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

    Active substance: glibenclamide 5 mg;

    Excipients: corn starch 68.0 mg, talc 2.0 mg, magnesium stearate 1.0 mg, lactose monohydrate 36.75 mg, silicon dioxide colloidal anhydrous 2.0 mg, sodium carboxymethyl starch 2.0 mg, methyl parahydroxybenzoate 0.13 mg, propyl parahydroxybenzoate 0.013 mg, dye crimson [Ponso 4R] 0.02 mg, dye sunset sunset yellow 0.02 mg.

    Description:

    Tablets of light red color, flat-cylindrical, with risk from one side.

    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. Stimulates insulin secretion by lowering the threshold of stimulation of pancreatic beta cells by glucose, increases insulin sensitivity and the degree of its binding to target cells, increases insulin release, enhances insulin action 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 the concentration of 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:

    When administered, 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 95-99%.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, diuretics 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;
    • state,accompanied by a violation of food intake and development of hypoglycemia;
    • pregnancy and the period of breastfeeding.
    Carefully:

    When:

    • febrile syndrome;
    • thyroid disease (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.
    Dosing and Administration:

    The drug is taken orally. The dose of the drug is selected individually.

    The initial dose is 2.5 mg (½ tablets) per day. If necessary, the dose is gradually increased by 2.5 mg tablets) a week before the achievement of compensation for carbohydrate metabolism.

    The maintenance daily dose of the drug is usually 5-10 mg (1-2 tablets). The maximum daily dose is 15 mg (3 tablets). Multiplicity of administration 1-3 times a day.

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

    Side effects:

    The most common undesirable action 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.In diabetic polyneuropathy or concomitant medication sympatholytic agents (see. The section "Interaction with other drugs") typical precursors of hypoglycemia can be quite weakly expressed or absent. The reasons for the development of hypoglycemia can be: drug overdose; incorrect reading; irregular eating; elderly patients; 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 medicines (see section "Interaction with other drugs"). Symptoms of hypoglycemia include: strong hunger, sudden sweating, palpitations, pallor, paresthesia in the mouth, trembling, general restlessness, headache, abnormal sleepiness, sleep disturbances, anxiety, impaired motor coordination, temporary neurological disorders (eg, disorders of vision and speech,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.

    Along with hypoglycemia are possible:

    Disorders from 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 (alkaline phosphatase, glutamic-oxaloacetic aminotransferase, glutamine-pyruvic aminotransferase) in the blood serum was described; drug hepatitis and jaundice.

    Rarely appear skin allergic reactions: rash, itching of the skin, urticaria, reddening of the skin, Quincke edema, pinpoint bleeding in the skin, flaky rash on large skin surfaces and increased photosensitivity. 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 are described severe generalized allergic reactions with a skin rash, pains in the joints, fever, the appearance of protein in the urine and jaundice.

    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.

    To other side effects, observed in a few cases, include: a weak diuretic effect, a temporary appearance of protein in the urine, visual and accommodation discomforts, and an acute reaction of alcohol intolerance after its use, expressed by complications from the circulatory and respiratory organs (disulfiram-like reaction: vomiting, fever and the upper part of the trunk, tachycardia, dizziness, headache).

    If any of the side effects indicated in the manual are aggravated, or any other side effects not indicated in the instructions are noted, you should inform the doctor immediately.

    Overdose:

    In case of an overdose, hypoglycemia may develop.

    With mild or moderate hypoglycemia, glucose or sugar solution is taken orally.

    In the case of severe hypoglycemia (loss of consciousness), a 40% solution of dextrose (glucose) or intravenously 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 glycemic effect of Glybex is observed with simultaneous use of angiotensin converting enzyme inhibitors, anabolic agents, other oral hypoglycemic drugs (eg acarbose, biguanides) and insulin, nonsteroidal anti-inflammatory drugs (NSAIDs), beta-blockers, quinine, quinolone derivatives, chloramphenicol, clofibrate, derivatives coumarin, disopyramide, fenfluramine, pheniramidol, fluoxetine, monoamine oxidase inhibitors, miconazole, para-aminosalicylic acid slots, pentoxifylline (in large doses administered parenterally), perhexiline derivatives, pyrazolones, phenylbutazone, phosphamide (e.g., cyclophosphamide, ifosfamide, trofosfamide), probenecid, salicylates, sulfinpirazona, sulphonamides, tetracyclines and tritokvalina. Urine acidifying agents (ammonium chloride, calcium chloride) enhance the action of Glybex by reducing the degree of its dissociation and increasing its reabsorption. Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

    The hypoglycemic effect of Glybex may decrease with simultaneous use of barbiturates, isoniazid, cyclosporine, diazoxide, glucocorticosteroids, glucagon, nicotinate (in high doses), phenytoin, phenothiazines, rifampicin, thiazide diuretics, acetazolamide, sex hormones (eg hormonal contraceptives), iodine-containing hormones thyroid gland, blockers of "slow" calcium channels, sympathomimetic agents and lithium salts.

    Chronic abuse of alcohol and laxatives can aggravate the violation of carbohydrate metabolism.

    H2-receptor antagonists can, on the one hand, weaken, and on the other increase the glybicemic action of Glybex. 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.

    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.

    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 Glybex to patients with impaired liver and kidney function, as well as hypothyroidism of the thyroid gland, anterior pituitary gland or adrenal cortex. Glibeks dosage adjustment is necessary for physical and emotional overstrain, changes in diet.

    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 alcohol intake, NSAIDs, and fasting.

    During treatment it is not recommended to stay in the sun for a long time.

    When treating patients with lactase deficiency, it should be taken into account that the preparation contains lactose.

    Effect on the ability to drive transp. cf. and fur:At the beginning of treatment, during the selection of a dose, patients prone to developing hypoglycemia are not recommended to engage in activities requiring increased attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets 5 mg.


    Packaging:

    For 10 tablets in a blister of PVC-aluminum foil.

    5, 6, 10 or 12 blisters in a cardboard box together with instructions for use.

    For 50, 60, 100 or 120 tablets in a vial of clear glass with a lid of low density polyethylene.

    1 bottle in a cardboard pack together with instructions for use.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N014959 / 01-2003
    Date of registration:18.10.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group India
    Information update date: & nbsp29.04.2017
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