Mapoli (Sitagliptin)

Sitagliptin is a DPP‑4 inhibitor used to improve glycaemic control in patients with type 2 diabetes mellitus.

• Type 2 diabetes mellitus: lowers fasting and post‑prandial blood glucose levels when combined with diet and exercise.
• Monotherapy in metformin‑intolerant patients: provides an oral glucose‑lowering option without metformin.
• Combination therapy with metformin or other antidiabetics: enhances overall glycaemic reduction compared with either agent alone.

• Sitagliptin selectively inhibits the dipeptidyl peptidase‑4 (DPP‑4) enzyme, preventing the rapid degradation of the incretin hormones GLP‑1 and GIP. Elevated incretin levels increase glucose‑dependent insulin secretion from pancreatic β‑cells and suppress glucagon release from α‑cells, resulting in improved post‑prandial and overall blood glucose regulation.

Sitagliptin is generally well tolerated, but adverse reactions can occur.

Common Side Effects

• Nasopharyngitis: mild upper respiratory symptoms.
• Headache: transient and usually mild.
• Nausea: occasional gastrointestinal discomfort.
• Diarrhoea: loose stools that resolve with continued therapy.
• Upper respiratory tract infection: mild cough or sore throat.

Serious or Rare Side Effects

• Pancreatitis: severe abdominal pain requiring immediate medical attention.
• Severe allergic reactions: rash, angioedema, or anaphylaxis.
• Hepatic injury: elevated liver enzymes or jaundice.
• Joint pain: unexplained arthralgia that may be persistent.
• Bullous pemphigoid: rare skin blistering disorder.

Before initiating sitagliptin therapy, several safety considerations should be reviewed.

• Renal function assessment: dose adjustment may be required in impaired renal function.
• Hepatic function monitoring: avoid use in patients with severe liver disease.
• Hypoglycaemia risk: caution when combined with insulin or sulfonylureas.
• Cardiovascular disease: monitor for any worsening of heart failure symptoms.
• Pregnancy and lactation: safety not established; use only if potential benefit justifies risk.
• Store at ambient temperature: keep in original container, protect from moisture and heat.

Sitagliptin may interact with other medicines, influencing efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole): may increase sitagliptin exposure.
• Insulin or sulfonylureas: heightened risk of hypoglycaemia.
• Rifampin: may reduce sitagliptin plasma concentrations.

Moderate Interactions (Monitor Closely)

• Diuretics: possible alteration of glucose control.
• ACE inhibitors: monitor blood pressure and renal function.
• Warfarin: observe INR for potential changes.