Ascorbic acid - instructions for use, dose, side effects, contraindications

Ascorbic acid (vitamin C) is not formed in the human body, but comes only with food.Is cofactor of some hydroxylation and amidation reactions - transfers electrons to enzymes, providing them with a replacement equivalent. Participates in the reactions of hydroxylation of proline and lysine residues of procollagen with formation of hydroxyproline and hydroxylizine (post-translational modification of collagen), oxidation of the side chains of lysine in proteins with the formation of hydroxytrimethyllysine (during the synthesis of the picture), the oxidation of folic acid to folinic, the metabolism of drugs in liver microsomes, and the hydroxylation of dopamine with the formation of noradrenaline. Increases the activity of amidating enzymes involved in the processing of oxytocin, antidiuretic hormone and holitsistokinina. Participates in steroidogenesis in the adrenal glands. Restores trivalent iron ions to the divalent iron ions in the intestine, promoting its absorption. The main role in the tissues is participation in the synthesis of collagen, proteoglycans and other organic components of the intercellular substance of the teeth, bones and endothelium of the capillaries. In low doses (150-250 mg / day inwards) improves the complexing function of deferoxamine in chronic intoxication with iron preparations,which leads to increased excretion of the latter.

Pharmacokinetics:

Absorbed in the gastrointestinal tract (mainly in the jejunum). With an increase in the dose up to 200 mg, up to 140 mg (70%) is absorbed; with a further increase in the dose, the absorption decreases (50-20%). Connection with plasma proteins - 25%. Diseases of the gastrointestinal tract (peptic ulcer of stomach and duodenum, constipation or diarrhea, helminthic invasion, giardiasis), the use of fresh fruit and vegetable juices, alkaline drink reduce the absorption of ascorbic acid in the intestine. The concentration of ascorbic acid in the plasma is normally about 10-20 μg / ml, the reserves in the body are about 1.5 g when taking daily recommended doses and 2.5 g when taking 200 mg / day. Time to reach the maximum concentration (TC_max) after ingestion - 4 hours.

Easily penetrates into leukocytes, platelets, and then into all tissues; the greatest concentration is achieved in glandular organs, leukocytes, liver and lens of the eye; penetrates the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and in plasma. With deficient states, the concentration in leukocytes decreases later and more slowly and is considered as the best criterion for assessing the deficit than the concentration in the plasma.

Metabolised mainly in the liver in desoxyascorbic and then in oxaloacetic acid and ascorbate-2-sulfate.

It is excreted by the kidneys, through the intestines, with sweat, breast milk in the unchanged form and in the form of metabolites.

At the appointment of high doses, the rate of excretion increases sharply. Smoking and the use of ethanol accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing the reserves in the body.

It is in hemodialysis.

Indications:

Treatment and prevention of hypo- and avitaminosis C.

The states of increased need for ascorbic acid: the period of artificial feeding and intensive growth, unbalanced nutrition, increased mental and physical loads, the period of reconvalescence after severe illnesses, alcoholism, burn disease, febrile state against the background of ARI, ARVI; long-term chronic infections, nicotine dependence, stress state, postoperative period, pregnancy (multicomponous against the background of nicotine or drug dependence).

Chronic intoxication with iron preparations (as part of complex therapy with deferoxamine).

Idiopathic methemoglobinemia.

Contraindications:

Hypersensitivity. With the introduction of large doses (more than 500 mg) - diabetes mellitus, hypercoagulation, thrombophlebitis, a tendency to thrombosis.

Carefully:Hyperoxalaturia, renal failure, hemochromatosis, thalassemia, polycythemia, leukemia, sideroblastic anemia, glucose-6-phosphate dehydrogenase deficiency, sickle cell anemia, progressive malignant diseases, oxalosis, kidney stone disease.

Pregnancy and lactation:

The minimum daily requirement for ascorbic acid in the II - III trimesters of pregnancy is about 60 mg.

The minimum daily requirement for breastfeeding is 80 mg.

A mother's diet containing an adequate amount of ascorbic acid is sufficient to prevent vitamin C deficiency in a child.

During pregnancy and breastfeeding, the recommended dosage of ascorbic acid should not be exceeded.

Dosing and Administration:

Inside, after eating.

Powder is used for making beverages - 2.5 g of powder (the contents of one package) for 2.5 liters of water. The solution is taken freshly prepared, according to the dosages proposed below. The prepared solution is not subject to long-term storage.

For prevention: adults 50-100 mg (50-100 ml) per day; children from 3 to 6 years - 25 mg (25 ml) per day; from 6 to 14 years - 50 mg (50 ml) per day; from 14 to 18 years - 75 mg (75 ml) per day.

For treatment: adults 50-100 mg (50-100 ml) 3-5 times a day, children from 5 years - 50-100 mg (50-100 ml) 2-3 times a day.

During pregnancy and breastfeeding - 300 mg (300 ml) per day for 10-15 days; further - 100 mg (100 ml) per day.

In the treatment of scurvy adults - up to 1000 mg (1000 ml) a day, children - up to 500 mg (500 ml) per day.

Chronic intoxication with iron preparations (as part of complex therapy with deferoxamine): adults - 200 mg (200 ml) per day, children under 10 years - 50 mg (50 ml) per day, children over 10 years -100 mg (100 ml) in day.

Idiopathic methemoglobinemia is not less than 150 mg (150 ml) per day.

For adults: the maximum single dose is 200 mg, the daily dose is 1 g; for children - 50-100 mg / day.

Side effects:

From the central nervous system (CNS): headache, fatigue, with prolonged use of large doses (more than 1000 mg) - increased excitability of the central nervous system, insomnia.

From the urinary system: moderate pollakiuria (when taking a dose of more than 600 mg / day), with long-use of large doses - hyperoxaluria, the formation of urinary stones from calcium oxalate, damage to the glomerular apparatus of the kidneys.

From the side digestive system: irritation of the mucous membrane of the gastrointestinal tract, with prolonged use of large doses - nausea, vomiting, diarrhea, hyperacid gastritis, ulceration of the mucous membrane of the gastrointestinal tract.

From the endocrine system: oppression of the insular pancreas function (hyperglycemia, glucosuria).

From the side of cardio-vascular system: thrombosis, with prolonged use of large doses - a decrease in the permeability of capillaries, (possibly worsening tissue trophism, increased blood pressure, hypercoagulation, development of microangiopathies).

Allergic reactions: skin rash, skin hyperemia.

Overdose:

Symptoms: diarrhea, nausea, irritation of the mucous membrane of the gastrointestinal tract, flatulence, abdominal pain of a spastic nature, frequent urination, nephrolithiasis, insomnia, irritability, hypoglycemia.

Treatment: symptomatic. Forced diuresis.

Interaction:

Absorption of ascorbic acid decreases with simultaneous use of oral contraceptives, acetylsalicylic acid, the use of fresh fruit or vegetable juices, alkaline drinks.

Ascorbic acid when taken orally increases the absorption of penicillin and iron, reduces the effectiveness of heparin and indirect anticoagulants, increases the risk of developing crystalluria in the treatment of salicylates.

With simultaneous use reduces the chronotropic effect of isoprenaline.

With prolonged use or application in large doses, it can disrupt the interaction of disulfiram and ethanol.

Barbiturates and primidon increase the excretion of ascorbic acid in the urine.

Reduces the therapeutic effect of antipsychotic drugs (phenothiazine derivatives), tubular reabsorption of amphetamine and tricyclic antidepressants.

Special instructions:

When using ascorbic acid in high doses, it is necessary to monitor the function of the kidneys, the pancreas and the level of blood pressure.

In patients with elevated iron levels in the body, ascorbic acid should be used in minimal doses.

Assigning ascorbic acid to patients with rapidly proliferating and intensely metastatic tumors can aggravate the course of the process.

Ascorbic acid, as a reducing agent, can distort the results of various laboratory tests (blood and urine glucose, bilirubin, transaminase activity, LDH).

High doses of ascorbic acid increase the excretion of oxalates, promoting the formation of kidney stones.

Effect on the ability to drive transp. cf. and fur:

Ascorbic acid does not adversely affect the ability to drive vehicles and perform work that requires an increased rate of psychomotor reactions.

Form release / dosage:Powder for solution for oral administration 2.5 g.

Packaging:

By 2.5 grams in heat-sealed bags of packaging material from the combined materials.

Packages are placed in a group package together with an equal number of instructions for application.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-001234

Date of registration:17.11.2011

Expiration Date:Unlimited

The owner of the registration certificate:TULA PHARMACEUTICAL FACTORY, LTD. TULA PHARMACEUTICAL FACTORY, LTD. Russia

Manufacturer: & nbsp

TULA PHARMACEUTICAL FACTORY, LTD. Russia

Information update date: & nbsp25.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)