Instructions Ascorbic acid-Darnitsa solution for injection 50 mg/ml ampoule 2 ml No. 10
Composition
active ingredient: ascorbic acid;
1 ml of solution contains: ascorbic acid 50 mg;
excipients: sodium bicarbonate, sodium metabisulfite (E 223), disodium edetate, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Simple preparations of ascorbic acid (vitamin C). ATX code A11G A01.
Pharmacological properties
Pharmacodynamics.
Ascorbic acid, or vitamin C, belongs to the group of water-soluble vitamins. It participates in redox reactions, participates in many metabolic processes, in particular in the regulation of carbohydrate metabolism, the metabolism of aromatic amino acids, thyroxine, in the synthesis of catecholamines, steroid hormones, insulin. It is a necessary component in the process of blood clotting, the synthesis of collagen, procollagen, the regeneration of connective and bone tissues. It regulates capillary permeability (inhibits hyaluronidase). It participates in the absorption of iron and the synthesis of hemoglobin.
Ascorbic acid inactivates free radicals, thereby preventing damage to cell membranes, particularly lymphocytes, from the harmful effects of peroxidation. This action causes a number of immunomodulatory effects, including enhancing chemotaxis, synthesis and release of interferon, and improving lymphocyte migration.
Increases the body's nonspecific and immune resistance.
It is not synthesized in the human body. Insufficient intake with food leads to the development of hypo- or avitaminosis.
Pharmacokinetics.
The connection with blood plasma proteins is 25%. The concentration of ascorbic acid in blood plasma is normally approximately 10-20 μg/ml, reserves in the body are about 1.5 g. The time to reach the maximum concentration in blood plasma with intramuscular injection Tmax is 15-20 minutes. It easily penetrates into leukocytes, platelets, and then into all tissues; it is deposited in the posterior pituitary gland, adrenal cortex, eye epithelium, intermediate cells of the seminiferous glands, ovaries, liver, spleen, pancreas, lungs, kidneys, intestinal wall, heart, muscles, thyroid gland; penetrates through the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and blood plasma. In deficient states, the concentration in leukocytes decreases later and more slowly and is considered a better criterion for assessing deficiency than the concentration in blood plasma. It is metabolized mainly in the liver. It is excreted by the kidneys, intestines, sweat, and enters breast milk in the form of unchanged ascorbate and metabolites. At high doses, when the concentration in blood plasma reaches more than 1.4 mg/dl, excretion is sharply increased, and increased excretion persists after discontinuation of the drug. Smoking and alcohol consumption accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing its reserves in the body.
Indication
Hypovitaminosis C, scurvy, bleeding (uterine, pulmonary, nasal, hepatic), hemorrhagic diathesis, bleeding as radiation sickness syndrome, intoxications and infectious diseases, nephropathy of pregnant women, Addisonian crisis, overdose of anticoagulants, bone fractures and flaccid wounds, various dystrophies, pregnancy and breastfeeding.
Contraindication
Hypersensitivity to the components of the drug, diabetes mellitus, increased blood clotting, tendency to thrombosis, thrombophlebitis, urolithiasis (including hyperoxaluria) when using more than 1 g, severe renal failure, progressive malignant diseases, hemochromatosis, thalassemia, polycythemia, leukemia, sideroblastic anemia, glucose-6-phosphate dehydrogenase deficiency, sickle cell anemia.
Interaction with other medicinal products and other types of interactions
When used simultaneously with salicylates and short-acting sulfonamides, the risk of urinary calculi formation increases.
With simultaneous use of ascorbic acid with salicylates, ethinyl estradiol, benzylpenicillin and tetracyclines, the concentration of these drugs in the blood increases.
When used simultaneously with ascorbic acid, coumarin and heparin derivatives, and antibiotics, the effectiveness of these drugs decreases.
High doses of ascorbic acid may lower urinary pH, resulting in decreased tubular reabsorption of amphetamine and tricyclic antidepressants used concomitantly.
When used simultaneously, ascorbic acid reduces the effectiveness of oral contraceptives.
Tetracyclines and acetylsalicylic acid increase the excretion of ascorbic acid in the urine.
When used simultaneously with barbiturates and pyrimidines, the excretion of ascorbic acid in the urine increases.
Increases the neutralization and total clearance of ethyl alcohol.
Increases the excretion of drugs that have an alkaline reaction (including alkaloids).
In high doses, it increases the renal excretion of mexiletine.
Simultaneous administration of ascorbic acid and deferoxamine increases tissue iron toxicity, especially in the heart muscle, which can lead to circulatory decompensation. Vitamin C can be taken only 2 hours after the injection of deferoxamine.
Reduces the chronotropic effect of isoprenaline and the therapeutic effect of phenothiazine derivatives.
Application features
Due to the stimulating effect of ascorbic acid on the synthesis of corticosteroid hormones, it is necessary to monitor kidney function and blood pressure.
With prolonged use of high doses, inhibition of the function of the insular apparatus of the pancreas is possible, therefore, during treatment, it must be regularly monitored.
In patients with elevated iron levels in the body, ascorbic acid should be used in minimal doses.
Patients undergoing chemotherapy should be administered the drug no earlier than 1-3 days (depending on the half-life of the anticancer drug) after chemotherapy, as there is no clinical data on a possible interaction.
The use of large doses of ascorbic acid may affect the results of some laboratory tests: a false-positive test for the presence of sugar in the urine and a negative test for the presence of occult blood in the stool, as well as a decrease in the results of studies of the concentration of lactate dehydrogenase and aminotransferases in serum.
High-dose therapy should not be administered to patients prone to recurrent urolithiasis. Patients with renal failure should be provided with adequate fluid intake (1.5-2 liters per day) to reduce the risk of crystalluria.
Patients on a low-sodium diet should not be prescribed high doses of the drug.
Use during pregnancy or breastfeeding
A lack of vitamin C in the diet of pregnant women can be dangerous for the fetus, but its use in high doses can negatively affect fetal development, there is also a threat of miscarriage. Therefore, ascorbic acid should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.
Ascorbic acid penetrates the placental barrier.
The minimum daily requirement for ascorbic acid in the II-III trimesters of pregnancy is about 60 mg. It is worth bearing in mind that the fetus can adapt to high doses of ascorbic acid taken by a pregnant woman, and then the newborn may develop ascorbic disease as a "withdrawal" syndrome (during pregnancy, ascorbic acid should not be taken in high doses, except in cases where the expected benefit to the mother outweighs the potential risk to the fetus).
The minimum daily requirement during breastfeeding is 80 mg. Ascorbic acid passes into breast milk, so during breastfeeding, vitamin C is taken only under the supervision of a doctor. Theoretically, there is a danger to the child if the mother uses high doses of ascorbic acid (during breastfeeding, it is not recommended to exceed the daily requirement for ascorbic acid). If it is necessary to prescribe increased doses of the drug, breastfeeding should be discontinued.
A mother's diet containing adequate amounts of ascorbic acid is sufficient to prevent vitamin C deficiency in the infant.
Ability to influence reaction speed when driving vehicles or other mechanisms
The effect of the drug in recommended doses on the reaction speed when driving or working with other mechanisms is unlikely.
Method of administration and doses
Ascorbic acid-Darnitsa should be administered intramuscularly and intravenously by jet or drip.
Intravenously, inject by jet over 1-3 minutes. For intravenous drip administration, dissolve a single dose 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. Intramuscularly, inject deeply into the muscle. Doses should be set individually, taking into account the nature and severity of the disease.
Adults and children over 12 years of age are prescribed 50-150 mg per day (1-3 ml of 5% solution). In case of poisoning, the daily dose can be increased to 500 mg. The maximum single dose is 200 mg, daily dose is 1 g.
Children under 12 years of age should be administered intravenously in a daily dose of 5-7 mg/kg of body weight in the form of a 5% solution (0.5-2 ml). Usually, daily doses for children are:
under 6 months of age – 30 mg;
aged 6 to 12 months – 35 mg;
aged 1 to 3 years – 40 mg;
ages 4 to 10 years – 45 mg;
aged 11 to 12 years – 50 mg.
The maximum daily dose for children under 12 years of age is 100 mg.
Special patient groups. For patients with recurrent kidney stones, the daily dose of ascorbic acid should not exceed 100-200 mg. For patients with severe or end-stage renal failure (patients on dialysis), the daily dose of ascorbic acid should not exceed 50-100 mg. For patients with glucose-6-phosphate dehydrogenase deficiency, the daily dose of ascorbic acid should not exceed 100-500 mg.
Children.
The drug can be used in children.
Overdose
Symptoms. Large doses of ascorbic acid can cause gastrointestinal disorders, including diarrhea, and also lead to hyperoxaluria and the formation of oxalate stones. With a single use of excessive doses of the drug, nausea, vomiting, bloating, abdominal pain, itching, skin rashes, increased excitability may occur. With intravenous administration of the drug in high doses, there may be a threat of abortion. Doses above 600 mg per day have a diuretic effect.
Treatment. It is necessary to stop using the drug, rinse the stomach, give the patient an alkaline drink, activated charcoal or other adsorbents, and conduct symptomatic therapy.
Adverse reactions
Ascorbic acid is generally well tolerated, but adverse reactions may occur.
From the side of the central and peripheral nervous system: headache, feeling of increased fatigue, with prolonged use in high doses - sleep disturbances, increased excitability of the central nervous system.
Gastrointestinal: stomach cramps, sometimes nausea, diarrhea.
Metabolic: hypervitaminosis C, with prolonged use in high doses - inhibition of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria) and glycogen synthesis, sodium and fluid retention, impaired zinc and copper metabolism.
From the cardiovascular system: decreased capillary permeability, deterioration of tissue trophism; with prolonged use in high doses - myocardial dystrophy, increased blood pressure, development of microangiopathies.
From the blood system: with prolonged use in high doses - thrombocytosis, hyperprothrombinemia, thromboembolism, erythrocytopenia, neutrophilic leukocytosis.
From the urinary system: hyperoxaluria is possible; with prolonged use in high doses - damage to the glomerular apparatus of the kidneys, formation of oxalate kidney stones.
Allergic reactions: hypersensitivity reactions, very rarely - skin rashes, skin hyperemia, itching, urticaria, increased body temperature, anaphylactic shock.
Injection site reactions: changes at the injection site.
Other: with intravenous administration, a feeling of heat is possible, with intravenous administration in high doses - the threat of abortion.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature of 2°C to 8°C.
Keep out of reach of children.
Incompatibility
The drug is incompatible with iron salts, oxidants, heavy metal salts, especially copper. There are reports that ascorbic acid injections are incompatible with aminophylline, bleomycin sulfate, erythromycin, nafcillin sodium, nitrofurantoin sodium, conjugated estrogens, sodium bicarbonate, diethanolamine sulfafurazole. Sometimes, depending on the pH level or concentration, incompatibility with chloramphenicol is noted.
Packaging
2 ml in an ampoule; 10 ampoules in a box; 5 ampoules in a contour blister pack; 2 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
