Repaglinide in the treatment of diabetes.doc

 PAGE \* MERGEFORMAT 13 Repaglinide in the treatment of diabetes [Keywords:] repaglinide Diabetes Non-sulfonylurea insulin secretion agent (Non-sulfonylureas, NSUR), also known as “prandial glucose regulator”, repaglinide (repaglinide) is one of the representatives. Repaglinide is a carbamoyl benzene acid derivatives, structure and traditions very different sulfonylurea drugs, can effectively control type 2 diabetes after meal glucose fluctuations, while significantly reducing the incidence of severe hypoglycemia, sulfonylureas overcome the above defects. Pharmacological properties of 1 Repaglinide Repaglinide (repaglinide) is methyl amine acid (CM2BA) derivatives outside the cell membrane with -ATP-dependent potassium channels on the 36KDA specific binding proteins, so that potassium channels close, calcium channel , calcium influx, promote insulin secretion, is characterized as a “quick - fast close” to quickly lower the postprandial blood glucose, and reduce the incidence of hypoglycemia. Repaglinide is rapidly absorbed after oral administration, completely, in the blood serum albumin and 98%, the maximum plasma concentrations in medication 1h, the biological availability of 56% to 63%, the maximum plasma concentration (Cmax) and plasma concentration - time area under the curve (AUC) with dose increases. Repaglinide is cleared rapidly in the blood, half-life 1h, oral 2mg repaglinide 4 ~ 5h medication can be reduced to a concentration within the ago levels. repaglinide mainly by cytochrome P450 metabolism in the liver non-active product, by biliary excretion into the feces. taking 2mg 14C labeled repaglinide 96h, 90% of repaglinide in the feces found that only 8% found in the urine. mild to moderate kidney damage in patients with type 2 diabetes, little change in its pharmacokinetics, in patients with severe renal injury (creatinine clearance lt;30ml/min) or chronic liver disease, The plasma levels than healthy people to increase significantly