Gemigliptin/rosuvastatin

A combination medication used in the management of type 2 diabetes and hyperlipidemia.

Gemigliptin/rosuvastatin is a fixed-dose combination medication used in the treatment of type 2 diabetes mellitus and hyperlipidemia. This combination includes two active pharmaceutical ingredients: gemigliptin, a DPP-4 inhibitor, and rosuvastatin, a statin used to lower cholesterol levels.

Pharmacology

Gemigliptin

Gemigliptin is a dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor) that works by increasing the levels of incretin hormones, which in turn increase insulin secretion and decrease glucagon levels in the blood. This helps to control blood sugar levels in patients with type 2 diabetes.

• Mechanism of Action: Gemigliptin inhibits the DPP-4 enzyme, which is responsible for the degradation of incretin hormones such as GLP-1 and GIP. By inhibiting this enzyme, gemigliptin prolongs the action of incretin hormones, enhancing insulin secretion and reducing glucagon release.

• Pharmacokinetics: Gemigliptin is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours. It is primarily metabolized in the liver and excreted in the urine.

Rosuvastatin

Rosuvastatin is a HMG-CoA reductase inhibitor (statin) that reduces cholesterol levels by inhibiting the enzyme responsible for cholesterol synthesis in the liver.

• Mechanism of Action: Rosuvastatin competitively inhibits HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This results in decreased cholesterol synthesis and increased uptake of LDL cholesterol from the blood.

• Pharmacokinetics: Rosuvastatin is absorbed in the gastrointestinal tract, with peak plasma concentrations reached within 3-5 hours. It is metabolized in the liver and excreted primarily in the feces.

Clinical Use

Gemigliptin/rosuvastatin is indicated for patients with type 2 diabetes who also have elevated cholesterol levels. The combination therapy aims to improve glycemic control while simultaneously managing dyslipidemia, reducing the risk of cardiovascular events.

Adverse Effects

Common side effects of gemigliptin/rosuvastatin may include:

• Hypoglycemia: Particularly when used in combination with other antidiabetic medications.
• Muscle pain: A known side effect of statins, which can lead to more serious conditions such as rhabdomyolysis.
• Gastrointestinal disturbances: Such as nausea and diarrhea.

Contraindications

This combination is contraindicated in patients with:

• Severe liver impairment
• Pregnancy and lactation
• Known hypersensitivity to either gemigliptin or rosuvastatin

Also see

• Type 2 diabetes mellitus
• Hyperlipidemia
• Dipeptidyl peptidase-4 inhibitor
• Statin