Glipterin (Sitagliptin)

Glipterin (sitagliptin) is indicated for the management of type 2 diabetes mellitus as part of a comprehensive treatment plan that includes diet, exercise, and other glucose‑lowering therapies.

• Use as monotherapy in patients who cannot achieve glycemic targets with diet and exercise alone.
• Combine with metformin when metformin alone does not provide adequate control.
• Add to sulfonylureas, thiazolidinediones, or insulin when additional reduction in HbA1c is needed.
• Consider in patients with renal impairment where dose adjustment is recommended according to renal function.
• May be used in elderly patients when individualized dosing is applied.

The safety profile of sitagliptin includes a range of adverse events that are generally classified by frequency and severity.

Common

• Upper respiratory tract infection (e.g., nasopharyngitis).
• Headache.
• Gastrointestinal discomfort such as nausea or abdominal pain.
• Mild hypoglycemia when combined with insulin or sulfonylureas.

Serious

• Pancreatitis (severe abdominal pain).
• Severe hypersensitivity reactions including angioedema or Stevens‑Johnson syndrome.
• Acute renal failure in patients with pre‑existing kidney disease.
• Heart failure exacerbation reported in rare cases.

Before initiating Glipterin, clinicians should evaluate several clinical factors to minimize risks and ensure appropriate use.

• Assess renal function; dose may need adjustment in moderate to severe impairment.
• Review history of pancreatitis; avoid use if active pancreatitis is present.
• Monitor for signs of hypersensitivity, especially skin rash or swelling.
• Use caution in patients with a history of heart failure.
• Consider pregnancy and lactation status; safety data are limited.
• Evaluate concomitant use of strong CYP3A4 or P‑glycoprotein inhibitors.

Sitagliptin can interact with other medicines, affecting its concentration or the effect of co‑administered drugs.

Avoid

• Strong CYP3A4 or CYP2C8 inhibitors (e.g., ketoconazole, gemfibrozil) that may increase sitagliptin exposure.
• Concurrent use with insulin secretagogues that may cause severe hypoglycemia without dose adjustment.

Use with caution

• Diuretics and antihypertensives, as fluid shifts may affect renal clearance.
• Rifampin or other enzyme inducers that can lower sitagliptin levels.
• Other DPP‑4 inhibitors; combined effect is not recommended.
• NSAIDs or nephrotoxic agents in patients with reduced kidney function.