Sitagliptin is an oral antihyperglycemic agent used to treat type 2 diabetes. It is a dipeptidyl peptidase-4 (DPP-4) inhibitor. Here’s an overview of its key aspects:
Mechanism of Action:
- Sitagliptin works by inhibiting the DPP-4 enzyme, which is responsible for breaking down incretin hormones like GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide).
- By inhibiting DPP-4, sitagliptin increases the levels of these hormones, which in turn:
- Enhances insulin release from the pancreas in a glucose-dependent manner.
- Suppresses glucagon secretion, reducing glucose production by the liver.
- Delays gastric emptying to help regulate blood sugar levels.
Indications:
- Sitagliptin is used to improve glycemic control in adults with type 2 diabetes mellitus, either as monotherapy or in combination with other antidiabetic medications like metformin, sulfonylureas, or insulin.
Dosage:
- The typical dose is 100 mg once daily, with or without food.
- Dosage adjustments may be needed for patients with renal impairment.
Side Effects:
Common side effects include:
- Upper respiratory tract infections
- Headache
- Nasopharyngitis
- Gastrointestinal symptoms (e.g., nausea, diarrhea)
Rare but serious side effects may include:
- Pancreatitis (inflammation of the pancreas)
- Severe allergic reactions (e.g., angioedema)
- Joint pain
- Hypoglycemia (when used with other antidiabetic drugs)
Contraindications:
- Sitagliptin is contraindicated in patients with a history of hypersensitivity to the drug or its components.
- It is not recommended for type 1 diabetes or diabetic ketoacidosis.
Drug Interactions:
- Sitagliptin has a low potential for drug interactions but may interact with:
- Other antidiabetic drugs (increased risk of hypoglycemia)
- Drugs that affect kidney function (e.g., NSAIDs, ACE inhibitors)
Special Considerations:
- Renal Impairment: Dose adjustment is required for patients with moderate to severe kidney disease.
- Pregnancy and Lactation: Use only if the potential benefit justifies the potential risk to the fetus or infant.
- Elderly Patients: No dose adjustment is needed based on age alone, but renal function should be monitored.
Brand Names:
- Sitagliptin is marketed under the brand name Januvia and is also available in combination with metformin as Janumet.
Consult a healthcare provider for personalized medical advice and treatment.