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1、藥物化學(xué)Medicinalchemistry第十章利尿藥及合成降血糖藥第十章利尿藥及合成降血糖藥口服降血糖藥利尿藥第一節(jié)口服降血糖藥Diabetes,chronicdisorderofglucose(sugar)metabolismcausedbyinadequateproductionoruseofinsulin,ahormoneproducedinspecializedcells(betacellsintheisletsofLangerhans)inthepancreasthatallowsthebodytouseandstoregluc
2、ose.糖尿?。阂葝u素分泌不足,糖代謝異常。I型糖尿病-胰島素依賴型(原發(fā)性糖尿?。㊣I型糖尿病-非胰島素依賴型糖尿病磺酰脲類降糖藥苯磺酰脲基本結(jié)構(gòu)作用機(jī)制:刺激胰島素分泌甲苯磺丁脲磺酰脲類降糖藥,刺激胰島素分泌,甲基易被氧化失活。特點(diǎn):降糖作用較弱、安全。用途:治療II型糖尿病。格列本脲磺酰胺基對位引入側(cè)鏈,脲基末端有脂環(huán)或含氮脂環(huán)。特點(diǎn):作用強(qiáng)。代謝產(chǎn)物有活性,腎功能不全慎用(引起低血糖)。用途:用于中、重度II型糖尿病人。鹽酸二甲雙胍(Metforminhydrochloride)用途:用于治療II型糖尿病Metforminisexc
3、retedunchangedintheurineanddoesnotundergohepaticmetabolism.Unlikesulfonylureas,metformindoesnotproducehypoglycemiaineitherpatientswithtype2diabetesMechanismofActionMetforminisanantihyperglycemicagentwhichimprovesglucosetoleranceinpatientswithtype2diabetes,loweringbothbasala
4、ndpostprandialplasmaglucose.Itsmechanismsofactionaredifferentfromotherclassesoforalantihyperglycemicagents.Metformindecreaseshepaticglucoseproduction,decreasesintestinalabsorptionofglucose,andimprovesinsulinsensitivitybyincreasingperipheralglucoseuptakeandutilization.INDICA
5、TIONSANDUSEMetforminhydrochloride,asmonotherapy,areindicatedasanadjuncttodietandexercisetoimproveglycemiccontrolinpatientswithtype2diabetes.Itmaybeusedconcomitantlywithasulfonylureaorinsulintoimproveglycemiccontrolinadults.第二節(jié)利尿藥DiureticsDiuretic,drugusedtoincreaseurineform
6、ationandoutput.Diureticsareprescribedforthetreatmentofedema(theaccumulationofexcessfluidsinthetissuesofthebody),whichisoftentheresultofunderlyingdiseaseofthekidneys,liver,lungs,orheart(e.g.,congestiveheartfailure).Theyarealsousedtotreathypertension(highbloodpressure)andglau
7、coma.Theyactonthekidneys,modifyingtheabsorptionandexcretionofwaterandelectrolytessuchassodiumandpotassium.呋塞米Furosemide磺酰胺類利尿藥。IthasbeendemonstratedthatfurosemideinhibitsprimarilythereabsorptionofsodiumandchloridenotonlyintheproximalanddistaltubulesbutalsointheloopofHenle.I
8、NDICATIONSANDUSAGEEdema:forthetreatmentofedemaassociatedwithcongestiveheartfailure