DPP-4 (dipeptidyl peptidase-4) inhibitors, also known as “gliptins,” are a class of oral medications used in the management of type 2 diabetes. Their mechanism of action involves the inhibition of the DPP-4 enzyme, which plays a crucial role in glucose metabolism.
Here’s how DPP-4 inhibitors work:
- Inhibition of DPP-4 enzyme: The DPP-4 enzyme normally degrades incretin hormones like GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide). These hormones stimulate insulin release from the pancreas in response to meals and suppress glucagon secretion, reducing blood glucose levels.
- Prolonging incretin activity: By inhibiting the DPP-4 enzyme, these medications increase the levels of active incretin hormones, which:
- Increase insulin secretion in a glucose-dependent manner.
- Decrease glucagon secretion, leading to reduced hepatic glucose production.
- Lowering blood glucose: This combined effect helps to lower postprandial (after-meal) and fasting blood glucose levels, improving overall glycemic control without the risk of significant hypoglycemia since the action of incretins is glucose-dependent.
DPP-4 inhibitors are commonly used in combination with other antidiabetic drugs like metformin to enhance glycemic control in patients with type 2 diabetes.
Here are the common dosages of DPP-4 inhibitors (gliptins) used for managing type 2 diabetes:
- Sitagliptin (Januvia)
- Standard dose: 100 mg once daily.
- Adjustments:
- For moderate renal impairment (eGFR 30-50 mL/min): 50 mg once daily.
- For severe renal impairment (eGFR <30 mL/min) or ESRD: 25 mg once daily.
- Saxagliptin (Onglyza)
- Standard dose: 2.5-5 mg once daily.
- Adjustments:
- For moderate to severe renal impairment or ESRD: 2.5 mg once daily.
- Linagliptin (Tradjenta)
- Standard dose: 5 mg once daily.
- No dose adjustment is needed for renal or hepatic impairment.
- Alogliptin (Nesina)
- Standard dose: 25 mg once daily.
- Adjustments:
- For moderate renal impairment (eGFR 30-59 mL/min): 12.5 mg once once daily.
- – For severe renal impairment (eGFR <30 mL/min) or ESRD: 6.25 mg once daily.
- 5) Vildagliptin: 50 to 100 mg in a day
- 6) Teneligiptin: 20 mg once daily
- These doses may vary based on patient factors such as renal function, and it’s important to monitor for any potential adverse effects or drug interactions during treatment.
Dpp4 inhibitors reduce fasting sugar by 10-30 mg and post prandial sugar by 50-100 mg.
They are very safe to use and only very rarely may cause hypoglycemia.