Type 2 diabetes (independent of insulin) in patients who are not satisfied with diet, exercise and weight loss to maintain normal blood glucose.
Composition:
1 tabl contains 80 mg gliclazide. The preparation contains lactose.
Action:
Oral hypoglycemic drug belonging to the second generation sulfonylurea. It reduces blood Glucose levels by direct stimulation of insulin release from active beta-cells of the pancreas, mainly in the first phase of secretion. The mechanism of increasing insulin secretion is not yet fully understood. It is known that after binding of the drug through the receptor, the function of ATP / K channels is inhibited+ in the cell membrane of beta cells and potassium outflow from the cell. This causes depolarization, the influx of Calcium into the interior of the cell, subsequent binding of calcium to calmodulin, activation of the kinase and release of the granule containing insulin as a result of exocytosis. Glucosidase, especially after prolonged use, is also responsible for the hypoglycaemic effect of gliclazide and peripheral tissues on insulin. Gliclazide prevents the formation of microvessel clots by reducing platelet aggregation and adhesion, and increasing the release of plasminogen activator. In fasting diabetic patients with gliclazide 80 mg, a maximum reduction in blood glucose (from approximately 135 to 100 mg / dl) is observed after 4-6 h. Therapeutic effects are maintained up to 24 hours after administration of the drug. . The drug works well, although it is absorbed from the intestines to a variable degree. Food delays the absorption of the drug. Bioavailability is about 80%. It binds to plasma proteins in 85-99%. It is metabolized in the liver to inactive pharmacologically metabolites. T0,5 is 8-12 h. It is mainly excreted in the urine.
Contraindications:
Hypersensitivity to gliclazide or other components of the preparation. Complications of diabetes (pre-comedic conditions, diabetic coma, ketonuria, acidosis). Severe renal and hepatic failure. Pregnancy and breastfeeding. Conditions of significantly increased insulin demand (high fever, severe infections, injuries and surgical procedures). Type 1 diabetes (insulin-dependent, juvenile-onset diabetes).
Precautions:
If you change your diet, you may need to adjust the dose. The preparation is not effective in the treatment of type 1 (insulin dependent) diabetes mellitus. Caution should be exercised in patients with renal and hepatic failure as well as in the elderly, starting with low doses and monitoring glucose. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation is contraindicated for use during pregnancy and during breastfeeding. Pregnant women with diabetes should be given insulin.
Side effects:
Common: hypoglycaemia (mild, transient); weight gain. Rarely: dizziness, headache, drowsiness; gastrointestinal symptoms (nausea, abdominal pain, vomiting, diarrhea, taste disorders); skin reactions (rash, pruritus, redness of the skin); hyponatraemia and water retention, haematological abnormalities, increase in serum transaminases, weight loss. Very rare: severe hypoglycaemia leading to coma, inflammation of the liver, allergy to light. Skin reactions and haematological disorders occur mainly during the first 6 weeks of treatment.
Dosage:
Orally. Adults and the elderly: 40-320 mg daily. A daily dose of up to 160 mg can be given once, while higher daily doses should be used in 2 doses. Treatment of newly diagnosed diabetes usually starts with a dose of 80 mg per day; this dose is increased by 40-80 mg a day every few days (usually every week) until the blood glucose levels stabilize. The maximum dose is 320 mg per day. In patients with hepatic impairment, the dose should be reduced.If a dose is missed, take it as soon as possible, unless it is already time for the Next dose - then take the next dose and then take the drug according to the current schedule. The drug should be taken with meals. The tablets can be divided.