MELANOV MR 60

Indications

• Type 2 diabetes mellitus
• Non-insulin dependent diabetes mellitus
• Management of hyperglycemia in patients not adequately controlled with diet and exercise

Dosage

Children: Not indicated for use in children.

Adults: Refer to BNF for specific dosing information.

Mechanism of action

Gliclazide enhances insulin secretion from the pancreatic beta cells by binding to the sulfonylurea receptor (SUR1) which is part of the ATP-sensitive potassium channels on the cell membrane. This action leads to closure of these channels, depolarization of the cell membrane, and subsequent influx of calcium ions, triggering insulin release. Additionally, gliclazide may improve insulin sensitivity in peripheral tissues and reduce hepatic glucose production.

Pharmacodynamics

Gliclazide lowers blood glucose levels through its insulinotropic effects, which lead to increased insulin release in response to glucose levels. It has a relatively low risk of inducing hypoglycemia compared to other sulfonylureas, due to its shorter duration of action and its ability to modulate insulin secretion based on blood glucose levels. Gliclazide also has antioxidant properties and may have a beneficial effect on endothelial function.

Pharmacokinetics

Gliclazide is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically occurring within 2-4 hours after ingestion. It is about 90% protein-bound and has a half-life of approximately 10-12 hours. The drug undergoes hepatic metabolism, primarily through cytochrome P450 enzymes, and is excreted in urine as metabolites, with less than 1% excreted unchanged. Renal impairment may affect its clearance, necessitating dosage adjustments in affected individuals.

Contra-indications

• Hypersensitivity to glicalazide or any of its components
• Type 1 diabetes mellitus
• Diabetic ketoacidosis
• Severe renal impairment
• Severe hepatic impairment

Adverse effects

• Hypoglycemia
• Weight gain
• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Allergic skin reactions (rash, pruritus)
• Hematological reactions (leukopenia, thrombocytopenia)

Interactions

• Other antidiabetic agents (increased risk of hypoglycemia)
• Beta-blockers (may mask symptoms of hypoglycemia)
• Corticosteroids (may reduce the hypoglycemic effect)
• Thiazide diuretics (may increase blood glucose levels)
• Alcohol (can potentiate hypoglycemia)

Precautions

• Monitor blood glucose levels regularly
• Caution in patients with renal or hepatic impairment
• Use with caution in elderly patients or those with a history of cardiovascular disease
• Regular monitoring of liver function tests is advisable

Pregnancy

Glicalazide is not recommended during pregnancy due to potential harm to the fetus. Insulin is the preferred treatment for managing diabetes during pregnancy.

Breast-feeding

Glicalazide is excreted in breast milk, and caution should be exercised when administering to nursing mothers. Monitoring of the infant for hypoglycemia is recommended.

Storage

Store in a cool, dry place at room temperature. Protect from light and moisture. Keep out of reach of children.

Formulations

• Tablets