PERGLIM 2

Indications

• Type 2 diabetes mellitus
• Non-insulin dependent diabetes

Dosage

Children: Refer to BNF for Children for specific dosing guidelines.

Adults: Refer to BNF for specific dosing guidelines.

Mechanism of action

Glimepiride acts by binding to the sulfonylurea receptor (SUR1) on the pancreatic beta cells, leading to the closure of ATP-sensitive potassium channels. This depolarization of the cell membrane results in an influx of calcium ions, ultimately stimulating insulin release. Additionally, glimepiride enhances insulin sensitivity in peripheral tissues, facilitating glucose uptake and utilization.

Pharmacodynamics

The pharmacodynamic effects of glimepiride include a reduction in blood glucose levels through increased insulin secretion and improved glycemic control. The onset of action typically occurs within 1 to 3 hours after administration, with a peak effect seen approximately 2 to 3 hours post-dose. The duration of action can last up to 24 hours, allowing for once-daily dosing in most patients.

Pharmacokinetics

Glimepiride is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 2 to 3 hours after oral administration. It undergoes extensive hepatic metabolism, primarily through the cytochrome P450 enzyme system, specifically CYP2C9. The drug has a half-life of approximately 5 to 9 hours, and its metabolites are primarily excreted via the urine. Renal function can significantly affect the clearance of glimepiride, necessitating dose adjustments in patients with renal impairment.

Contra-indications

• Hypersensitivity to glimepiride or any of the excipients
• Diabetic ketoacidosis
• Type 1 diabetes mellitus
• Severe renal impairment
• Severe hepatic impairment

Adverse effects

• Hypoglycemia
• Nausea
• Vomiting
• Diarrhea
• Dizziness
• Headache
• Weight gain
• Allergic skin reactions
• Hepatic enzyme elevation
• Jaundice
• Pancreatitis

Interactions

• Other antidiabetic agents may potentiate the hypoglycemic effect
• NSAIDs may enhance the hypoglycemic effect
• Beta-blockers may mask the symptoms of hypoglycemia
• Corticosteroids may decrease the hypoglycemic effect
• Alcohol can increase or decrease the hypoglycemic effect

Precautions

• Caution in patients with renal or hepatic impairment
• Monitor blood glucose levels regularly
• Caution in patients with a history of hypoglycemia
• Discontinue use if hypersensitivity occurs

Pregnancy

Glimepiride is generally not recommended during pregnancy due to potential effects on fetal insulin production and glucose metabolism. Alternative treatments should be considered.

Breast-feeding

Glimepiride is excreted in breast milk, and caution should be exercised when administering to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets: 1 mg, 2 mg, 3 mg, 4 mg