Pharmacodynamics. Ascoin is a combined preparation containing two preparations: water-soluble vitamin C - ascorbic acid and a trace element - zinc.
The mechanism of action of ascorbic acid. Ascorbic acid (vitamin C) as an antioxidant, metabolic and regulating redox processes agent increases the adaptive capabilities of the body, enhances its resistance to infections. It has anti-inflammatory and anti-allergic effects. Maintains the colloidal state of the intercellular substance and normal capillary permeability (inhibits hyaluronidase). Participates in the regulation of redox processes, the metabolism of carbohydrates, aromatic amino acids, pigments and cholesterol, in the synthesis of steroid hormones, catecholamines, blood coagulation. Strengthens collagen synthesis, stimulates regeneration processes, normalizes capillary permeability. By activating respiratory enzymes in the liver, it enhances its detoxification and protein-forming function, increases the synthesis of collagen and prothrombin. Improves bile secretion, restores the exocrine function of the pancreas. It inhibits the release and accelerates the degradation of histamine, inhibits the formation of prostaglandins and other mediators of inflammation and anaphylaxis. Regulates immunological reactions (activates the synthesis of antibodies, the C3 component of complement, interferon), promotes phagocytosis, increases the body's resistance to infections.
The mechanism of action of zinc. Zinc is a structural component of biological membranes, cell receptors, proteins, and is part of more than 200 enzymatic systems. Participates in the reactions of immune and antioxidant defense, hematopoiesis, synthesis of amino acids, in the preservation and transmission of genetic information. As a component of the retinol-transporting protein, zinc, together with vitamins A and C, prevents the occurrence of immunodeficiencies, stimulating antibody synthesis and exerting antiviral effect.
Zinc promotes cell growth and development, the proper functioning of the immune system and the provision of an immunological response, twilight vision, taste and smell. Influences the maintenance of normal levels of vitamin A in the blood, increases the time of action of insulin and facilitates its accumulation. In inflammatory conditions of the skin, it has a preventive and therapeutic effect.
Zinc deficiency causes difficulties in concentration and memory, poor appetite and distorted taste, decreased cellular and humoral immunity, poor wound healing, night blindness, carbohydrate imbalance, hypercholesterolemia, hypertension, mental and brain disorders, prostatic hypertrophy, impaired pregnancy, growth inhibition and hypogonadism in children and, in many respects, dermatological disorders (senile alopecia, alopecia areata, acne). In high doses, zinc inhibits copper absorption. Also, zinc deficiency increases the absorption of toxic cadmium.
Pharmacokinetics
For ascorbic acid. Absorption. Ascorbic acid is absorbed mainly in the upper part of the small intestine by active sodium-dependent transport. In the presence of ascorbic acid in a high concentration, its absorption also occurs through passive diffusion. With an increase in the dose of ascorbic acid taken orally, from 1 to 12 g, the specific gravity of the preparation that is absorbed decreases (from about 50 to 15%). The absorption of vitamin C can be impaired in case of gastrointestinal diseases (gastritis, ulcers, constipation, diarrhea, helminthic infestation, giardiasis), the use of fresh fruit and vegetable juices, and alkaline drinks.
Distribution. About 24% of ascorbic acid binds to blood plasma proteins. As a rule, with sufficient intake of ascorbic acid, its concentration in blood plasma is 10 mg / l (60 μmol / l). A decrease in the concentration of ascorbic acid in blood plasma of 4 mg / l (20 μmol / l) indicates insufficient intake of vitamin C.
Metabolism. Ascorbic acid is metabolized in part via dehydroascorbic acid to oxalic acid and other products. Provided that ascorbic acid enters the body in excessive quantities, it is excreted from the body unchanged with urine and feces. The urine also contains a metabolite of ascorbic acid - ascorbic acid-2-sulfate. Smoking and abuse of ethyl alcohol accelerates the breakdown of ascorbic acid (conversion into inactive metabolites), dramatically reducing its reserves in the body. The physiological level of the ascorbic acid depot in the body is about 1.5 g. It is deposited in the posterior part of the pituitary gland, adrenal cortex, epithelium of the eye, intermediate cells of the seminal glands, ovaries, liver, brain, spleen, pancreas, lungs, kidneys, intestinal wall, heart , muscles, thyroid gland. From blood plasma it easily penetrates into leukocytes, platelets and almost all tissues.
Excretion. Unchanged ascorbate and metabolites are excreted by the kidneys, intestines, and also with sweat and pass into breast milk. T½ of ascorbic acid depends on the route of administration, the amount and rate of its absorption. After ingestion of ascorbic acid in a dose of 1 g, T½ is about 13 hours. If doses of ascorbic acid are taken up to 3 g / day, it is excreted from the body with urine. When taking doses exceeding 3 g / day, excretion occurs both in the urine and in the feces (unchanged).
For zinc. Absorption. Zinc is absorbed along the entire small intestine. Provided that zinc is taken on an empty stomach and in the form of an aqueous solution, the amount of the preparation that is absorbed reaches 41-79%. When zinc is taken with food, the amount of the preparation that is absorbed is 10–40%.
Distribution and metabolism. Cmax of zinc in blood plasma is achieved 2 hours after taking the preparation. In the body, zinc accumulates mainly in leukocytes and erythrocytes, as well as in muscles, bones, skin, kidneys, liver, pancreas and prostate glands, retina. 60% of zinc binds to albumin, 30–40% - with alpha-2-macroglobulin, 1% - with amino acids, mainly with histidine and cysteine.
Excretion. Zinc is excreted from the body mainly in feces (90%), to a lesser extent in urine and sweat. Calcium supplements and calcium-rich diets (dairy products) have the ability to reduce zinc absorption by up to 50%, and caffeine and alcohol are more effective in removing zinc from the body.
As part of complex treatment for conditions and diseases that are caused or accompanied by zinc deficiency and hypovitaminosis of ascorbic acid: tendency to colds and infectious diseases; diseases accompanied by a decrease in immunity; bleeding (uterine, pulmonary, nasal, with radiation sickness), overdose of anticoagulants, increased permeability and fragility of blood vessels; liver diseases (hepatitis a, chronic hepatitis, cirrhosis); nephropathy of pregnant women; dystrophy, bone fractures and wounds that do not heal for a long time; connective tissue damage (rheumatoid arthritis, systemic lupus erythematosus, scleroderma); disorders of carbohydrate and fat metabolism; dysfunction of the endocrine glands, Addison's disease; hypofunction of the prostate gland; atherosclerosis; ba.
Ascocin is taken orally after meals; the tablet is chewed and washed down with a little water. the duration of treatment depends on the nature and course of the disease.
Adults - 1 tablet once a day.
The duration of treatment is determined by the doctor depending on the nature and course of the disease.
With severe hypovitaminosis and the treatment of infectious diseases for adults, it is recommended to take 1 tablet 2 times a day for 5-7 days.
Hypersensitivity to the components of the preparation. tendency to thrombosis; thrombophlebitis. diabetes. urolithiasis, severe kidney disease, severe renal failure. phenylketonuria. with extreme caution should be prescribed to patients with impaired iron metabolism (hemosiderosis, hemochromatosis, thalassemia).
From the digestive tract: irritation of the mucous membrane of the digestive tract, dyspepsia, nausea, vomiting, heartburn, abdominal pain, abdominal discomfort, diarrhea, gastritis, metallic taste in the mouth.
From the immune system: allergic reactions, including anaphylactic, anaphylactic shock, hypersensitivity reactions, including asthmatic syndrome, bronchospasm, cardiorespiratory distress, skin rashes, pruritus, eczema, urticaria, angioedema.
From the nervous system: increased excitability, increased fatigue, sleep disturbance, headache.
From the urinary system: damage to the glomerular apparatus of the kidneys, renal failure, crystalluria, the formation of urate, cystine and oxalate stones in the kidneys and urinary tract.
On the part of the skin and subcutaneous tissue: rash, itching.
From the side of the blood system: thrombocytosis, thrombosis, hemolytic anemia, hyperprothrombinemia, erythrocytopenia, neutrophilic leukocytosis; in patients with deficiency of glucose-6-phosphate dehydrogenase of blood cells, it can cause hemolysis of erythrocytes; hematological disorders due to copper deficiency, including leukopenia (fever, chills, sore throat), neutropenia (ulcers in the mouth and throat), sideroblastic anemia (feeling tired, weak).
From the endocrine system: damage to the insular apparatus of the pancreas (hyperglycemia, glucosuria) and impaired glycogen synthesis up to the development of diabetes mellitus.
From the side of the cardiovascular system: hypertension, myocardial dystrophy.
From the side of metabolism: metabolic disorders of zinc, copper.
Others: sensation of heat.
Associated with ascorbic acid. Because vitamin C is mildly stimulating, it is not recommended to take this preparation at the end of the day.
Due to the stimulating effect of ascorbic acid on the formation of corticosteroid hormones, when used in high doses, it is necessary to control renal function and blood pressure.
The preparation should be used with caution in case of increased blood clotting.
It is necessary to prescribe with caution to patients:
with a deficiency of glucose-6-phosphate dehydrogenase (high doses of ascorbic acid can provoke hemolytic anemia);
with a history of nephrolithiasis (risk of hyperoxaluria and precipitation of oxalates in the urinary tract after taking high doses of ascorbic acid).
Long-term use of high doses of ascorbic acid can accelerate its own metabolism, resulting in paradoxical hypovitaminosis after discontinuation of treatment. Do not exceed the recommended dose.
Should not be used concomitantly with other preparations containing vitamin C.
The preparation should be used with caution in case of polycythemia, leukemia.
The absorption of ascorbic acid can be changed in case of impaired intestinal motility, enteritis or achilia (inhibition of gastric secretion).
It should be borne in mind that the use of vitamin C in high doses can change some indicators of laboratory tests (blood glucose, bilirubin, transaminases, uric acid, creatinine, inorganic phosphates). There may be a negative test result for the presence of occult blood in the stool.
Zinc related. When using preparations containing zinc, the risk of copper deficiency should be considered. A diet rich in fibrin (such as bran), phosphates (such as dairy), whole grains, and phytinates reduces zinc absorption due to the formation of complexes. The break between the use of the above products and the intake of zinc preparations should be at least 2 hours.
The preparation contains the dye sunset yellow FCF (E110), which can cause allergic reactions aspartame (E951), which is a phenylalanine derivative, which is dangerous for patients with phenylketonuria.
Use during pregnancy and lactation. Pregnancy. Since controlled studies during pregnancy and controlled studies on animals have not been carried out, the preparation can only be used if, in the opinion of the doctor, the benefit to the mother outweighs the potential risk to the fetus.
Lactation. Ascorbic acid and zinc pass into breast milk. Therefore, during the period of breastfeeding, the preparation should be used under the supervision of a physician.
Children. Ascocin is not used in children.
The ability to influence the reaction rate when driving or working with other mechanisms. There is no indication that the preparation can adversely affect drivers or people who work with complex equipment.
Interactions related to ascorbic acid. with the simultaneous use of ascorbic acid enhances the absorption of iron, penicillin, ethinyl estradiol in the gastrointestinal tract. a similar effect applies to aluminum, therefore, this must be taken into account when simultaneously treating with antacids containing aluminum.
Ascorbic acid, with simultaneous use, reduces the effectiveness of heparin, anticoagulants.
The absorption of ascorbic acid is reduced with the simultaneous use of oral contraceptives, the use of fruit or vegetable juices, and alkaline drinks. The simultaneous intake of vitamin C and deferoxamine increases the tissue toxicity of iron, especially in the heart muscle, which can lead to decompensation of the circulatory system. Vitamin C can only be taken 2 hours after deferoxamine injection. Long-term use of high doses of ascorbic acid reduces the effectiveness of disulfiram treatment.
High doses of the preparation reduce the effectiveness of tricyclic antidepressants, neuroleptics - phenothiazine derivatives, tubular reabsorption of amphetamine, and disrupt the excretion of mexiletine by the kidneys.
Ascorbic acid increases the total clearance of ethyl alcohol. Quinolone preparations, calcium chloride, salicylates, tetracycline, corticosteroids, with prolonged use, reduce the reserves of ascorbic acid in the body.
At high doses, ascorbic acid affects the resorption of vitamin B12.
Vitamin C increases urinary excretion of oxalate, thus increasing the risk of urinary oxalate stones. Vitamin C increases the risk of crystalluria when treated with salicylates.
Zinc-related interactions
Tetracycline. Zinc reduces the absorption of tetracyclines and inhibits the absorption of copper (in the case of high doses of zinc), so the preparation should be used no earlier than 2 hours after taking these preparations.
Copper preparations. High doses of zinc can inhibit the absorption of copper (zinc salts should be used no earlier than 2 hours after taking these preparations).
Thiazide diuretics increase the excretion of zinc in the urine.
A diet rich in fibrin (such as bran), phosphates (such as dairy products), whole grains, and phytinates reduces zinc absorption due to the formation of complexes, so there should be at least 2 hours between eating the above foods and taking zinc supplements.
Folic acid slightly interferes with zinc absorption.
High doses of iron when administered orally reduce zinc absorption (the preparation should be used no earlier than 2 hours after taking these preparations).
Penicillamine and other chelating agents reduce zinc absorption (the preparation should be used no earlier than 2 hours after taking these preparations).
When used with Ascocin, multivitamin preparations with minerals that include zinc, one should remember about the possibility of an overdose.
Quinolones. Zinc reduces the absorption of quinolone-containing antibiotics and fluoroquinolones.
There is no evidence that this preparation can cause an overdose when used as recommended.
The intake of vitamin C and zinc from all sources should be considered.
Clinical signs and symptoms, laboratory results and consequences of overdose are very different, depending on individual susceptibility and circumstances.
Common manifestations of vitamin C and / or zinc overdose may include an increased incidence of gastrointestinal distress, including diarrhea, nausea, and vomiting.
If these symptoms occur, you should stop taking the preparation and consult a doctor.
Specific clinical manifestations of overdose may include:
vitamin C. In acute or chronic overdose of vitamin C, plasma and urine oxalate levels can be significantly increased. In some cases, this can lead to hyperoxaluria, calcium oxalate crystalluria, calcium oxalate deposition, renal calculi, tubulointerstitial nephropathy, and acute renal failure. Individuals with mild to moderate renal impairment may be susceptible to these toxic effects of vitamin C at lower doses and should consult a physician prior to taking the preparation.
An overdose of vitamin C can lead to oxidative hemolysis or disseminated intravascular coagulation in patients with glucose-6-phosphate dehydrogenase deficiency;
zinc. Zinc overdose can cause irritation and erosion of the gastrointestinal mucosa, acute tubular necrosis, interstitial nephritis, copper deficiency, sideroblastic anemia, and myeloneuropathy.
If you suspect an overdose of the preparation, you should stop taking it and consult a doctor for the treatment of clinical manifestations. Vitamin C is removed by hemodialysis.
At a temperature not higher than 25 ° C.
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