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

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 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 hydroxytrimethyllizine (during the synthesis of kartonite), the oxidation of folic acid to folinic acid, the metabolism of drugs in liver microsomes, and the hydroxylation of 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 intercellular substance of teeth, bones and endothelium of 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). Clinical situations associated with the need for additional administration of ascorbic acid, incl. 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 [51Cr]).

Contraindications:

Hypersensitivity to the components of the drug. With prolonged use in large doses (more than 500 mg) - diabetes mellitus, hyperoxaluria, nefrourolithiasis, 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 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 for a child when the mother uses high doses of ascorbic acid (it is recommended not to exceed the daily need for ascorbic acid by the nursing 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 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 red blood cells (together with sodium chromate [51Cr]) - 100 mg of ascorbic acid are injected into a vial of sodium chromate [51 Cr].

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 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: pain in the site of the / m introduction.

Other: at long application of the big doses (more than 1 g) - oppression of function of an insulin device of a pancreas (hyperglycemia, glucosuria), with iv introduction in high doses - the threat of abortion (due to hyperestrogenemia), hemolysis 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 those included in oral contraceptives). Reduces the effectiveness of heparin and indirect anticoagulants.

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

Increases the risk of developing crystalluria in the treatment of salicylates and sulfonamides short acts, 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.

Drugs quinoline series, calcium preparations, salicylates, glucocorticosteroids with long-term use depletes the supply of ascorbic acid.

With simultaneous use reduces the chronotropic effect of isoprenaline.

With prolonged use or use in high doses, it may interfere with the interaction 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) derivatives of phenothiazine, 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 corticosteroids hormones it is necessary to monitor the function of the adrenal and 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 function of the insular apparatus pancreas, so in the process of 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 glucose, urine glucose, bilirubin, hepatic 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 a car and engaging in potentially dangerous activities that require concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml.

Packaging:

2 ml per ampoule of neutral glass. For 10 ampoules with instruction for use and a knife for opening ampoules or a scarifier ampullum is placed in a box of cardboard.

5 or 10 ampoules are placed in a contoured cell pack of a polyvinyl chloride film or a polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating, or without a foil, or without paper.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Storage conditions:In the dark place at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:P N002218 / 01

Date of registration:18.03.2008 / 02.10.2012

Expiration Date:Unlimited

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

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Ascorbic acid (Ascorbic asid)