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. 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 for some reactions hydroxylation and amidation - transfers electrons to enzymes, supplying their reducing equivalents. 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.The main role in 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.

Pharmacokinetics:

Connection with plasma proteins - 25%. The concentration of ascorbic acid in the plasma is normally around 10-20 μg / ml. 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 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 of hypo-and avitaminosis C (if necessary, rapid replenishment of vitamin C and the impossibility of oral administration). Used for medicinal purposes in all clinical situations involving the need for additional administration of ascorbic acid, including parenteral nutrition, diseases of the gastrointestinal tract (persistent diarrhea, small bowel resection, peptic ulcer, gastrectomy), Addison's disease.

In laboratory practice: for marking erythrocytes (together with sodium chromate - Cr51).

Contraindications:

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

Carefully:Sideroblastic anemia, urolithiasis.

Pregnancy and lactation:

In pregnancy and during lactation apply only if the intended benefit to the mother exceeds the potential 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 the development of the "cancellation" syndrome is possible 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:

Intravenously, intramuscularly (slowly), adults between 100 and 500 mg(2-10 ml of a solution of 50 mg / ml or 1-5 ml of a solution of 100 mg / ml) per day, with scurvy treatment - up to 1000 mg per day.

Children from 100 to 300 mg (2-6 ml of a solution of 50 mg / ml or 1-3 ml of a solution of 100 mg / ml) per day, with scurvy therapy - up to 500 mg (10 ml of a solution of 50 mg / ml or 5 ml of 100 mg / ml) per day.

For the marking of erythrocytes (together with sodium chromate Cr51) - 100 mg of ascorbic acid is injected into a vial of sodium chromate Cr51.

Side effects:

Co side of the central nervous system: with rapid intravenous injection - dizziness, a feeling of fatigue, with prolonged use of large doses (more than 1 g) - headache,increased excitability of the central nervous system, insomnia.

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

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: allergic reactions up to the development of anaphylactic shock.

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

Local reactions: pain in the place of intramuscular injection.

Other: with prolonged use of large doses (more than 1 g) oppression of function insu(hyperglycemia, glucosuria), with intravenous administration - the threat of abortion (due to estrogenemia), hemolysis of erythrocytes.

Overdose:

Symptoms: nephrolithiasis, insomnia, irritability, hypoglycemia.

Treatment: symptomatic, forced diuresis.

Interaction:

Pharmaceutically incompatible with aminophylline, bleomycin, cefazolin, cefapyrin, chlordiazepoxide, estrogens, dextrans, doxapram, erythromycin, methicillin, nafcillin, benzylpenicillin, warfarin.

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).

Reduces the effectiveness of heparin and indirect anticoagulants.

With simultaneous application with acetylsalicylic acid, excretion with urine ascorbic acid and reduced excretion of acetylsalicylic acid.

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 at organism.

Quinoline drugs, calcium preparations, salicylates, glucocorticosteroids deplete the stores of ascorbic acid with prolonged use.

With simultaneous use reduces the chronotropic effect of isoprenaline. With prolonged use or use in high doses, 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:

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. High doses of ascorbic acid increase the excretion of oxalates, promoting the 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.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. 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).

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular injection 50 mg / ml and 100 mg / ml.

Packaging:

1 ml or 2 ml in ampoules.

By 5 ampoules in a contoured cell pack of a polyvinyl chloride film.

2 contour squares in a pack of cardboard.

For 10 ampoules in a box of cardboard with corrugated septa of paper, paper or bag.

Each instruction pack or box is supplied with instructions for use, an ampoule knife or a scarifier (when packing ampoules with a kink ring, notches and dots, the ampoule knife or scarifier does not insert).

Storage conditions:

In the dark place at a temperature of no higher than 15 ° C.

Keep out of the reach of children.

Shelf life:

1 year for a solution of 50 mg / ml;

1 year 6 months for a solution of 100 mg / ml.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-001815

Date of registration:13.07.2011

Expiration Date:Unlimited

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

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)