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

Active substance:
ascorbic acid	- 50.0 mg	-100.0 mg
Excipients:
sodium hydrogen carbonate	-23.85 mg	-47.7 mg
Sodium sulfite anhydrous	-2.0 mg	-2.0 mg
water for injections	- up to 1.0 ml	- up to 1.0 ml

Description:Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Vitamin

ATX: & nbsp

A.11.G.A.01 Ascorbic acid

Pharmacodynamics:

Ascorbic acid (vitamin C) is not formed in the human body, but comes only with food.

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), the oxidation of the side chains of lysine in proteins with the formation of hydroxytrimethyllysine (during the synthesis of carnitine), the oxidation of folic acid to folinic, the metabolism of drugs 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 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.

With the appointment of high doses, the rate of excretion increases dramatically. 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 labeling erythrocytes (together with sodium chromate [51 Сr]).

Contraindications:

Hypersensitivity, with prolonged use in large doses (more than 500 mg) - diabetes mellitus, hyperoxaluria, nephrourolythiasis, hemochromatosis, thalassemia, deficiency of glucose-6-phosphate dehydrogenase.

Carefully:

When used in doses less than 500 mg - diabetes mellitus, deficiency of glucose-6-phosphate dehydrogenase, hemochromatosis, sideroblastic anemia, thalassemia, hyperoxaluria, nephrourolythiasis.

Pregnancy and lactation:

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

The minimum daily requirement for ascorbic acid in the II - III trimesters of pregnancy is about 60 mg. The minimum daily requirement for lactation is 80 mg.A mother's diet containing an adequate amount of ascorbic acid is sufficient to prevent the deficiency of vitamin C in an infant. During pregnancy, do not exceed 300 mg per day of ascorbic acid.

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 as a consequence, a newborn can develop the "withdrawal" syndrome.

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.

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

For the marking of erythrocytes (together with sodium chromate [51 Cr]) - 100 mg of ascorbic acid are injected into a vial of sodium chromate [51 Cr].

Side effects:

From 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 (using a dose of 600 mg / day) for prolonged use of large doses - hyperoxaluria, nefrourolitiaz (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 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.

Local reactions: pain 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: nephrourolythiasis, insomnia, irritability, hypoglycemia.

Treatment: symptomatic, forced diuresis.

Interaction:

Increases the concentration in the blood of benzylpenicillin and tetracyclines, at a dose of 1 g per day increases the bioavailability of ethinyl estradiol (also included in the oral contraceptives).

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

Reduces the effectiveness of heparin, 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 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.

The drugs of quinoline series, calcium chloride, salicylates, glucocorticosteroid preparations 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.

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 iron levels in the body, ascorbic acid should be used in minimal doses. High doses of ascorbic acid increase the excretion of oxalates, promoting the formation of kidney stones. Ascorbic acid, as a reducing agent, can distort the results of various laboratory tests (blood glucose, glucose, bilirubin, transaminase 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 requiring increased concentration and speed of psychomotor reactions, due to possible dizziness, fatigue and increased blood pressure.

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml and 100 mg / ml.

Packaging:

For 1 or 2 ml in ampoules of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch. Ampoules can additionally be applied one, two or three color rings and / or a two-dimensional bar code,and / or alphanumeric encoding or without additional color rings, a two-dimensional barcode, alphanumeric encoding.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film. Or 5 ampoules in a prefabricated form (tray) made of cardboard with cells for laying ampoules.

1 or 2 contour squares or cardboard tracks together with the instruction for use and a scarifier or knife with an ampoule, or without a scarifier and an ampoule knife are placed in a cardboard box (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002092

Date of registration:04.06.2013 / 07.08.2015

Expiration Date:04.06.2018

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp25.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)