30.胰岛素——山东大学药理学英文课件Insulin.pptVIP

30.胰岛素——山东大学药理学英文课件Insulin.ppt

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30.胰岛素——山东大学药理学英文课件Insulin

Part 2 Oral hypoglycemic agents Common characteristics (1) Orally effective and convenient (2) Slow and weak (3) NIDDM Ⅰ insulin sensitizer Rosiglitazone(罗格列酮) Englitazone (恩格列酮) Pioglitazone (吡格列酮) Troglitazone (曲格列酮) Ciglitazone (环格列酮) Pharmacological action 1.Improve insulin resistance, lower hyperinsulinemia and hyperglycemia Limosis and after-meal BS Blood insulin and blood fatty acid used in combination with other drugs Low incidence of hypoglycemia 2.Correct lipodystrophy ↓TG,↑TC and ↑HDL-C 3.Improve complication of NIDDM anti-atherosclerosis effect delay occurrence of albuminuria 4.Improve β-cell function Mechanism (PPARγ )过氧化物酶增殖体受体γ Clinical use NIDDM and IR Adverse reaction general reaction heptic toxicity Ⅱ. Sulfonylureas(磺酰脲类) The first generation: Tolbutamide(甲苯磺丁脲), chlorpropamide(氯磺丙脲). The second generation: glyburide(格列本脲), glipizide(格列吡嗪), gliquidone, glimepiride(格列美脲) The third generation: gliclazide pharmacokinetics Absorption: P.O Distribution: PPBR Elimination: liver Excretion:kidney Pharmacological effects Hypoglycemic action: weaker than Insulin (1)Increasing the release of Insulin from pancreatic βcell: (2) Enhancing the sensitivity of target cell to insulin ①Increasing the numbers of insulin receptors ②Increasing the affinity of insulin receptors (3) Decreasing the release of glucagons from pancreatic A cell by stimulating the release of somatostatin 2.Antidiuretic action: chlorpropamide ↑secretion of ADH 3.Effects on coagulation ↓adhesion and agregation of PLT ↑synthesis of plasminogen ↓sensitivity of microvessel to CA Clinical uses 1.NIDDM control hyperglycemia in NIDDM who can not achieve appropriate control with exercise and dietary modification alone. (1)alone (2)plus insulin 2.Diabetes insipidus(尿崩症 ) Adverse reactions 1. Hypoglycemia reactions 2. Gastrointestinal tra

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