利尿藥和降血糖藥ppt課件(已修改)
2025-01-20 04:11 本頁(yè)面
【正文】 Medicinal chemistry Chapter 10 Diuretics and Synthetic Hypoglycemic Drugs College of Pharmacy, SDU Shutao Ma Email: Chapter 10 Diuretics and Synthetic Hypoglycemic Drugs Section 1 Hypoglycemic Drugs Section 2 Diuretics Section 1 Hypoglycemic Drugs The classic triad of symptoms in diabetes is polyphagia, polydypsia (thirst), and polyuria (excess urine). All three result directly from excessive serum glucose levels. Type 1 diabetes usually develops in an acute manner, although the destructive autoimmune process may have been underway for some time. Type 2 diabetes has a more insidious, often asymptomatic onset and its presence is usually detected by routine medical examinations. Definitions Type I Diabetes. Insulindependent diabetes mellitus (IDDM), this condition occurs when the βcells of the pancreatic islets of Langerhans are destroyed, probably by an autoimmune process, such that insulin production is deficient. Type 2 Diabetes. Noninsulindependent diabetes mellitus (NIDDM) is very frequently associated with obesity in its mainly adult victims. Serum insulin levels are normal or elevated, so in essence this is a disease of insulin resistance. Biochemistry and Pathogenesis of Diabetes Classifications First Generation Sulfonylureas: tolbutamide. Second Generation Sulfonylureas: glibenclamide. Third Generation Sulfonylureas: glimepiride, repaglinide. Biguanides: metformin. α Glucosidase Inhibitors: Acarbose, Miglitol. Mechanism of Action Sulfonylureas interact with receptors on pancreatic βcells to block ATPsensitive potassium channels. This in turn leads to opening of voltagesensitive calcium channels which produces an influx of calcium。 the influx of calcium results in βcells production of insulin. An additional effect of sulfonylureas is suppression of gluconeogenesis in the liver. PhysicalChemical Properties Sulfonylureas are weak acids due to the marked delocalization of the nitrogen lone electron pair by the sulfonyl group. Their pKa39。s cluster around and they are strongly protein bound. Structureactivity Relationships There must be reasonable bulk o
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