From the Guidelines
Sitagliptin is a DPP-4 inhibitor used to treat type 2 diabetes, with a standard dose of 100 mg once daily for patients with normal kidney function, but requiring dose adjustments for those with kidney problems, as indicated by a maximum dose of 50 mg daily for patients with an eGFR of 30-44 mL/min/1.73 m2 and 25 mg once daily for those with an eGFR of 15-29 mL/min/1.73 m2 1.
Key Characteristics of Sitagliptin
- Belongs to a class of drugs called DPP-4 inhibitors (dipeptidyl peptidase-4 inhibitors) 1
- Commonly sold under the brand name Januvia
- Works by increasing levels of incretin hormones in the body, which stimulate insulin release when blood sugar is high and reduce the amount of glucose made by the liver 1
- Does not cause weight gain and has a low risk of hypoglycemia when used alone 1
- May cause side effects such as upper respiratory infections, headache, and rarely joint pain
Dosage and Administration
- Typical dosage ranges from 25 to 100 mg once daily 1
- Patients with kidney problems may need a lower dose, with specific dose adjustments required for those with an eGFR of less than 45 mL/min/1.73 m2 1
- Blood sugar monitoring is important when starting or adjusting treatment
Combination Therapy
- Can be used alone or in combination with other diabetes medications like metformin 1
- Clinical studies have shown that HbA1c levels can be further reduced after adding glimepiride, gliclazide, repaglinide, or acarbose to the combination therapy with metformin and sitagliptin 1
From the Research
What is Sitagliptin
- Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used in the treatment of type 2 diabetes mellitus 2, 3, 4, 5, 6.
- It works by increasing the amount of circulating incretins, which stimulate insulin secretion and inhibit glucose production 2.
- Sitagliptin is approved by the US Food and Drug Administration (FDA) for use with diet and exercise to improve glycemic control in adult patients with type 2 diabetes 2.
Mechanism of Action
- Sitagliptin inhibits the DPP-4 enzyme, which is responsible for the inactivation of incretin hormones such as glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide 4.
- This increases the active incretin and insulin levels, and decreases glucagon levels and post-glucose-load glucose excursion 4.
Efficacy and Safety
- Sitagliptin has been shown to be effective in improving glycemic control in patients with type 2 diabetes, with significant reductions in glycosylated hemoglobin (HbA1c) levels 2, 3, 4, 5, 6.
- It is generally well tolerated, with a low risk of hypoglycemia and a neutral effect on body weight 2, 3, 4, 5, 6.
- Common side effects include gastrointestinal complaints, such as abdominal pain, nausea, and diarrhea 2.