Sitagliptin

What it is and how it works

Mechanism of Action Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4.

Mechanism class: Dipeptidyl Peptidase 4 Inhibitors

Indications

Sitagliptin Tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Sitagliptin Tablets is not recommended in patients with type 1 diabetes mellitus. Sitagliptin Tablets have not been studied in patients with a history of pancreatitis. It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using Sitagliptin Tablets. . Sitagliptin Tablets are a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use: Sitagliptin Tablets are not recommended in patients with type 1 diabetes mellitus. Sitagliptin Tablets has not been studied in patients with a history of pancreatitis.

Dosage and administration (summary)

The recommended dosage of Sitagliptin Tablets is 100 mg orally once daily. Sitagliptin Tablets can be taken with or without food. Dosage adjustment is recommended for patients with eGFR less than 45 mL/min/1.73 m 2 . Dosage Adjustment in Patients with Renal Impairment eGFR greater than or equal to 30 mL/min/1.73 m 2 to less than 45 mL/min/1.73 m 2 eGFR less than 30 mL/min/1.73 m 2 (including patients with end stage renal disease [ESRD] on dialysis) 50 mg once daily 25 mg once daily Recommended Dosage The recommended dosage of Sitagliptin Tablets is 100 mg orally once daily. Sitagliptin Tablets can be taken with or without food.

Contraindications

Sitagliptin Tablets is contraindicated in patients with a history of a serious hypersensitivity reaction to sitagliptin or any of the excipients in Sitagliptin Tablets. Serious hypersensitivity reactions, including anaphylaxis and angioedema have been reported with sitagliptin. . History of a serious hypersensitivity reaction to sitagliptin or any of the excipients in Sitagliptin Tablets, such as anaphylaxis or angioedema

Warnings and precautions

Pancreatitis: There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue Sitagliptin Tablets. Heart failure: Heart failure has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of Sitagliptin Tablets in patients who have known risk factors for heart failure. Monitor patients for signs and symptoms. Acute Renal Failure: Has been reported postmarketing, sometimes requiring dialysis.

Pregnancy

Pregnancy Risk Summary The limited available data with sitagliptin in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy .

Storage and supply

Sitagliptin Tablets are supplied as follows: Tablet Strength Physical Description How Supplied NDC # 25 mg sitagliptin White to off white, round, biconvex, film coated tablets debossed with "12" on one side and "40" on the other side Bottles of 30 tablets with child-resistant closure.

Source: Sitagliptin (Sitagliptin) — US FDA prescribing information, 2025-01-31, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.