Ascorbic acid
Storage:
active substance: ascorbic acid;
1 ml of solution contains ascorbic acid 50 mg or 100 mg;
excipients: sodium bicarbonate, sodium metabisulfite (E 223), disodium edetate, water for injections.
Medicinal form. Solution for injections.
Main physicochemical properties: 5% solution – transparent colorless or slightly yellowish liquid; 10% solution is a clear, colorless to yellowish liquid.
Pharmacotherapeutic group. Simple preparations of ascorbic acid. Ascorbic acid (vitamin C). ATX code A11G A01.
Pharmacological properties .
Pharmacodynamics.
Ascorbic acid (vitamin C) is a water-soluble vitamin that promotes optimal tissue metabolism. Takes an active part in redox reactions, forming a hydrogen proton transfer system with dehydroascorbic acid, exhibits antioxidant properties, due to which it ensures the stability of cell membranes. Participates in the synthesis of the main substance of the connective tissue of the vascular wall, thus preventing the development of hemorrhagic diathesis. It is not synthesized in the human body. In the case of insufficient intake of ascorbic acid with 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 in the tissue of the adrenal glands in particular, significantly decreases, which confirms the participation of ascorbic acid in adaptation reactions. Able to exert an anti-anemic effect due to the effect on iron metabolism. Restores trivalent iron to divalent iron, which is transported with the bloodstream.
Pharmacokinetics.
After parenteral administration, ascorbic acid easily penetrates into leukocytes, platelets, and then into all tissues; accumulates mainly in organs with an increased level of metabolic processes, in particular in the tissues of the adrenal glands. It is found in tissues both in a free state and in the form of compounds. It is excreted from the body with urine both unchanged and in the form of metabolites.
Alcohol consumption and smoking accelerate the destruction of ascorbic acid (transformation into inactive metabolites), sharply reducing its reserves in the body.
Clinical characteristics.
Indication.
Hypovitaminosis C; scurvy, bleeding (uterine, pulmonary, nasal, hepatic), hemorrhagic diatheses, bleeding as a syndrome of radiation sickness, various intoxications and infectious diseases, nephropathy of pregnant women, Addisonian crisis, overdose of anticoagulants, bone fractures and soft-granulating wounds, various dystrophies, pregnancy and the period of breastfeeding, increased mental stress and hard physical work.
Contraindication.
Increased individual sensitivity to ascorbic acid or to any of the auxiliary components of the drug; diabetes, increased blood coagulation, tendency to thrombosis, thrombophlebitis, urolithiasis (including hyperoxaluria), kidney failure, progressive malignant diseases, hemochromatosis, thalassemia, polycythemia, leukemia, sideroblastic anemia, sickle cell anemia, glucose deficiency 6-phosphate dehydrogenase.
Interaction with other medicinal products and other types of interactions.
Ascorbic acid increases the concentration of salicylates in the blood (increases the risk of crystalluria), ethinylestradiol, benzylpenicillin and tetracyclines, reduces the level of oral contraceptives in the blood. Increases the excretion of drugs that have an alkaline reaction (including alkaloids). In high doses, it increases the renal excretion of mexiletine.
Tetracyclines and acetylsalicylic acid increase the excretion of ascorbic acid in the urine.
With simultaneous use with salicylates and short-acting sulfonamides, the risk of formation of urinary stones increases.
High doses of ascorbic acid can lower urine pH, resulting in reduced tubular reabsorption of amphetamine and tricyclic antidepressants used simultaneously.
Increases iron excretion in patients taking deferoxamine.
Reduces the anticoagulant effect of coumarin and heparin derivatives, the effectiveness of antibiotics.
Increases neutralization and general clearance of ethyl alcohol.
Reduces the chronotropic effect of isoprenaline and the therapeutic effect of phenothiazine derivatives.
With simultaneous use with barbiturates, primidone increases the excretion of ascorbic acid with urine.
With the use of ascorbic acid in large doses and the simultaneous use of alcohol, a disulfiram-like reaction may develop.
Features of application.
If large doses are used, it is necessary to control kidney function, blood pressure (stimulation of corticosteroid formation by ascorbic acid), as well as pancreatic function (suppression of the insular apparatus).
Therapy with large doses cannot be carried out by patients with a tendency to recurrent urolithiasis. To reduce the risk of crystalluria, patients with renal insufficiency need to ensure adequate fluid intake (1.5–2 liters per day).
The use of large doses of ascorbic acid can affect the results of some laboratory tests: a false positive result of a test for the presence of sugar in the urine and a negative result of a test for the presence of hidden blood in the feces, as well as a decrease in the concentration of lactate dehydrogenase and aminotransferases in blood serum.
Patients with increased iron content in the body should use ascorbic acid in minimal doses.
Patients on a low-sodium diet should not be given high doses of the drug.
Administration of ascorbic acid to patients with rapidly proliferating and intensively metastasizing tumors can enhance these processes. For patients undergoing chemotherapy, the drug should be prescribed no earlier than 1-3 days after chemotherapy (depending on the half-life of the anticancer drug), since there is no clinical data on a possible interaction.
Use during pregnancy or breastfeeding.
The minimum daily need for ascorbic acid in the II-III trimesters of pregnancy is about 60 mg. Ascorbic acid penetrates the placental barrier. 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 ascorbic disease as a "withdrawal" reaction. Therefore, during pregnancy, the drug should not be prescribed in increased doses, except in cases where the potential benefit to the mother exceeds the possible risk to the fetus.
The minimum daily need for 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 penetrates into breast milk. Theoretically, there is danger for the child when the mother uses high doses of ascorbic acid (during breastfeeding, it is not recommended to exceed the daily need for ascorbic acid). If it is necessary to prescribe increased doses of the drug, you should stop breastfeeding.
The ability to influence the speed of reaction when driving vehicles or other mechanisms.
The drug in recommended doses does not affect the ability to drive vehicles or work with other mechanisms.
Method of application and dosage.
It is prescribed intravenously as a jet or drip and intramuscularly.
It is injected intravenously as a jet over 1–3 minutes. For intravenous drip administration, a single dose of the drug is dissolved in 50–100 ml of 0.9% sodium chloride solution and administered by slow intravenous infusion at a rate of 30–40 drops per minute.
It is injected intramuscularly deep into the muscle.
Doses are prescribed individually, taking into account the nature and severity of the disease.
Adults and children over 12 years of age are usually prescribed 50–150 mg per day. In case of poisoning, the daily dose is increased to 500 mg. The maximum single dose is 200 mg, daily – 1 g.
Children under the age of 12 are prescribed 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 the age of 6 months - 30 mg, 6-12 months - 35 mg, 1-3 years - 40 mg, 4-10 years - 45 mg, 11-12 years - 50 mg. The maximum daily dose is 100 mg.
Special groups of patients. 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 (dialysis patients), 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.
Use of the drug in children, see in the section "How to use and doses".
Overdose.
Large doses of ascorbic acid can cause gastrointestinal disturbances, including diarrhea, and lead to hyperoxaluria and the formation of oxalate stones. Doses over 600 mg per day have a diuretic effect.
With intravenous administration in high doses, there may be a threat of termination of pregnancy.
Treatment: discontinuation of the drug, symptomatic therapy.
Adverse reactions.
Ascorbic acid, as a rule, is well tolerated, however, the development of such side effects is possible.
Disorders of the blood and lymphatic system: with long-term use in high doses - thrombocytosis, hyperprothrombinemia, thrombus formation, erythrocytopenia, neutrophilic leukocytosis.
Neurological disorders: headache, feeling of fatigue, with long-term use in high doses - sleep disturbance, increased excitability of the central nervous system.
Gastrointestinal disorders: nausea, diarrhea, stomach cramps.
Disorders from the urinary system: hyperoxalaturia; with long-term use in high doses - damage to the glomerular apparatus of the kidneys, formation of kidney stones from calcium oxalate.
Disorders of the skin and subcutaneous tissue: very rarely - skin rash, skin hyperemia, itching, redness, urticaria, swelling.
Metabolism disorders: hypervitaminosis C, with long-term use in high doses - suppression of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria) and glycogen synthesis, sodium and fluid retention, zinc and copper metabolism disorders.
Vascular disorders: decrease in permeability of capillaries, deterioration of tissue trophism; with long-term use in high doses - myocardial dystrophy, increased blood pressure, development of microangiopathy.
General disorders: chills, increased body temperature.
Pregnancy: with intravenous administration in high doses - the threat of abortion.
Disorders of the immune system: very rarely - anaphylactic shock.
