Active substanceGlibenclamideGlibenclamide
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    BIOSINTEZ, PAO     Russia
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  • Dosage form: & nbsppills
    Composition:
    Active substance: glibenclamide 5 mg;
    Excipients: lactose monohydrate (sugar milk) - 74,770 mg, potato starch - 62,373 mg, magnesium stearate - 1,200 mg, sodium carboxymethyl starch (sodium starch glycolate, primogel) - 3,000 mg, povidone (polyvinylpyrrolidone low molecular weight medical) - 3,630 mg, dye azorubin (E122) -0.027 mg.
    Description:

    Round, flat-cylindricalpink tablets with inclusionsin a lighter and darker tone, with a facet and a risk.

    Pharmacotherapeutic group:hypoglycemic agent for oral use of the second-generation sulfonylurea group.
    ATX: & nbsp

    A.10.B.B.01   Glibenclamide

    Pharmacodynamics:

    Glibenclamide has pancreatic and extra-pancreatic effects. It stimulates the secretion of insulin by lowering the threshold for glucose stimulation of pancreatic beta cells and increases sensitivity to insulin and the degree of binding to target cells that increases insulin release, enhances the insulin effect on glucose uptake by muscles and the liver, inhibits lipolysis in adipose tissues (extra-pancreatic effects). It operates in the second stage of insulin secretion. Has hypolipidemic action, reduces thrombogenic properties of blood.

    Hypoglycemic effect develops after 2 hours, reaches a maximum after 7-8 hours and lasts 12 hours. The drug provides a smooth increase in the concentration of insulin and a smooth decrease in the concentration of glucose in the blood plasma, which reduces the risk of hypoglycemic conditions. The activity of glibenclamide is manifested with the preserved endocrine function of the pancreas.

    Pharmacokinetics:

    When administered, absorption from the gastrointestinal tract is 48-84%. Time to reach the maximum concentration in the blood (TMax) - 1-2 hours, the volume of distribution is 9-10 liters. The connection with plasma proteins is 95-99%. Bioavailability of glibenclamide is 100. The placental barrier passes badly. Almost completely metabolized in the liver with the formation of two inactive metabolites, one of which is excreted by the kidneys, and the other - with bile. Half-life (T1/2) - from 3 to 10-16 hours.

    Indications:

    Diabetes mellitus type 2 with ineffectiveness of diet therapy.

    Contraindications:
    • type 1 diabetes mellitus;
    • diabetic ketoacidosis, diabetic precoma and coma;
    • condition after resection of the pancreas
    • severe dysfunction of the liver and / or kidney;
    • known from the history of hypersensitivity to glibenclamide and / or other derivatives of sulfonylurea, sulfonamides, diuretics containing a sulfonamide group in the molecule, and probenecid;
    • decompensation of carbohydrate metabolism in infectious diseases or after major surgical operations, when insulin therapy is indicated;
    • leukopenia;
    • intestinal obstruction, paresis of the stomach;
    • conditions, accompanied by a violation of food intake and development of hypoglycemia;
    • pregnancy and the period of breastfeeding;
    • hereditary intolerance to galactose, deficiency of lactase or glucose-galactose malabsorption.
    Carefully:With febrile syndrome, thyroid diseases (with impaired function), hypofunction of the anterior lobe of the pituitary gland or adrenal cortex, alcoholism, in elderly patients because of the danger of developing hypoglycemia.
    Pregnancy and lactation:
    Do not use during pregnancy. There is information about the appearance of defects in the auricle of the fetus, the development of fetal hypoglycemia, fetal death during the intake of glibenclamide during pregnancy.
    There is no information on the penetration of glibenclamide into breast milk. If you need to use the drug gOrefeeding should be discontinued.
    Dosing and Administration:

    Inside. Tablets should be taken whole, with a small amount of liquid for 20-30 minutes before meals. The dose of the drug is selected individually depending on the age, the severity of the course of diabetes, the concentration of blood glucose on an empty stomach and 2 hours after eating. The initial dose is 2.5 mg (1/2 tablet) per day.If necessary, the dose is gradually increased by 2.5 mg (1/2 tablet) per week until the carbohydrate metabolism is compensated. The maintenance daily dose of the drug is usually 5-10 mg (1-2 tablets). The maximum daily dose is 15 mg (3 tablets).

    A dose of more than 15 mg is used in rare cases and does not cause a significant increase in the hypoglycemic effect.

    For elderly patients, the initial dose is 1 mg per day.

    Multiplicity of taking the drug -1-3 times a day.

    Side effects:

    The most frequent undesirable effect in the treatment of Glybenklamidom is hypoglycemia. This condition can take a protracted character and contribute to the development of severe conditions up to a comatose, life-threatening patient or ending lethally. With diabetic polyneuropathy or with concomitant treatment with sympatholytic drugs (see section "Interaction with other drugs"), typical precursors of hypoglycemia may be mild or absent altogether.

    The reasons for the development of hypoglycemia can be: drug overdose; lack of evidence for his appointment; irregular eating; elderly patients; vomiting; diarrhea; large physical exertion; diseases,reducing the need for insulin (violations of liver and kidney function, hypofunction of the adrenal cortex, pituitary gland or thyroid gland); alcohol abuse, as well as interaction with other drugs.

    Symptoms of hypoglycemia are: a strong feeling of hunger, sudden profuse sweating, palpitations, pallor and a decrease in skin temperature, paresthesia of the oral mucosa, tremors, general anxiety, headache, pathological drowsiness, sleep disorders, feelings of fear, impaired coordination of movements, temporary neurologic disorders (eg, visual and speech disorders, manifestations of paresis and paralysis, or altered perception of sensations). With the progression of hypoglycemia, patients may lose self-control and consciousness, a predisposition to convulsions develops.

    Along with hypoglycemia are possible:

    On the part of the digestive system: rare nausea, eructation, vomiting, "metallic" taste in the mouth, a feeling of heaviness and fullness in the stomach, abdominal pain and diarrhea. In some cases, a temporary increase in the activity of "hepatic" enzymes (glutamino-oxaloacetic aminotransferase, glutamino-pyruvic aminotransaminase, alkaline phosphatase) in the blood serum, drug-induced hepatitis and jaundice.

    Skin allergic reactions: Rare, itchy skin, urticaria, redness of the skin, Quincke's edema, pinpoint bleeding to the skin, flaky rash on large skin surfaces and photosensitivity can rarely occur. Very rarely skin reactions can serve as the beginning of the development of severe conditions, accompanied by shortness of breath and lowering blood pressure until the onset of shock, threatening the life of the patient. Separate cases of severe generalized allergic reactions with skin rash, pain in the joints, fever, the appearance of protein in the urine and jaundice are described.

    On the part of the system of hemopoiesis: rarely there is thrombocytopenia or very rarely leukocytopenia, agranulocytosis. In isolated cases, hemolytic anemia or pancytopenia develops.

    Other side effects observed in isolated cases include a mild diuretic effect, the temporary appearance of a protein in the urine, impaired vision and accommodation, as well as an acute reaction of alcohol intolerance after its use,expressed by complications from the circulatory and respiratory organs (disulfiram-like reaction: vomiting, sensation of fever in the face and upper body, tachycardia, dizziness, headache).

    If any side effects occur, tell your doctor.

    Overdose:

    In case of an overdose, hypoglycemia may develop.

    With hypoglycemia of mild or moderate severity, glucose or a solution of sugar must be ingested.

    In the case of severe hypoglycemia accompanied by loss of consciousness, intravenously administered 40% solution of dextrose (glucose) or glucagon intravenously, intramuscularly, subcutaneously. After the restoration of consciousness, the patient needs to give food rich in carbohydrates, in order to avoid the re-development of hypoglycemia.

    Interaction:

    An increase in the hypoglycemic effect of Glibenclamide is observed with the simultaneous use of angiotensin converting enzyme inhibitors, anabolic agents, other oral hypoglycemic drugs (eg, acarbose, biguanides) and insulin, nonsteroidal anti-inflammatory drugs (NSAIDs), azapropion, beta adrenoblockers, quinine, quinolone derivatives,chloramphenicol, clofibrate, coumarin derivatives, disopyramide, fenfluramine, feniramidola, fluoxetine, monoamine oxidase inhibitors, miconazole, p-aminosalicylic acid, pentoxifylline (in large doses administered parenterally), perhexiline derivatives, pyrazolones, phenylbutazone, phosphamide (e.g., cyclophosphamide, ifosfamide, trofosfamide), probenecid, salicylates, sulfinpyrazone, sulfonamides, tetracyclines and tritvaline. The risk of hypoglycemia increases with alcohol abuse. Urine acidifying agents (ammonium chloride, calcium chloride) increase the effect of glibenclamide due to a decrease in the degree of its dissociation and increase its reabsorption.

    Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

    Along with the increase in hypoglycemic action, beta-blockers, clonidine, guanethidine and reserpine, as well as drugs with a central mechanism of action, can weaken the sensation of precursors of hypoglycemia.

    The hypoglycemic effect of glibenclamide may decrease with simultaneous use of barbiturates, isoniazid, cyclosporin, diazoxide,glucocorticosteroids, glucagon, nicotinate (in high doses), phenytoin, phenothiazines, rifampicin, saluretics, acetazolamide, sex hormones (eg, hormonal contraceptives), drugs of iodine-containing thyroid hormones, blockers of "slow" calcium channels, sympathomimetic agents, indomethacin and lithium salts . Chronic abuse of alcohol and laxatives can aggravate the violation of carbohydrate metabolism.

    Antagonists of H2-receptors may on one side weaken, and on the other, increase the hypoglycemic effect of glibenclamide. Pentamidine in a few cases can cause a strong decrease or increase in the concentration of glucose in the blood. The effect of coumarin derivatives may be enhanced or weakened.

    Special instructions:
    The drug should be taken regularly and, if possible, at the same time.
    It is necessary to carefully observe the regimen of the drug and the diet.
    The doctor should carefully consider the appointment of glibenclamide to patients with impaired liver and kidney function, as well as hypothyroidism of the thyroid gland, anterior pituitary gland or adrenal cortex.It is necessary to correct the dose of glibenclamide in case of physical and emotional overstrain, change in diet. During treatment it is not recommended to stay in the sun for a long time. Large surgical interventions and trauma, extensive burns, infectious diseases with febrile syndrome may require the abolition of oral glycopolic drugs and the administration of insulin.
    Patients should be warned about the increased risk of hypoglycemia in cases of taking ethanol, non-steroidal anti-inflammatory drugs, and fasting.
    When taking ethanol and ethanol-containing drugs, development of disulfiram-like reactions is possible: abdominal pain, nausea, vomiting, headache.
    Effect on the ability to drive transp. cf. and fur:At the beginning of treatment, during the selection of a dose, patients who are prone to developing hypoglycemia are not recommended to engage in activities requiring increased attention and speed of psychomotor reactions (including driving and handling mechanisms).
    Form release / dosage:
    Tablets 5 mg.
    Packaging:
    10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.
    1, 2, 3, 4 or 5 contour cell packs with instructions for medical use of the drug are placed in a pack of cardboard
    Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:

    2 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002056
    Date of registration:30.12.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp26.04.2017
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