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

Pharmacological effects: in amounts 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 of some reactions hydroxylation and amidation - transfers electrons to enzymes, providing them with a replacement equivalent. Participates in the reactions of hydroxylation of proline and lysine residues of procollagen with formation of hydroxyproline and hydroxylizine (posttranslational modification collagen), the oxidation of the side chains of lysine in proteins with the formation of hydroxytrimethyllizine (during the synthesis of kartonite), the oxidation of folic acid to folinic acid, the metabolism of the drug in liver microsomes, and hydroxylation of dopamine with the formation of noradrenaline.

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

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.

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 of the 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 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).

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

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

Contraindications:Hypersensitivity to the components of the drug, with prolonged use in large doses (more than 500 mg) - diabetes mellitus, hyperoxaluria, nephrolithiasis, hemochromatosis, thalassemia, deficiency of glucose-6-phosphate hydrogenase.

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

Pregnancy and lactation:The use of the drug during pregnancy and lactation is possible only according to the prescription of the doctor in the event that the intended use for the mother exceeds the potential risk to the fetus or baby.

Dosing and Administration:

Intramuscularly, intravenously (slowly).

Adults from 100 to 500 mg (2 to 10 ml of 50 mg / ml solution) per day, with scurvy therapy - up to 1000 mg per day.

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

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

Side effects:

From the central nervous system: with rapid intravenous injection - headache, dizziness, a sense 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 application of 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 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 hyperestrogenemia), hemolysis of erythrocytes.

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 that of 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 (ASA) 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 the drug,(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.

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 content of glucose, bilirubin, activity of "liver" transaminases and lactate dehydrogenase (LDH).

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

The drug has no effect on driving vehicles, working with mechanisms and occupations requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

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

Packaging:

1, 2, 5 or 10 ml into neutral glass ampoules.

10 ampoules together with instructions for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard.

5 ampoules (for ampoules 1, 2 and 5 ml) into the contour cell packaging made of polyvinyl chloride film EP-73 and foil of aluminum printed lacquered or foil-free.

2 contoured cell packs together with instructions for use and a knife for opening of ampoules or scarifier ampullum in a pack of cardboard.

When using ampoules with notches, rings and dots, the ampoule opener or ampoule scaper is not inserted.

Storage conditions:

In the dark place at a temperature of 5 to 25 ° C.

Keep out of the reach of children.

Shelf life:

1 year 6 months.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000511

Date of registration:06.05.2010 / 01.09.2016

Expiration Date:Unlimited

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

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic acid)