Maysiglu (Sitagliptin)

Sitagliptin is used in the treatment of type 2 diabetes mellitus, a chronic metabolic disorder characterized by insulin resistance and impaired insulin secretion.

• Type 2 diabetes mellitus: improves glycemic control as monotherapy when diet and exercise are insufficient.
• Combination with metformin: provides additional glucose‑lowering effect for patients inadequately controlled on metformin alone.
• Use with sulfonylureas or insulin: allows dose reduction of the co‑administered agents to minimize hypoglycemia risk.

• Sitagliptin selectively inhibits the dipeptidyl peptidase‑4 (DPP‑4) enzyme, which degrades the incretin hormones glucagon‑like peptide‑1 (GLP‑1) and glucose‑dependent insulinotropic polypeptide (GIP). By blocking DPP‑4, sitagliptin raises circulating levels of GLP‑1 and GIP, enhancing glucose‑dependent insulin secretion from pancreatic β‑cells and suppressing glucagon release from α‑cells, thereby reducing post‑prandial and fasting blood glucose concentrations.

Sitagliptin may be associated with a range of adverse reactions, which are classified by frequency and severity.

Common Side Effects

• Nausea: mild to moderate stomach upset.
• Headache: transient cranial pain.
• Nasopharyngitis: inflammation of the nasal passages and throat.
• Upper respiratory tract infection: symptoms such as cough and congestion.
• Dizziness: occasional light‑headedness.
• Arthralgia: joint pain without swelling.

Serious or Rare Side Effects

• Pancreatitis: severe abdominal pain with elevated enzymes.
• Severe allergic reactions: including anaphylaxis and angioedema.
• Stevens‑Johnson syndrome or toxic epidermal necrolysis: extensive skin detachment.
• Hepatic injury: marked elevation of liver enzymes.
• Hypoglycemia: when combined with insulin or sulfonylureas.
• Bullous pemphigoid: autoimmune blistering skin disorder.

Before initiating sitagliptin therapy, clinicians should consider several safety and monitoring measures.

• Renal function: assess creatinine clearance and adjust dose in moderate to severe impairment.
• Pancreatitis risk: discontinue if patient develops persistent severe abdominal pain.
• Hypersensitivity: monitor for signs of rash, angioedema, or anaphylaxis.
• Concomitant sulfonylureas or insulin: reduce their dose to avoid hypoglycemia.
• Hepatic impairment: use with caution in patients with liver disease.
• Store at ambient temperature: keep below 25 °C in the original container, protected from moisture and light.

Sitagliptin can interact with other medicines, altering its efficacy or safety profile.

Major Interactions (Avoid)

• Insulin: combined use may cause severe hypoglycemia.
• Sulfonylureas: increased risk of low blood glucose.
• Strong CYP2C8 inhibitors (e.g., gemfibrozil): may raise sitagliptin plasma levels.

Moderate Interactions (Monitor Closely)

• ACE inhibitors: possible additive effect on blood pressure.
• Diuretics: monitor renal function and electrolytes.
• Rifampin: may reduce sitagliptin exposure, decreasing effectiveness.
• NSAIDs: can affect renal function, especially in dehydrated patients.
• Digoxin: potential increase in serum digoxin concentrations.