolic acid from folic. Its ability to stimulate an angenesis, and also a mitosis of cells is explained by it.
Takes part in formation of the main substance of a connecting tissue which decrease in a vascular wall leads to hemorrhagic diathesis. The lesion of a connecting tissue at a failure of vitamin is bound to the fact that ascorbic acid takes part in education and ensuring the normal state of a collagen — an albuminous matrix of cartilages, bones, a dentine of teeth. The oxyproline which is formed by a proline amino acid gidroksirovaniye with the assistance of free radicals of ascorbic acid is a part of a collagen.
Influence of ascorbic acid on carbohydrate metabolism is explained by intensifying of oxidation of a glucose.
Ascorbic acid participates in a cholesterol catabolism, synthesis of corticosteroids. At stresses contents it in an organism considerably decreases, especially in adrenals. This vitamin activates synthesis of antibodies, an interferon, renders assistance to phagocytosis and restores function of polymorphonuclear leucocytes. Thus it increases adaptic ability of an organism to adverse conditions of the environment — to an infection, intoxication, a frigorism, etc.
Antianemic effect of ascorbic acid is bound to influence on iron exchange, namely to restoration of trivalent iron in divalent which is easily soaked up in an intestine.
Indications to use: a Barlow's disease, hypovitaminosis, especially during the winter and spring period, during an intensive exercise stress, stresses; infectious diseases, hemorrhagic diathesis, capillary toxicosis, anemia, radial illness, long adhesion of wounds, fractures of bones, inflammation of joints, periodontal disease, ulitis, intoxication industrial poisons.
Side effects: long use of ascorbic acid even in therapeutic doses can cause appreciable disturbances in an organism — there is a damage of islands of a pancreas, insulin remission is slowed down. Excess formation of degidroaskorbinovy acid which turns into oxalic acid leads to formation of concrements in urinary tract and to disturbance of a metabolism in a vascular wall. Permeability of capillaries and the gistogematicheskikh of barriers decreases owing to what the trophicity of tissues is broken. Long administration of drug results in the accelerated coagulability of a blood and a thrombogenesis, and use in high doses — to abortions.
Bioflavonoids (Vit. Ð). From big group of bioflavonoids (Rutinum, Quercetinum, a hesperidin, etc.) in medicine use Rutinum beta ramnoglyukozil-3,5,7,3,4-pentaoksiflavon) and Quercetinum.
In the form of glycosides bioflavonoids contain in many plants, especially in hips and a citrus, berries of blackcurrant, mountain ash, green leaves of tea, in flowers and leaves of a buckwheat.
The main disturbance in an organism at a vitamin P disadvantage — rising of fragility and fragility of capillaries.
Pharmakokinetics. Bioflavonoids are soaked up from the intestinal channel moderately, in an organism biotransformations are exposed. Rutinum turns into gomovanilinovy, oksifeniluksusny and dioksifeniluksusny acids which are removed with urine.
Pharmacodynamics. Bioflavonoids have antioxidatic properties, protect ascorbic acid from excess oxidation, keeping its biological activity. Promote transport and deposition of ascorbic acid, enlarge its accumulation in adrenals, a liver and other organs and at the same time slow down removal it from an organism. Strengthen walls of capillaries, showing a synergy with ascorbic acid. Together with it this vitamin brakes activity of Hyaluronidasum thanks to what intercellular substance is stabilized, permeability of a wall of capillaries decreases and their fragility decreases.
Vitamin slows down oxidation of an adrenaline thanks to ability to bind ions of iron and copper which catalyze oxidation of an adrenaline in strong complexes.
Use of Rutinum and other flavonoids increases firmness of tissues at radiation injuries.
Indications to use: diseases which are followed by rising of permeability of vessels (hemorrhagic diathesis, a capillary toxicosis, a radial illness, etc.), prophylaxis of the damage of a wall of capillaries bound to use of anticoagulants of indirect action and Salicylas.
Side effects at use of Rutinum aren't established.
Quercetinum — glikozidny drug of Rutinum — shows properties of the modulator of various enzymes which are taking part in degradation of phospholipids (phospholipases, ôîñôîãåíàç, cyclooxygenases) which influence free radical processes and are responsible for a biosynthesis in cells of nitrogen oxide, proteinases, etc. The imitating action of Quercetinum on membranotropny enzymes and, first of all, on a 5-lipooksigenaza affects inhibition of synthesis of leykotriyen of LTC4 and LTB4. Along with it drug äîçîçàâèñèìî increases nitrogen oxide level in endothelial cells that explains its cardiotyre-tread action, antioxidatic, neyromoduliruyushy properties, neurotyre-tread, hepatoprotective effect. Quercetinum reduces development of a cytotoxic superoksidanion, normalizes activation of subpopulation structure of lymphocytes and reduces activation level. Braking production of pro-inflammatory cytokines (the OOZE-1beta, the OOZE-8), drug promotes decrease of volume of a nekrotizirovanny myocardium, regenerative processes in myocardium tissues, on a skin, mucous. Reduces ulcerogenic effect of non-steroidal anti-inflammatory drugs, possesses some antiinflammatory action. At Quercetinum radio tire-tread action is noted.
Indications to use: in granules — in stomatologic practice, for neogenesis acceleration, in a complex pharmacotherapy of diseases of the digestive channel and a liver, for decrease of influence of the ionizing radiation. Water-soluble drug of Quercetinum — êîðâèòèí use as a cardiotyre-tread agent in a complex pharmacotherapy at an acute disorder of a coronary circulation and a myocardial infarction, for prophylaxis of a reperfusion syndrome at surgical treatment of patients with an obliterating atherosclerosis of an abdominal aorta and peripheric arteries. Lipoflavon containing Quercetinum and possessing antigipoksantny, antioxidatic, reparative, membrane stabilizing action prescribe at wounds and postoperative wounds of a cornea, a keratitis, inflammatory diseases of eyes.
Side effects: can cause the hypersensitivity phenomena.
Vicasolum (Vit. To) see. "The agents influencing blood formation and processes of a blood coagulation".
The biotype plays a role in synthesis of a purin, nucleic acids, proteins.
Polyvitaminic drugs are complexes of separate vitamins B the balanced physiological ratios. A basis for the combined use of vitamin drugs is mutual intensifying of their effect (for example, ascorbic acid strengthens protective influence of Rutinum on permeability of a wall of vessels; folic acid — influence of cyancobalamine on a hemopoiesis), and also decrease of toxicity of vitamins at their combined use (for example, toxicity of Calciferolum decreases under the influence of Retinolum).
Some polyvitaminic drugs for intensifying of effect unite to amino acids, ions of metals and trace substances. The tablets "Dekamevit" contain 10 vitamins and amino acid a methionine, the tablets "Glutamevit" — 10 vitamins, glutaminic acid, copper, iron, a potassium and a calcium.
The drug Multi-tabs classical contains vitamins of group B and trace substances (also Multi-tabs polyvitaminic with minerals are known and (3 Carotinum, Multi-tabs plus with liposoluble vitamins, Multi-tabs of a yodopro-filaktik).
Neyrovitan (an octothiamine, Riboflavinum, a pyridoxine a hydrochloride, cyancobalamine), the neurone (Thiaminum monosodium nitritum, Riboflavinum, a pyridoxine a hydrochloride, cyancobalamine) is often prescribed at neurologic diseases. Combine drugs of vitamins A and E (Aevitum, àåêàïñ), vitamin B drugs, with drugs of B6 vitamin or BP (a milgamma, a neuroruby, a neyroru-bin forte, ëàêòàá), B6 — with a magnesium (magnevit Wb, the mayena of B6).
Revalid contains a calcium a pantothenate, Thiaminum a hydrochloride, a pyridoxine a hydrochloride in combination with methionine, cystine, para-aminobenzoic acid, extract of millet, wheat sprouts, yeast, Zincum, iron).
Tri-vi beta carotene, ascorbic acid, and - a tocopherol an acetate), in addition to previous Zincum, selenium, copper contain three-vi plus.
Trivit-Se-KB (and - a tocopherol an acetate, R-carotene, ascorbic acid, sodium selenit) also, as well as other drugs of Polyvitaminums, recommend to inhabitants of ecologically adverse districts, allocate in group of Polyvitaminums antioxidants. Also other polyvitaminic complexes, for example the drug Bitam, except vitamins of group B and trace substances are issued, contains acid mefenamovy which stabilizes albuminous metastructures and cellular membranes, reduces permeability of vessels, puffiness of cells, increases resistance of cells.
Pharmacodynamics. Polyvitaminic drugs activate various biochemical processes in an organism, strengthen tissue respiration, stimulate oxidizing phosphorylation, protein synthesis, strengthen oxidizing âîñòàíîâèòåëüíûå reactions, etc. They activate physical and cerebration, strengthen the belkovoobrazuyushchy, vneshnesekretorny and decontaminating functions of a liver, increase immunologic reactivity and protective properties of an organism.
Indications to use: polyhypovitaminoses, for improvement of a metabolism and the general state in old age, mental and physical attrition, during convalescence after a serious illness, long treatment by antimicrobic agents, a radial illness, rising of adaptation of an organism to influence of extreme factors (adverse climatic conditions, vibration, etc.), sports activities.
Influence of vitamin drugs on efficiency of athletes
Thiamini chloridum (B1 vitamin drug). So far the researches concerning the isolated influence of Thiaminum on physical working capacity weren't conducted. Anabolic action is also not characteristic of this vitamin drug. However it is necessary to consider its participation in synthesis of Acetylcholinum and a possibility of rising of a tonus of a sceletal musculation. Besides, drug possesses cardiotrophic, neurotyre-tread action, is a synergist of insulin. In some works its positive influence on acoustical and visual analyzers and consequently, on expediency of use by athletes who specialize in different types of firing is confirmed. It is necessary to take realization of analgetichesky influence and antioxidatic effect into account.
To relatives on a structure to Thiaminum drug which is recommended at asthenic states is. We find possible including it in schemes of appointment to athletes before competitions.
Perhaps, the drug of a milgamm including derivative Thiaminum — Benphothiaminum differing in the best pharmacokinetic parameters, first of all more bystry rate of an absorption is of a certain interest to athletes. Now it is applied at neurologic diseases. We consider rational including of drug in schemes of reception by athletes both before competitions, and during the period after them.
Riboflavinum (B2 vitamin drug). Investigated influence of additional consumption of Riboflavinum on physical efficiency of 14 Canadian swimmers of high qualification with the normal status for this vitamin and the regimen of its consumption with a nutrition meeting the recommended standards. Surveyed one subgroup for 16 — 20 days accepted it in a dose of 60 mg a day whereas for surveyed other subgroup drug replaced placebo. Physical working capacity was estimated in the swimming test consisting in sixfold overcoming a 50-meter distance freestyle. Besides, in the tredmilny test defined the maximum aerobic power and a ventilating anaerobic threshold. Drug considerably increases visual acuity and fastness to a hypoxia; at the same time consumption of Riboflavinum in long tests didn't affect indicators of its level in a blood, on indicators of physical working capacity. The conclusion was drawn that in the course of the sports training swimmers completely can support the normal riboflavinovy status without additional consumption of this vitamin. Besides, it is obvious, it is necessary to fulfill its dosages for the athletes specializing in firing and also in other sports, taking into account antigipoksiche-sky effect.
B2 vitamin in itself has no anabolic activity, and its kofermentny forms — Riboflavinum a mononucleotide and Flavinatum which in Ukraine aren't issued — possess. Drugs activate the enzymes participating in synthesis of amino acids, lipids and carbohydrates. They normalize the course of oxidation-reduction processes, holesterolovy exchange, strengthen hemoglobin synthesis, accelerate a jelly absorption - for, improve vision. For the growing organism these drugs are an irreplaceable growth factor.
The nicotinic acid, Niacinum (drug of PP, B3 vitamin) entered into an organism in quite appreciable doses improves oxidation-reduction reactions, shifting equilibrium towards restoration processes. RR vitamin strengthens effects of endogenic insulin with anabolic action inherent in it. Under its influence in an organism the content of serotonin is enlarged. Nicotinic acid increases acidity of a gastric juice and its digesting ability, improving thereby comprehensibility of a nutrition. At the same time rate of a peristalsis of the digestive channel increases and appetite increases. RR vitamin is a part of ferment systems (the nikotinamidnykh of coenzymes) which in a varying degree take part in exchange of all other vitamins therefore introduction it considerably improves the overall vitamin balance of an organism. Nicotinic acid can have vasodilating and tranquilizing effect (influences the same benzodiazepine receptors, as tranquilizers), possesses cardiotrophic action, accelerates a peristalsis.
Everything stated, except for vasodilating action, characterizes also Nicotinamidum therefore both nicotinic acid, and Nicotinamidum are widely used in clinical practice.
Nicotinic acid possesses anabolic action, shown in doses several times larger, than those which are applied in usual medical practice. If usually it is used in doses 50 — 300 mg of days-1, then for intensifying of an anabolism prescribe up to 3 — 9 g of days-1. Such high doses can have appreciable side effects therefore treatment by nicotinic acid needs to be carried out with care. She impoverishes an organism metilny radicals owing to what the fatty dystrophia of a liver can develop, function of a pancreas is broken. For prevention of it along with nicotinic acid it is necessary to prescribe lipotropic agents — methionine, vitamin U, a choline Sodium chloridum. The diet has to contain enough cottage cheese. In an initiation of treatment nicotinic acid right after administration (reception) of drug observes sharp vasodilatation of a skin with reddening which lasts 10 — 20 min. after reception. Such reaction at injection introduction is especially strongly expressed. Because of strong vasodilatation at the persons inclined to a hypotension, pressure therefore after an injection they need to have a rest 15 — 20 min. in a prone position can sharply go down. High doses of drug lead to a hypertrophy of adrenals and considerably increase shipping of exercise stresses. As contraindications for use of nicotinic acid serve the peptic ulcer of a stomach and a duodenum, a hyperoxemia of a gastric juice, a liver obesity. At these diseases treatment of nicotinic acid can cause reaction of an exacerbation.
Acute influence on power exchange of Niacinum (75 mg), glycine (750 mg), their combination and placebo at 86 surveyed was investigated. Definition of physical working capacity consisted in performance two the veloergometricheskikh of loads with five-minute rest between them. Results showed that the applied substances don't influence physical working capacity.
During studying of acute influence of Niacinum (300 mg and 1 g) both during the recovery period, and during performance of exercise stresses the depression of content in plasma of free fatty acids which was a consequence of mobilization of the last of adipozny body tissue is revealed. It is possible to assume that this phenomenon will promote development of a fatigue when performing the exercise stresses bound to endurance implication as in this case use of a muscular glycogen has to happen quicker.
At a research of influence of nicotinic acid on implication of endurance it is found out that at consumption of this vitamin when performing short-term muscular work of approximately maximum power or a continuous duty of the submaximum intensity indicators of physical working capacity remain almost invariable. However after reception of Niacinum the carried-out load seemed for surveyed more serious and tiresome. Thus, in spite of the fact that use of a muscular glycogen at an exercise stress happened more intensively, than at oxidation of fats, objective indicators of an acceptability of the performed muscular work were incompatible with value judgment.
Subsequently it was established that how glycogen stocks in muscles were exhausted, the exercise stress can proceed with power, a component less than 60% of MT To, due to utilization of the free fatty acids arriving in enough for performance of such work. However decrease of maintenance of a glycogen in muscles when performing exercise stresses and depression of entering of free fatty acids under the influence of Niacinum reduces further ability to endurance implication.
Pantothenic acid, a calcium a pantothenate (B5 vitamin drug), possesses potent anabolic action, it is promoted by its participation in synthesis of a coenzyme A. Preparat surpasses all other vitamin drugs in anabolic action. Considerably reduces the main exchange that leads to rapid growth of lump of a body as to result of decrease of a share of oxidable proteins, lowers glucose level in a blood that promotes emission of somatotropic hormone, increases synthesis of Acetylcholinum, the ATP raising a tonus of a parasympathetic nervous system that promotes augmentation of force of the neuromuscular device. A calcium a pantothenate strengthens synthesis of steroid and other hormones and a hemoglobin. It is drug of "ekonomiziruyushchy action" as does work of an organism of more economic. Drug participates in the most important reactions of transfer of energy and phosphoric bonds, improves work of a liver and promotes removal from an organism of toxins, alcohol, poisons, medicinal substances. Has the expressed radioprotective properties, removal of radi