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Pharmacology of Sitagliptin ; Mechanism of action, Pharmacokinetics, Uses, Effects
Sitagliptin is an oral antihyperglycemic agent used to treat type 2 diabetes mellitus. Here are some key points about its pharmacology:
Mechanism of Action
Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It works by inhibiting the DPP-4 enzyme, which is responsible for the degradation of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By preventing the breakdown of these hormones, sitagliptin increases their levels, leading to enhanced insulin secretion in response to meals and improved glycemic control.
Pharmacokinetics
Absorption: Sitagliptin is well absorbed orally, with peak plasma concentrations typically occurring within 1 to 4 hours after ingestion.
Metabolism: It is extensively metabolized in the liver to inactive metabolites.
Excretion: The metabolites are excreted in the urine (80%) and feces.
Elimination Half-Life: The half-life is approximately 8 to 14 hours.
Indications
Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is also available in combination with metformin (Janumet) and other antidiabetic medications1.
Dosage
Adults: The usual dose is 100 mg once daily, taken with or without food.
Administration: Take sitagliptin at the same time each day to help you remember.
Side Effects
Common: Headache, upper respiratory tract infection, and swelling of the legs.
Serious: Hypoglycemia (especially when used with other antidiabetic medications), pancreatitis, and allergic reactions.
Contraindications
Hypersensitivity to sitagliptin or any of its components.
Type 1 Diabetes Mellitus: Not for treating type 1 diabetes mellitus.
Diabetic Ketoacidosis: Not for treating diabetic ketoacidosis.
Special Precautions
Hypoglycemia: Monitor blood glucose levels regularly and be cautious with dosing to avoid hypoglycemia.
Pancreatitis: Be aware of the signs and symptoms of pancreatitis and discontinue use if pancreatitis is suspected
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