Sitagliptin

 Sitagliptin – Full Introduction

Sitagliptin is an oral antihyperglycemic agent used in the management of type 2 diabetes mellitus (T2DM). It belongs to the dipeptidyl peptidase-4 (DPP-4) inhibitor class and works by enhancing the body’s natural incretin system to regulate blood glucose.

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Drug Class

• DPP-4 inhibitor (Gliptin)

• Oral antidiabetic agent

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Mechanism of Action

Sitagliptin inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which breaks down incretin hormones (GLP-1 and GIP). By increasing incretin levels, sitagliptin:

• Stimulates glucose-dependent insulin release from pancreatic beta cells

• Suppresses glucagon secretion from pancreatic alpha cells

• Reduces hepatic glucose production

• Does not cause significant hypoglycemia when used alone

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Therapeutic Uses

• Type 2 diabetes mellitus (as monotherapy or in combination with metformin, sulfonylureas, or insulin)

• Suitable for patients who cannot tolerate other oral antidiabetics

• Can be used for weight-neutral glycemic control

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Benefits

• Effective in lowering fasting and postprandial blood glucose

• Weight neutral (does not cause weight gain)

• Low risk of hypoglycemia when used alone

• Oral once-daily dosing

• Can be combined safely with other antidiabetic agents

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Common Side Effects

• Nasopharyngitis (common cold symptoms)

• Headache

• Mild gastrointestinal symptoms (nausea, diarrhea)

• Upper respiratory tract infection

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Serious but Rare Side Effects

• Acute pancreatitis (rare)

• Severe hypersensitivity reactions (angioedema, anaphylaxis)

• Joint pain (arthralgia, rare)

• Severe renal impairment may require dose adjustment

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Contraindications & Precautions

• Type 1 diabetes or diabetic ketoacidosis (not effective)

• History of pancreatitis

• Severe renal impairment (dose adjustment required)

• Hypersensitivity to sitagliptin

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Dosage & Administration

• Standard dose: 100 mg orally once daily

• Dose adjustment required in renal impairment

• Can be taken with or without food

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Conclusion

Sitagliptin is a safe, weight-neutral, and effective oral antidiabetic agent for type 2 diabetes, particularly useful in combination therapy or for patients at risk of hypoglycemia. Regular monitoring of renal function is recommended, and caution should be taken in patients with a history of pancreatitis.