ASCORBIC ACID

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ASCORBIC ACID

Composition:

Active substance: ascorbic acid;

1 tablet contains ascorbic acid (vitamin C), recalculated to 100% substance
25 mg;

Excipients: white sugar, potato starch, povidone 25, hypromellose, magnesium stearate, powdered flavor "Orange", curcumin coloring agent (E 100).

Pharmaceutical form. 25 mg tablets.

Main physicochemical properties: single-layer, round-shaped tablets, light yellow in color, with a score line; upper and lower surfaces are flat, edges are beveled. Specks of yellow and white colors may be present on the tablet surface. Under magnification, the cross-section reveals a relatively homogeneous structure.

Pharmacotherapeutic group. Simple ascorbic acid (vitamin C) preparations.

Ascorbic acid (vitamin C). ATC code A11G A01.

Pharmacological Properties.

Pharmacodynamics.

Ascorbic acid (vitamin C) has pronounced reducing properties. It belongs to the group of water-soluble vitamins. It participates in redox reactions, regulation of carbohydrate metabolism, influences the metabolism of aromatic amino acids, thyroxine metabolism, biosynthesis of catecholamines, steroid hormones and insulin, and is essential for blood coagulation, synthesis of collagen and procollagen, and regeneration of connective and bone tissue. It improves capillary permeability. It promotes iron absorption in the intestine and participates in hemoglobin synthesis. It enhances non-specific resistance of the body and has antidotal properties. Vitamin C deficiency in the diet leads to the development of hypovitaminosis and avitaminosis C, as this vitamin is not synthesized in the body.

Pharmacokinetics.

Absorption of ascorbic acid occurs mainly in the small intestine. The absorption process may be impaired in intestinal dyskinesias, enteritis, achylia, helminthic infestations, giardiasis, as well as when consuming alkaline beverages, fresh fruits, and vegetable juices. Maximum plasma concentration of the drug after oral administration is reached within 4 hours. It readily penetrates into leukocytes and platelets, and then into all tissues; it accumulates in the posterior lobe of the pituitary gland, adrenal cortex, ocular epithelium, interstitial cells of the testes, ovaries, liver, brain, spleen, pancreas, lungs, kidneys, intestinal wall, heart, muscles, and thyroid gland. It is metabolized predominantly in the liver into dehydroascorbic acid, and further into oxalic acid and diketogulonic acid. Unchanged ascorbate and metabolites are excreted in urine and feces; they also pass into breast milk. When high doses are administered, and plasma concentration exceeds 1.4 mg/dL, excretion is markedly enhanced, and increased excretion may persist after discontinuation of the drug.

Clinical characteristics.

Indications.

Prevention and treatment of vitamin C deficiency.

Meeting increased body requirements for vitamin C during periods of growth, pregnancy or breastfeeding, during increased physical and mental stress, in infectious diseases and intoxications, hemorrhagic diatheses, as part of combined therapy for bleeding (nasal, pulmonary, uterine), in radiation sickness, Addison's disease, anticoagulant overdose, muscle tissue injuries, and slowly healing infected wounds, as well as in bone fractures.

Contraindications.

Hypersensitivity to ascorbic acid or to any of the excipients of the medicinal product. Thrombosis, predisposition to thrombosis, thrombophlebitis, diabetes mellitus, severe kidney diseases. Urolithiasis – when doses exceeding 1 g per day are used.

Fructose intolerance, glucose-galactose malabsorption syndrome.

Interaction with other medicinal products and other forms of interaction.

Oral administration of ascorbic acid enhances the absorption of penicillin, tetracycline, and iron; promotes intestinal absorption of aluminium, which should be considered during concomitant treatment with aluminium-containing antacids.

Concomitant use of vitamin C and deferoxamine increases tissue toxicity of iron, especially in the myocardium, potentially leading to circulatory decompensation. Vitamin C may be administered only 2 hours after deferoxamine injection.

Prolonged use of high doses by patients undergoing disulfiram treatment inhibits the disulfiram-alcohol reaction.

High doses of the medicinal product reduce the effectiveness of tricyclic antidepressants, phenothiazine derivative neuroleptics, tubular reabsorption of amphetamine, impair renal elimination of mexiletine, and affect vitamin B12 resorption.

Ascorbic acid increases the total clearance of ethanol.

When high doses of ascorbic acid are used concomitantly with alcohol consumption, disulfiram-like reactions may develop.

The medicinal product reduces the toxicity of sulfonamide drugs, decreases the effectiveness of heparin and indirect anticoagulants.

Vitamin C enhances oxalate excretion in urine, thereby increasing the risk of urinary oxalate stone formation, and increases the risk of crystalluria during treatment with salicylates.

Medicinal products of the quinolone series, calcium chloride, salicylates, and corticosteroids, when used long-term, reduce ascorbic acid reserves in the body.

Absorption of ascorbic acid is reduced when used concomitantly with oral contraceptives, consumption of fruit or vegetable juices, or alkaline drinks.

Acetylsalicylic acid (aspirin) may reduce the absorption of ascorbic acid.

Special precautions for use

When using high doses or prolonged administration of the drug, it is necessary to monitor kidney function, arterial blood pressure, and pancreatic function. The drug should be administered with caution to patients with a history of kidney disease.

In patients with urolithiasis, the daily dose of ascorbic acid should not exceed 1 g.

High doses of the drug should not be prescribed to patients with increased blood coagulation.

Since ascorbic acid enhances iron absorption, its use in high doses may be dangerous for patients with hemochromatosis, thalassemia, polycythemia, leukemia, or sideroblastic anemia. Patients with high iron levels in the body should receive the drug in minimal doses.

Concurrent use of the drug with alkaline drinks reduces absorption of ascorbic acid; therefore, it should not be taken with alkaline mineral water. Absorption of ascorbic acid may also be impaired in intestinal dyskinesia, enteritis, and achylia.

Use with caution in the treatment of patients with glucose-6-phosphate dehydrogenase deficiency.

As a reducing agent, ascorbic acid may interfere with laboratory test results, for example, when measuring blood glucose, bilirubin, transaminase activity, and lactate dehydrogenase activity.

Since ascorbic acid has a mild stimulating effect, it is not recommended to take the drug late in the day. Due to the stimulatory effect of ascorbic acid on corticosteroid hormone production, when using the drug in high doses, kidney function and arterial blood pressure should be monitored.

Ascorbic acid should be used with caution in patients with progressive malignant disease, as its use may complicate the course of the disease.

The drug may be harmful to teeth.

Use during pregnancy or breastfeeding

The drug may be used during pregnancy or breastfeeding according to dosage recommendations and as prescribed by a physician. Recommended doses should be strictly followed and not exceeded.

Ability to affect reaction rate when driving or operating machinery

No effect at therapeutic doses.

Dosage and Administration.

Take the medicinal product orally after meals.

For prophylactic purposes, adults and children aged 14 years and older should take 2–4 tablets (50–100 mg) per day; children aged 3 to 14 years should take 2 tablets (50 mg) per day.

Treatment doses: for adults and adolescents aged 14 years and older – 2–4 tablets (50–100 mg) 3–5 times daily; for children aged 3 to 7 years – 2–4 tablets (50–100 mg) 2–3 times daily; for children aged 7 to 10 years – 4 tablets (100 mg) 2–3 times daily; for children aged 10 to 14 years – 4–6 tablets (100–150 mg) 2–3 times daily.

Pregnant women, postpartum women, and women with low levels of vitamin C in breast milk should take 12 tablets (300 mg) daily for 10–15 days, followed by 4 tablets (100 mg) daily for prophylaxis throughout the entire breastfeeding period.

The duration of treatment depends on the nature and course of the disease and is determined individually by the physician.

Children.

The medicinal product is indicated for children aged 3 years and older.

Overdose.

Ascorbic acid is well tolerated. It is a water-soluble vitamin, and any excess amount is excreted in urine.

Symptoms. Prolonged use of high doses of vitamin C may lead to suppression of the insular apparatus function of the pancreas, requiring monitoring of pancreatic status.

Overdose may cause changes in renal excretion of ascorbic acid and uric acid during urine acidification, increasing the risk of precipitation of oxalate calculi.

Administration of high doses of the drug may result in vomiting, nausea, or diarrhea, which resolve after discontinuation of the drug.

Treatment. Symptomatic therapy.

Side effects.

Gastrointestinal disorders: when administered at doses exceeding 1 g per day – irritation of the gastrointestinal mucosa, heartburn, nausea, vomiting, diarrhea.

Renal and urinary system disorders: damage to the glomerular apparatus of kidneys, crystalluria, formation of urate, cystine and/or oxalate concretions in kidneys and urinary tract, renal failure.

Immune system disorders: Quincke's edema, occasionally anaphylactic shock in the presence of sensitization.

Skin and subcutaneous tissue disorders: skin rashes, pruritus, urticaria, eczema.

Endocrine system disorders: damage to the islet apparatus of the pancreas (hyperglycemia, glucosuria) and impaired glycogen synthesis up to the development of diabetes mellitus.

Cardiovascular system disorders: arterial hypertension, myocardial dystrophy.

Blood and lymphatic system disorders: thrombocytosis, hyperprothrombinemia, thrombosis, erythrocytopenia, neutrophilic leukocytosis; in patients with glucose-6-phosphate dehydrogenase deficiency may cause hemolysis of erythrocytes, hemolytic anemia (in patients with glucose-6-phosphate dehydrogenase deficiency).

Nervous system disorders: increased excitability, sleep disturbances, headache, sensation of heat, increased fatigue.

Metabolic and nutritional disorders: disturbances in zinc and copper metabolism.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25°C.

Keep out of reach of children.

Packaging.

50 or 100 tablets in a container; 1 container per cardboard box.

Prescription status.

Over-the-counter.

Manufacturer.

JSC "Tekhnolohiya".

Manufacturer's address and location of business activity.

8 Stara Prorynna Street, Uman, Cherkasy region, 20300, Ukraine.