Index of drugs

Type 2 (non-insulin dependent) diabetes mellitus in adults when adherence to diet, exercise and weight loss are not sufficient to maintain normal blood glucose.

1 tabl contains 80 mg gliclazide. The preparation contains lactose.

Oral hypoglycemic drug from the sulfonylurea group. The effect is to stimulate the pancreatic beta cells to secrete endogenous insulin in both the first and the second stage of secretion. Non-pancreatic action consists in restoring peripheral insulin sensitivity to insulin by decreasing Glucose production in the liver, increasing glucose clearance and increasing glycogen synthase activity in skeletal muscles. It does not seem that these effects could be a consequence of the effect on the number, affinity and function of insulin receptors. Glycaside shows specific hematological effects - it reduces the adhesion and aggregation of platelets, increases the release of plasminogen activators in vascular wall cells and reduces the amount of free radicals, causing an increase in peroxide dismutase activity. Gliclazide is actively absorbed from the gastrointestinal tract. The rate of absorption varies greatly in different people, which can be described as absorbing slowly or quickly. The stationary concentration is determined after 2 days of use. Medium T_0,5 in plasma is 10 h. In about 95%, the drug is associated with plasma proteins, mainly with albumin. Gliclazide is extensively metabolised by oxidation to inactive metabolites. Gliclazide and its inactive metabolites are excreted by the kidneys (less than 20% of the dose - unchanged).

Hypersensitivity to gliclazide or to any of the excipients, and to other sulfonylurea derivatives or sulfonamides. Type 1 diabetes. Pre-coma or diabetic coma. Ketosis and diabetic acidosis. Severe renal or hepatic failure - in these cases the use of insulin is recommended. Miconazole treatment. Breastfeeding period.

Due to the risk of hypoglycaemia, oral hypoglycaemic agents can be used only in patients who are regularly and properly nourished. Hypoglycaemia occurs more frequently when low-calorie diets are used, following prolonged or strenuous exercise, drinking alcohol, or when the combination therapy is used with antidiabetic agents. Factors that increase the risk of hypoglycaemia: lack of cooperation on the part of the patient; the use of the drug in people who only have a proper diet of glucose in their diet; malnutrition, irregular meal times, leaving meals, periods of fasting or changes in diet; long-lasting nausea and vomiting; incorrectly selected dose or overdose; imbalance between physical effort and the supply of carbohydrates; renal failure; severe liver failure; some endocrine disorders (thyroid dysfunction, hypopituitarism and adrenal insufficiency), concomitant administration of other drugs affecting glycemia. The pharmacokinetics and / or pharmacodynamics of gliclazide may be altered in patients with hepatic impairment or severe renal impairment. Hypoglycaemia may be prolonged in these patients, which may require special treatment. The following situations can affect glycemic control in patients receiving antidiabetic treatment: fever, trauma, infection or surgery. In some cases, insulin may need to be given. The effectiveness of the hypoglycaemic effect of antidiabetic drugs, including gliclazide, decreases over time; this may be due to a gradual increase in diabetes or a reduction in response to treatment. This phenomenon is known as secondary therapeutic failure (as opposed to primary failure when the active substance is ineffective as the first-line treatment) - prior to finding a patient's secondary therapeutic failure, appropriate dose adjustment and diet development should be considered.The determination of glycosylated hemoglobin (or fasting plasma glucose) is recommended for the assessment of glycemic control. Self-monitoring of blood glucose is also useful. The product should not be used in children. The product contains lactose - should not be used in people with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Normoglycemia should be obtained before conception to reduce the risk of birth defects in the fetus as a result of uncontrolled maternal diabetes. The use of oral hypoglycemic agents is inappropriate. The first choice in the treatment of diabetes in pregnant women is insulin. It is recommended to discontinue oral hypoglycemic agents and initiate insulin therapy before attempting to become pregnant or immediately after pregnancy. Due to the risk of hypoglycaemia in a child, the use of gliclazide is contraindicated in breast-feeding women.

Common: hypoglycaemia (symptoms of hypoglycaemia are: headache, severe hunger, nausea, vomiting, tiredness, drowsiness, sleep disturbances, agitation, weakened concentration, disturbed consciousness and slowing of reactions, depression, feeling of confusion, blurred vision and speech, dementia, tremor, paresis, sensation, dizziness, feelings of powerlessness, self-control, seizures, convulsions, shallow breathing, bradycardia, drowsiness and loss of consciousness, which can lead to coma and death, signs of adrenergic stimulation such as sweating, skin moisture, aggression , tachycardia, palpitations, increased blood pressure, chest pain and arrhythmias). Uncommon: abdominal pain, nausea, vomiting, indigestion, diarrhea and constipation (can be avoided or minimized by taking gliclazide during breakfast). Rare: rash, pruritus, urticaria, erythema, maculopapular eruptions, bullous reactions, changes in the hematological picture (anemia, leukopenia, thrombocytopenia, granulocytopenia), increased liver enzymes (AST, ALAT, alkaline phosphatase), hepatitis (individual cases ), transient visual disturbances (especially at the beginning of treatment due to changes in blood glucose). Treatment should be discontinued if cholestatic icterus occurs. Side effects of the drug group (sulfonylurea): anemia, agranulocytosis, haemolytic anemia, pancytopenia and allergic vasculitis; cases of elevated liver enzymes and even hepatic impairment (eg cholestasis and jaundice) and hepatitis which have passed after discontinuation of a sulphonylurea or (in some cases) lead to life-threatening liver failure have also been observed.

Orally. The expected blood glucose and drug dosage should be selected individually, depending on the severity of diabetes. Adults: the usual starting dose is 40-80 mg a day before breakfast. If necessary, the dose can be increased by 40-80 mg every 7 to 14 days until satisfactory metabolic control is achieved. The maximum dose is 320 mg / day. The maintenance dose is usually 80-160 mg in two divided doses (before breakfast and before supper). Higher doses (up to 320 mg / day) may be used, although an increase in the dose above 160 mg / day has not been shown to improve glycemic control. In elderly patients, the usual starting dose is 40 mg before breakfast, with the possibility of increasing the dose by 40 mg every 7 to 14 days. The doses above 160 mg / day should be used with caution, especially in the presence of renal dysfunction. The tablets should be swallowed without chewing, with water, preferably 30 minutes before a meal.