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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、）乙酯鹽酸鹽，又名鹽酸奴佛卡因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、堿及體內(nèi)酶均使其水解。pH3-3.5最穩(wěn)定，在堿性、中性及強酸性條件下易水解。Oxidization：含芳伯氨基，易被氧化變色。Activityandclinicalapplication:Procaine具有良好的局麻作用，毒性低，無成癮性，是國內(nèi)外臨床廣泛應(yīng)用的局麻藥之一，主要用于浸潤麻醉，傳導(dǎo)麻醉和封閉療法。Withgoodlocalanesthesia,lowtoxicityandnon-addictionUsed
