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ID:19453361
大小:313.00 KB
页数:22页
时间:2018-10-02
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1、Chapter1AnestheticsAnestheticisadrugthatcausesreversibleanesthesiaandalossofconsciousness(includingthefeelingofpain).Thisallowspatientstoundergosurgeryandotherprocedureswithoutthedistressandpaintheywouldotherwiseexperience.LocalanestheticsGeneralanestheticsLocalanestheticisusedonspecificnerv
2、epathways,haseffectofalossofawarenessofapartofthebody.Whreasgeneralanestheticisusedoncentralnervoussystem,haseffectofatotalunconsciousness.1.1.1DiscoveryanddevelopmentoflocalanestheticsPeruvianwereknownchewingcocaleavesfromSouthAmericaforpainin1532.Analkaloidwasextractedfromtheleavesofcocaan
3、dnamedCocainein1860.Cocainewasusedasalocalanestheticinclinicin1884.Chemicalstructurewasmodifiedbecauseofsevereside-effectsuchasaddiction,allergy,tissueirritatingandunstableinaqueoussolution1.1LocalanestheticsCocaineChemicalmodificationofCocaineStudyingresultsshowedthatbenzoatefractionplayedt
4、heimportantrolebutmethoxycarbonylisnotnecessaryfortheactivityofanesthesia.Ontheotherhand,simplificationofecgonineledtothediscoveryofsyntheticcompoundsα-Eucaineandβ-Eucaine.Thisresultedthattropinewasnotnecessaryfortheactivity.ecgonineα-Eucaineβ-EucaineAccordingtotheobtainedresults,researchers
5、beguntostudythesyntheticbenzoicacidestersasthelocalanesthetics.Firstofall,Benzocainewasdiscoveredin1890.Shortlyafter,OrthoformandOrthoformNewwerefoundwithstronglocalanesthesiaeffect.Atlast,Procainewasdiscoveredin1904.BenzocaineProcaineOrthoformOrthoformNewProcainehydrochloride4-氨基苯甲酸-2-(二乙氨基
6、)乙酯盐酸盐,又名盐酸奴佛卡因4-Aminobenzoicacid2-(diethylamino)ethylestermonohydrochloride,orNovocainehydrochloride)Physicalproperties:whitecrystalorcrystallinepowder,odorless,bittertasteandthenasenseofparalysis.Mp.154~157℃.Solubleinwater(1:1),slightlysolubleinethanol(1:30)andchloroform,hardlysolubleineth
7、er.Chemicalproperties:Hydrolysis:酸、碱及体内酶均使其水解。pH3-3.5最稳定,在碱性、中性及强酸性条件下易水解。Oxidization:含芳伯氨基,易被氧化变色。Activityandclinicalapplication:Procaine具有良好的局麻作用,毒性低,无成瘾性,是国内外临床广泛应用的局麻药之一,主要用于浸润麻醉,传导麻醉和封闭疗法。Withgoodlocalanesthesia,lowtoxicityandnon-addictionUsed
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