Active substanceGlibenclamideGlibenclamide
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  • Glibenclamide
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  • Glibenclamide
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  • Glibenclamide
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    BIOSINTEZ, PAO     Russia
  • Glibenclamide
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  • Glimidstad®
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  • Dosage form: & nbsppills
    Composition:

    Active ingredient: glibenclamide - 3.50 mg.

    Other ingredients, lactose monohydrate - 129.25 mg, corn starch - 34.30 mg, povidone-K25 - 2.52 mg, magnesium stearate - 0.43 mg.

    The theoretical weight of the tablet is 170.00 mg.

    Description:

    Round flat tablets of white color, 8 mm in diameter, on the one side of risk and marking "G4", on the other hand - marking "STADA".

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

    A.10.B.B.01   Glibenclamide

    Pharmacodynamics:

    Has pancreatic and extra-pancreatic effects. It stimulates insulin secretion by lowering the threshold for stimulation of pancreatic beta cells by glucose, increases insulin sensitivity and its binding to target cells, increases insulin release, enhances insulin effect on glucose uptake by muscles and liver, inhibits lipolysis in adipose tissue. 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 glucose in the plasma, which reduces the risk of hypoglycemic conditions. The activity of glibenclamide is manifested with the preserved endocrine function of the pancreas to synthesize insulin.

    Pharmacokinetics:

    At ingestion, absorption from the gastrointestinal tract is 48-84%. The time to reach the maximum concentration is 1-2 hours, the volume of distribution is 9-10 liters. The connection with plasma proteins is 95%.Bioavailability of glibenclamide is 100%, which allows you to take the drug almost before eating. 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 is 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 violations of liver function;
    • severe renal dysfunction;
    • known from the history of hypersensitivity to glibenclamide and / or other derivatives of sulfonylureas, sulfonamides, diuretic drugs containing a sulfonamide group in the molecule, and probenecid, t. there may be cross reactions;
    • 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;
    • lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the preparation contains lactose);
    • children's age till 18 years.
    Carefully:

    Feverish syndrome, adrenal insufficiency, thyroid disease (with impaired function), hypofunction of the anterior lobe of the pituitary gland or adrenal cortex, alcoholism, elderly age (due to the risk of hypoglycemia).

    Pregnancy and lactation:

    The use of the drug is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    The dose is determined by the doctor and depends 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 daily dose ranges from 1.75 mg to 10.5 mg.

    At the initial stage of treatment and when transferring the patient to this drug from other oral hypoglycemic agents, it is recommended to increase the dose gradually. Treatment is advisable to begin with the appointment of 1.75 mg of Glimidstad® (1/2 Glimidstad® tablets 3.5 mg) once a day. This dose can be gradually increased at intervals of several days to 1 week, until a therapeutic dose is reached. The maximum effective dose is 10.5 mg of Glimidstad®.

    When replacing hypoglycemic drugs with a similar type of action glibenclamide appoint according to the scheme given above, and the previous drug is immediately canceled.

    A daily dose of up to 2 Glimidstad® tablets is taken without chewing, with a small amount of liquid 1 time per day before breakfast. At a higher daily dose, it is recommended to divide it into 2 divided doses in a ratio of 2: 1 in the morning and in the evening.

    If you miss a drug, you can not take its double dose in return for the missed dose. Gliwidstad® can be used in combination with other hypoglycemic agents, incl. with insulin.

    Side effects:

    Classification of undesirable adverse reactions (NDP) according to the frequency of development: Often: ≥1/10; often: ≥1 / 100 and <1/10; infrequently: ≥1 / 1000 and <1/100; rarely: ≥1 / 10000 and <1/1000; very rarely: < 1/10000 assignments or frequency is not known (can not be calculated based on available data).

    Disorders from the metabolism and nutrition: often - hypoglycemia, weight gain.

    The most common undesirable effect of the drug is hypoglycemia. It can take a protracted character and promote 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; application is not according to the indication; irregular eating; elderly patient; vomiting, diarrhea; large physical exertion; diseases that reduce 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, pale skin, paresthesia in the mouth, tremors, general anxiety, headache, pathological drowsiness, sleep disorders, feelings of fear, impaired coordination of movements, temporary neurological disorders (eg, visual and speech disorders, manifestations of paresis or paralysis, or altered perception of sensations).With the progression of hypoglycemia, patients may lose self-control and consciousness. Often such a patient has moist cold skin and a predisposition to convulsions.

    Violations of the blood and lymphatic system: rarely - thrombocytopenia; rarely - leukocytopenia, erythrocytopenia, granulocytopenia (up to agranulocytosis); in isolated cases - hemolytic anemia, pancytopenia.

    Disturbances on the part of the organ of sight: rarely - visual impairment and accommodation (these phenomena are more often observed at the beginning of treatment due to changes in blood glucose level).

    Disorders from the gastrointestinal tract: infrequently - nausea, discomfort in the stomach, a feeling of heaviness and overflow in the stomach, vomiting, abdominal pain, diarrhea, belching, "metallic" taste in the mouth.

    Disturbances from the skin and subcutaneous tissues: not often - itching, urticaria, skin rash (including flaky), photosensitization, skin hyperemia, Quincke's edema, purpura; rarely - generalized allergic reactions with skin rash, pain in the joints, fever, the appearance of protein in the urine and jaundice; rarely - life-threatening allergic vasculitis.

    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.

    Disturbances from the liver and bile ducts: rarely - a temporary increase in the activity of "hepatic" enzymes (alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase), drug hepatitis, intrahepatic cholestasis.

    Other: rarely - increased diuresis, transient proteinuria, hyponatremia, acute reaction of alcohol intolerance after its use, expressed by complications from the circulatory and respiratory organs (disulfiramoid-like reaction: vomiting, sensation of fever of the face and upper body, tachycardia, dizziness, headache).

    Overdose:
    Symptoms: hypoglycemia (hunger, increased sweating, severe weakness, palpitation, tremor, anxiety, headache, dizziness, insomnia, irritability, depression, cerebral edema, speech and vision impairment, impaired consciousness), hypoglycemic coma.
    Treatment: if the patient is conscious, take sugar inside, lose consciousness - intravenously inject dextrose (intravenously bolus - 50% dextrose, then 10% solution), 1-2 mg glucagon, subcutaneously, intramuscularly or intravenously, diazoxide 30 mg intravenously for 30 min, monitoring the glucose concentration every 15 minutes, as well as determining pH, urea nitrogen, creatinine, electrolytes in the blood. After the restoration of consciousness it is necessary to give the patient food that is rich in easily assimilated carbohydrates (in order to avoid the re-development of hypoglycemia). With edema of the brain - mannitol and dexamethasone.
    Interaction:
    Angiotensin converting enzyme inhibitors (captopril, enalapril), H2-histamine receptor blockers (cimetidine), antifungal medicines (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, azapresene, oxyphenbutazone), fibrates (clofibrate, bezafibrate), antituberculous (ethionamide) medicines, salicylates, coumarinic anticoagulants, anabolic steroids, beta-blockers, monoamine oxidase inhibitors, long-acting sulfonamides, cyclophosphamides, biguanides, chloramphenicol, fenfluramine, acarbose, fluoxetine, guanethidine, pentoxifylline, tetracycline, theophylline, tubular secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine, insulin, allopurinol enhance the effect. Weaken the effect of barbiturates, glucocorticosteroids, adrenomimetics (epinephrine, clonidine), antiepileptic drugs (phenytoin), blockers of "slow" calcium channels, inhibitors of carbonic anhydrase (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, ritodrin, salbutamol, terbutaline, glucagon, rifampicin, iodine-containing thyroid hormones, lithium salts, in high doses - a nicotinic acid, chlorpromazine, oral contraceptives and estrogens. Urine acidifying drugs (ammonium chloride, calcium chloride, ascorbic acid in high doses) enhance the effect by reducing the degree of dissociation and increasing the reabsorption of glibenclamide.
    Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.
    Special instructions:
    It is necessary to regularly monitor the blood glucose in the blood on an empty stomach and after eating, the daily curve of the glucose content in the blood.
    Large surgical interventions and trauma, extensive burns, infectious diseases with febrile syndrome may require the abolition of oral hypoglycemic drugs and the administration of insulin.
    Patients should be warned about the increased risk of hypoglycemia in cases of taking ethanol (including the development of disulfiram-like reactions: abdominal pain, nausea, vomiting, headache), non-steroidal anti-inflammatory drugs, and fasting.
    During treatment it is not recommended to stay in the sun for a long time.
    Dose correction is necessary in case of physical and emotional overstrain, changes in diet.
    Clinical manifestations of hypoglycemia can be masked when taking beta-blockers, clonidine, reserpine, guanetidine.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Tablets 3,5 mg.

    Packaging: For 10 tablets in a blister of PVC / aluminum foil. 3 or 12 blisters with instructions for medical use of the drug in a cardboard bundle.
    Storage conditions:

    In dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years. Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014128 / 01
    Date of registration:01.04.2011
    Expiration Date:Unlimited
    Date of cancellation:2017-09-26
    The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany
    Manufacturer: & nbsp
    Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia
    Information update date: & nbsp26.09.2017
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