Meliglix (Sitagliptin)

Sitagliptin is used in the treatment of type 2 diabetes mellitus, targeting the incretin pathway to improve glycaemic control.

• Type 2 diabetes mellitus: improves blood glucose control as monotherapy or in combination with other antidiabetic agents.
• Inadequate control with metformin alone: provides additional HbA1c reduction when added to metformin therapy.
• Patients intolerant to sulfonylureas: offers an oral alternative with a low risk of hypoglycaemia.

• Sitagliptin selectively inhibits the enzyme dipeptidyl peptidase‑4 (DPP‑4), which degrades the incretin hormones GLP‑1 and GIP. By blocking DPP‑4, sitagliptin increases circulating levels of these hormones, enhancing glucose‑dependent insulin secretion from pancreatic β‑cells and suppressing glucagon release from α‑cells, thereby lowering post‑prandial and fasting plasma glucose concentrations. The effect is glucose‑dependent, minimizing the risk of hypoglycaemia, and it does not significantly affect gastric emptying or carbohydrate absorption.

Sitagliptin may be associated with several adverse reactions, which are categorized by frequency and severity.

Common Side Effects

• Nasopharyngitis: inflammation of the nasal passages and throat.
• Headache: mild to moderate pain in the head.
• Upper respiratory tract infection: symptoms such as cough and congestion.
• Gastrointestinal discomfort: includes nausea, abdominal pain or dyspepsia.

Serious or Rare Side Effects

• Pancreatitis: severe abdominal pain with elevated enzymes.
• Severe allergic reactions: including anaphylaxis, angioedema or skin rash.
• Stevens‑Johnson syndrome: rare but serious skin eruption.
• Hepatic injury: abnormal liver function tests or hepatitis.

When prescribing sitagliptin, clinicians should consider several safety considerations to minimize risk.

• Renal impairment: dose adjustment may be required in patients with reduced kidney function.
• Hepatic impairment: use with caution and monitor liver enzymes.
• History of pancreatitis: avoid use due to potential recurrence.
• Concomitant sulfonylurea therapy: monitor for signs of hypoglycaemia.
• Pregnancy and lactation: safety not established; use only if potential benefit justifies the risk.
• Store at room temperature: keep in the original container, protect from moisture and light.

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

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors: may increase sitagliptin plasma concentrations.
• Combination with insulin or sulfonylureas: heightened risk of severe hypoglycaemia.

Moderate Interactions (Monitor Closely)

• Diuretics: may affect glycaemic control, requiring monitoring.
• ACE inhibitors: monitor blood pressure and renal function.
• Rifampin: may reduce sitagliptin exposure, potentially decreasing effectiveness.