GLUSTAL-2-TABLETS

Indications

• Type 2 diabetes mellitus
• Non-insulin dependent diabetes mellitus

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: Refer to the BNF for specific dosing guidelines based on individual patient needs and considerations.

Mechanism of action

Glimipride acts by binding to the sulfonylurea receptor (SUR1) on the pancreatic beta cells, which is part of the ATP-sensitive potassium (K-ATP) channel. This binding leads to the closure of the K-ATP channel, resulting in cell depolarization and an influx of calcium ions. The increase in intracellular calcium triggers the exocytosis of insulin granules, enhancing insulin secretion and subsequently lowering blood glucose levels. Additionally, glimipride may improve peripheral insulin sensitivity.

Pharmacodynamics

The pharmacodynamics of glimipride include its ability to stimulate insulin release in a glucose-dependent manner, meaning that it enhances insulin release primarily when blood glucose levels are elevated. This characteristic helps to minimize the risk of hypoglycemia compared to other sulfonylureas. Glimipride also exhibits effects on reducing hepatic glucose production and improves insulin sensitivity in peripheral tissues.

Pharmacokinetics

Glimipride is well absorbed from the gastrointestinal tract, with a peak plasma concentration typically reached within 1 to 3 hours after oral administration. It is highly protein-bound (approximately 99%) and has a relatively long half-life of about 5 to 9 hours, which allows for once-daily dosing in most cases. The drug is metabolized in the liver primarily via CYP2C9 to its inactive metabolites, and excretion is mainly through urine, with a small fraction eliminated in feces.

Contra-indications

• Hypersensitivity to glimipiride or any of its components
• Diabetes type 1 (insulin-dependent diabetes)
• Diabetic ketoacidosis
• Severe renal or hepatic impairment

Adverse effects

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

Interactions

• Coadministration with other antidiabetic agents may increase the risk of hypoglycemia
• Sulfonamide antibiotics may potentiate the effects of glimipiride
• Corticosteroids may reduce the hypoglycemic effect
• Beta-blockers may mask the symptoms of hypoglycemia
• Alcohol can increase the risk of hypoglycemia or hyperglycemia

Precautions

• Monitor blood glucose levels regularly, especially during initiation and dose adjustment
• Use with caution in patients with liver or kidney impairment
• Assess for signs of hypoglycemia, especially in the elderly and those with irregular meal patterns
• Inform patients about the risk of hypoglycemia and how to manage it

Pregnancy

Use during pregnancy is not recommended unless clearly needed. The potential risk to the fetus should be considered against the benefits to the mother.

Breast-feeding

Caution is advised when using glimipiride during breastfeeding. It is not known if glimipiride is excreted in human milk.

Storage

Store at room temperature (15-30°C) in a tightly closed container, protected from light and moisture.

Formulations

• Tablets: 1 mg, 2 mg, 3 mg, 4 mg