Gliclamet is a combination of gliclazide, an oral hypoglycemic agent from the sulfonylurea class that primarily works by increasing insulin secretion, and metformin, a biguanide that primarily acts by reducing insulin resistance.
Each uncoated tablet contains:
Gliclazide BP – 80 mg
Metformin Hydrochloride BP – 500 mg
Gliclamet is a combination of gliclazide, an oral hypoglycemic agent from the sulfonylurea class that primarily works by increasing insulin secretion, and metformin, a biguanide that primarily acts by reducing insulin resistance.
Sulfonylureas and biguanides have complementary mechanisms of action.
Both agents provide an additive antihyperglycemic effect without increasing the adverse effects typically associated with their respective pharmacological classes.
Mechanism of Action:
Gliclazide is a hypoglycemic sulfonylurea derivative structurally distinguished by the presence of a nitrogen-containing heterocyclic ring with an endocyclic bond.
It lowers blood glucose levels primarily by stimulating insulin secretion from pancreatic β-cells. This effect is mediated through the closure of ATP-sensitive potassium (K⁺) channels in the β-cell membrane, resulting in membrane depolarization, opening of calcium (Ca²⁺) channels, increased intracellular calcium concentration, and subsequent insulin release. Gliclazide also enhances the sensitivity of β-cells to glucose.
Gliclazide improves peripheral insulin sensitivity by reducing hepatic glucose production and increasing peripheral glucose utilization and clearance. Enhanced postprandial insulin and C-peptide secretion is maintained even during long-term treatment.
It also exhibits hemovascular properties, including antiplatelet and antioxidant effects, which may contribute to the prevention of microvascular complications. Repeated administration has also been associated with reductions in plasma cholesterol and triglyceride levels.
Mechanism of Action:
Metformin is an antihyperglycemic agent of the biguanide class. It lowers both fasting and postprandial plasma glucose levels without stimulating insulin secretion and therefore does not cause hypoglycemia.
Metformin primarily acts by reducing hepatic glucose production through inhibition of gluconeogenesis and glycogenolysis. It also improves insulin sensitivity in peripheral tissues, particularly skeletal muscle, thereby enhancing glucose uptake and utilization. In addition, it decreases intestinal glucose absorption.
Metformin stimulates intracellular glycogen synthesis by acting on glycogen synthase and increases the transport capacity of glucose transporters (GLUT). It also has beneficial effects on serum lipid levels and fibrinolytic activity and is not associated with weight gain.
Gliclamet is indicated for the treatment of Type 2 diabetes mellitus, in combination with diet and exercise, when these measures alone are insufficient to achieve adequate glycemic control.
The recommended starting dose is one tablet once daily after breakfast.
If adequate glycemic control is not achieved, the dose may be increased to one tablet twice daily.
The maximum daily dose is four tablets, administered in divided doses.
Gliclamet is contraindicated in patients with:
Type 1 diabetes mellitus
Hypersensitivity to sulfonylureas, metformin, or any component of the product
Renal disease or renal impairment (e.g., serum creatinine ≥1.5 mg/dL in men or ≥1.4 mg/dL in women, or impaired creatinine clearance), including conditions associated with renal dysfunction such as cardiovascular collapse (shock), acute myocardial infarction, or septicemia
Severe hepatic impairment
Congestive heart failure requiring pharmacological treatment
Pregnancy and breastfeeding
Diabetic ketoacidosis
Patients undergoing surgery or experiencing severe trauma or severe infections
Treatment with Gliclamet should be temporarily discontinued before radiological procedures involving intravascular administration of iodinated contrast agents, as these may cause acute deterioration of renal function.
Store in a dry place at a temperature below 30°C.
Protect from light.
Keep out of the reach of children.
