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

The pharmacological effects of ascorbic acid are few. In amounts significantly exceeding the daily requirement (60 mg), almost no effect, except for the rapid elimination of scurvy symptoms.

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, there may be "ricochet" 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 (poststranslational 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,metabolism of drugs in liver microsomes and hydroxylation of 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. The main role at the tissue level 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 the form of unchanged ascorbate and 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).

Applied for medical purposes in all clinical situations associated with the need for additional administration of ascorbic acid, including: parenteral nutrition, diseases of the gastrointestinal tract (persistent diarrhea, resection of the small intestine, peptic ulcer, gastrectomy), Addison's disease.

In laboratory practice: for marking red blood cells (together with sodium chromate Cr51).

Contraindications:

Hypersensitivity, with prolonged use in large doses (more than 500 mg) - diabetes mellitus, 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 potential risk to the fetus and the baby.

The minimum daily requirement for ascorbic acid in the II-III trimesters of pregnancy is 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:

Intramuscularly, intravenously (slowly), adults from 100 to 500 mg (2-10 ml of 5% solution) per day, with scurvy therapy - up to 1000 mg per day.

Children from 100 to 300 mg (2-6 ml of 5% solution) per day, with scurvy therapy - up to 500 mg (10 ml of 5% solution) 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:

From the side of the central nervous system: with rapid intravenous injection - dizziness, 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 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.

Local Reactions: soreness in the place of intramuscular injection.

Other: with prolonged use of large doses (more than 1 g) - suppression of the function of the insulin pancreas apparatus (hyperglycemia, glucosuria), with intravenous administration - the threat of abortion (due to estrogenemia), hemolysis of red blood cells.

Overdose:

Symptoms: 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 oral contraceptives).

Reduces the effectiveness of heparin and indirect anticoagulants.

With simultaneous use with acetylsalicylic acid, urinary excretion of ascorbic acid increases and the excretion of acetylsalicylic acid decreases.

Increases the risk of developing crystalluria in the treatment of salicylates and sulfonamides short-acting, slows the excretion of acid by the kidneys, increases the excretion of drugs that have an alkaline reaction (incl.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) - phenothiazine derivatives, tubular reabsorption of amphetamine and tricyclic antidepressants.

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

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.

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 levels Fe in the body should use ascorbic acid in minimal doses.

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

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml.

Packaging:

1 ml, 2 ml and 5 ml in neutral glass ampoules

For 10 ampoules of neutral glass with a knife ampoule or scarifier and instructions for use in a pack

When packing ampoules with notches, rings and dots for kink, the ampoules or scarifiers do not put the knives.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

1 year.The drug should be used before the date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002095/10

Date of registration:16.03.2010

Expiration Date:Unlimited

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Ascorbic acid bufus (Ascorbic acid bufus)