Monotherapy and Combination Therapy: Sitagliptin is used as an add-on to diet and exercise to improve blood sugar control in adults with type 2 diabetes mellitus.

Important Limitations of Use: Sitagliptin should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis, as it is not effective in these conditions. It has not been studied in patients with a history of Pancreatitis, and it is not known whether such patients have a higher risk of developing pancreatitis while using this medicine.

Sitagliptin is a DPP-4 inhibitor that works by slowing the breakdown of incretin hormones. This increases the level of active hormones and prolongs their effect. Incretin hormones, such as GLP-1 and GIP, are released from the intestine throughout the day and increase after meals. These hormones are normally broken down quickly by the DPP-4 enzyme. When blood glucose levels are normal or high, GLP-1 and GIP increase insulin production and release from pancreatic beta cells. GLP-1 also reduces glucagon release from alpha cells, which decreases glucose production in the liver. By increasing active incretin levels, Sitagliptin enhances insulin release and lowers glucagon levels in a glucose-dependent manner. It selectively inhibits DPP-4 and does not significantly affect DPP-8 or DPP-9 at usual therapeutic doses.

The recommended dose of sitagliptin is 50 mg twice a day and 100 mg once daily. Sitagliptin can be taken with or without food.

Effects of sitagliptin on other drugs: Sitagliptin does not significantly affect the pharmacokinetics of drugs such as metformin, glyburide, simvastatin, rosiglitazone, warfarin, or oral contraceptives.

Digoxin: Sitagliptin may cause a slight increase in digoxin levels, but no dose adjustment is generally required for either medication.

Patients with a history of serious hypersensitivity reactions to Sitagliptin, such as anaphylaxis or angioedema, should not use this medicine.

Common side effects include headache, upper respiratory tract infection, and nasopharyngitis. Hypoglycemia may occur when Sitagliptin is used with sulfonylurea or insulin.

Pregnancy Category B. Animal studies (rats and rabbits) have not shown harmful effects, but human data are limited. This drug should be used during pregnancy only if clearly needed.
Sitagliptin is found in the milk of lactating rats, but it is not known whether it passes into human breast milk. Caution is advised when used in breastfeeding mothers.

If Pancreatitis is suspected, Sitagliptin should be stopped immediately and appropriate treatment started.

Use in patients with renal insufficiency: Dose adjustment is required in moderate to severe renal impairment and in patients with ESRD undergoing dialysis.

Use with hypoglycemia-causing drugs: Dose adjustment of sulfonylurea or insulin may be necessary when used together to reduce hypoglycemia risk.

Hypersensitivity reactions: Serious allergic reactions such as anaphylaxis, angioedema, and severe skin reactions (including Stevens-Johnson syndrome) have been reported. If such reactions occur, discontinue the drug and start alternative therapy.

Pediatric Use: The safety and effectiveness of Sitagliptin in children and adolescents under 18 years of age have not been established.

Geriatric Use: This medicine is mainly eliminated through the kidneys. Since older patients are more likely to have reduced kidney function, careful dose selection is required. Kidney function should be assessed before starting treatment and monitored periodically during therapy.

Renal impairment dosing: Mild renal impairment: (CrCl <50 mL/min or serum creatinine <1.7 mg/dL in men and <1.5 mg/dL in women) → No dose adjustment required

Moderate renal impairment: (CrCl 30–<50 mL/min or serum creatinine >1.7–<3.0 mg/dL in men and >1.5–<2.5 mg/dL in women) → 50 mg once daily

Severe renal impairment / ESRD: (CrCl <30 mL/min or serum creatinine >3.0 mg/dL in men and >2.5 mg/dL in women, including dialysis patients) → 25 mg once daily
Sitagliptin can be given without considering timing of hemodialysis.

In clinical studies, healthy subjects received single doses of up to 800 mg Sitagliptin without clinically significant harmful effects. A small increase in QTc interval (about 8 msec) was observed at this dose, which is not considered clinically important. No experience is available with doses above 800 mg. In multiple-dose studies, no dose-related serious adverse effects were seen with doses up to 600 mg/day for 10 days and 400 mg/day for 28 days.

In case of overdose, supportive treatment should be provided, such as removing unabsorbed drug from the stomach, monitoring the patient (including ECG if needed), and giving appropriate symptomatic care. Sitagliptin can be partially removed by hemodialysis (about 13.5% over 3–4 hours). Prolonged dialysis may be considered if necessary. It is not known whether peritoneal dialysis can remove this drug.

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Store below 25°C in a dry place, protected from light. Keep out of reach of children. Do not use after expiry. Use only with a registered physician’s prescription.