Ascorbic acid

General characteristics. Structure:

Active ingredient: 50 mg of ascorbic acid in 1 ml of solution.

Excipients: Natrii hydrocarbonas, sodium sulfite anhydrous, water for injections.

Pharmacological properties:

Pharmacodynamics. The medicine having activity of vitamin C. Has metabolic effect, it is not formed in a human body, and arrives only with food. Participates in regulation of oxidation-reduction processes, carbohydrate metabolism, coagulability of blood, an angenesis; increases resistance of an organism to infections, reduces vascular permeability, reduces the need for B1, B2, A, E vitamins, folic acid, pantothenic acid. Participates in metabolism of phenylalanine, tyrosine, folic acid, Norepinephrinum, histamine, iron, utilization of karbogidrat, synthesis of lipids, proteins, a carnitine, immune responses, a serotonin hydroxylation, strengthens absorption of negeminovy iron. Regulates transport of ions of hydrogen in many biochemical reactions, improves use of glucose in a cycle of tricarboxylic acids, participates in formation of tetrahydrofolic acid and an angenesis, synthesis of steroid hormones, collagen, procollagen.

Maintains colloidal state of intercellular substance and normal permeability of capillaries (oppresses hyaluronidase). Activates proteolytic enzymes, participates in exchange of aromatic amino acids, pigments and cholesterol, promotes accumulation in a glycogen liver. Due to activation of respiratory enzymes in a liver strengthens its disintoxication and belkovoobrazovatelny functions, increases synthesis of a prothrombin. Improves bile secretion, recovers vneshnesekretorny function of a pancreas and incretory - thyroid. Regulates immunological reactions (activates synthesis of antibodies, C3 component of a complement, interferon), promotes phagocytosis, increases body resistance to infections. Slows down release and accelerates degradation of a histamine, formation of prostaglandins, etc. mediators of an inflammation and allergic reactions oppresses.

Pharmacokinetics. Communication with proteins of plasma – 25%. Concentration of ascorbic acid in plasma normal makes about 10-20 mkg/ml, stocks in an organism - about 1,5 g at reception of the daily recommended doses and 2,5 g at reception of 200 mg/days. Easily gets into leukocytes, thrombocytes, and then - into all fabrics; the greatest concentration is reached in ferruterous bodies, leukocytes, a liver and lens; it is deposited in a back share of a hypophysis, bark of adrenal glands, an eye epithelium, interstitial cells of seminal glands, ovaries, a liver, a spleen, a pancreas, lungs, kidneys, an intestines wall, heart, muscles, a thyroid gland; gets through a placenta. Concentration of ascorbic acid in leukocytes and thrombocytes is higher, than in erythrocytes and in plasma. At scarce states concentration in leukocytes decreases later and more slowly and is considered as the best criterion for evaluation of deficit, than concentration in plasma.

It is metabolized preferential in a liver in dezoksiaskorbinovy and further in oxalacetic and diketogulonic acids. It is removed by kidneys, with then, breast milk in the form of not changed ascorbate and metabolites. At purpose of high doses removal speed sharply amplifies. Smoking and the use of ethanol accelerate destruction of ascorbic acid (transformation into inactive metabolites), sharply reducing stocks in an organism. It is removed at a hemodialysis.

Indications to use:

Treatment hypo - and avitaminosis of C (in need of bystry completion of vitamin C and impossibility of oral administration).

The clinical situations connected with need of additional administration of ascorbic acid including parenteral food, digestive tract diseases (persistent diarrhea, resection of a small intestine, round ulcer, gastrectomy), Addison's disease.

Route of administration and doses:

Solution of a plant louse of injections is entered intravenously or intramusculary with the medical purpose on 0,05 - 0,15 (1 - 3 ml of 5% of solution), at poisonings - to 2 g (40 ml); the maximum single dose - 0,20 g (4 ml), daily - 1 g (20 ml); to children – 0,05 - 0,10 g/days (1 - 2 ml).

Terms of treatment depend on character and the course of a disease.

Features of use:

In connection with a promoting effect of ascorbic acid on synthesis of corticosteroid hormones it is necessary to monitor function of kidneys and arterial pressure.

At prolonged use of high doses oppression of function of the insulyarny device of a pancreas therefore in the course of its treatment it is regularly necessary to control is possible.

At patients with the increased content of iron in an organism it is necessary to apply ascorbic acid in the minimum doses.

Purpose of ascorbic acid to patients with quickly proliferating and intensively metastasizing tumors can aggravate the course of process. Ascorbic acid as a reducer can distort results of various laboratory tests (content in blood of glucose, bilirubin, activity of "hepatic" transaminases and a lactate dehydrogenase).

Use at pregnancy and in the period of a lactation. At pregnancy and in the period of a lactation apply only if the estimated advantage for mother exceeds potential risk for a fruit and the child. Theoretically there is a danger to the child at use by mother of high doses of ascorbic acid (it is recommended not to exceed the nursing mother of a maximum of daily need for ascorbic acid).

The minimum daily need for ascorbic acid for the II-III trimesters of pregnancy – about 60 mg. It must be kept in mind that the fruit can adapt to high doses of ascorbic acid which is accepted by the pregnant woman, and then at the newborn development of a syndrome of "cancellation" is possible.

The minimum daily requirement in the period of a lactation − 80 mg. Mother's diet containing adequate amount of ascorbic acid sufficient for prevention of deficit at the baby.

Influence on ability to drive the car and work with moving mechanisms: does not influence.

Side effects:

From the central nervous system: at bystry in introduction - dizziness, feeling of fatigue, at prolonged use of high doses (more than 1 g) - a headache, increase in excitability of TsNS, sleeplessness.

From an urinary system: a moderate pollakiuria (at use of a dose more than 600 mg/days), at prolonged use of high doses - a hyperoxaluria, a nephrolithiasis (from oxalate calcium), damage of the glomerular device of kidneys.

From cardiovascular system: at prolonged use of high doses - decrease in permeability of capillaries (deterioration in a trophicity of fabrics, increase in arterial pressure, hypercoagulation, development of mikroangiopatiya is possible).

Allergic reactions: skin rash, dermahemia.

Laboratory indicators: thrombocytosis, giperprotrombinemiya, erythropenia, neutrophylic leukocytosis, hypopotassemia, glucosuria.

Local reactions: morbidity in the place in oil of introduction.

Others: at prolonged use of high doses (more than 1 g) - oppression of function of the insulyarny device of a pancreas (a hyperglycemia, a glucosuria), at in introduction in high doses - threat of abortion (owing to a hyperestrogenemia), hemolysis of erythrocytes.

Interaction with other medicines:

Increases concentration in blood of benzylpenicillin and tetracyclines; in a dose of 1 g/days increases bioavailability of ethinylestradiol (including being a part of oral contraceptives).

Reduces efficiency of heparin and indirect anticoagulants.

Increases risk of development of a crystalluria at treatment by salicylates and streptocides of short action, slows down removal by kidneys of acids, increases removal of the medicines having alkali reaction (including alkaloids), reduces concentration in blood of oral contraceptives.

Increases the general clearance of ethanol which in turn reduces concentration of ascorbic acid in an organism.

Medicines of a quinolinic row, Calcii chloridum, salicylates, glucocorticosteroids at prolonged use exhaust reserves of ascorbic acid.

At simultaneous use reduces chronotropic action of an izoprenalin.

At prolonged use or use in high doses can interfere with interaction of Disulfiramum and ethanol.

In high doses increases removal of a meksiletin kidneys.

Barbiturates and Primidonum increase removal of ascorbic acid with urine.

Reduces therapeutic effect of antipsychotic medicines (neuroleptics) − derivatives of a fenotiazin, a canalicular reasorbtion of amphetamine and tricyclic antidepressants.

Pharmaceutical it is incompatible with Aminophyllinum, bleomycin, cefazolin, tsefapiriny, chlordiazepoxide, estrogen, dextrans, doksapramy, erythromycin, Methicillinum, naftsilliny, benzylpenicillin, warfarin.

Contraindications:

Hypersensitivity to drug components. Introduction of high doses − hypercoagulation, thrombophlebitis, tendency to fibrinferments, diabetes mellitus, nephrolithiasis, deficit glyukozo-6-fosfatdegidrogenazy.

With care. Hyperoxaluria, renal failure, hemochromatosis, thalassemia, polycythemia, leukemia, sideroblastny anemia, sickemia, malignant new growths.

Overdose:

Symptoms of overdose arise at administration of ascorbic acid in high doses or during a long span. Development of arterial hypertension, a hyperglycemia, glucosuria, tromboembolic episodes, a nephrolithiasis is characteristic.

Measures of the help include drug withdrawal and symptomatic therapy. There is no specific antidote.

Storage conditions:

In the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 1 year. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 1 or 2 ml in packaging No. 10, No. 10 x 1.