Ascorbic acid (vitamin C)

General characteristics. Structure:

Active agent - ascorbic acid 100, 0 of mg.

Excipients: Natrii hydrocarbonas of 47,7 mg, sodium of sulfite anhydrous 4,0 mg, water for injections to 2,0 ml.

Pharmacological properties:

Pharmacokinetics. It is soaked up in digestive tract (preferential in a jejunum). Communication with proteins of a blood plasma - 25%.

Concentration of ascorbic acid in a blood plasma normal makes about 10-20 mkg/ml, stocks in an organism - about 1.5 g at reception of the daily recommended doses. Time of achievement of the maximum concentration in a blood plasma (TCmax) after intake - 4 h.

Ascorbic acid is widely distributed in body tissues. 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 a blood plasma.

It is metabolized preferential in a liver in dezoksiaskorbinovy and further in oxalacetic and diketogulonic acids.

It is removed by kidneys, through intestines, with then, breast milk in the form of not changed ascorbate and metabolites.

At purpose of high doses removal speed sharply amplifies and ascorbic acid is quickly removed in not changed view with urine.

Pharmacodynamics. Ascorbic acid participates in regulation of oxidation-reduction processes, carbohydrate metabolism, coagulability of blood, an angenesis, in synthesis of steroid hormones; increases resistance of an organism to infections, reduces vascular permeability, reduces the need for B1, B2, A, E vitamins, folic acid, pantothenic acid. Has the expressed antioxidant properties. Regulates hydrogen transport 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 detoksikatsionny and belkovoobrazovatelny functions, increases synthesis of a prothrombin. Improves bile secretion, recovers secretory function of pancreatic and thyroid glands. 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 and other mediators of an inflammation oppresses.

Indications to use:

- prevention and treatment hypo - and avitaminosis With;

- hemorrhagic diathesis;

- uterine, nasal, pulmonary bleedings;

- liver diseases;

- inertly healing wounds and fractures of bones;

- period of pregnancy and feeding by a breast;

- physical and intellectual overworks, overfatigue, stressful states;

- growth period;

- the reconvalescence period after a long serious illness;

- infectious diseases;

- intoxications.

Route of administration and doses:

Acid solution ascorbic is appointed intravenously or intramusculary. The adult on 1-3 ml a day, at poisonings enter up to 60 ml/days.

To children on 1-2 ml a day.

Duration of treatment depends on character and the course of a disease.

Features of use:

At prolonged use of high doses of ascorbic acid oppression of function of the insulyarny device of a pancreas therefore in the course of treatment it is necessary to control functional capacity of the last regularly is possible. At use in high doses the hyperoxaluria and formation of nephroliths from calcium oxalate are possible. In connection with the stimulating influence of ascorbic acid on formation of corticosteroid hormones at treatment by high doses it is necessary to monitor function of kidneys and arterial pressure. As ascorbic acid increases iron absorption, its use in high doses can be dangerous at patients with hemochromatosis, a thalassemia, leukemia and sideroblastny anemia. Purpose of ascorbic acid to patients with quickly proliferating and intensively metastasizing tumors can aggravate the course of process.

Reception of high doses of ascorbic acid can affect results of some laboratory researches: wrong positive test for availability of sugar in urine and the negative test for existence of the occult blood in Calais, and also understating of results at a research of concentration of a lactate dehydrogenase and aminotransferase in blood serum.

The minimum daily need for ascorbic acid for the II-III trimesters of pregnancy makes about 60 mg. Ascorbic acid gets through a placental barrier. It must be kept in mind that the fruit can adapt to high doses of the ascorbic acid accepted by the pregnant woman with the subsequent development in a newborn withdrawal. Therefore at pregnancy it is not necessary to accept ascorbic acid in the raised doses. The minimum daily requirement during breastfeeding – 80 mg. Ascorbic acid is emitted with breast milk therefore it is recommended not to exceed the nursing mother a maximum of daily need for ascorbic acid.

At reception of vitamin C in high doses more than 1 g a day abortion because of the raised estrogen synthesis is possible.

Side effects:

- headache, feeling of fatigue, sleep disorder;

- hypervitaminosis, disbolism.

Are possible:

- stomach spasms, nausea and vomiting;

- feeling of heat;

- a delay of sodium and liquid, disturbance of exchange of zinc and copper at prolonged use of high doses.

Seldom:

- skin reactions;

- acute anaphylaxis.

Interaction with other medicines:

Oral contraceptives, fresh fruit, vegetable juice and alkaline drink reduce utilization of vitamin C in digestive tract. Ascorbic acid increases concentration in blood of salicylates (the risk of a crystalluria increases), benzylpenicillin, tetracycline and reduces – peroral anticoagulants; reduces anticoagulating effect of derivatives of coumarin; improves absorption in intestines of iron preparations; increases alcohol removal. Calcii chloridum, salicylates and glucocorticosteroids at prolonged use exhaust reserves of ascorbic acid in an organism.

At simultaneous use reduces chronotropic action of an izoprenalin. In high doses raises renal excretion of a meksiletin. Barbiturates and Primidonum increase removal of ascorbic acid with urine. Reduces therapeutic action of neuroleptics (derivatives of a fenotiazin), a canalicular reabsorption of amphetamine and tricyclic antidepressants.

Ascorbic acid cannot be entered in one syringe or in the infusional environment together with Riboflavinum mononucleotide (B2 vitamin), cyanocobalamin (B12 vitamin) and analginum as they enter with it chemical interaction.

Contraindications:

- hypersensitivity to ascorbic acid;

- thrombophlebitis, tendency to fibrinferments;

- diabetes mellitus;

- urolithiasis;

- deficit glyukozo-6-fosfatdegidrogenazy.

Overdose:

Symptoms: at reception more than 1 g a day heartburn, diarrhea, the complicated urination or coloring of urine in red color, hemolysis are possible (at patients with deficit glyukoz-6-fosfatdegidrogenaza).

Treatment: reduction of a dose or drug withdrawal, symptomatic treatment.

Storage conditions:

To store in the dry, protected from light place, at a temperature not over 25 ºС. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

5% solution for injections on 2 ml in ampoules, a cardboard box on 10 pieces, in a blister strip packaging on 5 and 10 pieces with the application instruction.