Ascorbic acid-zdorovya

INSTRUCTION for medical use of the medicinal product Ascorbic Acid-Zdorovye (ASCORBIC ACID-ZDOROVYE)

Composition:

Active substance: ascorbic acid;

1 ml of solution contains 50 mg or 100 mg of ascorbic acid;

Excipients: sodium hydrocarbonate, sodium metabisulfite (E 223), disodium edetate, water for injections.

Medicinal form. Injection solution.

Main physicochemical properties: 50 mg/ml solution – clear, colorless or slightly yellowish solution; 100 mg/ml solution – clear yellowish solution.

Pharmacotherapeutic group. Simple ascorbic acid preparations. Ascorbic acid (vitamin C). ATC code A11G A01.

Pharmacological Properties.

Pharmacodynamics.

Ascorbic acid (vitamin C) is a water-soluble vitamin that supports optimal tissue metabolism. It actively participates in redox reactions, forming with dehydroascorbic acid a hydrogen proton transfer system, exhibits antioxidant properties, thereby ensuring the stability of cellular membranes. It participates in the synthesis of the ground substance of vascular wall connective tissue, thus preventing the development of hemorrhagic diathesis. It is not synthesized in the human body. With insufficient intake of ascorbic acid from food, bleeding from the gums and mucous membranes develops. It participates in glucose metabolism, cholesterol catabolism, and synthesis of steroid hormones. During stress reactions, the content of ascorbic acid in the body and particularly in adrenal gland tissue decreases significantly, confirming the involvement of ascorbic acid in adaptation responses. It can exert an anti-anemic effect due to its influence on iron metabolism. It reduces trivalent iron to divalent iron, which is then transported in the bloodstream.

Pharmacokinetics.

After parenteral administration, ascorbic acid readily penetrates leukocytes and platelets, and then into all tissues; it accumulates mainly in organs with high metabolic activity, particularly in adrenal gland tissue. In tissues, it exists both in free form and as various compounds. It is excreted from the body in urine, both in unchanged form and as metabolites.

Alcohol consumption and smoking accelerate the breakdown of ascorbic acid (conversion into inactive metabolites), sharply reducing its reserves in the body.

Clinical characteristics.

Indications. Hypovitaminosis C; scurvy, hemorrhages (uterine, pulmonary, nasal, hepatic), hemorrhagic diatheses, bleeding as a symptom of radiation sickness, various intoxications and infectious diseases, Addisonian crisis, anticoagulant overdose, bone fractures and poorly healing wounds, various dystrophies, increased cerebral strain and heavy physical exertion.

Contraindications. Hypersensitivity to ascorbic acid or to any of the excipients; diabetes mellitus, increased blood coagulation, predisposition to thrombosis, thrombophlebitis, urolithiasis (including hyperoxaluria), renal insufficiency, progressive malignant diseases, hemochromatosis, thalassemia, polycythemia, leukemia, sideroblastic anemia, sickle cell anemia, glucose-6-phosphate dehydrogenase deficiency.

Interaction with other medicinal products and other forms of interaction. Ascorbic acid increases blood concentrations of salicylates (increasing the risk of crystalluria), ethinylestradiol, benzylpenicillin, and tetracyclines, while decreasing blood levels of oral contraceptives. It enhances the excretion of drugs with alkaline reaction (including alkaloids). In high doses, it increases renal excretion of mexiletine.

Tetracyclines and acetylsalicylic acid enhance urinary excretion of ascorbic acid.

Concomitant use with salicylates and short-acting sulfonamides increases the risk of urinary stone formation.

High doses of ascorbic acid can reduce urine pH, thereby decreasing tubular reabsorption of concurrently administered amphetamines and tricyclic antidepressants.

It reduces the anticoagulant effect of coumarin derivatives and heparin, as well as the efficacy of antibiotics.

It enhances detoxification and total clearance of ethanol.

It reduces the chronotropic effect of isoprenaline and the therapeutic effect of phenothiazine derivatives.

Concomitant use with barbiturates and primidone increases urinary excretion of ascorbic acid.

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

When ascorbic acid is used in high doses concomitantly with alcohol, disulfiram-like reactions may develop.

Special precautions for use

When using high doses, monitoring of kidney function and blood pressure is required (due to ascorbic acid stimulation of corticosteroid production), as well as monitoring of pancreatic function (due to inhibition of the islet apparatus).

High-dose therapy should not be administered to patients with a predisposition to recurrent urolithiasis.

Administration of high doses of ascorbic acid may affect the results of certain laboratory tests: false-positive glucose tests in urine and false-negative tests for occult blood in feces, as well as decreased serum levels of lactate dehydrogenase and aminotransferases.

Patients with increased iron levels in the body should receive ascorbic acid in minimal doses.

Administration of ascorbic acid to patients with rapidly proliferating and intensively metastasizing tumors may enhance these processes. For patients undergoing chemotherapy, the drug should be administered no earlier than 1–3 days after chemotherapy (depending on the half-life of the antineoplastic agent), due to lack of clinical data on possible interactions.

This medicinal product contains 7.1 mg/mL of sodium (at a dosage of 50 mg/mL) or 13.9 mg/mL of sodium (at a dosage of 100 mg/mL), i.e., it is practically sodium-free.

Use during pregnancy or breastfeeding.
Vitamin C deficiency in the diet of pregnant women may be hazardous to the fetus; however, high-dose administration may adversely affect fetal development and may increase the risk of pregnancy termination. Therefore, ascorbic acid should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.

The minimal daily requirement of ascorbic acid during the II–III trimesters of pregnancy is approximately 60 mg. Ascorbic acid crosses the placental barrier. It should be noted that the fetus may adapt to high doses of ascorbic acid taken by the pregnant woman, and subsequently, scurvy may develop in the newborn as a withdrawal reaction. Therefore, high doses of the drug should not be prescribed during pregnancy, except when the potential benefit to the mother outweighs the possible risk to the fetus.

The minimal daily requirement of ascorbic acid during breastfeeding is 80 mg. A mother's diet containing an adequate amount of ascorbic acid is sufficient to prevent deficiency in the infant. Ascorbic acid passes into breast milk. Theoretically, there is a potential risk to the infant when the mother takes high doses of ascorbic acid (during breastfeeding, exceeding the daily requirement of ascorbic acid is not recommended). If high-dose administration is necessary, breastfeeding should be discontinued.

Ability to influence reaction speed when driving vehicles or operating machinery.
The drug, when used at recommended doses, does not affect the ability to drive vehicles or operate machinery.

Method of Administration and Dosage

Administer intravenously (either as a bolus or by infusion) or intramuscularly.

For intravenous bolus administration, inject over 1–3 minutes. For intravenous infusion, dissolve a single dose of the drug in 50–100 mL of 0.9% sodium chloride solution and administer by slow intravenous infusion at a rate of 30–40 drops per minute.

For intramuscular administration, inject deeply into the muscle.

Dosage should be individualized depending on the nature and severity of the disease.

Adults and children aged 12 years and older: The usual daily dose is 50–150 mg. In cases of poisoning, the daily dose may be increased up to 500 mg. Maximum single dose – 200 mg; maximum daily dose – 1 g.

Children under 12 years of age: Administer intravenously at a daily dose of 5–7 mg/kg body weight as a 5% solution (0.5–2 mL). Typical daily doses for children are: under 6 months – 30 mg; 6–12 months – 35 mg; 1–3 years – 40 mg; 4–10 years – 45 mg; 11–12 years – 50 mg. Maximum daily dose – 100 mg.

Special patient groups: For patients with recurrent kidney stone formation, the daily dose of ascorbic acid should not exceed 100–200 mg.

Children: See section "Method of Administration and Dosage" for pediatric use.

Overdose. High doses of ascorbic acid may cause gastrointestinal disturbances, including diarrhea, and may lead to hyperoxaluria and formation of oxalate calculi. Doses exceeding 600 mg per day may produce a diuretic effect.

After single administration of excessive doses, nausea, vomiting, bloating, abdominal pain, itching, skin rashes, and increased excitability may occur.

Intravenous administration of high doses may pose a risk of pregnancy termination.

Treatment: Discontinue the drug and provide symptomatic therapy.

Adverse Reactions. Ascorbic acid is generally well tolerated; however, the following adverse effects may occur.

Blood and lymphatic system disorders: With prolonged use at high doses – thrombocytosis, hyperprothrombinemia, thrombosis, erythrocytopenia, neutrophilic leukocytosis.

Nervous system disorders: Headache, fatigue; with prolonged use at high doses – sleep disturbances, increased central nervous system excitability.

Gastrointestinal disorders: Nausea, diarrhea, stomach cramps.

Urinary system disorders: Hyperoxaluria; with prolonged use at high doses – damage to renal glomerular apparatus, formation of calcium oxalate kidney stones.

Skin and subcutaneous tissue disorders: Hypersensitivity reactions; very rarely – skin rashes, skin hyperemia, pruritus, urticaria, fever, injection site reactions.

Metabolism and nutritional disorders: Hypervitaminosis C; with prolonged use at high doses – suppression of pancreatic islet function (hyperglycemia, glucosuria) and glycogen synthesis, sodium and fluid retention, disturbances in zinc and copper metabolism.

Vascular disorders: Decreased capillary permeability, impaired tissue trophism; with prolonged use at high doses – myocardial dystrophy, increased arterial pressure, development of microangiopathies.

General disorders: With intravenous administration, sensation of warmth or chills may occur.

Pregnancy: Intravenous administration at high doses may pose a risk of pregnancy termination.

Immune system disorders: Very rarely – anaphylactic shock.

Sodium metabisulfite (E 223) may rarely cause hypersensitivity reactions and bronchospasm.

Shelf life. 2 years.

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

Keep out of reach of children.

Incompatibility. Ascorbic acid has a high redox potential and may alter the chemical composition of other drugs. Therefore, compatibility must be confirmed before considering concomitant use with other medicinal products.

Packaging. 2 mL in ampoules, pack of 10 in a box; 5×2, 10 in blister packs in a box.

Prescription category. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION 'ZDOROV'YA".

Manufacturer's address and place of business.

Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, building 22.