Oral antidiabetics are used for the treatment of diabetes mellitus type 2 DPP-4 inhibitors act antihyperglycemically by influencing the hormonal control circuit of insulin release by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4).
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Dpp-4 inhibitors
DefinitionThis section has been translated automatically.
Spectrum of actionThis section has been translated automatically.
Insulin secretion is regulated, among other things, by the incretin hormone glucagon-like peptide 1 (GLP-1), which is produced in the intestine. The GLP-1 level rises postprandial. This stimulates the release of insulin from the beta cells of the endocrine pancreas. They are sensitized by GLP-1 to elevated blood sugar levels.
The glucagon-like peptide 1 is degraded to an inactive metabolite by the enzyme dipeptidylpeptidase-4. This reduces the release of insulin. The enzyme "dipeptidylpeptidase-4" degrades the hormone glucagon-like peptide 1 to an inactive metabolite and thus reduces the release of insulin. Inhibition of this key enzyme by DPP-4 inhibitors prolongs the period of elevated GLP-1 levels and thus insulin secretion.
Furthermore, extrapancreatic effects slow down gastric emptying and stimulate the feeling of satiety.
Undesirable effectsThis section has been translated automatically.
It has been observed several times that DPP-4 inhibitors can contribute to the outbreak of bullous pemphigoid. Among 217,331 cases in a French pharmkovigilance database (FPVD), 1,297 cases were found with DDP4 inhibitors, and among these 42 cases were those involving bullous pemphigoid (vildagliptin: n=31; sitagliptin: n=10,jeSaxagliptin: n=1). Since the side effects occurred with each of the DDP-4 inhibitors, this suggests side effects of the entire substance group (Bené 2016).
PreparationsThis section has been translated automatically.
Sitagliptin (Januvia®, Xelevia®), vildagliptin (Galvus®, Eucreas®), saxagliptin (Onglyza®)