Active substanceGlipizideGlipizide
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  • Dosage form: & nbsppills
    Composition:

    Active substance: glipizide - 5 mg;

    Excipients: Lactose 130 mg Starch pregelatinized 30 mg, 30 mg microcrystalline cellulose, hypromellose (hydroxypropyl methylcellulose) 0.8 mg stearic acid 1.6 mg.

    Description:

    Tablets of cylindrical round form of white color with engraving "U" in a circle on the one hand and risk on the other.

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

    A.10.B.B.07   Glipizide

    Pharmacodynamics:

    Glipizide has pancreatic and extra-pancreatic effects. It stimulates the secretion of insulin by lowering the threshold for glucose stimulation of pancreatic beta cells and increases sensitivity to insulin and the degree of binding to target cells that increases insulin release, enhances the action of insulin on glucose uptake by muscles and the liver, inhibits lipolysis in adipose tissue. The severity of hypoglycemic action depends on the number of functioning beta cells. Has also hypolipidemic, fibrinolytic action,inhibits platelet aggregation, has a mild diuretic effect.

    Pharmacokinetics:

    After oral administration glipizide quickly and almost completely absorbed in the human gastrointestinal tract. The maximum concentration in the plasma is achieved in 1-3 hours after taking a single dose. The intake of food does not affect the overall absorption and accumulation of the drug, but the suction time increases by 40 minutes. Bioavailability is 90%, the connection with plasma proteins is 98-99%.

    Metabolized in the liver to inactive metabolites. It is excreted by the kidneys - 90% in the form of metabolites, 10 % - unchanged.

    The half-life is 2-4 hours.

    Indications:

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

    Contraindications:
    • Hypersensitivity to sulfonylurea derivatives, sulfonamides;
    • hypersensitivity to glipizide or any other component of the drug;
    • type 1 diabetes mellitus;
    • diabetic ketoacidosis, diabetic precoma and coma;
    • hyperosmolar coma;
    • conditions requiring insulin therapy (extensive burns, large surgical interventions, severe injuries and infectious diseases);
    • marked violations of the liver and kidneys;
    • deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;
    • pregnancy, lactation.
    Carefully:

    The drug is used for febrile syndrome, alcoholism, adrenal insufficiency, thyroid diseases with a violation of its function (hypothyroidism or hyperthyroidism), hepatic and / or renal failure of mild and moderate severity, and leukopenia.

    Pregnancy and lactation:

    Glipizide contraindicated in pregnancy.

    Not recommended for use during lactation.

    Dosing and Administration:

    The dose depends on the age, severity of the course of diabetes, fasting blood glucose and 2 hours after eating.

    Assign inside, 30 minutes before eating. The initial daily dose is 5 mg before breakfast, if the effect is absent, the dose is increased by 2.5-5 mg with a constant control of the concentration of glucose in the blood.

    In diseases of the liver, kidneys and in elderly patients - the initial daily dose is 2.5 mg.

    The maximum single dose is 15 mg, the maximum daily dose is 40 mg. Multiplicity of administration - once a day, daily doses of more than 15 mg should be divided into 2-4 reception.

    Side effects:

    From the endocrine system: hypoglycemia, hypoglycemic coma.

    From the nervous system: dizziness, headache, drowsiness.

    From the skin: rash on the skin and mucous membranes, itching, hives, eczema, photosensitivity.

    From the hematopoiesis: oppression of bone marrow hematopoiesis (anemia, including aplastic and hemolytic, pancytopenia, leukopenia, agranulocytosis, thrombocytopenia).

    From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, cholestatic jaundice, hepatic insufficiency, hepatitis, acute porphyria, hepatic porphyria.

    From the sense organs: blurred vision, visual impairment.

    Laboratory indicators: increased activity of aspartate aminotransferase (ACT), lactate dehydrogenase (LDH), alkaline phosphatase (FA), an increase in residual urea nitrogen in the blood plasma, hypercreatininaemia.

    Other: weight gain, myalgia, convulsions, hyponatremia, disulfiramopogood reactions.

    From the gastrointestinal tract: nausea, vomiting, constipation, diarrhea, epigastric pain, hepatitis.

    From the skin: urticaria rash, itchy skin, multiforme exudative erythema.

    From the hematopoiesis: anemia, aplastic and hemolytic anemia, pancytopenia, leukopenia, agranulocytosis, eosinophilia, thrombocytopenia.

    Other: Perhaps the development of hyponatremia and the violation of the secretion of antidiuretic hormone.

    Overdose:

    Overdose of the drug may lead to the development of hypoglycemia.

    Symptoms of hypoglycemia: hunger, increased sweating, severe weakness, palpitations tremor, anxiety, headache, insomnia, irritability, depression, speech and vision impairment, difficulty concentrating, impaired consciousness, hypoglycemic coma.

    Treatment: if the patient is conscious, taking glucose or sugar internally, a loss of consciousness requires intravenous administration of 40 % solution of dextrose (glucose), then - infusion 5% dextrose, 1-2 mg glucagon subcutaneously, intramuscularly or intravenously. After the restoration of consciousness, it is necessary to give the patient food that is rich in easily digestible carbohydrates (in order to avoid the re-development of hypoglycemia). With edema of the brain - mannitol and dexamethasone.

    Interaction:

    Increase hypoglycemic effect Glipizide with simultaneous use of angiotensin converting enzyme (captopril, enalapril), H2-histamine receptor blockers (cimetidine), antifungal drugs (miconazole, fluconazole), non-steroidal anti-inflammatory drugs (phenylbutazone, azapresene, oxyphenbutazone), fibrates (clofibrate, bezafibrate), antituberculous (ethionamide), alicilates, coumarinic anticoagulants, anabolic theroids, beta-adrenoblockers, monoamine oxidase inhibitors, long-acting sulfonamides, cyclophosphamides, biguanides, acarbose, insulin, chloramphenicol, fenfluramine, fluoxetine, guanethidine, pentoxifylline, tetracyclinetheophylline, tubular secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine and allopurinol.

    Weaken Effect Barbiturates, glucocorticosteroids, adrenostimulators (epinephrine, clonidine), antiepileptic agents (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.

    Antithyroid and myelotoxic drugs increase the likelihood of agranulocytosis; the latter, in addition, provoke the development of thrombocytopenia.

    Special instructions:

    Regularly monitor the concentration of glucose in the blood on an empty stomach and after eating.

    It is necessary to correct the dose of the drug for physical and emotional overstrain, change in diet.

    In the case of surgical interventions or with decompensation of diabetes mellitus, it is necessary to consider the possibility of carrying out insulin therapy.

    Patients should be warned about the increased risk of hypoglycemia in cases of taking ethanol (including the development of a disulfiram-like syndrome: abdominal pain, nausea, vomiting, headache), NSAIDs, with starvation.

    Clinical manifestations of hypoglycemia may be masked when taking beta-blockers, clonidine, reserpine, guanetidine.

    Against the background of long-term use, addiction to hypoglycemic action and decreased glipizide efficacy may develop.

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

    During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, 5 mg.

    Packaging:

    For 24 tablets in a blister of PVC / aluminum foil.

    2 blisters together with instructions for use in a cardboard box.

    Storage conditions:

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

    Keep out of the reach of children.

    Shelf life:

    3,5 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001191
    Date of registration:11.11.2011
    Expiration Date:11.11.2016
    The owner of the registration certificate:Juhai United Laboratories Co., Ltd.Juhai United Laboratories Co., Ltd. China
    Manufacturer: & nbsp
    Representation: & nbspInstitute of Health CJSCInstitute of Health CJSC
    Information update date: & nbsp10.06.2018
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