title: Gliquidone contributes to improvement of type 2 diabetes mellitus management: a review of pharmacokinetic and clinical trial data.
abstract: Diabetes mellitus is a global health problem of steadily increasing proportions, with approximately 95% of patients being affected by the type 2 form of the disease. The growing challenge to healthcare systems presented by this disorder has prompted ongoing research into novel therapies with which to improve management. The sulfonylureas constitute a long-established group of drugs with a proven track record in the treatment of type 2 diabetes, but efforts to improve the overall metabolic profile and safety of these agents have led over time to the addition of newer agents such as the second-generation benzenesulfonylurea gliquidone. Gliquidone has extrapancreatic effects that result in increased numbers of insulin receptors in peripheral tissues. The drug is rapidly and almost completely absorbed after oral administration, and has a short elimination half-life (around 1.5 hours). Metabolism is maintained in patients with hepatic insufficiency, and accumulation does not take place in patients with impaired renal function. Plasma glucose levels are controlled for several hours as a result of glucose-induced insulin secretion, and beneficial effects on plasma lipids have been described. In clinical studies, gliquidone has been associated with less hypoglycaemia than glibenclamide (glyburide), and with metabolic control at least as good as that seen with a number of other sulfonylureas. Beneficial effects on platelet aggregation have been documented, and the drug is described by WHO as the preferred sulfonylurea for patients with mild to moderate renal insufficiency. Importantly, in the light of the well documented consequences of increased bodyweight and the large growth in obesity worldwide, gliquidone is not associated with significant bodyweight gain. Thus, gliquidone is a sulfonylurea with proven efficacy and good safety and metabolic profiles that is only rarely associated with hypoglycaemia. In particular, the metabolism and route of excretion of the drug allow its use in patients who have or may be at risk of diabetic nephropathy.
authors.affiliation: Laboratory of Experimental Hormonology, Brussels Free University, Brussels, Belgium. malaisse@ulb.ac.be
authors.forename: Willy J
authors.initials: WJ
authors.lastname: Malaisse
mesh_terms: D001786:Blood Glucose / Q000378:metabolism; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D015394:Molecular Structure; D013453:Sulfonylurea Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D013453:Sulfonylurea Compounds; C010969:gliquidone