Incretin and its use in the treatment of type 2 diabetes mellitus
Keywords:
incretin, GLP-1, incretin mimetics, analogues/ derivates of GLP-1, type 2 diabetes, DPP-4 inhibitorsAbstract
Oral glucose administration results in more insulin release
than intravenous injection of the same amount of glucose. This
phenomenon has been designated as the “incretin effect”. This
effect is caused by the gastrointestinal peptides “gastric inhibitory polypeptide” (GIP) and “glucagon-like peptide-1” (GLP-1).
These incretin hormones are responsible for the major part of postprandial insulin secretion.
Preparations based on GLP-1 are able to reduce the incretin
effect in type 2 diabetes mellitus. However, oral administration of
GLP-1 is inefficient as GLP-1 is destroyed in the gastrointestinal
tract. Subcutaneous or intravenous bolus GLP-1 is inactivated by
plasma enzyme dipeptidyl-peptidase IV (DPP-4). GLP-1 is only
efficient by continuous parenteral infusion.
GLP-1 analogues/derivatives or incretin mimetics exendine-4,
are active after subcutaneous injection, and DPP-4 inhibitors,
sitagliptin and vildagliptin, given orally, are used in the treatment
of type 2 diabetes mellitus.
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