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

Pharmacological effects: in quantities significantly exceeding the daily requirement (90 mg), almost no effect, except for the rapid elimination of symptoms of hypo- and avitaminosis (scurvy).

Physiological functions: is a 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 the 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 synthesis of the picture), the oxidation of folic acid to folinic, the metabolism of drugs in liver microsomes and hydroxylation dopamine with the formation of norepinephrine.Increases the activity of amidating enzymes involved in the processing of oxytocin, antidiuretic hormone and holitsistokinina. Participates in steroidogenesis in the adrenal glands. Restores iron (III) up to iron (II) in the intestines, contributing to 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 with 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 _/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 plasma is approximately 10-20 μg / ml, stocks in the body - about 1.5 g with daily recommended doses and 2.5 g when taken 200 mg / day. Time to reach the maximum concentration 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. In the case of deficient states, the concentration in leukocytes decreases later and more slowly and is considered as the best criterion assessment of 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 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 diet, increased mental and physical loads, the period of reconvalescence after severe illnesses, alcoholism, burn disease, febrile state against the background of acute respiratory disease, acute respiratory viral infection; long-term chronic infections, nicotine dependence, stress, postoperative period, pregnancy (multiple birth, against nicotine or drug dependence). Chronic intoxication with iron preparations (as part of complex therapy with deferoxamine). Idiopathic methemoglobinemia.

Contraindications:

If you have any of these diseases, consult a doctor before taking the drug.

Hypersensitivity, with prolonged use in high doses (more than 500 mg) - diabetes mellitus, hyperoxaluria, nephrolithiasis, hemochromatosis, thalassemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, glucose-6-phosphate dehydrogenase deficiency, sugarase / isomaltase deficiency, fructose intolerance ,children's age up to 3 years.

Carefully:

Sideroblastic anemia.

Pregnancy and lactation:Ascorbic acid is used only if the intended benefit to the mother exceeds the risk to the fetus and the baby.

Dosing and Administration:

Inside, after eating.

For the prevention of hypovitaminosis C: adults - 50-100 mg / day. Children: 3-6 years - 25 mg / day; 6-14 years - 50 mg / day; 14-18 years - 75 mg / day; during pregnancy and lactation - 300 mg / day for 10-15 days; further on 100 mg / sut.

With a curative purpose: children - but 50-100 mg 2-3 times a day, adults - 50-100 mg 3-5 times a day for 2 weeks.

In the treatment of scurvy adults - up to 1000 mg per day, children - up to 500 mg per day. The maximum daily intake for adults is 1000 mg.

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

Idiopathic methemoglobinemia - not less than 150 mg / day.

Side effects:

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

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

From the digestive system: when ingested - 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 cardiovascular system: with prolonged use of large doses - a decrease in the permeability of capillaries (possibly worsening of tissue trophism, increased blood pressure, hypercoagulation, development of microangiopathies).

Allergic reactions: skin rash, skin hyperemia.

Laboratory indicators: thrombocytosis, hyperprothrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia, glucosuria.

Other: oppression of the insular pancreas function (hyperglycemia, glucosuria).

If any of the side effects indicated in the manual are aggravated or you notice any other side effects not listed in the instructions, inform your doctor.

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:

Increases the concentration in the blood of benzylpenicillin and tetracyclines; in a dose of 1 g / day increases the bioavailability of ethinyl estradiol (including that of oral contraceptives).

Improves absorption in the intestines of iron preparations (converts trivalent iron into bivalent); can increase the excretion of iron with simultaneous use with deferoxamine.

Reduces the effectiveness of heparin and indirect anticoagulants.

Acetylsalicylic acid, oral contraceptives, fresh juices and alkaline drink reduce absorption and absorption. With simultaneous use with acetylsalicylic acid, urinary excretion of ascorbic acid increases and the excretion of acetylsalicylic acid decreases. Acetylsalicylic acid reduces absorption of ascorbic acid by about 30%. ,

Increases the risk of developing crystalluria in the treatment of salicylates and sulfonamides short-acting, slows the excretion of acids, increases the excretion of drugs that have an alkaline reaction (including alkaloids).

Reduces the concentration in the blood of oral contraceptives.

Increases the total clearance of ethanol, which, in turn, reduces the concentration of ascorbic acid in the body.

The drugs of quinoline series, calcium chloride, salicylates, glucocorticosteroids with long-term use deplete the stores of ascorbic acid.

With simultaneous use reduces the chronotropic effect of isoprenaline.

With prolonged use or use in high doses, it can interfere with the interaction of disulfiram and ethanol.

In high doses increases the excretion of mexiletine by the kidneys.

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

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

Special instructions:

Foods rich in ascorbic acid: citrus fruits, greens, vegetables (peppers, broccoli, cabbage, tomatoes, potatoes). When storing products (including long-term storage freezing, drying, pickling, marinating), cooking (especially in copper vessels),crushing vegetables and fruits in salads, the preparation of puree is a partial destruction of ascorbic acid (with a temperature treatment - up to 30-50%). High doses of ascorbic acid increase the excretion of oxalates, promoting the formation of stones in the nights. In newborns, whose mothers took high doses of ascorbic acid, and in adults who took high doses, there may be a "ricochet" scurvy. In connection with the stimulating effect of ascorbic acid on the synthesis of corticosteroid hormones, it is necessary to monitor the function of the adrenals and arterial pressure. With prolonged use of large doses, oppression of the insulin function of the pancreas is possible, so during treatment it must be regularly monitored. In patients with elevated iron levels in the body, ascorbic acid should be used in minimal doses. Frequent resorption of oral forms can cause damage to tooth enamel. Ascorbic acid as a reducing agent can distort the results of various laboratory tests (blood and urine glucose content, bilirubin, activity "liver" transaminases and lactate dehydrogenase).

The minimum daily requirement for ascorbic acid in II-III trimesters of pregnancy - about 60 mg. It should be borne in mind that the fetus can adapt to high doses of ascorbic acid, which is taken by a pregnant woman, and then a "cancellation" syndrome may develop in a newborn. The minimum daily requirement for lactation is 80 mg. A mother's diet containing an adequate amount of ascorbic acid is sufficient to prevent her deficiency in an infant. Theoretically, there is a danger to the child when the mother uses high doses of ascorbic acid (it is recommended not to exceed the daily need for ascorbic acid by the lactating mother).

Form release / dosage:

Tablets of 50 mg.

Packaging:

For 50 tablets in jars of orange glass or in cans of polymer.

For 10 tablets in a contour mesh box made of polyvinylchloride film and foil of aluminum printed lacquered or paper with polyethylene coating.

For 10 tablets in a contour non-cellular package of paper with polyethylene coating.

1 jar or 1, 2, 3, 4, 5 contour mesh or contour non-jawed packages together with instructions for use are placed in a pack of cardboard.

100 contour mesh or contour non-jawed packages with an equal number of instructions for use are placed in a cardboard box.

Storage conditions:

In dry, the dark place at a temperature not higher than 15 ° С. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-001929

Date of registration:22.07.2011

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp25.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)