《利尿药及》PPT课件.ppt

药物化学Medicinal chemistry,第十章 利尿药及合成降血糖药,第十章 利尿药及合成降血糖药,口服降血糖药 利尿药,第一节 口服降血糖药,Diabetes,chronic disorder of glucose(sugar)metabolism caused by inadequate production or use of insulin,a hormone produced in specialized cells(beta cells in the islets of Langerhans)in the pancreas that allows the body to use and store glucose.,糖尿病：胰岛素分泌不足，糖代谢异常。I 型糖尿病胰岛素依赖型（原发性糖尿病）II型糖尿病非胰岛素依赖型糖尿病,磺酰脲类降糖药,苯磺酰脲基本结构作用机制：刺激胰岛素分泌,甲苯磺丁脲,磺酰脲类降糖药，刺激胰岛素分泌，甲基易被氧化失活。特点：降糖作用较弱、安全。用途：治疗II型糖尿病。,格列本脲,磺酰胺基对位引入侧链，脲基末端有脂环或含氮脂环。特点：作用强。代谢产物有活性，肾功能不全慎用（引起低血糖）。用途：用于中、重度II型糖尿病人。,盐酸二甲双胍（Metformin hydrochloride）,用途：用于治疗II型糖尿病 Metformin is excreted unchanged in the urine and does not undergo hepatic metabolism.Unlike sulfonylureas,metformin does not produce hypoglycemia in either patients with type 2 diabetes,Mechanism of Action,Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes,lowering both basal and postprandial plasma glucose.Its mechanisms of action are different from other classes of oral antihyperglycemic agents.Metformin decreases hepatic glucose production,decreases intestinal absorption of glucose,and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.,INDICATIONS AND USE,Metformin hydrochloride,as monotherapy,are indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes.It may be used concomitantly with a sulfonylurea or insulin to improve glycemic control in adults.,第二节 利尿药 Diuretics,Diuretic,drug used to increase urine formation and output.Diuretics are prescribed for the treatment of edema(the accumulation of excess fluids in the tissues of the body),which is often the result of underlying disease of the kidneys,liver,lungs,or heart(e.g.,congestive heart failure).They are also used to treat hypertension(high blood pressure)and glaucoma.,They act on the kidneys,modifying the absorption and excretion of water and electrolytes such as sodium and potassium.,呋塞米 Furosemide,磺酰胺类利尿药。It has been demonstrated that furosemide inhibits primarily the reabsorption of sodium and chloride not only in the proximal and distal tubules but also in the loop of Henle.,INDICATIONS AND USAGE,Edema:for the treatment of edema associated with congestive heart failure,cirrhosis of the liver,and renal disease.Hypertension:for the treatment of hypertension alone or in combination with other antihypertensive agents.,氢氯噻嗪 Hydrochlorothiazide,磺酰胺类利尿药。Affect the renal tubular mechanisms of electrolyte reabsorption,directly increasing excretion of sodium and chloride in approximately equivalent amounts.,INDICATIONS AND USAGE,Hydrochlorothiazide is indicated in the management of hypertension either as the sole therapeutic agent,or in combination with other antihypertensives.,乙酰唑胺 Acetazolamide,碳酸酐酶抑制剂(inhibitor of carbonic anhydrase)。口服，治疗青光眼。,螺内酯 Spironolactone,醛固酮受体拮抗剂，抑制钠和氯离子的重吸收。,用于醛固酮增多的顽固性水肿（肝硬化腹水、肾病、伴充血性心衰水肿）,氨苯蝶啶,保钾排钠。临床用于心脏性、肝性、肾性腹水。,学习重点,掌握甲苯磺丁脲、格列本脲、盐酸二甲双胍的结构和用途。了解甲苯磺丁脲、格列本脲、盐酸二甲双胍的作用特点。掌握呋塞米、氢氯噻嗪、乙酰唑胺、螺内酯、氨苯蝶啶的结构和用途。,