青霉素类抗生素概述.docx
《青霉素类抗生素概述.docx》由会员分享，可在线阅读，更多相关《青霉素类抗生素概述.docx（16页珍藏版）》请在冰豆网上搜索。
青霉素类抗生素概述
青霉素类抗生素概述
主要内容:
一、青霉素由来
二、结构特点
三、抗菌作用机制
四、分类
五、不良反应
六、青霉素临床应用注意事项
七、青霉素使用现状
一、青霉素由来
首先先来看看青霉素的由来,早在唐朝的时候,长安城的裁缝会把长有绿毛的糨糊涂在被剪刀划破的手指上来帮助伤口愈合,就是因为绿毛产生的物质（青霉素）有杀菌作用,这也是人们andperformancetestcopiesoftherecord.Ifnecessary,reviewshouldbecarriedout;4）forspringhangers（includedsimplespring,hangersandconstantsupporthangers）itshouldalsoberecognizedassettingandlockingofloads.5）checkthesurfacequality,foldedlayeringandwithoutcracks,rustandotherdefects.5）aftercompletionofthetestandcontroldrawingnumberonebyone,byseriesbaled.Coloralloysteelparts,thepartsmarkinginstallationlocationandrotationaboutthedirectionyouwant.7.3.14.hangersinstallation7.3.14.1hangerlayouta.acleardesignofhangershouldbeinstalledstrictlyinaccordancewiththedrawingsanddesignsshallnotbeinstalledwrong,missing,etc.B.ownarrangementofpipingsupportandhangersetandselectionshouldbebasedoncomprehensiveanalysisofgenerallayoutofpipingsystems;coldinstallationofsteampipewithparticularattentionreservedforcompensationofthermalexpansiondisplacementandorientation.C.supportsystemsshouldberationaltowithstandpipeloads,staticloadandincidentalload;reasonablepipingdisplacement;guaranteedundervariousconditions,stressarewithintheallowedrange.Strength,stiffness,andmeetrequirementstopreventvibrationandsoothingwater,withoutaffectingtheadjacentequipmentmaintenanceandotherpipinginstallationandexpansion.D.equipmentconnectedtotheinterfacetomeetpipelinethrust（torque）limitrequirements;increasethestabilityofpipingsystemstopreventpipeline...Tubewallthickness（mm）2-34-67-10weldformnoslopemouthweldstrengtheningheighth（mm）1-1.51.5-2weldwidthb（mm）5-67-6hasslopemouthweldstrengtheningheighth（mm）1.5-22weldwidthb（mm）coverhadeachedgeslopemouthabout2mmargonarcweldingweldstrengtheningsurfaceheightandwidthtubewallthickness（mm）2--33--45--6weldformweldstrengtheningheighth（mm）1-1.51.5-22-2.5widthb（mm）
最早使用青霉素类药物来杀菌。
但是当时他并不知道绿毛里产生
的哪种物质,也不知道这种物质的作用机理,而是根据自己日常
的生活发现总结出来的生活经验。
那么青霉素最开始是如何被发
现和产生的呢?
它的作用机制又是什么呢?
下面让我们带着这两
个问题一起来探索一下青霉素的奥秘!
andperformancetestcopiesoftherecord.Ifnecessary,reviewshouldbecarriedout;4）forspringhangers（includedsimplespring,hangersandconstantsupporthangers）itshouldalsoberecognizedassettingandlockingofloads.5）checkthesurfacequality,foldedlayeringandwithoutcracks,rustandotherdefects.5）aftercompletionofthetestandcontroldrawingnumberonebyone,byseriesbaled.Coloralloysteelparts,thepartsmarkinginstallationlocationandrotationaboutthedirectionyouwant.7.3.14.hangersinstallation7.3.14.1hangerlayouta.acleardesignofhangershouldbeinstalledstrictlyinaccordancewiththedrawingsanddesignsshallnotbeinstalledwrong,missing,etc.B.ownarrangementofpipingsupportandhangersetandselectionshouldbebasedoncomprehensiveanalysisofgenerallayoutofpipingsystems;coldinstallationofsteampipewithparticularattentionreservedforcompensationofthermalexpansiondisplacementandorientation.C.supportsystemsshouldberationaltowithstandpipeloads,staticloadandincidentalload;reasonablepipingdisplacement;guaranteedundervariousconditions,stressarewithintheallowedrange.Strength,stiffness,andmeetrequirementstopreventvibrationandsoothingwater,withoutaffectingtheadjacentequipmentmaintenanceandotherpipinginstallationandexpansion.D.equipmentconnectedtotheinterfacetomeetpipelinethrust（torque）limitrequirements;increasethestabilityofpipingsystemstopreventpipeline...Tubewallthickness（mm）2-34-67-10weldformnoslopemouthweldstrengtheningheighth（mm）1-1.51.5-2weldwidthb（mm）5-67-6hasslopemouthweldstrengtheningheighth（mm）1.5-22weldwidthb（mm）coverhadeachedgeslopemouthabout2mmargonarcweldingweldstrengtheningsurfaceheightandwidthtubewallthickness（mm）2--33--45--6weldformweldstrengtheningheighth（mm）1-1.51.5-22-2.5widthb（mm）
6APA
HHSCHOH3
1
CCRCNC2165CH3BA43
CNCCOR2二、青霉素类结构特点
OHO青霉素自20世纪40年代
酰胺酶青霉素酶作用点投入使用以来，一直是应作用点
用广泛和重要的一类抗生
素，基本结构如右图所示，
由母核6-APA（6-氨基青霉烷酸）
和侧链组成。
母核结构—青酶烷酸（双环结构）
（β-内酰胺环并氢化噻唑环）,其中β-内酰胺环为维持抗菌活性的最基本结构。
二环的张力都比较大，其稳定性极差，易受到亲核性或亲电性试剂的进攻，使β-内酰胺环破裂，导致青霉素失效并产生致敏物。
由于临床上抗菌的需要，人们对侧链上的R经结构改造接上不同的基团，形成各种性能更好的半合成青霉素。
三、抗菌作用机制
（1）通过竞争性抑制细菌的青霉素结合蛋白（PBPs）?
?
细胞壁的粘肽合成受阻?
?
细菌细胞壁缺损?
?
大量的水分涌进细andperformancetestcopiesoftherecord.Ifnecessary,reviewshouldbecarriedout;4）forspringhangers（includedsimplespring,hangersandconstantsupporthangers）itshouldalsoberecognizedassettingandlockingofloads.5）checkthesurfacequality,foldedlayeringandwithoutcracks,rustandotherdefects.5）aftercompletionofthetestandcontroldrawingnumberonebyone,byseriesbaled.Coloralloysteelparts,thepartsmarkinginstallationlocationandrotationaboutthedirectionyouwant.7.3.14.hangersinstallation7.3.14.1hangerlayouta.acleardesignofhangershouldbeinstalledstrictlyinaccordancewiththedrawingsanddesignsshallnotbeinstalledwrong,missing,etc.B.ownarrangementofpipingsupportandhangersetandselectionshouldbebasedoncomprehensiveanalysisofgenerallayoutofpipingsystems;coldinstallationofsteampipewithparticularattentionreservedforcompensationofthermalexpansiondisplacementandorientation.C.supportsystemsshouldberationaltowithstandpipeloads,staticloadandincidentalload;reasonablepipingdisplacement;guaranteedundervariousconditions,stressarewithintheallowedrange.Strength,stiffness,andmeetrequirementstopreventvibrationandsoothingwater,withoutaffectingtheadjacentequipmentmaintenanceandotherpipinginstallationandexpansion.D.equipmentconnectedtotheinterfacetomeetpipelinethrust（torque）limitrequirements;increasethestabilityofpipingsystemstopreventpipeline...Tubewallthickness（mm）2-34-67-10weldformnoslopemouthweldstrengtheningheighth（mm）1-1.51.5-2weldwidthb（mm）5-67-6hasslopemouthweldstrengtheningheighth（mm）1.5-22weldwidthb（mm）coverhadeachedgeslopemouthabout2mmargonarcweldingweldstrengtheningsurfaceheightandwidthtubewallthickness（mm）2--33--45--6weldformweldstrengtheningheighth（mm）1-1.51.5-22-2.5widthb（mm）
菌体内?
?
细菌肿胀、破裂、死亡。
（2）触发自溶酶活性，使细菌溶解。
四、分类
常见的有以下三种:
天然青霉素半合成青霉素（耐酶青霉素、广谱青霉素）
（一）、天然青霉素
由青霉菌培养液提取获得，含有5种（X、F、G、K、双氢F），其中以青霉素G性质较稳定，作用最强，低毒价廉，可用于治疗敏感菌所致的各种感染。
目前市场上常见的有两种:
注射用青霉素钠和注射用苄星青霉素。
下面以青霉素最广泛使用的青霉素G（苄青霉素）为例来进行说明。
药理特性:
繁殖期杀菌药
抗菌作用:
主要用于G+菌、G-球菌、螺旋体，放线菌感染，对G-杆菌不敏感。
作用特点:
不耐酸、不耐酶、窄谱
适应症:
1.G+菌感染:
肺炎球菌、葡萄球菌、链球菌（溶血性链球菌、草绿色链球菌）、肠球菌白喉杆菌、炭疽杆菌、破伤风杆菌、产气夹膜杆菌等。
2.G-球菌:
脑膜炎双球菌、淋球菌。
3.螺旋体:
梅毒、钩端、回归热螺旋体。
andperformancetestcopiesoftherecord.Ifnecessary,reviewshouldbecarriedout;4）forspringhangers（includedsimplespring,hangersandconstantsupporthangers）itshouldalsoberecognizedassettingandlockingofloads.5）checkthesurfacequality,foldedlayeringandwithoutcracks,rustandotherdefects.5）aftercompletionofthetestandcontroldrawingnumberonebyone,byseriesbaled.Coloralloysteelparts,thepartsmarkinginstallationlocationandrotationaboutthedirectionyouwant.7.3.14.hangersinstallation7.3.14.1hangerlayouta.acleardesignofhangershouldbeinstalledstrictlyinaccordancewiththedrawingsanddesignsshallnotbeinstalledwrong,missing,etc.B.ownarrangementofpipingsupportandhangersetandselectionshouldbebasedoncomprehensiveanalysisofgenerallayoutofpipingsystems;coldinstallationofsteampipewithparticularattentionreservedforcompensationofthermalexpansiondisplacementandorientation.C.supportsystemsshouldberationaltowithstandpipeloads,staticloadandincidentalload;reasonablepipingdisplacement;guaranteedundervariousconditions,stressarewithintheallowedrange.Strength,stiffness,andmeetrequirementstopreventvibrationandsoothingwater,withoutaffectingtheadjacentequipmentmaintenanceandotherpipinginstallationandexpansion.D.equipmentconnectedtotheinterfacetomeetpipelinethrust（torque）limitrequirements;increasethestabilityofpipingsystemstopreventpipeline...Tubewallthickness（mm）2-34-67-10weldformnoslopemouthweldstrengtheningheighth（mm）1-1.51.5-2weldwidthb（mm）5-67-6hasslopemouthweldstrengtheningheighth（mm）1.5-22weldwidthb（mm）coverhadeachedgeslopemouthabout2mmargonarcweldingweldstrengtheningsurfaceheightandwidthtubewallthickness（mm）2--33--45--6weldformweldstrengtheningheighth（mm）1-1.51.5-22-2.5widthb（mm）
4.放线菌感染:
但对大多数的G-杆菌无效，对金葡菌产生的β-内酰胺酶不稳定。
【药物相互作用】:
与丙磺舒合用?
效能?
与氨基苷类合用?
协同，但不能混合静注与抑菌药合用?
效能?
不能与重金属，铜、锌、汞配伍
不能与氨基酸营养液合用
半合成青霉素
1、口服青霉素类:
苯氧青霉素类青霉素?
（penicillinV）
非奈西林（phenethicillin）特点:
1）耐酸不耐酶
2）可口服
3）抗菌谱与青霉素同，用于轻症感染
2.耐酶青霉素类
苯唑西林（oxacillin）
氯唑西林（cloxacillin）
双氯西林（dicloxacillin）
氟氯西林（flucloxacillin）特点:
耐酸耐酶
andperformancetestcopiesoftherecord.Ifnecessary,reviewshouldbecarriedout;4）forspringhangers（includedsimplespring,hangersandconstantsupporthangers）itshouldalsoberecognizedassettingandlockingofloads.5）checkthesurfacequality,foldedlayeringandwithoutcracks,rustandotherdefects.5）aftercompletionofthetestandcontroldrawingnumberonebyone,byseriesbaled.Coloralloysteelparts,thepartsmarkinginstallationlocationandrotationaboutthedirectionyouwant.7.3.14.hangersinstallation7.3.14.1hangerlayouta.acleardesignofhange
升级会员 