अमूर्त
Incretin for the continuing treatment of secondary failure to metformin in Type 2 diabetes
Baptist GallwitzFor the treatment of Type 2 diabetes, incretin-based therapies have been an established treatment since their introduction in 2006. GLPâ1 receptor agonists as an injectable therapy and DPPâ4 inhibitors as oral antidiabetic agents have a strictly glucose-dependent action on insulin and glucagon secretion, resulting in a negligible intrinsic hypoglycemia risk. The GLPâ1 receptor agonists only act by stimulating the GLPâ1 receptor directly at receptor ligand concentrations in the pharmacological concentration range. They decelerate gastric emptying dependent on their duration of action and also act directly by stimulating satiety signals in the CNS. These effects lead to a loss of body weight. DPPâ4 inhibitors primarily elevate endogenous active GLPâ1 plasma concentrations by two- to three-fold. They are body weight neutral since only higher concentrations of GLPâ1 than those elicited by DPPâ4 inhibitors have direct effects on the CNS or on the retardation of gastrointestinal motility. Novel studies suggest beneficial cardiovascular effects of incretin-based therapies. This article gives an overview of developments in this therapeutic area.