Glybomet® (Glibomet® )

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceGlibenclamide + MetforminGlibenclamide + Metformin
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    • Dosage form: & nbspfilm-coated tablets
    Composition:

    Active substances: metformin hydrochloride - 400 mg, glibenclamide - 2.5 mg.

    Excipients: core: cellulose microcrystalline - 65.0 mg, corn starch - 57.5 mg, silicon dioxide colloid - 20.0 mg, gelatin - 40.0 mg, glycerol (glycerol) - 17.5 mg, talc - 15.0 mg, magnesium stearate 7.5 mg;

    sheath: acetylphthalylcellulose 2.0 mg, diethyl phthalate 0.5 mg, talc 2.5 mg.

    Description:

    White round biconvex tablets, coated with a shell, with a one-sided risk, odorless.

    Pharmacotherapeutic group:hypoglycemic, means for oral administration combined (a preparation of the group of sulfonylurea of ​​the second generation + biguanide).
    ATX: & nbsp

    A.10.B.D.02   Metformin and sulfonamides

    Pharmacodynamics:

    Glybomet® is an oral combined hypoglycemic agent, a second generation sulfonylureas derivative and a biguanide. Has pancreatic and extra-pancreatic effects.

    Glibenclamide belongs to the group of derivatives of sulfonylurea of ​​the second generation. It stimulates insulin secretion by lowering the threshold for stimulation of pancreatic beta cells by glucose, increases insulin sensitivity and the degree of its binding to target cells, increases insulin release, enhances the effect of insulin on glucose uptake by muscles and liver, inhibits lipolysis in adipose tissue. It operates in the second stage of insulin secretion.

    Metformin belongs to the biguanide group. Stimulates the peripheral sensitivity of tissues to the action of insulin (increases the binding of insulin to receptors, enhances insulin effects at the post-receptor level), reduces absorption of glucose in the intestine, suppresses gluconeogenesis and has a beneficial effect on lipid metabolism, helps to reduce excess body weight in patients with diabetes mellitus, and also has a fibrinolytic effect by suppressing the plasminogen activator inhibitortissue type.

    The hypoglycemic effect of the drug develops after 2 hours and lasts for 12 hours. A synergistic combination of the two active ingredients of the preparation is the stimulating effect of the sulfonylurea derivative on the production of endogenous insulin, (pancreatic effect) and the direct influence of biguanide on muscle and adipose tissue (a significant increase in glucose uptake ) and hepatic tissue (reduction of gluconeogenesis), allows to reduce the content of each component at a certain dose ratio. This helps to avoid excessive stimulation of the beta cells of the pancreas, and hence to reduce the risk of impairment, its function, and also provides increased safety of hypoglycemic drugs and a reduction in the incidence of side effects.

    Pharmacokinetics:

    Glibenclamide quickly and fairly fully (84%) is absorbed in the gastrointestinal tract (GIT), the time to reach a maximum concentration of 1-2 hours. The connection with plasma proteins is 97%. Almost completely metabolized in the liver with the formation of inactive metabolites. It is excreted by the kidneys - 50% and with bile - 50 %. The half-life is 5 to 10 hours.

    Metformin sufficiently absorbed in the gastrointestinal tract, quickly distributed into tissues, practically does not bind to blood plasma proteins. It is not exposed to metabolism in the body, it is excreted unchanged mainly by the kidneys and, in part, by the intestine. The half-life is approximately 7 hours.

    Indications:

    Type 2 diabetes mellitus (with ineffectiveness of diet therapy and previous therapy with sulfonylurea derivatives or biguanides, as well as other oral hypoglycemic agents).

    Contraindications:

    • increased sensitivity to metformin, glibenclamide or other derivatives of sulfonylurea, as well as to other components of the preparation;

    • type 1 diabetes mellitus;

    • gestational diabetes;

    • Diabetic ketoacidosis, diabetic precoma, diabetic coma;

    • lactoacidosis (including in the anamnesis);

    • conditions, accompanied by a violation of food intake and development of hypoglycemia;

    • abnormal liver function;

    • acute conditions that can lead to a change in kidney function: dehydration, severe infection, shock, intravascular injection of iodine-containing contrast agents;

    • renal failure or renal dysfunction (creatinine levels above 135 mmol / L for men and above 110 mmol / L for women);

    • infectious diseases, gangrene, large surgical interventions, trauma, acute massive blood loss, extensive burns and other conditions, requiring insulin therapy;

    • hypoxic conditions (cardiac or respiratory failure, recent myocardial infarction, shock, severe respiratory disease);

    • 48 hours before the start and 48 hours after radioisotope or X-ray studies with the introduction of iodine-containing contrast medium;

    • period for 48 hours before the beginning and 48 hours after the surgical intervention;

    • dystrophic diseases (myotonic dystrophy, lipodystrophy);

    • leukopenia;

    • porphyria;

    • chronic alcoholism, acute alcohol intoxication;

    • compliance with a strict hypocaloric diet (less than 1000 kcal / day);

    • deficiency of glucose-6-phosphodiesterase;

    • pregnancy, the period of breastfeeding;

    • age to 18 years.

    It is not recommended to use the drug in people over 60 years of age who perform heavy physical work, which is associated with an increased risk of developing lactic acidosis.

    Carefully:

    • febrile syndrome;

    • thyroid disease (with impaired function); hypofunction of the anterior lobe of the pituitary gland and / or the adrenal cortex;

    • heavy physical work (risk of developing lactic acidosis).

    Pregnancy and lactation:

    The use of Glybomet® during pregnancy and during breastfeeding is contraindicated.

    Dosing and Administration:

    Inside.

    The dose and mode of administration of the drug, as well as the duration of treatment, are established by the attending physician, primarily in accordance with the state of carbohydrate metabolism of the patient, depending on the concentration of glucose in the blood plasma. Typically, the initial dose is 1-3 tablets per day with the main meal, with a gradual selection of the dose until a steady normalization of the concentration of glucose in the blood plasma. The maximum daily dose is 6 tablets of Glybomet®.

    Side effects:

    Possible side effects with the use of the drug Glybomet® are given below on the descending frequency of occurrence: often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1/10000, <1/1000), very rarely (<1/10000), including individual messages.

    From the digestive system:

    Rarely: nausea, vomiting, loss of appetite, abdominal pain, diarrhea, a sense of "metallic" taste;

    in some cases: increased activity of "liver" enzymes.

    On the part of the hematopoiesis system:

    Rarely: leukopenia, thrombocytopenia, erythrocytopenia;

    rarely: agranulocytosis, hemolytic or megaloblastic anemia, pancytopenia.

    From the central nervous system:

    Infrequently: headache.

    From the skin:

    Rarely: urticaria, erythema, pruritus, photosensitivity.

    From the side of metabolism:

    Rarely: hypoglycemia.

    Rarely: lactic acidosis.

    When symptoms of lactic acidosis (vomiting, abdominal pain, general weakness, muscle cramps) appear, stop taking the medication immediately and seek medical attention immediately.

    Other: disulfiram-like reaction with simultaneous intake of alcohol (the most common signs: reddening of the face and upper body, headache, nausea and vomiting, palpitation, increased blood pressure).

    Overdose:

    Overdose can provoke the development of lactic acidosis, since the composition of the drug is metformin. Symptoms of lactic acidosis are severe weakness, pain in the muscles, respiratory disorders, drowsiness, nausea, vomiting, diarrhea, abdominal pain, hypothermia, lowering of blood pressure, reflex bradyarrhythmia, confusion and loss of consciousness.If suspected of developing lactic acidosis, immediate discontinuation of the drug and emergency hospitalization are recommended.

    The most effective method of removing lactate and metformin from the body is hemodialysis. Overdose can also lead to the development of hypoglycemia due to the presence of glibenclamide in the formulation. Symptoms of hypoglycemia: hunger, increased sweating and palpitations, weakness, pale skin, paresthesia in the mouth, tremor, general anxiety, headache, pathological drowsiness, sleep disorders, feelings of fear, impaired coordination of movements, temporary neurological disorders. With progression, hypoglycemia, it is possible for patients to lose self-control and consciousness.

    In mild hypoglycemia, you should take a piece of sugar, food or drinks high in carbohydrates (jam, honey, a glass of sweet tea) inside.

    In case of unconsciousness, 40-80 ml of 40% dextrose solution (glucose) should be administered intravenously, then infuse 5-10% dextrose solution. Then you can additionally administer 1 mg of glucagon intravenously (intramuscularly or subcutaneously).If the patient does not regain consciousness, it is recommended that these actions be repeated. If there is no effect, intensive care is indicated.

    Interaction:

    The hypoglycemic effect of the drug Glybomet® is enhanced by the simultaneous administration of coumarin derivatives (warfarin, sincomar), beta adrenoblockers, cimitidine, oxytetracycline, allopurinol, monoamine oxidase (MAO) inhibitors, sulfonamides, phenylbutazone and its derivatives, chloramphenicol, probenecid and salicylates, cyclophosamide, sulfonamide , perhexylin, pheniramidol, miconazole in oral forms, sulphinpyrazone and alcohol.

    Adrenaline, glucocorticosteroids, oral contraceptives, thyroid hormone preparations, thiazide diuretics and barbiturates reduce the hypoglycemic action of the Glybomet® drug.

    With simultaneous application, the effect of anticoagulants can be enhanced.

    Simultaneous administration with cimitidine may increase the risk of developing lactic acidosis.

    The use of beta-blockers can mask the symptoms of hypoglycemia (with the exception of sweating).

    The use of iodine-containing radiocontrast preparations (for intravascular administration) can lead to the development of renal dysfunction and cumulation of metformin, which increases the risk of lactic acidosis.

    Special instructions:

    During treatment, patients should strictly follow the doctor's recommendations regarding the dosage and method of administration of the drug, as well as concomitant nutrition, exercise and self-monitoring of glucose in the blood plasma.

    Lactic acidosis - a rare and life-threatening pathological condition, characterized by accumulation, in the blood of lactic acid, the cause may be the accumulation of metformin. The described cases of lactic acidosis in patients who received metformin, were observed mainly in patients. with diabetes mellitus with severe cardiac, and renal insufficiency. Prevention of lactic acidosis involves the identification of all associated risk factors, such as decompensated diabetes mellitus, ketosis, prolonged fasting, excessive alcohol consumption, liver failure and any condition associated with hypoxia.

    When taking Glybometh®, the serum creatinine concentration should be monitored regularly:

    • at least once a year in patients with normal renal function;

    • at least 2-4 times a year in patients with a serum creatinine concentration close to the upper limit of the norm, as well as in elderly patients.

    Caution should be observed in cases where there is a risk of impaired renal function, for example, with the appointment of antihypertensive or diuretics, at the beginning of therapy with nonsteroidal anti-inflammatory drugs (NSAIDs).

    Treatment with Glybomet® should be stopped 48 hours before the X-ray examination with intravenous iodine-containing contrast agents and replaced with other hypoglycemic agents (for example, insulin).

    The use of Glybomet® should be discontinued 48 hours before the planned operation under anesthesia with spinal or epidural anesthesia. Continue therapy should be after the resumption of oral nutrition, or no earlier than 48 hours after surgery, subject to confirmation of normal kidney function.

    Alcohol can trigger the development of hypoglycemia, as well as a disulfiram-like reaction (nausea, vomiting, abdominal pain, a feeling of fever in the face and upper body, tachycardia, dizziness, headache), so you should refrain from alcohol during treatment with Glybomet®.

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

    When taking Glybometh ®, hypoglycemia may develop, and as a consequence, a decrease in the ability to concentrate attention and reaction, therefore, during the period of treatment with Glybomet ®, caution should be exercised when managing vehicles, mechanisms and occupations with potentially dangerous activities.

    Form release / dosage:

    Coated tablets, 2.5 mg + 400 mg.


    Packaging:

    20 tablets per blister (PVC / PVDC / aluminum foil).

    For 2, 3 or 5 blisters together with the instructions for use are placed in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 30 ° C.

    Keep the medicine out of the reach of children!

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N012183 / 01
    Date of registration:16.09.2011
    The owner of the registration certificate:Laboratory Guidotti SpALaboratory Guidotti SpA Italy
    Manufacturer: & nbsp
    Information update date: & nbsp22.12.2015
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