Τόμος 22 (2008) – Τεύχος 2 – Άρθρο 70 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 22 (2008) – Issue 2 – Article 70 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

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

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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