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

Ascorbic acid (vitamin C) is not synthesized in the human body, but comes only with food. The intake of doses significantly exceeding the daily requirement (90 mg), by persons without pronounced hypovitaminosis (scurvy) does not lead to an increase in the therapeutic effect.

Participates in the regulation of oxidation-reduction processes, carbohydrate metabolism, blood coagulation, tissue regeneration. Increases the body's resistance to infections, reduces vascular permeability, reduces the need for vitamins B1, B2, A, E, folic and pantothenic acids.

It promotes the reactions of hydroxylation of proline and lysine procolagene residues 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 the synthesis of kartonite), the oxidation of folic acid to folinic acid. Promotes the acceleration of the metabolism of drugs in liver microsomes and the 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, in the synthesis of collagen, proteoglycans and other organic components of the intercellular substance of the teeth, bones and endothelium of the capillaries.

It improves bile secretion, restores the exocrine function of the pancreas and the endocrine function of the pancreas.

It inhibits the release and accelerates the degradation of histamine, inhibits the formation of prostaglandins and other mediators of inflammation and allergic reactions.

Pharmacokinetics:

Connection with plasma proteins - 25%. Normally, the concentration of ascorbic acid in the plasma is approximately 10-20 μg / ml. Easily penetrates into leukocytes, platelets, the greatest concentration is achieved in glandular organs, leukocytes, liver and lens of the eye; deposited in the posterior lobe of the pituitary gland, adrenal cortex, ocular epithelium, interstitial cells of the seminal glands, ovaries, liver, spleen, pancreas, lungs, kidneys, intestinal wall, heart, muscles, thyroid gland; penetrates the placenta.The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and in plasma. With hypovitaminosis, 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 diketogulonovoy acid.

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).

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

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

Contraindications:

Hypersensitivity. With prolonged use in large doses (more than 500 mg) - diabetes mellitus, hyperoxaluria, renal stone disease, 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 III trimester of pregnancy is about 60 mg. It should be borne in mind that the fetus can adapt to high doses of ascorbic acid, which takes a pregnant woman, and then a newborn can develop the syndrome of "cancellation."

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 during breast-feeding (it is not recommended to administer a feeding mother of vitamin C at a dose exceeding her daily requirement).

Dosing and Administration:

Therapeutic doses for adults - from 100 to 500 mg per day (2-10 ml of 5% solution).

In the treatment of scurvy - up to 1000 mg per day (up to 10 ml of a 5% solution).

Therapeutic doses for children - from 100 to 300 mg (2-6 ml of 5% solution) per day.

In the treatment of scurvy - up to 500 mg per day (10 ml of 5% solution) per day.

The duration of treatment depends on the nature and course of the disease.

For the marking of red blood cells (together with sodium chromate CrS) - 100 mg of ascorbic acid is injected into a bottle of sodium chromate Cr51.

Side effects:

From the central nervous system (CNS): 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 a worsening of tissue trophism, an increase in blood pressure, hypercoagulation, the 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 erythrocytes.

Overdose:

FROMImplications: nephrolithiasis, insomnia, irritability, hypoglycemia.

Treatment is symptomatic, effective diuresis is effective.

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 (ASA), urinary excretion of ascorbic acid increases and the excretion of ASA decreases.

Increases the risk of developing crystalluria with the simultaneous administration 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.

Preparations 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 application in high doses, it can eliminate the effect of disulfiram on the metabolism of 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, dextrins, doxapram, erythromycin, methicillin, nafcillin, benzylpenicillin, warfarin.

Special instructions:

In connection with the stimulating effect of ascorbic acid on the synthesis of glucocorticosteroid hormones, it is necessary to monitor the function of the adrenal glands and the level of blood 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 insular pancreas function may be possible, therefore, during the treatment it is necessary to regularly monitor the level of glycemia.

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 (determination of blood and urine glucose, bilirubin, activity of "hepatic" transaminases and lactate dehydrogenase).

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

The drug does not affect the ability to drive vehicles, work with mechanisms and exercises that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection, 50 mg / ml.

Packaging:

1, 2, 5 ml into ampoules.

For 10 ampoules of 1, 2, 5 ml, together with a knife for opening ampoules and instructions for use, put in a box of cardboard. For 10 ampoules of 1, 2 ml or 5 ampoules of 5 ml in a blister pack. For 1 blister pack of 10 ampoules or 2 blister packs of 5 ampoules together with a knife for opening ampoules and instructions for use in the pack.

10 ampoules together with a knife for opening ampoules and instructions for medical use in a pack with a cardboard insert for fixing ampoules.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

In a place inaccessible to children.

Shelf life:1 year. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015991 / 01

Date of registration:18.09.2009 / 28.07.2015

Expiration Date:Unlimited

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)