西格列汀（Sitagliptin）
Overview
Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor indicated for the treatment of type 2 diabetes mellitus. It can be used as monotherapy or in combination with other oral antidiabetic agents like metformin or sulfonylureas.
Mechanism of Action
It inhibits the DPP-4 enzyme, which is responsible for the degradation of incretin hormones such as GLP-1 and GIP. By prolonging the action of these incretins, sitagliptin enhances glucose-dependent insulin secretion from the pancreas and suppresses glucagon secretion, leading to lower blood glucose levels.
Dosage and Administration
The recommended dose is 100 mg once daily, taken with or without food. Dosage adjustments are necessary for patients with moderate to severe renal impairment to prevent drug accumulation.
Side Effects
Sitagliptin is generally well-tolerated. Common side effects include upper respiratory tract infections, headache, and nasopharyngitis. Unlike sulfonylureas, it has a low risk of causing hypoglycemia when used alone and is weight-neutral. Rare but serious side effects include acute pancreatitis and severe joint pain.
Contraindications
It is contraindicated in patients with a history of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema. It is not for the treatment of type 1 diabetes or diabetic ketoacidosis.
Pregnancy and Lactation
There is limited data on the use of sitagliptin in pregnant women. It should be used during pregnancy only if clearly needed. It is unknown whether sitagliptin is excreted in human milk, so caution should be exercised when administered to a nursing woman.
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