Vitamin c
Ukraine
Table of Contents
INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT VITAMIN C
Composition:
Active substances: ascorbic acid, sodium ascorbate;
1 tablet contains ascorbic acid 199.5 mg, sodium ascorbate 338.0 mg (equivalent to 300.5 mg of ascorbic acid);
Excipients:
chewable tablets
sorbitol (E 420), microcrystalline cellulose, potassium acesulfame (E 950), aspartame (E 951), magnesium stearate, colloidal anhydrous silicon dioxide, tartrazine dye (E 102);
chewable tablets with orange flavor
sorbitol (E 420), microcrystalline cellulose, potassium acesulfame (E 950), aspartame (E 951), magnesium stearate, colloidal anhydrous silicon dioxide, natural orange flavor, yellow dye FCF (E 110).
Pharmaceutical form. Chewable tablets.
Main physicochemical properties:
chewable tablets
yellow-colored tablets, flat cylindrical in shape with a bevel; non-uniformity of color is allowed (specks of white and yellow); a powdery deposit on the tablet surface is permitted;
chewable tablets with orange flavor
pink-orange colored tablets, flat cylindrical in shape with a bevel; non-uniformity of color is allowed (specks of white and pink-orange); a powdery deposit on the tablet surface is permitted.
Pharmacotherapeutic group.
Simple preparations of ascorbic acid (vitamin C). Ascorbic acid (vitamin C).
ATC code A11G A01.
Pharmacological properties.
Pharmacodynamics.
Ascorbic acid (vitamin C) belongs to the group of water-soluble vitamins.
Ascorbic acid has pronounced reducing properties, participates in many redox reactions, and regulates carbohydrate, lipid, and protein metabolism. It affects the metabolism of aromatic amino acids, folic acid, histamine, thyroxine, steroid hormones, and insulin. It is necessary for the synthesis of intercellular substance and for the regeneration of connective and bone tissues. Ascorbic acid participates in essential hydroxylation reactions, including the formation of the neurotransmitter norepinephrine from dopamine and the conversion of proline into hydroxyproline (thus participating in the processes of collagen synthesis and maturation in connective tissue). Ascorbic acid plays an important role in metal ion metabolism, including iron absorption from the gastrointestinal tract (enhances iron absorption) and its transport to tissues and organs. Ascorbic acid influences hemoglobin synthesis and erythrocyte maturation, stabilizes capillary walls, and is essential for blood coagulation. Ascorbic acid enhances the body's resistance to infections and adverse environmental influences, improves appetite, promotes normalization of sleep, and possesses antioxidant and radioprotective properties, reducing hemorrhagic manifestations of radiation sickness and stimulating hematopoiesis.
Deficiency of ascorbic acid in the diet leads to the development of ascorbic acid deficiency, as it is not synthesized in the body. Under certain conditions, the body's requirement for ascorbic acid may increase, for example, during periods of rapid growth, physical or mental overexertion, and acute respiratory and other infectious diseases.
Pharmacokinetics.
Absorption
After oral administration, ascorbic acid is well absorbed in the gastrointestinal tract, primarily in the small intestine.
Distribution
Maximum plasma concentration of ascorbic acid is reached within 4–7 hours. It readily penetrates into leukocytes, thrombocytes, and erythrocytes (concentration in leukocytes and thrombocytes is higher than in erythrocytes and blood plasma), and subsequently into all tissues. It accumulates in the posterior pituitary gland, adrenal cortex, interstitial cells of the testes, ovaries, thyroid gland, pancreas, liver, intestinal wall, brain, ocular epithelium, spleen, lungs, kidneys, heart, and muscles. The physiological depot level of ascorbic acid in the body is approximately 1.5 g.
Metabolism
Ascorbic acid is primarily metabolized in the liver into dehydroascorbic acid, and further into diketogulonic and oxalic acids.
Excretion
Excess ascorbic acid entering the body (usually > 200 mg/day) is rapidly excreted; unchanged ascorbic acid and its inactive metabolites are primarily eliminated via urine. The amount of ascorbic acid excreted unchanged in urine depends on the dose; a slight diuretic effect is possible. When large doses of ascorbic acid are administered, resulting in plasma concentrations exceeding 1.4 mg/dL, excretion is markedly enhanced, and increased excretion may persist after discontinuation of the drug.
Ascorbic acid crosses the placenta and is excreted into breast milk.
Clinical characteristics.
Indications.
For the treatment of ascorbic acid deficiency.
To meet the increased demand of the body for ascorbic acid:
- during acute respiratory and other infectious diseases;
- during convalescence after severe illnesses, surgical interventions;
- in various intoxications, hemorrhagic diatheses, connective tissue diseases (rheumatoid arthritis), hemorrhages (nasal, pulmonary, uterine);
- in radiation sickness, hepatitis, cholecystitis, Addison's disease, slowly healing soft tissue injuries, infected wounds, and bone fractures.
Contraindications.
Hypersensitivity to ascorbic acid or to other components of the medicinal product, predisposition to thrombosis, thrombophlebitis, diabetes mellitus, severe kidney diseases, urolithiasis (when doses exceeding 1000 mg per day are used), hyperoxaluria, phenylketonuria.
Children under 14 years of age. Pregnancy or breastfeeding period.
Interaction with other medicinal products and other forms of interaction.
When used simultaneously, ascorbic acid enhances gastrointestinal absorption of penicillin, tetracycline, ethinylestradiol, and iron.
Concomitant use of ascorbic acid with deferoxamine increases urinary excretion of iron. Cases of cardiomyopathy and congestive heart failure have been reported in patients with idiopathic hemochromatosis and thalassemia who started taking ascorbic acid while on deferoxamine therapy. Use of ascorbic acid in these patient groups requires caution and cardiac function monitoring.
Concomitant use of ascorbic acid with antacids containing aluminum may increase urinary excretion of aluminum. Concurrent use of ascorbic acid and antacids is not recommended, especially in patients with renal insufficiency.
Ascorbic acid reduces the toxicity of sulfonamide medicinal products and decreases the effectiveness of heparin and indirect anticoagulants.
When used simultaneously, ascorbic acid reduces the chronotropic effect of isoprenaline.
High doses of ascorbic acid reduce the therapeutic effect of tricyclic antidepressants and neuroleptics (phenothiazine derivatives), increase renal excretion of amphetamine and mexiletine, and affect vitamin B12 resorption.
Long-term or high-dose use of ascorbic acid in combination with disulfiram reduces the efficacy of disulfiram treatment.
Ascorbic acid increases the total clearance of ethanol.
Concomitant use with amygdalin (within complementary medicine) may cause symptoms of cyanide toxicity.
Barbiturates and primidone may increase urinary excretion of ascorbic acid.
Fruit or vegetable juices and alkaline beverages reduce the absorption of ascorbic acid.
Oral contraceptives and tobacco smoking reduce plasma concentration of ascorbic acid.
Intake of acetylsalicylic acid (aspirin) reduces absorption of ascorbic acid by approximately one-third, which necessitates an increase in the dose of the latter. When used simultaneously with acetylsalicylic acid, urinary excretion of ascorbic acid increases; urinary excretion of acetylsalicylic acid remains unaffected and does not reduce its anti-inflammatory effect. Ascorbic acid increases the risk of crystalluria during salicylate therapy.
Medicinal products of the quinolone group, calcium chloride, salicylates, tetracyclines, and glucocorticosteroids reduce body reserves of ascorbic acid when used long-term.
Special precautions for use.
Concurrent intake of the medicinal product with alkaline drinks reduces the absorption of ascorbic acid; therefore, it should not be taken with alkaline mineral water. The absorption process of ascorbic acid may be impaired in intestinal dyskinesia, enteritis, achylia (suppressed gastric secretion), helminthic infestation, and giardiasis.
The medicinal product should be used with special caution in patients:
- with glucose-6-phosphate dehydrogenase deficiency (ascorbic acid may provoke hemolytic anemia);
- with a history of nephrolithiasis (risk of hyperoxaluria and precipitation of oxalates in the urinary tract after administration of high doses of ascorbic acid);
- with disorders of iron metabolism (hemochromatosis, thalassemia, hemosiderosis).
Since ascorbic acid enhances iron absorption, its use in high doses may be hazardous for patients with hemochromatosis, thalassemia, polycythemia, leukemia, and sideroblastic anemia. Patients with high iron content in the body should use ascorbic acid in minimal doses.
The medicinal product should be used cautiously in patients with a history of kidney disease. Ascorbic acid increases oxalate excretion in urine, increasing the risk of formation of oxalate kidney stones. Patients at risk of developing hyperoxaluria should not take ascorbic acid in doses exceeding 1000 mg. However, patients not belonging to this risk group are not subject to this risk. In urolithiasis, the daily dose of ascorbic acid should not exceed 1000 mg (see section "Contraindications").
High doses of ascorbic acid should not be administered to patients with increased blood coagulation. Ascorbic acid should be used cautiously in patients with progressive oncological diseases, as its use may complicate the course of the disease.
When high doses or prolonged administration of ascorbic acid are used, kidney function and arterial blood pressure should be monitored due to the stimulatory effect of ascorbic acid on corticosteroid hormone production.
Prolonged use of high doses of ascorbic acid may suppress the function of the islet apparatus of the pancreas, requiring monitoring of its condition.
Long-term use of high doses of ascorbic acid may accelerate its renal clearance, so after abrupt dose reduction or discontinuation of treatment, paradoxical deficiency of ascorbic acid may occur.
The recommended dose should not be exceeded.
It is not recommended to use simultaneously with other medicinal products containing ascorbic acid.
Since ascorbic acid has a mild stimulant effect on the central nervous system, the medicinal product VITAMIN C is not recommended to be taken at the end of the day.
Effect on laboratory test results
As a reducing agent, ascorbic acid may affect laboratory test results when measuring blood levels of glucose, bilirubin, uric acid, creatinine, inorganic phosphates, lactate dehydrogenase activity, and transaminases; it may cause false-positive or false-negative results (depending on the method used) in determining glucose in urine; it may influence the results of biochemical determination of creatinine and uric acid concentrations in urine. When high doses of ascorbic acid are used, fecal occult blood testing may yield false-negative results.
1 tablet of the medicinal product VITAMIN C contains 1.7 mmol (or 39 mg) of sodium; therefore, patients on a sodium-controlled diet should use this medicinal product with caution.
1 chewable tablet of the medicinal product VITAMIN C contains 506.26 mg of sorbitol (E 420).
1 chewable tablet with orange flavor of the medicinal product VITAMIN C contains 484.80 mg of sorbitol (E 420).
Patients with known sugar intolerances should consult a physician before taking this medicinal product. The additive effect of concurrently administered medicinal products containing sorbitol (or fructose), as well as dietary intake of sorbitol (or fructose), should be considered. The sorbitol content in orally administered medicinal products may affect the bioavailability of other orally administered medicinal products when used concomitantly.
The medicinal product contains aspartame (E 951), a source of phenylalanine, which poses a risk for patients with phenylketonuria (see section "Contraindications").
The medicinal product contains the colorant tartrazine (E 102) or Sunset Yellow FCF (E 110), which may cause allergic reactions.
Use during pregnancy or breastfeeding.
The medicinal product in this dosage form is not intended for use during pregnancy or breastfeeding.
Ability to affect reaction speed when driving or operating machinery.
There is no evidence that the medicinal product negatively affects reaction speed when driving or operating complex machinery, provided the recommended dosage regimen is followed.
Dosage and Administration.
Take the medicinal product orally after meals, chewing the tablet.
For adults and children aged 14 years and older, the therapeutic dose is 1 tablet (500 mg) daily. Treatment duration is 10–15 days.
In acute respiratory and other infectious diseases, adults are recommended to take 1–2 tablets (500–1000 mg) daily (in two divided doses) for 7–10 days, followed by 250 mg daily. For such dosing, ascorbic acid preparations with appropriate active ingredient content should be used.
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 recommended for children under 14 years of age in a different dosage form.
Overdose.
Acute overdose of the medicinal product is practically impossible. Excess ascorbic acid is rapidly excreted from the body. When doses exceeding 3000 mg daily are administered, unabsorbed ascorbic acid is predominantly excreted unchanged in feces.
Symptoms. High-dose administration of ascorbic acid may cause diarrhea and formation of oxalate kidney stones. Symptomatic treatment may be required.
High-dose ascorbic acid may cause vomiting and nausea, which resolve after discontinuation of the medicinal product.
Ascorbic acid may induce acidosis or hemolytic anemia in some patients with glucose-6-phosphate dehydrogenase deficiency.
Prolonged administration of high doses of ascorbic acid may lead to suppression of the pancreatic islet apparatus function, impaired kidney function, increased arterial pressure, and development of other adverse effects listed in the section "Adverse Reactions."
Massive overdose of ascorbic acid may result in renal failure.
Treatment. If an excessive dose of ascorbic acid has been recently ingested, gastric lavage should be performed; otherwise, general supportive measures should be implemented. Ascorbic acid can be removed from the body by hemodialysis.
Adverse reactions.
The medicinal product is very well tolerated at the recommended dose, and adverse reactions usually do not occur when the recommended dosage regimen is followed. However, the following adverse reactions may occur with prolonged use in high doses.
Psychiatric disorders: increased excitability, increased fatigue, sleep disturbances.
Nervous system disorders: increased excitability of the central nervous system, headache.
Cardiovascular disorders: myocardial dystrophy, arterial hypertension, hot flushes.
Blood and lymphatic system disorders: thrombosis, hyperprothrombinemia, thrombocytosis, erythrocytopenia, neutrophilic leukocytosis; hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency may lead to erythrocyte hemolysis.
Gastrointestinal disorders: irritation of the gastrointestinal mucosa, heartburn, nausea, vomiting, stomach spasms; diarrhea when administered in doses exceeding 1000 mg per day.
Endocrine disorders: damage to the islet apparatus of the pancreas (hyperglycemia, glucosuria), impaired glycogen synthesis up to the development of diabetes mellitus.
Metabolism and nutrition disorders: disturbances in zinc and copper metabolism.
Renal and urinary disorders: damage to the glomerular apparatus of the kidneys, crystalluria, formation of urate, cystine and/or oxalate kidney stones and urinary tract stones, renal failure; diuretic effect when administered in doses exceeding 600 mg per day.
Immune system disorders: allergic reactions, angioneurotic edema, anaphylactic shock in case of sensitization.
Skin and subcutaneous tissue disorders: skin redness, skin rashes (including urticaria), itching, eczema.
General disorders: sensation of warmth, dental enamel erosion, occasionally back pain.
Shelf life. 2 years.
Storage conditions.
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging.
8 tablets in a blister; 3 or 7 blisters per pack.
Prescription status.
Over-the-counter.
Manufacturer.
Limited liability company "INTERKHIM".
Manufacturer's address and location of business activity.
40-A, 21st km of Starokyivska Road, Odesa, 65025, Ukraine.