Ascorutin

Instruction manual

For medical use of the drug

Ascorutin

(ascorutin)

Structure:

Active ingredients: ascorbic acid (vitamin C), rutoside;

1 tablet contains ascorbic acid (vitamin C) in terms of 100% substance

50 mg; rutoside trihydrate in terms of 100% anhydrous substance 50 mg;

excipients: white sugar, potato starch, corn starch, magnesium stearate, talc.

Dosage form.

Tablets.

The main physical and chemical properties: single-layer tablets, round in shape, light yellow with a greenish tint, the upper and lower surfaces of which are flat, the edges of the surfaces are chamfered. On the surface of the tablets blotches are allowed. A relatively uniform structure is visible on the fault under the magnifying glass.

Pharmacotherapeutic group.

Capillary stabilizing agents. bioflavonoids. rutoside, combinations. ath code c05s a51.

Pharmacological properties.

Pharmacodynamics

A combined drug whose effect is due to the effects of the components that make up its composition.

Rutoside (vitamin P) promotes the conversion of ascorbic acid to dehydroascorbic acid and prevents further transformation of the latter into diketogulonic acid. Therefore, most of the effects of rutoside are indirectly via ascorbic acid.

Rutoside in combination with ascorbic acid reduces the permeability and fragility of capillaries, strengthens the cell wall, reduces platelet aggregation, has an anti-inflammatory effect (including due to inhibition of the activity of hyaluronidase), antioxidant properties, and takes part in redox processes.

In addition, rutozide is characterized by such effects as a decrease in the exudation of the liquid part of the blood plasma and diapedesis of blood cells through the vascular wall; choleretic and mild antihypertensive effects.

In patients with chronic venous insufficiency, rutoside leads to a decrease in swelling and pain syndromes, trophic disorders, reduction or disappearance of paresthesia and seizures. Helps reduce the severity of side effects of radiation therapy (cystitis, enteroproctitis, dysphagia, cutaneous erythema), and also slows the progression of diabetic retinopathy.

Pharmacokinetics

Each vitamin that is part of the drug undergoes its own transformations. Ascorbic acid is rapidly absorbed mainly in the duodenum and small intestine. 30 minutes after ingestion, the content of ascorbic acid in the blood increases markedly, its uptake by tissues begins, and it first turns into dehydroascorbic acid, which penetrates through cell membranes without energy costs and quickly recovers in the cell. Ascorbic acid in tissues is almost exclusively intracellular; it is determined in three forms - ascorbic acid, dehydroascorbic acid and ascorbigen (bound ascorbic acid). It is distributed unevenly between organs. A lot of it is contained in the endocrine glands, especially in the adrenal glands, less - in the brain, kidneys, liver, in the heart and skeletal muscles. The content of ascorbic acid in leukocytes and platelets is higher than in blood plasma. It is metabolized and excreted by up to 90% of the kidneys in the form of oxalate, partially in free form.

Rutoside, absorbed in the digestive tract, promotes the transport and deposition of ascorbate. It is excreted unchanged and in the form of metabolites, mainly with bile and to a lesser extent - with urine.

The half-life is 10–25 hours.

Clinical characteristics.

Indications.

• Rutoside and ascorbic acid deficiency. as part of complex therapy of diseases, which are accompanied by an increase in vascular permeability. prevention of colds and flu symptoms. to enhance immunity.

Contraindications

• Hypersensitivity to any components of the drug. increased blood coagulability, thrombophlebitis, tendency to thrombosis. gout, urolithiasis with the formation of urate stones, cystinuria, hypokalemia and hypercalcemia, oxalaturia. diabetes. severe kidney disease. simultaneous use with sulfonamides or aminoglycosides. fructose intolerance, glucose-galactose malabsorption syndrome.

Interaction with other drugs and other types of interactions.

Acetylsalicylic acid, oral contraceptives: decreased absorption of the drug.

Ascorbic acid in a dose of ≥1 g increases the bioavailability of oral contraceptives (estrogens, including ethinyl estradiol), increases the concentration of salicylates in the blood, increasing their side effect (risk of crystalluria, effect on the gastric mucosa).

Acetylsalicylic acid, barbiturates, tetracyclines: increased urinary excretion of ascorbic acid.

Penicillin (including benzylpenicillin), tetracycline, iron preparations: high doses of ascorbic acid can increase their absorption and concentration in the blood.

Desferioxamine (deferoxamine): increased absorption of iron, its excretion in the urine; tissue toxicity of iron increases, especially cardiotoxicity, which can lead to decompensation of the circulatory system. Cardiac dysfunction (usually reversible after vitamin C withdrawal) was reported in patients with idiomatic hemochromatosis and thalassemia who used desferioxamine and high doses of ascorbic acid (more than 500 mg per day). Such a combination in this category of patients requires caution and careful monitoring of cardiac function. Ascorbic acid can be taken only 2 hours after the injection of despherioxamine.

Heparin, indirect anticoagulants, phenothiazines, fluphenazine, sulfonamide drugs, aminoglycoside antibiotics: a decrease in the effectiveness of these drugs.

Cyclosporin A: may decrease its bioavailability.

B vitamins: mutual enhancement of the therapeutic effect. High doses of ascorbic acid poured on vitamin B resorption₁₂.

Corticosteroids, paracetamol: the half-life of the latter increases with the use of high doses of ascorbic acid (this interaction has no clinical consequences when taking therapeutic doses).

Calcitonin: the rate of absorption of ascorbic acid increases.

Amphetamine: its renal excretion increases with the use of high doses of ascorbic acid.

Aluminum antacids: it should be borne in mind that ascorbic acid promotes the absorption of aluminum from the intestine, it is possible to increase the elimination of aluminum in the urine. The combined use of antacids and ascorbic acid is not recommended, especially in patients with renal failure.

With prolonged use (more than 4 weeks), the drug should not be prescribed simultaneously with cardiac glycosides, antihypertensive drugs or non-steroidal anti-inflammatory drugs, since it can enhance their effect.

Ascorbic acid enhances the excretion of oxalates in the urine, thus increasing the risk of formation of oxalate stones in the urine.

The combined use of very high doses of ascorbic acid with amygdalin (complementary medicine) may increase the risk of cyanide toxicity.

Smoking, alcohol: reduce the concentration of ascorbate in blood plasma.

Disulfiramine: prolonged use of large doses of ascorbic acid inhibits the disulfiram-alcohol reaction.

Large doses of ascorbic acid (more than 2 g / day) can affect the results of biochemical determinations of the level of creatinine, uric acid and glucose in blood and urine samples, and determine the level of inorganic phosphates, liver enzymes, and bilirubin in the blood. Fecal occult blood screening test may be false negative.

The simultaneous use with alkaline drink, the use of fresh fruit or vegetable juices reduces the absorption of ascorbic acid.

Features of the application.

The simultaneous use of the drug with alkaline drink, fresh fruit or vegetable juices reduces the absorption of vitamin C. absorption of ascorbic acid may be impaired with intestinal dyskinesia, enteritis and achilia.

Since ascorbic acid increases iron absorption, its use in high doses can be dangerous for patients with hemochromatosis, thalassemia, polycythemia, leukemia and sideroblastic anemia. Patients with a high iron content in the body should use the drug in minimal doses.

Ascorbic acid should be used with caution to treat patients with a deficiency of glucose-6-phosphate dehydrogenase, patients with a history of kidney disease.

With prolonged use of high doses of ascorbic acid, kidney function, blood pressure, and pancreatic function should be monitored.

With urolithiasis, the daily dose of ascorbic acid should not exceed 1 g.

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

Since ascorbic acid has a mild stimulating effect, it is not recommended to take the drug at the end of the day.

Due to the content of ascorbic acid in the medicinal product, it can change the results of a number of laboratory tests (see the section “Interaction with other medicines and other types of interactions”).

The drug contains sugar, which should be considered for patients with diabetes mellitus.

Use during pregnancy or lactation.

During pregnancy, the drug can be used only after consulting a doctor. the drug is contraindicated in the first trimester of pregnancy. in the third and third trimesters of pregnancy or during lactation, the drug should be prescribed taking into account the benefit / risk ratio for the woman and the fetus / child under conditions of strict adherence to the recommended doses and duration of treatment.

According to the available clinical data on the use by pregnant women of rutin and vitamin C in the form of separate drugs, no significant risks to the fetus were identified. However, appropriate and well-controlled clinical trials of the safety of using combination preparations containing vitamin C and rutin were not performed for pregnant women.

There are no reports of embryotoxicity of rutin or its penetration into breast milk.

Vitamin C is excreted in breast milk, but doses, even 10 times higher than the recommended daily dose, did not lead to a significant increase in its concentration in breast milk.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

There is no data on the effect of ascorutin on the ability to drive vehicles or work with other mechanisms.

Dosage and administration.

The drug should be administered orally after a meal. tablets should be swallowed whole with a little water.

For therapeutic purposes, appoint 1 tablet 2-3 times a day for adults; children from 3 years old - up

1 tablet 2 times a day. As a prophylactic, the drug is recommended: for adults - 1 tablet 2 times a day, for children from 3 years old - 1 tablet per day.

The duration of the course of treatment is 3-4 weeks (depending on the nature of the disease and the effectiveness of the treatment).

Children.

The drug is prescribed for children from 3 years.

Overdose.

Symptoms: epigastric pain, nausea, vomiting, diarrhea, itching and skin rash, increased irritability of the nervous system, headache, increased blood pressure, thrombosis. amplification of adverse reactions is possible.

An overdose can lead to changes in the renal excretion of ascorbic and uric acids during urine acetylation with the risk of precipitation of oxalate calculi.

With prolonged use in large doses, inhibition of the function of the insular apparatus of the pancreas, impaired renal function.

Ascorbic acid in doses exceeding 3 g / day can lead to the development of acidosis or hemolytic anemia in some individuals with a deficiency of glucose-6-phosphate dehydrogenase.

Treatment: gastric lavage, the use of sorbents, symptomatic treatment.

Adverse Reactions

From the central nervous system: headache, feeling tired, with prolonged use of high doses - sleep disturbances, increased excitability of the central nervous system.

On the part of the kidneys and urinary tract: urine acidification, hyperoxalaturia in patients at risk at doses exceeding 1 g / day; with prolonged use in high doses - damage to the glomerular apparatus of the kidneys, the formation of urate and oxalate stones in the urinary tract, renal failure. Doses of ascorbic acid more than 600 mg / day have a diuretic effect.

On the part of the blood system: with prolonged use of high doses - thrombocytosis, hypertrombinemia, thrombosis, erythrocytopenia, neutrophilic leukocytosis, hemolytic anemia in some individuals with a deficiency of glucose-6-phosphate dehydrogenase.

From the side of metabolism: hypervitaminosis C, deterioration of tissue trophism, with prolonged use of high doses - inhibition of the function of the pancreatic insular apparatus (hyperglycemia, glucosuria) and glycogen synthesis, sodium and fluid retention, impaired zinc and copper metabolism.

From the cardiovascular system: with prolonged use in high doses - myocardial dystrophy, increased blood pressure, the development of microangiopathies.

From the digestive system: with prolonged use of high doses - irritation of the mucous membrane of the digestive tract, heartburn, stomach cramps, nausea, vomiting, diarrhea.

From the side of the immune system: hypersensitivity reactions, incl. skin hyperemia, skin rash, eczema, itching, Quinckes edema, urticaria, anaphylactic shock, respiratory hypersensitivity reactions.

Shelf life.

4 years.

Storage conditions.

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

Keep out of the reach of children.

Packaging.

10 tablets in a blister.

10 tablets in a blister; 5 blisters per pack.

10 tablets in a blister; 80 blisters in a box with cardboard.

50 tablets in containers; 1 container per pack.

Vacation category.

Over the counter.

Manufacturer.

Chao "technologist."

The location of the manufacturer and his address of the place of business.

Ukraine, 20300, Cherkasy region, Uman city, street old proreznaya, house 8.