DPP-4 inhibitors

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| above = DPP-4 inhibitors

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| headerstyle = background: #e8e8e8; | header1 = Class identifiers

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| label4 = Use | data4 = Type 2 diabetes

| label5 = ATC code | data5 = A10

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| label7 = Mechanism of action | data7 =

| label8 = Biological target | data8 = Dipeptidyl peptidase-4

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| header10 = Clinical data

| label11 = Drugs.com | data11 = DPP-4 inhibitors

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| label15 = MeSH | data15 = D064730

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DPP-4 inhibitors, also known as gliptins, are a class of oral hypoglycemics that block Dipeptidyl peptidase-4 (DPP-4), an enzyme involved in the inactivation of the incretin hormones GLP-1 and GIP. These hormones are responsible for increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. By inhibiting DPP-4, these drugs increase the levels of active incretin hormones, which in turn increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner.

Mechanism of Action

DPP-4 inhibitors work by blocking the enzyme DPP-4, which is responsible for degrading the incretin hormones GLP-1 and GIP. These hormones play a crucial role in the regulation of glucose metabolism by enhancing the secretion of insulin and suppressing the release of glucagon during meals. As a result, DPP-4 inhibitors help in reducing blood glucose levels without causing significant hypoglycemia.

Clinical Use

DPP-4 inhibitors are primarily used in the treatment of Type 2 diabetes to improve blood sugar control. They are often prescribed as part of a combination therapy with other antidiabetic medications such as metformin or sulfonylureas.

Examples of DPP-4 Inhibitors

• Sitagliptin
• Vildagliptin
• Saxagliptin
• Linagliptin
• Alogliptin

Side Effects

Common side effects of DPP-4 inhibitors include nasopharyngitis, headache, and upper respiratory tract infections. There is also a concern about the risk of pancreatitis and joint pain associated with this class of drugs.

Advantages

DPP-4 inhibitors do not usually cause weight gain, which is a common side effect of many other antidiabetic medications. They also have a low risk of causing hypoglycemia compared to other therapies.

Limitations

The efficacy of DPP-4 inhibitors in reducing HbA1c is moderate. They are less effective than some other classes of diabetes medications like GLP-1 receptor agonists. Additionally, the long-term effects on cardiovascular outcomes are still being studied.

See Also

• Antidiabetic drug
• Incretin
• Diabetes management