Glimepiride/rosiglitazone

A combination medication used in the management of type 2 diabetes mellitus

Glimepiride/rosiglitazone is a combination medication used in the management of type 2 diabetes mellitus. It combines two antidiabetic agents: glimepiride, a sulfonylurea, and rosiglitazone, a thiazolidinedione. This combination is designed to improve glycemic control in patients who require treatment with both a sulfonylurea and a thiazolidinedione.

Pharmacology

Glimepiride

Glimepiride is a sulfonylurea that works by stimulating the release of insulin from the pancreatic beta cells. It binds to the sulfonylurea receptor on the beta cell surface, leading to closure of ATP-sensitive potassium channels, depolarization of the cell membrane, and subsequent opening of voltage-gated calcium channels. The influx of calcium ions triggers the exocytosis of insulin-containing granules.

Rosiglitazone

Rosiglitazone is a thiazolidinedione that acts as an agonist of the peroxisome proliferator-activated receptor gamma (PPAR-γ). Activation of PPAR-γ modulates the transcription of genes involved in glucose and lipid metabolism, enhancing insulin sensitivity in adipose tissue, skeletal muscle, and the liver. This results in improved glycemic control by increasing peripheral glucose uptake and decreasing hepatic glucose production.

Indications

Glimepiride/rosiglitazone is indicated for the treatment of type 2 diabetes mellitus in patients who do not achieve adequate glycemic control with diet, exercise, and monotherapy with either glimepiride or rosiglitazone alone. It is used as an adjunct to diet and exercise to improve glycemic control.

Contraindications

The use of glimepiride/rosiglitazone is contraindicated in patients with:

• Type 1 diabetes mellitus
• Diabetic ketoacidosis
• Severe heart failure (NYHA Class III or IV)
• Known hypersensitivity to either glimepiride, rosiglitazone, or any of the excipients in the formulation

Adverse Effects

Common adverse effects of glimepiride/rosiglitazone include:

• Hypoglycemia
• Weight gain
• Edema
• Headache
• Upper respiratory tract infection

Serious adverse effects may include:

• Cardiovascular events (e.g., myocardial infarction)
• Hepatic dysfunction
• Hematologic effects (e.g., anemia)

Drug Interactions

Glimepiride/rosiglitazone may interact with other medications, including:

• Insulin or other antidiabetic agents, which may increase the risk of hypoglycemia
• CYP2C8 inhibitors or inducers, which may affect the metabolism of rosiglitazone
• Drugs that affect renal function, which may alter the pharmacokinetics of glimepiride

Monitoring

Patients on glimepiride/rosiglitazone should be monitored for:

• Blood glucose levels to assess efficacy
• Signs and symptoms of heart failure
• Liver function tests
• Hemoglobin and hematocrit levels

Also see

• Type 2 diabetes mellitus
• Sulfonylurea
• Thiazolidinedione
• Insulin
• Metformin