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

Pharmacological effects: in amounts,significantly exceeding the daily requirement (90 mg), has 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 reactions hydroxylation of proline and lysine residues procollagen to form hydroxyproline and hydroxylysine (postranslyatsionnaya collagen modification), the oxidation of the side chains of lysine in proteins to form gidroksitrimetillizina (during synthesis kartinita) oxidation of folic acid to folinic, drug metabolism in liver microsomes and hydroxylation dopamine with the formation of norepinephrine.

Increases activity amidating enzymes involved in the processing of oxytocin, antidiuretic hormone and holitsistokinina. Participates in steroidogenesis in the adrenal glands.

Recovers Fe3+ before Fe2+ in the intestines, contributing to its absorption. The main role in the tissues is the 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, the absorption decreases (50-20%). Connection with plasma proteins - 25%. Diseases of the gastrointestinal tract (gastric ulcer and duodenal ulcer, constipation or diarrhea, helminthic invasion, giardiasis), the use of fresh fruit and vegetable juices, alkaline drink reduces 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 taken at 200 mg / day. Time to reach the maximum concentration (TCmah) 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 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 accelerates the destruction of ascorbic acid (conversion into inactive metabolites), drastically reducing reserves in the body.

It is in hemodialysis.

Indications:

Treatment and prevention of hypo - and avitaminosis of vitamin C.

The states of increased need for ascorbic acid: the period of artificial feeding and intensive growth, unbalanced nutrition, increased physical and mental loads, the period of reconvalescence after severe diseases, alcoholism, burn disease, long-term chronic infections; nicotinic dependence, prolonged stressful condition,postoperative period, pregnancy (multiple, with nicotine or drug dependencies).

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

Idiopathic methemoglobinemia.

Contraindications:

Hypersensitivity, with prolonged use at high doses (over 500 mg) - diabetes, hyperoxaluria, nephrolithiasis, hemochromatosis, thalassemia, deficiency of glucose-6-phosphate dehydrogenase.

Carefully:Diabetes mellitus, deficiency of glucose-6-phosphate dehydrogenase, hemochromatosis, sideroblastic anemia, thalassemia, hyperoxaluria, kidney stone disease.

Pregnancy and lactation:

In pregnancy and during lactation apply only if the intended benefit to the mother exceeds the risk to the fetus and the baby.

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).

Dosing and Administration:

Inside, after eating.

Powder is used for making beverages - 1 g of ascorbic acid powder (contents of one sachet-bag) - per 1 l of water (juice). The solution is taken freshly prepared (within no more than 8 hours after preparation), in accordance with the dosages suggested below.

For dosing, the use of a medical measuring cup is recommended.

For the prevention of hypovitaminosis C: adult - 50-100 mg (50-100 ml) per day.

Children: 3-6 years - 25 mg (25 ml) per day, 6-14 years-50 mg (50 ml) per day, 14-18 years-75 mg (75 ml) per day; during pregnancy and lactation - 300 mg (300 ml) per day for 10-15 days, then - 100 mg (100 ml) per day.

With a curative purpose: children - 50-100 mg (50-100 ml) 2-3 times a day, adults - 50-100 mg (50-100 ml) 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 (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.

Note: the medical measuring cup is not included in the kit.

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 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: ingestion - irritation of the mucous membrane of the gastrointestinal tract (GIT), with prolonged use of large doses - nausea, vomiting, diarrhea, hyperacid gastritis, ulceration of the gastrointestinal mucosa.

From the side of the cardiovascular system: 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.

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

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

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 those included in the composition 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 (ASA), oral contraceptives, fresh juices and alkaline drink reduce absorption and absorption.

With simultaneous application with ASA, urinary excretion of ascorbic acid increases and the excretion of ASA decreases. ASA reduces the 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 kidney acids, increases the excretion of drugs that have an alkaline reaction (including alkaloids), reduces the concentration of oral contraceptives in the blood.

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

Drugs quinoline series, calcium chloride, salicylates, glucocorticosteroids with prolonged 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) - derivativesphenothiazine, 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 prolonged freezing, drying, pickling, pickling), cooking (especially in copper vessels), chopping vegetables and fruits in salads, preparing purees, partial destruction of ascorbic acid occurs (up to 30-50% in the case of temperature treatment).

High doses of ascorbic acid increase the excretion of oxalates, facilitating formation of kidney stones. 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 should be used ascorbic acid in minimal doses.

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

Form release / dosage:

Powder for oral administration of 1000 mg.

Packaging:

For 1 g in heat-sealing bags of material combined or from packaging material.

3 or 5 packages, together with the instruction for use, are placed in a pack of cardboard for consumer containers.

Packages with an equal number of instructions for use are allowed in a carton box box (group packaging).

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:LS-002248

Date of registration:07.11.2011 / 30.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:MARBIOFARM, OJSC MARBIOFARM, OJSC Russia

Manufacturer: & nbsp

MARBIOFARM, OJSC Russia

Information update date: & nbsp25.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)