[Non-SU, insulin secretagogues].
The chemical structures, mechanisms of actions, bioavailabilities, insulinotrophic and hypoglycemic actions, and clinical trials of three novel oral hypoglycemic agents, NN-623, A-4166 and KAD-1229 are overviewed. They are non-SU insulin secretagogues and they induce quicker and shorter hypoglycemia than sulphonylureas do, presumably because they are rapidly absorbed into (Tmax: < 30 min) and excreted from blood (T 1/2: < 60 min). They bind to the SU-receptors and suppress K-ATP channels like sulphonylureas do. They stimulate mainly the initial phase of insulin release and evoke a decrease in postprandial rises in plasma glucose in several animals and humans. Clinical trials demonstrated they are efficacious and safe in the treatment of NIDDM subjects. They are useful as a first choice drug for the early stage of NIDDM.
Kikuchi
M
M
Institute for Adult Diseases, Asahi Life Foundation.
D003510:Cyclohexanes / Q000627:therapeutic use*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D006801:Humans; D007004:Hypoglycemic Agents / Q000627:therapeutic use*; D007211:Indoles / Q000627:therapeutic use*; D054833:Isoindoles; D000077715:Nateglinide; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000627:therapeutic use
D003510:Cyclohexanes; D007004:Hypoglycemic Agents; D007211:Indoles; D054833:Isoindoles; D000077715:Nateglinide; D010649:Phenylalanine; C087255:mitiglinide