Glimecomb® (Glimekomb)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceGliklazid + MetforminGliklazid + Metformin
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  • Glimecomb®
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
    • Dosage form: & nbsppills
    Composition:

    Active substances: metformin hydrochloride in terms of 100% substance - 500 mg, gliclazide in terms of 100% substance - 40 mg;

    Excipients: sorbitol, povidone, croscarmellose sodium, magnesium stearate.

    Description:

    Tablets from white to white with a cream or yellowish hue of color, flat-cylindrical, with a facet and a risk. Presence of "marble" is admissible.

    Pharmacotherapeutic group:Hypoglycemic agent for oral administration combined (biguanide + sulfonylurea group preparation)
    ATX: & nbsp

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

    Pharmacodynamics:

    Glimecomb® is a fixed combination of two oral hypoglycemic agents of various pharmacological groups: gliclazide and metformin. Has pancreatic and extra-pancreatic effects.

    Gliclazide stimulates the secretion of insulin by the pancreas, increases the sensitivity of peripheral tissues to insulin. Stimulates the activity of intracellular enzymes - muscle glycogen synthetase. It restores the early peak of insulin secretion, shortens the time from the time of food intake to the onset of insulin secretion, reduces postprandial hyperglycemia.Besides effects on carbohydrate metabolism, influences the microcirculation, decreases platelet adhesion and aggregation, retards the development of membrane thrombosis, normalizes vascular permeability and prevents the development of atherosclerosis and mikrotromboza, restores the physiological process of membrane fibrinolysis, elevated counteracts the reaction to adrenalin vessels at microangiopathies. Slows the development of diabetic retinopathy at the non-proliferative stage; with diabetic nephropathy against a background of prolonged use, there is a significant decrease in proteinuria. It does not increase body weight, as has predominant effects on early insulinosekretsii peak and does not cause hyperinsulinemia; helps to reduce body weight in obese patients while observing an appropriate diet.

    Metformin belongs to the biguanide group. Decreases in blood glucose concentration by inhibiting hepatic gluconeogenesis, reduce glucose absorption from the gastrointestinal tract and enhance its utilization in tissues. Reduces the concentration of serum triglycerides,cholesterol and low-density lipoprotein (determined on an empty stomach) and does not change the concentration of lipoproteins of other densities. Able tostabilization or weight loss. If there is no insulin in the blood, the therapeutic effect is not manifested. Hypoglycemic reactions do not cause. Improves the fibrinolytic properties of the blood by suppressing the inhibitor of the activator of plasminogen (tissue-type) plasminogen.

    Pharmacokinetics:

    Gliclazide. Absorption is high. After oral administration of 40 mg, the maximum concentration in the blood plasma is achieved after 2 to 3 hours and is 2-3 μg / ml. Relationship with plasma proteins - 85 - 97%. The half-life is 8 to 20 hours. It is metabolized in the liver. It is excreted mainly in the form of metabolites by the kidneys - 70%, through the intestine - 12%. In elderly patients there are no clinically significant changes in pharmacokinetic parameters.

    Metformin. Absorption - 48 - 52%. Quickly absorbed in the gastrointestinal tract. Absolute bioavailability (fasting) is 50 - 60%, intake with food reduces the maximum concentration by 40% and slows its achievement by 35 minutes. The concentration in the blood plasma is reached through 1,81 - 2,69 h and does not exceed 1 mcg / ml.The connection with plasma proteins is insignificant, it is able to accumulate in erythrocytes. The half-life period is 6.2 hours. It is excreted by the kidneys, mainly in the unchanged form (glomerular filtration and tubular secretion) and through the intestine (up to 30%).

    Indications:
    • Diabetes mellitus type 2 with ineffectiveness of diet therapy, exercise and previous therapy with metformin or gliclazide.
    • Substitution of previous therapy with two drugs (metformin and gliclazide) in patients with type 2 diabetes with stable and well-controlled blood glucose level.
    Contraindications:
    • hypersensitivity to metformin, gliclazide or other sulfonylurea derivatives, as well as to auxiliary substances;
    • type 1 diabetes mellitus;
    • Diabetic ketoacidosis, diabetic precoma, diabetic coma; hypoglycemia;
    • severe renal dysfunction;
    • acute conditions that can lead to a change in kidney function: dehydration, severe infection, shock;
    • acute or chronic diseases accompanied by tissue hypoxia: cardiac or respiratory failure, recent myocardial infarction, shock;
    • liver failure;
    • porphyria;
    • pregnancy, the period of breastfeeding;
    • simultaneous administration of miconazole;
    • infectious diseases, large surgical interventions, traumas, extensive burns and other conditions requiring insulin therapy;
    • chronic alcoholism, acute alcohol intoxication;
    • lactoacidosis (including in the anamnesis);
    • application for at least 48 hours before and within 48 hours after carrying out radioisotope or radiographic studies with the introduction of an iodine-containing contrast medium;
    • adherence to a hypocaloric diet (less than 1000 calories / day).

    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:

    Feverish syndrome, adrenal insufficiency, hypofunction of the anterior lobe of the pituitary gland, thyroid gland diseases with violation of its function.

    Pregnancy and lactation:

    During pregnancy, the use of Glimecomb® is contraindicated. When planning pregnancy, as well as in case of pregnancy in the period of taking Glimecomba®, the drug should be canceled and insulin therapy prescribed.

    Glimecomb® is contraindicated in breastfeeding because the drug is capable of penetrating into breast milk. In this case, you need to switch to insulin therapy or stop breastfeeding.

    Dosing and Administration:

    The drug is administered orally, during or immediately after a meal. The dose of the drug is determined by the doctor individually for each patient, depending on the level of blood glucose. Usually, the initial dose is 1-3 tablets per day with a gradual selection of a dose until a stable compensation of the disease.

    Usually the drug is taken 2 times a day (morning and evening). The maximum daily dose is 5 tablets.

    Side effects:

    From the side of metabolism: when the dosing regimen is violated and the diet is inadequate - hypoglycemia (headache, fatigue, hunger, increased sweating, severe weakness, palpitations, dizziness, impaired coordination of movements, temporary neurological disorders, with progression of hypoglycemia, patients may lose self-control and consciousness); in some cases, lactic acidosis (weakness, myalgia, respiratory disorders, drowsiness, abdominal pain, hypothermia, lowering blood pressure, reflex bradyarrhythmia).

    From the digestive system: dyspepsia (nausea, diarrhea, a feeling of heaviness in the epigastrium, a "metallic" taste in the mouth), a decrease in appetite - the severity decreases with taking the drug while eating; rarely - liver damage (hepatitis, cholestatic jaundice - requires withdrawal of the drug, increased activity of "liver" transaminases, alkaline phosphatase).

    From the hematopoiesis: rarely - oppression of bone marrow hematopoiesis (anemia, thrombocytopenia, leukopenia).

    Allergic reactions: itching, urticaria, maculopapular rash.

    In case of side effects, the dose should be reduced or the drug should be temporarily discontinued.

    Other: impaired vision.

    Common side effects of sulfonylureas: erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis; life-threatening liver failure.

    Overdose:

    Overdose or presence of risk factors can provoke the development of lactic acidosis, since the composition of the drug includes metformin. When symptoms of lactic acidosis appear, stop taking the drug. Lactic acidosis is a condition,requiring urgent medical assistance; treatment of lactic acidosis should be carried out in a hospital. The most effective method of treatment is hemodialysis.

    Overdose can also lead to the development of hypoglycemia due to the presence of the drug gliclazide. With mild or moderate hypoglycemia, glucose (dextrose) 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, underskin. After the restoration of consciousness, the patient needs to give food rich in 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 (NSAIDs) (phenylbutazone, azapresene, oxyphenbutazone), fibrates (clofibrate, bezafibrate), antituberculous (ethionamide), salicylates, coumarinic anticoagulants, anabolic steroids, beta-adrenoblockers, monoamine oxidase inhibitors, long-acting sulfonamides, cyclophosphamide, chloramphenicol, fenfluramine, fluoxetine, guanethidine, pentoxifylline, tetracycline, theophylline, tubular secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine, other hypoglycemic drugs (acarbose, biguanides, insulin, etc.) allopurinol, oxytetracycline.

    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, thyroid hormones, lithium salts, in high doses - a nicotinic acid, chlorpromazine, oral contraceptives and estrogens.

    Increases the risk of developing ventricular extrasystole against the background of cardiac glycosides.Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

    Ethanol increases the likelihood of lactic acidosis.

    Metformin reduces the maximum concentration in the blood (Сmах) and T1/2 furosemide at 31 and 42.3 % respectively.

    Furosemide increases the Сmах of metformin by 22%.

    Nifedipine increases absorption, Сmах, slows the excretion of metformin.

    Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene and vancomycin), secreted in tubules, compete for tubular transport systems and, with prolonged therapy, can increase Сmах metformin by 60%.

    Special instructions:

    Treatment with Glimecomb® is done only in combination with a low-calorie diet with a low carbohydrate content. It is necessary to regularly monitor the glucose level in the blood on an empty stomach and after meals, especially in the first days of treatment with the drug.

    Glimecomb® can only be prescribed to patients who receive regular meals, including breakfast and adequate intake of carbohydrates.When prescribing the drug, it should be borne in mind that hypoglycemia may develop, due to the administration of sulfonylurea derivatives, and in some cases, in severe and prolonged form, requiring hospitalization and administration of glucose for several days. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or while taking several hypoglycemic drugs at the same time.

    In order to avoid the development of hypoglycemia, a careful and individual selection of doses is necessary, as well as providing the patient with complete information about the proposed treatment.

    In case of physical and emotional overstrain, a dose adjustment of Glimecomba® is necessary when changing the diet.

    Particularly sensitive to the effects of hypoglycemic drugs: the elderly; patients who do not receive a balanced diet, with a general weakened state; patients suffering from pituitary-adrenal insufficiency. Beta- adrenoblockers, clonidine, reserpine, guanethidine may mask the clinical manifestations of hypoglycemia.

    Patients should be warned about the increased risk of hypoglycemia in cases of taking ethanol, NSAIDs, with fasting.

    Large surgical interventions and trauma, extensive burns, infectious diseases with febrile syndrome may require the abolition of oral hypoglycemic drugs and the appointment of insulin therapy. In the treatment of kidney function; the definition of lactate in plasma should be carried out at least 2 times a year, as well as with the appearance of myalgia. The development of lactic acidosis requires discontinuation of treatment.

    48 hours before surgery or intravenous iodine-containing radiopaque, Glimecombe® should be discontinued; treatment is recommended to resume after 48 h.

    On the background of therapy with Glimecomb®, the patient should stop using alcohol and / or containing ethanol preparations and food products.

    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 of 40 mg + 500 mg.

    Packaging:

    For 30, 60 or 120 tablets in a bottle of low-density polyethylene, capped with a cap screwed from polypropylene with an integrated desiccant and control of the first opening.

    For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil.

    Each vial or 6 contiguous cell packs of 10 tablets, or 5 out-of-round cell packs of 20 tablets, together with instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    In a dry, the dark place 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.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009886/09
    Date of registration:04.12.2009 / 20.10.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp29.04.2017
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