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• W1860171645 abstract "Abstract The article contains sections titled: 1. Introduction 2. Stimulators of Insulin Secretion 2.1. Sulfonylureas and Related Compounds 2.2. Benzoic Acid Derivatives 2.3. Amino Acid Derivatives 2.4. Mode of Action 2.5. New Insulinotropic Mechanisms 2.5.1. Dipeptidyl Peptidase IV Inhibition 2.5.2. Dipeptidyl Peptidase IV Inhibitors in Clinical Development 3. Biguanides 4. Inhibitors of Intestinal Carbohydrate Digestion 4.1. α‐Glucosidase Inhibitors 4.1.1. Mode of Action 4.1.2. Pharmacology 4.1.3. Individual Compounds 4.2. Plant Fibers 5. Enhancers of Insulin Action 5.1. Mode of Action 5.2. Pharmacology of PPARγ agonists 5.3. Thiazolidine‐2,4‐Dione Derivatives (Glitazones) The review describes all oral drugs used for the treatment of type 2 diabetes mellitus which are marketed or in late clinical development. Stimulators of insulin secretion are the most prescribed class of antidiabetic drugs. These compounds increase insulin secretion from pancreatic β‐cells via the closure of the ATP‐sensitive K + channel. Sulfonylurea (SU) derivatives bind to the SU receptor on a regulatory protein of the ATP‐sensitive K + channel. Since various binding sites exist, also other compounds like benzoic acid or amino acid derivatives are able to bind and to stimulate insulin secretion via the closure of the ATP‐sensitive K+ channel. Very new mechanisms, not yet approved and still in late clinical development, prevent the degradation of glucagons‐like‐peptide‐1 (GLP‐1), an intestinal hormone, which stimulates insulin secretion by increasing intracellular cAMP levels of β‐cells. Those compounds, which inhibit the GLP‐1 degrading enzyme dipeptidyl peptidase IV (DPP IV), sustain the insulinotropic effect of GLP‐1. The antidiabetic action of biguanides, only metformin is marketed today, is still not fully understood. Metformin improves insulin sensitivity probably by an increase in peripheral glucose utilization and additionally metformin reduces hepatic gluconeogenesis. Alpha‐glucosidase inhibitors are enzyme inhibitors of small intestinal carbohydrate digesting glucosidases. They display their antidiabetic effect by delaying the postprandial (pp) carbohydrate absorption resulting in reduced pp hyperglycemia and ‐insulinemia, which finally improves insulin sensitivity. Enhancers of insulin action are ligands of the peroxisome proliferator activated receptor γ (PPARγ). PPARs belong to the nuclear receptor family of ligand‐activated transcription factors. The major antidiabetic and blood glucose lowering effect of the PPARγ agonists is the improvement of insulin sensitivity, however, the mechanism is not fully elucidated yet." @default.
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• W1860171645 date "2006-12-15" @default.
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• W1860171645 title "Oral Antidiabetic Drugs" @default.
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