10 Properties and Benefits of Gliptins: How They Work and When to Prescribe Them
General practitioners can now prescribe oral antidiabetics from the group of gliptins to patients with type 2 diabetes. Their therapeutic options are significantly expanded in the care of these patients. In the following text, we briefly summarize the mechanism of action of gliptins and their advantages over other oral antidiabetics.
Mechanism of Action of Gliptins
Gliptins (alogliptin, linagliptin, saxagliptin, sitagliptin, and vildagliptin) belong to oral antidiabetics with an incretin effect. They act as selective inhibitors of dipeptidyl peptidase 4 (DPP-4), an enzyme that inactivates incretin GLP-1 (glucagon-like peptide 1). Therefore, when using gliptins, the plasma concentration of endogenous GLP-1 is increased and its action is prolonged.
In diabetics, gliptins stimulate insulin secretion from the β-cells of the pancreatic islets of Langerhans during hyperglycemia. In non-diabetics, they do not increase insulin secretion, do not lower blood glucose, and do not induce hypoglycemia. Depending on hyperglycemia, they also reduce glucagon secretion from the α-cells and thus inhibit hepatic gluconeogenesis. Other positive effects include slowing gastric emptying and reducing appetite.
Gliptin Decalogue: Benefits, Properties, and Indications for Prescription
- Gliptins are taken orally, usually once daily.
- They are most often added to a combination with metformin. However, they are also a very good alternative for patients who cannot be given metformin due to some of its contraindications or intolerance.
- Fixed combinations of gliptins and metformin are already available on the market.
- Gliptins are safer than sulfonylurea derivatives (4–5 times lower risk of hypoglycemia).
- They do not significantly affect body weight.
- Neutral cardiovascular effects are assumed (unlike, for example, thiazolidinediones, whose use is unsuitable in patients with heart failure).
- Linagliptin is excreted renally only 5%, so it can also be administered to patients with renal insufficiency, even in the stage of renal failure/dialysis (CKD 5), in non-reduced doses. Other gliptins need to be administered at half or quarter dose in renal insufficiency.
- Linagliptin can also be used by patients with liver disease - dosing does not need to be adjusted even in severe liver dysfunction. Saxagliptin and sitagliptin can also be given in mild liver function restriction.
- When used long-term in monotherapy, gliptins reduce glycated hemoglobin (HbA1c) by about 10 mmol/mol. In patients inadequately compensated with metformin, adding gliptin leads to a reduction in HbA1c by another 8–10 mmol/mol during six-month treatment.
- Gliptins can be given in the following combinations:
- with metformin in patients inadequately compensated with the maximum tolerated dose of metformin in monotherapy;
- with sulfonylurea derivatives in patients inadequately compensated with maximum dose in monotherapy, for whom metformin is unsuitable due to contraindication or intolerance;
- with thiazolidinedione (pioglitazone);
- with SGLT-1 or SGLT-2 inhibitors (gliflozins);
- with insulin*.
* However, in combination with insulin, gliptins are no longer covered by public health insurance. It is recommended to always verify the indication limitation of coverage on the website of the State Institute for Drug Control (SÚKL).
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Source: Karen I., Svačina Š. Diabetes mellitus. Update 2020. Recommended diagnostic and therapeutic procedures for general practitioners. Society of General Practice by ČLS JEP, 2020. Available at: www.svl.cz/files/files/Doporucene-postupy/2020/DIABETES-MELLITUS-2020.pdf
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