Title | Glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes | ||
Authors | Th. Mavrakanas, E. Tsirella and M. Mironidou-Tzouveleki
A΄ Laboratory of Pharmacology, Medical School, Aristotelian University, Thessaloniki, Greece |
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Citation | Mavrakanas, T., Tsirella, E., Mironidou-Tzouveleki, M.: Glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes, Epitheorese Klin. Farmakol. Farmakokinet. 22(2): 243-245 (2008) | ||
Publication Date | 23-25 May 2008 | ||
Full Text Language | English | ||
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Keywords | GLP-1, DPP-4, exenatide, liraglutide, vildagliptin, sitagliptin. | ||
Other Terms | Review article | ||
Summary | The alimentary enhancement of insulin release is known as the ‘incretin’ effect, and is attributed to the incretin hormones: glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1). Activation of GIP and GLP-1 receptors is followed by insulin exocytosis in a glucose dependent manner. GLP-1 also inhibits glucagon secretion, gastric emptying and food ingestion. Exenatide, the first GLP-1R agonist, is administered subcutaneously twice daily. It is more efficacious in reducing postprandial than fasting glucose levels. The most common adverse effects are gastrointestinal. Liraglutide, the other GLP-1 analogue, has a longer half life and can be given as a once daily injection. As GLP-1 is rapidly degraded by DPP-4, development of DPP-4 inhibitors is particularly interesting. Thus, vildagliptin is administrated per os once daily, is better tolerated than metformin and as effective as glitazone. Sitagliptin, the other agent of this group, is also well tolerated and can be used as monotherapy or in combination with metformin or pioglitazone. No characteristic adverse effects have been associated with the use of the DPP-4 inhibitors. | ||
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