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

    Active substance: glibenclamide 5.00 mg;

    Excipients: lactose monohydrate (sugar milk) - 90,00 mg, potato starch - 33,25 mg, povidone (polyvinylpyrrolidone low molecular weight medical) - 0.45 mg, magnesium stearate - 1.30 mg.

    Description:

    Tablets white or white with a weak yellowish hue of color, round, flat-cylindrical, with a bevel.

    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. 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 fat lipolysis (extra-pancreatic effects) . It operates in the second stage of insulin secretion. Has hypolipidemic action, reduces thrombogenic properties of blood. The hypoglycemic effect develops after 2 hours, reaches a maximum after 7-8 hours and lasts for 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:

    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.

    In patients with impaired hepatic function, the excretion of glibenclamide is slowed down. In patients with renal insufficiency, the excretion of metabolites with bile increases. With creatinine clearance ≥30 ml / min, glibenclamide elimination remains unchanged, with severe renal failure, cumulation of glibenclamide in the body is possible.

    Indications:

    Diabetes mellitus type 2 (with ineffectiveness of diet therapy).

    Contraindications:
    • Hypersensitivity to glibenclamide, including other derivatives of sulfonylurea, sulfonamides, diuretics containing a sulfonamide group, probenecid;
    • type 1 diabetes mellitus;
    • diabetic ketoacidosis, diabetic precoma and coma;
    • severe hepatic and / or renal insufficiency;
    • condition after resection of the pancreas;
    • Some acute conditions (for example, decompensation of carbohydrate metabolism in infectious diseases or after major surgical operations, when insulin therapy is indicated);
    • intestinal obstruction, paresis of the stomach;
    • conditions, accompanied by a violation of food intake and development of hypoglycemia;
    • leukopenia;
    • lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
    • pregnancy and lactation;
    • children under 18 years of age (efficacy and safety not studied).
    Carefully:

    Feverish syndrome, thyroid disease (with impaired function), hypofunction of the anterior lobe of the pituitary or adrenal cortex, alcoholism, adrenal insufficiency, cerebral atherosclerosis, dementia, deficiency of glucose-6-phosphate dehydrogenase, elderly patients due to the danger of hypoglycemia.

    Pregnancy and lactation:

    The use of the drug during pregnancy and during breastfeeding is contraindicated.

    Dosing and Administration:

    The dose of the drug is selected individually, depending on the age, the severity of the course of diabetes, the concentration of glucose in the blood plasma 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). Doses of more than 15 mg / day do not increase the severity of hypoglycemic effect. The initial dose in elderly patients is 1 mg per day.

    The drug is used inside, whole, not liquid, with a small amount of liquid for 20-30 minutes before meals. Multiplicity of drug intake is 1-3 times a day.

    If you miss one dose of the drug, the next dose of the drug should be taken at the usual time, while not allowed to take a higher dose.

    Side effects:

    The most common undesirable effect in the treatment with Glibenclamide 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; 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 drugs. Symptoms of hypoglycemia are: a strong feeling of hunger, sudden profuse sweating, palpitations, pallor of the skin, paresthesia of the oral mucosa, tremors, general anxiety, headache, pathological drowsiness, sleep disorders, fear, coordination of movements, temporary neurological disorders , 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, increased convulsive readiness. Along with hypoglycemia are possible:

    From the digestive system: infrequently - nausea, eructation, vomiting, "metallic" taste in the mouth, a feeling of heaviness and overflow in the stomach, abdominal pain, diarrhea; very rarely - a temporary increase in the activity of "hepatic" enzymes (alkaline phosphatase, glutaminoschaveulose acetic aminotransferase, glutamine-pyruvic aminotransferase), hepatitis, jaundice.

    Allergic reactions: infrequent - skin rash, including flaky, itching, urticaria, skin hyperemia, Quincke edema, petechiae, photosensitivity; very rarely - allergic vasculitis, 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. Individual cases of severe generalized allergic reactions with skin rash, arthralgia, fever, proteinuria, jaundice are described.

    From the hematopoiesis: rarely thrombocytopenia, very rarely leukocytopenia, agranulocytosis. In a few cases, hemolytic anemia, pancytopenia develops.

    Other: very rarely - increased diuresis; temporary proteinuria; visual impairment and accommodation; abdominal pain; cross-allergicreaction to probenecid, sulfonylurea derivatives, sulfonamides, diuretics containing a sulfonamide group in the molecule; acute reaction of alcohol intolerance after its use, expressed by complications from the circulatory and respiratory organs (disulfiramoid-like reaction: vomiting, sensation of fever in the face and upper body, tachycardia, dizziness, headache).

    Overdose:

    Symptoms: hypoglycemia, hypoglycemic coma.

    Treatment: with mild or moderate hypoglycemia (patient in consciousness) glucose or sugar solution is taken orally.

    In case of severe hypoglycemia (loss of consciousness), 40% dextrose (glucose) solution or 1-2 mg glucagon intravenously, intramuscularly, subcutaneously.

    It is necessary to monitor the glucose concentration every 15 minutes, as well as the determination of pH, urea nitrogen, creatinine, electrolytes in blood plasma. 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).

    Interaction:

    Increase the hypoglycemic effect of the drug inhibitors of the angiotensin-converting enzyme (captopril, enalapril), H2-histamine receptor blockers (cimetidine), antifungal medicines (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, azapresene, oxyphenbutazone), fibrates (clofibrate, bezafibrate), antituberculous (ethionamide), salicylates, coumarinic anticoagulants, anabolic steroids, beta-adrenoblockers, monoamine oxidase inhibitors, long-acting sulfonamides, phosphamides, biguanides, chloramphenicol, fenfluramine, acarbose, fluoxetine, guanethidine, pentoxifylline, tetracycline, theophylline, tubular secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine, insulin, allopurinol.

    Weaken the effect of barbiturates, glucocorticosteroids, adrenostimulants (epinephrine, clonidine), antiepileptic drugs (phenytoin), blockers of "slow" calcium channels, inhibitors of carboxy anhydrase (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, ritodrin, salbutamol, terbutaline, glucagon, rifampicin, 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.

    Clinical manifestations of hypoglycemia may be weakened by taking beta-blockers, clonidine, reserpine, guanetidine.

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

    Special instructions:

    It is necessary to regularly monitor the concentration of glucose in the blood on an empty stomach and after eating.

    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.

    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 alcohol intake (including the development of disulfiram-like reactions: abdominal pain, nausea, vomiting, headache), non-steroidal anti-inflammatory drugs, and fasting.

    Glibenclamide dose adjustment is necessary in case of physical and emotional overstrain, changes in diet.

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

    Effect on the ability to drive transp. cf. and fur:

    During the period of treatment it is not recommended to engage in potentially dangerous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets 5 mg.

    Packaging:For 10 tablets in a contour mesh box made of PVC film and aluminum foil. 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Storage conditions:

    In dry, the dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002499
    Date of registration:11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspMOSHIMFARM PREPARATES them. NA Semashko OJSC MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia
    Information update date: & nbsp26.04.2017
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