What it does
Sitagliptin is a medication used to help control blood sugar levels in adults with type 2 diabetes.
Commonly used for: type 2 diabetes, diabetes mellitus
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 20:38:11 · updated 2026-07-26 11:28:43
About this medicine
Sitagliptin is a medication used to help control blood sugar levels in adults with type 2 diabetes.
What it treats
- type 2 diabetes
- diabetes mellitus
How it works
Sitagliptin works by increasing the levels of certain hormones that help your body produce more insulin and lower blood sugar levels after meals.
Who it's for
This medicine is for adults with type 2 diabetes who need help managing their blood sugar levels.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: sitaglitin
Sitagliptin is an oral hypoglycemic agent belonging to the class of DPP-4 inhibitors. It is primarily used in the management of type 2 diabetes mellitus. By inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), sitagliptin increases the levels of incretin hormones, which help to regulate glucose metabolism. It is often used in conjunction with diet and exercise to improve glycemic control.
Indications
- Type 2 diabetes mellitus
- Improvement of glycemic control in adults
Dosage
Children: Refer to the BNF for Children for pediatric dosing guidelines.
Adults: Refer to the BNF for specific dosing guidelines.
Mechanism of action
Sitagliptin works by inhibiting the DPP-4 enzyme, which is responsible for the degradation of incretin hormones such as GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). By preventing the breakdown of these hormones, sitagliptin increases their levels, leading to enhanced insulin secretion in response to meals and decreased glucagon release from the pancreas. This results in lower blood glucose levels.
Pharmacodynamics
Sitagliptin enhances insulin secretion in a glucose-dependent manner, meaning it is more effective when blood glucose levels are elevated. This leads to a reduced risk of hypoglycemia compared to some other antidiabetic medications. It also contributes to a decrease in hepatic glucose production and promotes increased uptake of glucose by peripheral tissues, especially muscle and adipose tissue.
Pharmacokinetics
Sitagliptin is well absorbed after oral administration, with peak plasma concentrations occurring approximately 1-4 hours post-dose. It has a bioavailability of around 87%. The drug is primarily eliminated unchanged in the urine, with a half-life of about 12.4 hours. The pharmacokinetics can be affected by renal function, necessitating dose adjustments in patients with renal impairment.
Contra-indications
- Hypersensitivity to sitagliptin or any of its excipients
- History of serious hypersensitivity reactions (e.g., anaphylaxis, angioedema) associated with sitagliptin
Adverse effects
- Pancreatitis
- Hypoglycemia (especially when used with other antidiabetic agents)
- Nausea
- Diarrhea
- Upper respiratory tract infections
- Headache
- Skin reactions (e.g., rash, urticaria)
Interactions
- May enhance the effects of other antidiabetic medications, leading to increased risk of hypoglycemia
- Concomitant use with medications that induce or inhibit CYP enzymes may alter sitagliptin levels
Precautions
- Monitor for signs and symptoms of pancreatitis
- Exercise caution in patients with renal impairment (dose adjustment may be required)
- Assessment of liver function is advisable before initiation
- Consider risk of hypoglycemia when used with other antidiabetic agents
Pregnancy
Sitagliptin should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. Limited data are available regarding its safety in pregnancy.
Breast-feeding
It is not known whether sitagliptin is excreted in human milk. Caution should be exercised when administering to nursing mothers.
Storage
Store at room temperature, away from moisture and heat. Keep out of reach of children.
Formulations
- Tablets: 25 mg, 50 mg, 100 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.