利尿藥和降血糖藥ppt課件-資料下載頁
2025-01-08 04:11本頁面
【正文】 sed primarily for the treatment of glaua and absence seizures. N NSN SN H 2OO OHMechanism of Action The action of the enzyme carbonic anhydrase catalyzes the formation of carbonic acid from carbon dioxide and water. Carbonic anhydrase inhibitors induce diuresis by inhibiting the formation of carbonic acid within proximal and distal tubular cells to limit the number of hydrogen ions available to promote sodium reabsorption. Spironolactone The adrenal (7β17α)7(Acetylthio)17hydroxy3oxopregn4ene21carboxylic acid ?lactone Spironolactone is a petitive antagonist to the mineralocorticoids such as aldosterone. O SOOO螺 內(nèi) 酯 Mechanism of Action The adrenal cortex secretes a potent mineralocorticoid called aldosterone which promotes salt and water retention and potassium and hydrogen ion excretion. Spironolactone inhibits reabsorption of sodium and chloride ion and increased potassium ion excretion. Metabolism Spironolactone is significantly metabolized in liver to its major active metabolite, canrenone, which is interconvertible with its canrenoate anion. Canrenone is an antagonist to aldosterone and it has been suggested as the active form of spironolactone. The canrenoate anion is not active per se but acts as aldosterone antagonist because of its conversion to canrenone. The most serious side effect of spironolactone is hyperkalemia because it has a potassiumsparing effect. Triamterene 6Phenyl2,4,7pteridiriamine The diuretic effect of triamterene occurs rapidly, in 30 minutes, and reaches a peak plasma concentration in 24 hours, with a duration of action of more than 24 hours. NNNNN H 2N H 2H 2 N Structural Modification Activity is retained if an amine group is replaced with a lower alkylamine group. Introduction of a paramethyl group on the phenyl ring decreases the activity about onehalf. Introduction of a parahydroxyl group on the phenyl ring yields a pound that is essentially inactive as a diuretic. 重點(diǎn)內(nèi)容 掌握磺酰脲類的作用機(jī)制、構(gòu)效關(guān)系。 掌握甲苯磺丁脲、格列本脲、鹽酸二甲雙胍的結(jié)構(gòu)、性質(zhì)、代謝和用途。 掌握呋塞米、氫氯噻嗪、乙酰唑胺、螺內(nèi)酯、氨苯蝶啶的結(jié)構(gòu)和用途。 熟悉各類利尿藥的 作用機(jī)制、構(gòu)效關(guān)系。 熟悉 格列本脲和 氨苯蝶啶的合成。
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