Ascorbic acid

Registration number: ЛП-004207

Trade name of the drug: Ascorbic acid

International non-parietary name: Ascorbic acid

Dosage form: powder for preparation of oral solution

Composition for 1 package:

Ascorbic acid - 2.5 g.

Description: Crystalline powder from white to slightly yellowish color, almost odorless.

Pharmacotherapeutic group: vitamin.

ATC code: A11GA01.

Pharmacological properties

Pharmacodynamics

Ascorbic acid (vitamin C) is not formed in the human body, but comes only with food. It is a cofactor of some hydroxylation and amidation reactions - electrons are transferred to enzymes, supplying them with a reducing equivalent. Participates in hydroxylation reactions of proline and lysine procollagen residues with the formation of hydroxyproline and hydroxylysine (post-translational modification of collagen), oxidation of lysine side chains in proteins with the formation of hydroxymethyllysine (in the synthesis of picturete), oxidation of folic acid to folic acid, metabolism of drugs in liver microsomes and hydroxylation of dopamine with the formation of norepinephrine. Increases the activity of amidating enzymes involved in the processing of oxytocin, antidiuretic hormone and cholystokinin. Participates in steroidogenesis in the adrenal glands. Restores trivalent iron ions to divalent iron ions in the intestine, contributing to its absorption. The main role in tissues is participation in the synthesis of collagen, proteoglycans and other organic components of the intercellular substance of teeth, bones and endothelium of capillaries. In low doses (150-250 mg/day orally) improves the complex-forming function of deferoxamine in chronic intoxication with iron preparations, which leads to increased excretion of the latter.

Pharmacokinetics

Absorbed in the gastrointestinal tract (mainly in the small intestine). With an increase in the dose to 200 mg, it is absorbed to 140 mg (70%); with a further increase in the dose, absorption decreases (50-20%). Communication with plasma proteins - 25%.
Diseases of the gastrointestinal tract (gastric and duodenal ulcer, constipation or diarrhea, worm invasion, giardiasis), consumption of fresh fruit and vegetable juices, alkaline drinking reduce the absorption of ascorbic acid in the intestine. The concentration of ascorbic acid in the plasma is normally approximately 10-20 μg/ml, the reserves in the body are about 1.5 g when taking the daily recommended doses and 2.5 g when taking 200 mg/day. The time to reach the maximum concentration (TSM) after ingestion is 4 hours.
Easily penetrates leukocytes, platelets, and then all tissues; the highest concentration is achieved in the glandular organs, leukocytes, liver and lens of the eye; penetrates through the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and plasma. In deficit states, the concentration in leukocytes decreases later and more slowly and is considered as a better criterion for assessing the deficit than the concentration in plasma.

It is metabolized mainly in the liver into deoxyascorbic acid and then into oxalic-acetic 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.

When high doses are prescribed, the rate of removal increases dramatically. Smoking and ethanol use accelerate the destruction of ascorbic acid (turning into inactive metabolites), dramatically reducing the body's reserves.

It is excreted in hemodialysis.

Indications for use

Contraindications

Hypersensitivity. With long-term use in large doses (more than 500 mg) - diabetes mellitus, hypercoagulation, nephrourolithiasis, thrombophlebitis, tendency to thrombosis, glucose-6-phosphate dehydrogenase deficiency, hemochromatosis, thalassemia.

With caution

Hyperoxalaturia, renal failure, polycythemia, leukemia, sideroblast anemia, sickle cell anemia, progressive malignant diseases, oxalosis, kidney stone disease.

Use during pregnancy and breastfeeding

During pregnancy and breastfeeding, the recommended doses of ascorbic acid should not be exceeded.
Pregnancy
The minimum daily requirement for ascorbic acid in the II-III trimesters of pregnancy is about 60 mg. It should be borne in mind that the fetus can adapt to high doses of ascorbic acid taken by a pregnant woman, and then the newborn may develop "cancellation" syndrome. During pregnancy, the dose of ascorbic acid should not exceed 300 mg per day.

The period of breastfeeding

Ascorbic acid is excreted with breast milk. The minimum daily requirement during breastfeeding is 80 mg. The mother's diet, which contains an adequate amount of ascorbic acid, is sufficient to prevent vitamin C deficiency in a child.

Method of application and doses

Inside, after a meal. The powder is used to make drinks: the contents of one bag are dissolved in 2500 ml of water. The solution is used freshly prepared, in accordance with the dosages proposed below. For dosing, it is recommended to use a measuring cup*.

Treatment

Adults 50-100 mg (50-100 ml) 3-5 times a day.
Children from 5 years old 50-100 mg (50-100 ml of solution) 2-3 times a day.
During pregnancy and breastfeeding, 300 mg (300 ml) per day for 10-15 days; then - 100 mg (100 ml) per day.

Prevention

Adults 50-100 mg (50-100 ml of solution) per day.
Children from 3 to 6 years old 25 mg (25 ml of solution) per day, from 6 to 14 years old - 50 mg (50 ml of solution) per day, from 14 to 18 years old - 75 mg (75 ml of solution) per day.
The duration of treatment depends on the nature and course of the disease.
For adults: the maximum single dose is 200 mg, the daily dose is 1000 mg; for children the maximum single dose is 100 mg, the daily dose is 500 mg
* measuring cup is not included in the set.

Side effect

From the central nervous system (CNS): headache, feeling of fatigue, with long-term use of large doses (more than 1000 mg) - increased excitability of the CNS, insomnia.
From the urinary system: moderate pollakiuria (when taking a dose of more than 600 mg/day), with long-term use of large doses - hyperoxaluria, formation of urinary stones from calcium oxalate, damage to the glomerular apparatus of the kidneys.
From the digestive system: irritation of the mucous membrane of the gastrointestinal tract, with prolonged use of large doses - nausea, vomiting, diarrhea, hyperacid gastritis, ulceration of the mucous membrane of the gastrointestinal tract.
From the endocrine system: suppression of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria).
From the cardiovascular system: thrombosis, with long-term use of large doses - reduced capillary permeability (possible deterioration of tissue trophy, increased blood pressure, hypercoagulation, development of microangiopathies).
Allergic reactions: skin rash, skin hyperemia.
Laboratory indicators: thrombocytosis, hyperprothrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia.

Overdose

Symptoms: diarrhea, nausea, irritation of the gastrointestinal mucosa, flatulence, abdominal pain of a spastic nature, urination, nephrolithiasis, insomnia, irritability, hypoglycemia.
Treatment: symptomatic, forced diuresis.

Interaction with other drugs

Absorption of ascorbic acid is reduced with the simultaneous use of oral contraceptives, acetylsalicylic acid, the use of fresh fruit and vegetable juices, alkaline drinks.
Ascorbic acid when taken orally increases the absorption of penicillin, iron, reduces the effectiveness of heparin and indirect anticoagulants, increases the risk of crystalluria in the treatment of salicylates.
When used simultaneously, it reduces the chronotropic effect of isoprenaline. With prolonged use or use in large doses, it may disrupt the interaction of disulfiram and ethanol.
Barbiturates and primidon increase the excretion of ascorbic acid in the urine.