пеницилин

Въведение в съединението

Основна информация

Китайско име: пеницилин

Китайски псевдоним: пеницилин

Име на английски: benzylpenicillin

Englishalias:cilloral;pradupen;Ursopen;benzylpenicillin;cosmopen;

CASNомер:61-33-6

Молекулярна формула: C₁₆H₁₈N₂O₄S

Молекулно тегло: 334.39000

Точна маса: 334.09900

PSA: 112.01000

LogP:1.18960

Физични и химични свойства

Плътност: 1,42 g/cm3³

Точка на кипене: 663,3ºCat760 mmHg

Точка на запалване: 355ºC

Индекс на пречупване: 1,655

Условия на съхранение: проветриво, ниска температура и сухо

Информация за безопасност

Митнически код:32041900

WGKГермания:2

Код на категорията на опасност: R42/43

Инструкции за безопасност: S36/37

RTECS номер: XH9700000

Знак за опасни стоки: Xn

R&DHistory

Beforethe1940s,humanshadnotbeenabletomasteradrugthatcouldeffectivelytreatbacterialinfectionswithlowsideeffects.Ifsomeonehastuberculosisatthattime,itmeansthatthepersonwilldiesoon.Inordertochangethissituation,scientificresearchershavecarriedoutlong-termexploration,butthebreakthroughprogressmadeinthisregardisduetoanaccidentaldiscovery.

Inmoderntimes,in1928,BritishbacteriologistFlemingfirstdiscoveredtheworld'sfirstantibiotic,penicillin.AlexanderFlemingdiscoveredpenicillinduetoaluckymistake.

In1928,BritishscientistFlemingfirstdiscoveredpenicillininexperimentalresearch,butduetothelackofadvancedtechnologyanddeepunderstandingatthattime,Flemingdidnotseparatepenicillinalone.

In1929,Flemingpublishedhisresearchresults.Unfortunately,thispaperhasnotreceivedtheattentionofthescientificcommunitysinceitwaspublished.

Whenviewingthepetridishwithamicroscope,Flemingfoundthatthestaphylococcalcoloniessurroundingthemoldhadbeendissolved.ThismeansthatacertainsecretionofmoldcaninhibitStaphylococcus.Thesubsequentidentificationshowedthattheabove-mentionedmoldwasPenicilliumspp.Therefore,Flemingcalledtheantibacterialsubstancesecretedbyitaspenicillin.Unfortunately,Fleminghasnotbeenabletofindawaytoextracthigh-puritypenicillin,sohecultivatedthepenicilliumstrainsforgenerations,andin1939providedthestrainstotheBritishpathologistFlo,whowaspreparingtosystematicallystudypenicillin.Li(HowardWalterFlorey)andbiochemistQianEn.

През 1938 г. германският химик Ернст Чансоу Флеминг написва купчина свити книги и започва експерименти за пречистване.

FloryandChanre-experimentedwithpenicillinin1940.TheyinjectedeightmicewithalethaldoseofStreptococcusandthentreatedfourofthemwithpenicillin.Withinafewhours,onlythefourmicethathadbeentreatedwithpenicillinwerealiveandhealthy.Sincethen,aseriesofclinicaltrialshaveconfirmedtheefficacyofpenicillinonvariousbacterialinfectionssuchasstreptococcusanddiphtheriabacillus.Thereasonwhypenicillincankillbacteriawithoutharminghumancellsisthatthepenicillanecontainedinpenicillincanhinderthesynthesisofthecellwallofthebacteria,causingthebacteriatodissolveanddie,whilehumanandanimalcellshavenocellwall.

Inthewinterof1940,QianEnextractedalittlepenicillin.Althoughthiswasamajorbreakthrough,itwasfarfromclinicalapplication.

In1941,thebatonofpurificationofpenicillinwaspassedtothehandsofAustralianpathologistWalterFlory.WiththeassistanceoftheU.S.military,Floryseparatedstrainsfromthesoilbroughtbackfromtheairportsofvariouscountrieswhenthepilotswentoutformissions,increasingtheproductionofpenicillinfrom2unitspercubiccentimeterto40units.

About1941,thepathologistHowardFloryofOxfordUniversityinEnglandandthebiochemistQianEnrealizedtheseparationandpurificationofpenicillin,anddiscovereditscurativeeffectoninfectiousdiseases,butpenicillincanmakesomepeopleAnallergicreactionoccurs,soaskintestmustbedonebeforeapplication.Mostoftheantibioticsusedareextractedfrommicrobialculturefluid,andsomeantibioticscanbesynthesizedartificially.Becausedifferenttypesofantibioticshavedifferentchemicalcomponents,theirmechanismofactiononmicroorganismsisalsoverydifferent.Someinhibitthesynthesisofproteins,someinhibitthesynthesisofnucleicacids,andsomeinhibitthesynthesisofcellwalls.

Throughaperiodofintenseexperimentation,FloryandChannfinallyusedfreeze-dryingtoextractpenicillincrystals.Later,Floryfoundamoldonamelonthatcouldextractalargeamountofpenicillin,andusedcornflourtoprepareacorrespondingculturesolution.Drivenbytheseresearchresults,Americanpharmaceuticalcompaniesbeganmassproductionofpenicillinin1942.

By1943,pharmaceuticalcompanieshaddiscoveredawaytomass-producepenicillin.AtthattimeBritainandtheUnitedStateswereatwarwithNaziGermany.Thisnewdrugisveryeffectiveincontrollingwoundinfections.

InOctober1943,FlorysignedthefirstbatchofpenicillinproductioncontractswiththeUSmilitary.PenicillinwasbornattheendofWorldWarIIandquicklyreversedthebattleoftheAllies.Afterthewar,penicillinwaswidelyused,savingtensofmillionsoflives.By1944,thesupplyofmedicinewassufficienttotreatallAlliedsoldierswhoparticipatedinthewarduringtheSecondWorldWar.Becauseofthisgreatinvention,in1945,Fleming,FloryandChannwontheNobelPrizeinPhysiologyorMedicineforthe"discoveryofpenicillinanditsclinicaleffects".

През 1945 г. британският химик D.C.Hodgkin използва рентгенова дифракция, за да определи молекулярната структура на пеницилина.

На 5 септември 1944 г. се ражда първата китайска партида пеницилини, произведени в страната, разкривайки историята на китайското производство на антибиотици. Към края на 2001 г. годишното производство на пеницилин в Китай представлява 60% от общото годишно производство на пеницилин в света, което се нарежда на първо място в света.

In2002,Biroletal.proposedamodelbasedontheprocessmechanism.Theprocesscomprehensivelyconsideredthevariousphysiologicalchangesofmicroorganismsduringfermentationandfoundthatthisisaverycomplicatedprocess.Inordertostudythepenicillinprocessmoreconveniently,Birolextendedthenon-structuralmodelproposedbyBajpaiandReuss,andfurthersimplifiedthemodeltofacilitateresearch.

Mainfunctions

Penicillinisanimportantantibioticwithhighefficiency,lowtoxicityandwideclinicalapplication.Itssuccessfuldevelopmentgreatlyenhancedtheabilityofhumanstoresistbacterialinfectionsandledtothebirthoftheantibioticfamily.Itsappearanceopenedupanewerainthetreatmentofdiseaseswithantibiotics.Throughdecadesofimprovement,penicillininjectionandoralpenicillinhavebeenabletotreatpneumonia,meningitis,endocarditis,diphtheria,anthraxandotherdiseasesrespectively.Followingpenicillin,antibioticssuchasstreptomycin,chloramphenicol,oxytetracycline,tetracycline,etc.continuetobeproduced,enhancingtheabilityofhumanstotreatinfectiousdiseases.Butatthesametime,theresistanceofsomebacteriaisgraduallyincreasing.Inordertosolvethisproblem,researchersarecurrentlydevelopingmorepotentantibiotics,exploringhowtopreventgermsfromacquiringresistancegenes,anddevelopingantibacterialdrugsusingplantsasrawmaterials.

Penicillincannottoleratetheenzymesproducedbydrug-resistantstrains(suchasdrug-resistantStaphylococcusaureus),andiseasilydestroyedbyit,anditsantibacterialspectrumisnarrow,anditismainlyeffectiveagainstGram-positivebacteria.PenicillinGcanbedividedintopotassiumsaltandsodiumsalt.Potassiumsaltcannotbedirectlyinjectedintravenously.Whenintravenousinfusion,theamountofpotassiumionsmustbecarefullycalculatedtoavoidtheformationofhyperkalemiaandinhibitheartfunctionandcausedeath.

Thetoxicityofpenicillinantibioticsisverysmall.Becauseβ-lactamsactonthecellwallofbacteria,whilehumanshaveonlycellmembraneswithoutcellwalls,theyarelesstoxictohumans.Inadditiontocausingsevereallergicreactions,Undernormaldosage,itstoxicityisnotobvious.

Tousethisproduct,anintradermaltestmustbedonefirst.Penicillinallergytestincludesskintestmethod(referredtoaspenicillinskintest)andinvitrotestmethod,ofwhichintradermalinjectionismoreaccurate.Theskintestitselfisalsodangerous.About25%ofpatientswhodiefromanaphylacticshockdiefromtheskintest.Therefore,adequaterescuepreparationsshouldbemadeduringskintestorinjectionadministration.Whenchangingtoadifferentbatchofpenicillin,itisalsonecessarytorepeattheskintest.Thedrypowdercanbestoredformanyyearswithoutexpiration,buttheinjectionsolutionandtheskintestsolutionareunstable,anditisbettertoprepareitfresh.Andforthosewithrenaldysfunction,thedosageshouldbeadjustedappropriately.Inaddition,topicalapplicationhasmanychancesofsensitization,andbacteriaarepronetodrugresistance,soitisnotrecommended.

Classification

Picillinwasusedclinicallyintheearly1940s.Afteralotofresearchonpenicillin,somepenicillinwasdiscovered.Whenpeoplechemicallymodifiedpenicillin,someeffectivepenicillinwasobtained.Semi-syntheticpenicillins.Inthe1970s,somepenicillinswerefoundfrommicrobialmetabolitesthataresimilartopenicillinandalsocontainβ-lactamringsinsteadoftetrahydrothiazoleringstructures.Thesepenicillinscanbedividedintothreegenerations:Thefirst-generationpenicillinreferstonaturalpenicillin,suchaspenicillinG(benzylpenicillin);thesecond-generationpenicillinreferstothesemi-syntheticpenicillinbychangingthesidechainofpenicillinnucleus-6-aminopenicillanicacid(6-APA),Suchasmethicillin,carbenicillin,andampicillin;thethird-generationpenicillinhasacorestructurewiththesameβ-lactamringaspenicillin,butdoesnothaveatetrahydrothiazolering,suchasthiomycinandnocardinWhite.

Според характеристиките си може да се раздели на:

ПеницилинG:като пеницилин Gкалий, пеницилинGнатрий, дългодействащ Cillin`penicillinG, peillinG, пеницилин, пеницилин, пеницилиннатрий, бензилпеницилиннатрий, пеницилинкалий, бензилпеницилинкалий и др.

Пеницилин V: (псевдоним: феноксиметилпеницилин, 6-феноксиацетамидопенициланова киселина) като пеницилин V калий (включително разнообразие от дозирани форми)).

Ензимно-устойчив пеницилин:сухазоксацилин (XinqingII), хлоразолпеницилин и др.

Ампицилин:като сампицилин, амоксицилин и др.

Анти-псевдомонаспеницилин:като карбеницилин, пиперацилин, тикарцилин и др.

MecillinanditsestersofPimethicillin:SuchasmecillinanditsestersofPimethicillin,etc.,whicharemoreresistanttoenzymesandareresistanttocertainnegativebacilli(suchaslargeintestine,gramLebsiellaandSalmonella)areeffectivebutpoorlyeffectiveagainstPseudomonasaeruginosa.

Метицилини: такивастамоксицилин и др.

Метод на приготвяне

Методът на производство на естествен пеницилин и полусинтетичен пеницилин е напълно различен.

[Естествен пеницилин]

TheproductionofpenicillinGcanbedividedintotwosteps:strainfermentationandextractionandpurification.①Fermentationofstrains:inoculatethePenicilliumchrysogenumonasolidmediumandcultivatefor7-10daysat25°CtoobtainasporecultureofPenicillium.Usesterilewatertomakeasuspensionofsporesandinoculateitintothesterilizedmediumintheseedtank,passinsterileair,stir,andincubateat27°Cfor24to28hours,andtheninoculatetheseedculturesolutionintothefermentor.Inthesterilizedmediumcontainingthephenylaceticacidprecursor,sterileairwaspassedthrough,stirred,andculturedat27°Cfor7days.Thephenylaceticacidprecursorandanappropriateamountofculturemediumneedtobesupplementedduringthefermentationprocess.②Extractionandpurification:coolingandfilteringthepenicillinfermentationbroth.Thefiltrateissubjectedtomulti-stagecountercurrentextractionwithbutylacetateintheextractionmachineundertheconditionofpH2to2.5toobtainthebutylesterextract,whichistransferredtothebuffersolutionofpH7.0to7.2,andthentransferredtothebutylester.Thisbutylesterextractisdecolorizedbyactivatedcarbon,addedwithasalt-formingagent,andsubjectedtoazeotropicdistillationtoobtainpenicillinGpotassiumsalt.PenicillinGsodiumsaltispreparedbypassingpenicillinGpotassiumsaltthroughionexchangeresin(sodiumtype).

[Полусинтетичен пеницилин]

Using6APAasanintermediateandavarietyofchemicallysynthesizedorganicacidsforacylationreaction,varioustypesofSemi-syntheticpenicillin.

6APAisobtainedbycleavingpenicillinGorVwithpenicillinacylaseproducedbymicroorganisms.Enzymereactionisgenerallycarriedoutundertheconditionsof40～50℃andpH8～10;enzymeimmobilizationtechnologyhasbeenappliedtotheproductionof6APA,whichsimplifiesthecleavageprocess.6APAcanalsobemadebychemicallycrackingfrompenicillinG,butthecostishigher.Theintroductionofthesidechainistofirstmakethecorrespondingorganicacidintoanacidchloridewithachlorinatingagent,andthenuseaninorganicororganicbaseasacondensingagenttocarryoutanacylationreactionwith6APAaccordingtothestabilityoftheacidchlorideinwaterororganicsolvents.Thecondensationreactioncanalsobecarriedoutdirectlyinthelysatewithoutseparating6APA.

[Метод за концентрация на пеницилин]

Amethodofusingpenicillintospecificallykillwild-typecellsandretainauxotrophiccells.Penicillincaninhibitthesynthesisofbacterialcellwalls,soitcanonlykillbacteriathataregrowingandreproducing,butnotbacteriathatstopdividing.Intheselectiveliquidmediumthatcanonlygrowthewildtypebutnotthemutanttype,thewildtypeiskilledbypenicillin,whilethemutanttypeisnotkilled,sothatthewildtypeiseliminatedandthemutanttypeisconcentrated.Itcanbeappliedtobacteriaandactinomycetes,andisoneofthecommonmethodsforscreeningauxotrophicmutants.

Drugdescription

Pharmacologicalefficacy

Picillinantibioticsarethegeneraltermforalargeclassofantibioticsinβ-lactams,duetotheactionofβ-lactamsBecauseofthecellwallsofbacteria,humanshaveonlycellmembraneswithoutcellwalls.Penicillinantibioticshavelittletoxicityandaretheantibioticswiththehighestchemotherapyindex.However,thecommonallergicreactiontopenicillinantibioticsranksfirstamongvariousdrugs,withanincidenceofupto5%to10%.Itisaskinreaction,showingrash,angioedema,andthemostseverecaseisanaphylacticshock,mostlyafterinjectionItoccurswithinafewminutes,andthesymptomsaredyspnea,cyanosis,bloodpressuredrop,coma,stifflimbs,andfinallyconvulsions.Failuretorespondintimecancausedeath.

Variousroutesofadministrationorapplicationofvariouspreparationscancauseanaphylacticshock,butinjectionshavethehighestincidence.Theoccurrenceofallergicreactionshasnothingtodowiththesizeofthedrugdose.Peoplewhoarehighlyallergictothisproductcancauseshockeveninverysmallamounts.Injectionintothebodycancauseepilepticseizures.Large-doselong-terminjectionistoxictothecentralnervoussystem(suchascausingconvulsions,coma,etc.),anditcanberecoveredbystoppingthedrugorreducingthedose.

Oraluseiseasilydestroyedbygastricacidanddigestiveenzymes.Afterintramuscularinjectionorsubcutaneousinjection,theabsorptionisfaster,andthepeakbloodconcentrationisreachedwithin15-30minutes.Penicillinhasashorthalf-lifeinthebodyandismainlyexcretedintheurineinitsoriginalform.

Thepharmacologicaleffectofpenicillinistointerferewiththesynthesisofbacterialcellwalls.ThestructureofpenicillinissimilartotheD-alanyl-D-alanineinthestructureofthecellwallmucopeptide.Itcancompetewiththelatterfortranspeptidase,hindertheformationofmucopeptides,causecellwalldefects,andmakebacterialosetheircellwalls.Permeablebarrier,killingbacteria.

Pharmacokinetics

Picillinisnotacidresistantandshouldnotbetakenorally.Afterintramuscularinjection,thepeakbloodconcentration(Cmax)isreachedwithin0.5hours,whichcanbewidelydistributedintissuesandbodyfluids,andeasilypenetratesintoinflammatorytissues.Theconcentrationinthechest,abdominalcavityandjointcavityfluidisabout50%oftheserumconcentration.Thisproductcanpassthroughtheplacenta,butitisdifficulttopassthroughtheblood.Thecerebrospinalfluidbarrier,milkmaycontainasmallamountofpenicillin,whichisnoteasytopenetrateintotheeyes,bonetissues,areaswithoutbloodsupplyandabscesses.Theplasmaproteinbindingrateis45%-65%,andthebloodeliminationhalf-life(t1/2β)isabout30minutes.Itcanbeextendedto2.5-10hoursforpeoplewithimpairedrenalfunction,anditcanalsobeextendedfortheelderlyandnewborns.About19%ofthisproductismetabolizedintheliver,mainlysecretedandexcretedthroughtherenaltubules.Undernormalrenalfunction,about75%ofthedoseisexcretedfromthekidneywithin6hours,andasmallamountisexcretedthroughthebiliarytract.Hemodialysiscanremovethisproduct,butperitonealdialysiscannot.

Combinedreaction

Theproblemofdrugabuseintheclinichascausedsomeadversereactions,especiallythecompatibilityofpenicillinwithotherdrugs.Theinteractionsandadversereactionsproducedcannotbeignoredof.

1. Пеницилинът не може да се комбинира с подобни антибиотици

Becausetheirantibacterialspectrumandantibacterialmechanismaremostlysimilar,thecombinedeffectisnotadditive.Onthecontrary,combinedmedicationaggravateskidneydamage,andcanalsocausedyspneaorrespiratoryarrest.Thereiscross-resistancebetweenthem,andthecombinedapplicationoftwoβ-lactamantibioticsisnotrecommended.

2. Пеницилинът не може да се използва в комбинация със сулфатни лекарства и тетрациклини

Picillinisa"bactericide"duringthebreedingperiod,whichhindersthesynthesisofbacterialcellwallsTetracyclineisa"bacteriostaticagent",whichaffectsthesynthesisofbacterialprotein.Thecombinedeffectofthetwoisanantagonisticeffect.Undernormalcircumstances,itshouldnotbeusedincombination.Clinicaldatashowthattheantibacterialefficacyofpenicillinaloneis90%,theefficacyofsulfadrugsaloneis81%,andtheantibacterialefficacyofthecombinationofthetwodrugsis75%.Itcannotbeusedincombinationunlesstherearespecialcircumstances.

3. Пеницилинът не може да се смесва с аминогликозидни лекарства за инфузия

Mixingthetwoisthesameastheinfusionsetforpatientinfusion,becauseoftheβ-lactamofpenicillinGentamicincanbeinactivated.Themechanismisachemicalinteractionbetweenthetwo.Therefore,mixedapplicationisstrictlyprohibited.Penicillinintravenousdripandgentamicinintramuscularinjectionshouldbeused.

Tosumup,theimpropercombinationofpenicillin,duetodruginteractions,leadingtoadversedrugreactionscannotbeunderestimated.Penicillinisthemostcommonlyusedantibioticforthetreatmentofvariousinfectiousdiseases.Strictlygrasptheindicationsofthemedication,rationallyuseitincombination,andtakeeffectivemeasurestoreduceunnecessaryadversereactions.

⒋Chloramphenicol,erythromycin,tetracyclines,sulfadrugsandotherbacteriostaticagentscaninterferewiththebactericidalactivityofpenicillin,andshouldnotbecombinedwithpenicillins,especiallyinthetreatmentofmeningitisorseverecasesthatrequirerapidsterilizationWheninfected.

⒌Probenecid,aspirin,indomethacin,phenylbutazone,andsulfadrugscanreducetheexcretionofpenicillinsintherenaltubules,therebyincreasingthebloodconcentrationofpenicillinsandmaintainingthemforalongtime.Thehalf-lifeisprolonged,andtoxicitymayalsoincrease.

⒍Picillinpotassiumorsodiumisincompatiblewithheavymetals,especiallycopper,zincandmercury,becausethelattercandestroytheoxidizedthiazoleringofpenicillin.Rubbertubesorbottlestoppersmadeofzinccompoundscanalsoaffecttheviabilityofpenicillin.Acidicglucoseinjectionortetracyclineinjectioncandestroytheactivityofpenicillin.Penicillincanalsobeinactivatedbyoxidizingorreducingagentsorhydroxylcompounds.

⒎Цефлотин, линкомицин, тетрациклин, ванкомицин, еритромицинетилсукцинат, амфотерицин В, норепинефрин, мета-хидроксиламин, фенитоиннатрий, хидроксихидрохлорид, добавен топпеницилин, интравенозна инфузия Мътност ще се появи на рафтероксазин, прохлорперазин, прометазин, продукт от групата на витамин В, докато не се появи витамин C, и т.н. therwithotherdrugs.

⒏Пеницилинът може да засили ефекта на варфарин.

⒐Aftertheproductismixedwithaminoglycosideantibiotics,theantibacterialactivityofthetwodrugsissignificantlyweakened,sothetwodrugscannotbeadministeredinthesamecontainer.

Лекарствена токсичност

Алергия към пеницилин

Той се абсорбира бързо след перорално приложение, около 75%～90% може да се абсорбира от стомашно-чревния тракт. Храната няма значителен ефект върху абсорбцията на лекарството. Степента на свързване с протеини е 17%-20%, а периодът на полуразпад на елиминиране на кръвта (t1/2) е 1 до 1,3 часа. 6 часа, 46% до 68% от дозата се екскретират в урината като прототип на лекарството, а някои лекарства се екскретират през жлъчните пътища. Този серумен полуживот на пациенти с тежка бъбречна недостатъчност може да бъде удължен до 7 часа. Серумната диализа може да отстрани пеницилина, но перитонеалната диализа няма ефект върху отстраняването на продукта.

Picillinistheleasttoxicsideeffectofvariousantibiotics,becauseitsmechanismofactionistodestroytheprocessandstructureofcellwallformation,andthehumanbodyhasnocellwall.Penicillinhasbasicallynopharmacologicaltoxicitytothehumanbody,butlargedosesofpenicillinmayalsocausenervoussystempoisoning.Themainreasonforthesideeffectsofpenicillinistheinsufficientpurificationofpenicillin,andtheimpuritiesinitareeasytomakethehumanbodyallergic.

⒈Allergicreactions:Penicillinallergicreactionsaremorecommon,rankingfirstamongvariousdrugs.Severeallergicreactionsareanaphylacticshock(typeIallergy),theincidencerateis0.004%to0.015%,typeIIallergiesarehemolyticanemia,drugeruption,contactdermatitis,interstitialnephritis,asthmaattacks,etc.,typeIIIallergiesThereaction,theserotypereaction,isalsomorecommon,withanincidenceof1%to7%.Patientswithanaphylacticshockwhoarenotrescuedintimehaveahighmortalityrate.Therefore,onceitoccurs,itmustberescuedonthespot,immediatelygivethepatientanintramuscularinjectionof0.1%epinephrine0.5-1ml,ifnecessary,dilutewith5%glucoseorsodiumchlorideinjectionforintravenousinjection,iftheclinicalmanifestationdoesnotimprove,repeatithalfanhourlater.Iftheheartbeatstops,adrenalinecanbeinjectedintotheheart.Atthesametime,intravenousinfusionoflargedosesofadrenalcortexhormonestosupplementbloodvolume;patientswithpersistentlypersistentbloodpressurewillbegivenvasoactivedrugssuchasdopamine.Canalsoconsidertheuseofantihistaminestorelieveurticaria.Patientswithbreathingdifficultiesshouldbegivenoxygeninhalationorartificialrespiration,andthosewithobviouslaryngealedemashouldhaveatracheotomyintime.Theapplicationofpenicillinaseisoflittlesignificance.

Принцип на алергия

Picillinisunstableandcanbedecomposedintopenicillinthiazolicacidandpenicillonicacid.Theformercanbepolymerizedintopenicillinthiazolicacidpolymer,combinedwithpolypeptidesorproteinstoformpenicilliumthiazolicacidprotein,whichisanimmediateallergenandthemaincauseofallergicreactions;thelattercanalsointeractwithcysteine​​inthebodyAcidformsadelayedallergen-penicillinacidprotein,whichisrelatedtoserumsickness-likereactions.

⒉Toxicreaction:Penicillintoxicreactionisrare,andperipheralneuritismayoccurintheareaof​​intramuscularinjection.Intrathecalinjectionofmorethan20,000unitsorintravenousinfusionoflargedosesofpenicillincancausemuscleclonus,convulsions,comaandotherreactions(penicillinencephalopathy),whicharemorecommonininfants,theelderlyandpatientswithimpairedrenalfunction.Penicillincanoccasionallycausepsychoticepisodes,andindividualpatientsmayexperienceanxiety,fever,shortnessofbreath,highbloodpressure,rapidheartrate,hallucinations,convulsions,coma,etc.aftertheapplicationofprocainepenicillin.Themechanismofthisreactionisunknown.

⒊Doubleinfection:Penicillin-resistantStaphylococcusaureus,Gram-negativebacilliorCandidaalbicansinfectioncanoccurduringtreatmentwithpenicillin.Over-proliferationofCandidacanmakethetonguecoatingbrownorevenblack.

⒋Hyperkalemia(hypokalemia)andhypernatremia:Ifalargeamountofpenicillinpotassiumisadministeredintravenously,hyperkalemiaorpotassiumpoisoningmayoccur.High-dosepenicillinsodium,especiallyforpatientswithimpairedrenalfunctionorcardiacinsufficiency,cancausehypernatremia.Aftergivingpatients100millionunitsofpenicillinsodiumdaily,asmallnumberofpatientsmaydevelophypokalemia,metabolicalkalosisandhypernatremia.

⒌Hertzianreactionandtreatmentcontradiction:whenpenicillinisusedtotreatsyphilis,leptospirosisorotherinfections,symptomsmayincrease.ItiscalledHerxianreaction,whichisasystemicreactioncausedbythekillingofalargenumberofpathogens.Treatmentcontradictionsarealsoseeninpatientswithsyphilis,becausethesyphilislesionsdisappeartooquicklyaftertreatment,butthetissuerepairisslow,orthefibroustissueshrinks,whichhindersorganfunction.

6. Ветеринарно клиничните алергии обикновено са леки, главно се проявяват изпотяване, възбуда, безпокойство, мускулен тремор, диспнея, ускорен пулс, нестабилно стоене, понякога тръпка, оток на клепачите и лицето, подуване на вулвата и ректума и септичен целулит, шок и дори смърт в тежки случаи.

[Причина]

Penicillinisunstableandcanbedecomposedintopenicillinthiazolicacidandpenicillonicacid.Theformercanbepolymerizedintopenicillinthiazolicacidpolymer,combinedwithpolypeptidesorproteinstoformpenicilliumthiazolicacidprotein,whichisanimmediateallergenandthemaincauseofallergicreactions;thelattercanalsointeractwithcysteine​​inthebodyAcidformsadelayedallergen-penicillinacidprotein,whichisrelatedtoserumsickness-likereactions.Patientswithahistoryofdrugallergyorallergicreactionshaveahigherincidenceoftopicalmedicationsandlong-actingpreparations.

Inclinicaluse,hightemperature,acid-base,andheavymetalionsshouldbeavoided.TrytoavoidusingglucoseinjectionwithanacidicPHvalueasasolvent,andwhenusing0.9%sodiumchlorideasasolvent,itshouldbepreparedimmediately,otherwiseitwillbeplacedfortoolonganditwillcausethedecompositionofpenicillin.Causestheoccurrenceofallergicreactions.

[Първи мерки]

⒈Спрете лекарството незабавно, легнете и спасете на място, с главата ниско и краката.

⒉Подкожно инжектиране на 0,1% епинефринхидрохлорид 0,5～1 ml, деца могат да го намалят и след това подкожно инжектиране на 0,5 ml след половин час, до рисковия период, добавете кортикостероиди или антихистамини, ако е необходимо.

⒊Patientswithcardiacarrestshouldundergocardiacchestcompressionorintracardiacinjectionof0.1%epinephrinehydrochloride1ml.

⒋Oxygeninhalation,mouth-to-mouthartificialrespirationwhenbreathingisinhibited,andintramuscularinjectionofnicotinicacidorlobelineandotherrespiratorystimulants.

Laryngealedemaaffectsthetracheotomyduringbreathing.

⒌Използвайте хидрокортизон 200 mg, или дексаметазон 5-10 mg към 50% глюкоза 40 ml венозна инжекция или добавете 5-10% глюкоза 500 ml венозно.

⒍Вазоактивни лекарства, като допамин, аламин и др., могат да се използват според нуждите на заболяването.

⒎Correctacidosisandtheapplicationofhistaminedrugs.

⒏Пазете се на топло, предотвратявайте настинки, водете документация за кърмене и не мърдайте.

⒐AcupunctureacupuncturepointsinRenzhong,Neiguan,Yintang,Hegu,Yongquan,etc.

⒑MoxamoxibustioncanbeusedatacupointssuchasNeiguan,Hegu,Yongquan,Guanyuan,andZhongwan.

Пеницилиненцефалопатия

Picillinencephalopathyisararecentralnervoussystemtoxicreactionofpenicillin.Usuallyonlyasmallamountofpenicillinpassesthroughtheblood-brainbarrier.Whentheintravenousinfusionspeedistoolarge,alargeamountofdrugswillquicklyenterthebraintissue,thatis,theconcentrationofthedruginthebloodandcerebrospinalfluidwillincrease,whichinterfereswithnormalnervefunctionsandcausesseverecentralnervoussystemresponses,suchashyperreflexia,impairedperception,andhallucinations,Convulsions,lethargy,etc.,called"penicillinencephalopathy."

Thepathogenesisofpenicillinencephalopathyisunknown.Thereasonisthatthedruginhibitsthesynthesisandtransportofcentralnervoussysteminhibitorytransmitterγ-aminobutyricacid(GABA)toacertainextent,andinhibitscentralnervoussystemNa+-K+-ATPasereducestherestingmembranepotential.Someliteraturebelievesthatitmayberelatedtothecationsinthesodiumsaltofpenicillin.Itisbelievedthatthetoxiceffectsofsodium,lithium,ammonium,strontium,calcium,magnesium,andpotassiumincreaseinorder.Inaddition,itisrelatedtothepurityofthepreparation,individualdifferences,dosesize,injectionmethod,speed,Theconcentrationisallrelated.SomescholarshaveprovedthatwhentheconcentrationofpenicillinGinthecerebrospinalfluidexceeds8u-10u/ml,toxicreactionscanoccur.Somepeoplethinkthatthepoorfunctionoftheblood-brainbarrieristhemainreason.Afterpenicillinentersthebody,90%isexcretedbythekidneys.Infantshavepoorkidneyfunction,whichprolongstheirhalf-life,increasestheirbloodconcentration,increasestoxicity,andproducesneurotoxiceffects.Leadtoincreasedexcitabilityofthebrain-convulsions,thatis,"penicillinencephalopathy.Atpresent,itisrecommendedthatthedosageofpenicillinininfantsis<600,000u/kg·d,andneonates<400,000u/kg·d.Patientswithinsufficiencyandpoorcirculationshouldbeusedwithcaution.

Поради намаляването на бъбречната функция при възрастните хора, пеницилинът и други широкоспектърни пеницилини имат удължен полуживот? Например, пеницилинът интравенозно има полуживот от 0,55 при 25-годишен младеж. Полуживотът на прокаинпеницилин е 10 часа при 25-годишните и 18 часа при 70-годишните 70-годишни; диклоксацилин е на по-малко от 30 години-полуживотът е 0 .88 часа и 3,97 часа при възрастни над 65 години; полуживотът на фамоксицилин е 1 час до 1,5 часа при младите хора и 2,67 часа при 89-годишните възрастни хора. Когато възрастните хора използват големи дози пеницилин и карбеницилин, могат да се появят неврологични и топпсихиатрични симптоми, като хиперрефлексия, перцептивни смущения, халюцинации, конвулсии, летаргия и др. ., както и временни психични разстройства, склонни към "пеницилиненцефалопатия".

Duetotheblood-brainbarrierfunctioninchildrenAndrenalfunctionisimmature,largedosesofpenicillincansignificantlyincreasetheconcentrationofcerebrospinalfluid,whichhasatoxiceffectonthecentralnervoussystem,leadingtopenicillinencephalopathy.Inaddition,onemillionpenicillinGsodiumcontainsNa+39mg,andonemillionpenicillinGpotassiumcontainsK+66mg,whenalargeamountofintravenousinjectionshouldpayattentiontotheretentionofK+andNa+inthebody.Itisalsoeasytoform"penicillinencephalopathy".

Whenthesystemicdosageofpenicillins,especiallypenicillinG,istoolargeortheintravenousdripistoofast,Theconcentrationofpenicillininthecerebrospinalfluidexceeds8U/ml,whichcandirectlystimulatethecerebralcortex,causingseverereactionssuchasconvulsions,convulsions,epilepsyandevencoma.Itusuallyappearswithin24-72haftermedication.Itoftenoccursinnewborns,childrenandtheelderly.,Becausethedrugeasilypenetratestheblood-brainbarrier.Forpatientswithrenaldysfunctionorrenalfailure,itisalsopronetooccurduetodrugexcretiondisorders.

Peripheralneuritismayoccurinthepenicillinintramuscularinjectionarea。Intrathecalinjectionofmorethan20,000unitsorintravenousinfusionoflargedosesofpenicillincancausemuscleclonus,convulsions,comaandotherreactions.Thisreactionismorecommonininfants,theelderlyandpatientswithimpairedrenalfunction.Penicillincanoccasionallycausepsychoticepisodes.UseIndividualpatientsmayexperiencehighfever,anxiety,fever,etc.afterprocainepenicillin.

Theconditionisserious.Themainmanifestationisthesuddenappearanceofconvulsions,dehydration,hypoxia,shortnessofbreath,andbloodproductiononthebasisoftheoriginaldisease.Chemicalchanges(suchashypoglycemia,hyponatremia,acidemia),highbloodpressure,rapidheartrate,hallucinations,convulsions,coma,andrespiratoryfailure,etc.Themechanismofthisreactionisunknown.Somechildrenmayalsohavelimbparalysisandfontanelle.TheclosedchildcanseethefontanelleBeginning,asmallnumberofchildrenmayhaveuncoordinatedmovements.Theabovesymptomsmostlyappear1to2weeksaftertheoriginalillness.

Комата продължава дълго време и може да има сериозни последствия. Тези последствия могат да включват тъпота, слепота, глухота, парализа и др. Тъй като малък брой пациенти може да умрат поради сериозно заболяване.

[Лечение]

⒈StoppenicillinIfpenicillinencephalopathyoccurs,stoppenicillinintime.2.Takeoxygenimmediately.Forcomapatients,sputumshouldbesuckedout,breathingshouldbekeptunobstructed,andoxygenshouldbesuppliedintimeforalongerperiodoftimetopromotetheresolutionofcerebraledema.Ifnecessary,performtracheotomyandartificialrespiration.3.Anticonvulsant,usesedativeandantipsychoticdrugs,intramuscularinjectionofluminalsodium,diazepam,etc.4.Adrenalcortexhormones.Forexample,hydrocortisone,prednisone,anddexamethasoneallhavetheeffectofquicklyreducinginflammationandreducingedema,andshouldbeusedforshort-termuse,generallywithinaweek.5.Anti-cerebraledemadrug20%​​mannitolisinjectedintravenously.Itshouldbeusedrepeatedlyincasesofrepeatedintracranialpressureincreasetopreventbrainherniation.Atthesametime,fastdiureticscanbeaddedtoenhancetheeffectofdehydratingagents.6.Strengthendialysisandcooperatewithhemoperfusion,bloodpurification,etc.7.Properlyhandlehighfever,dehydration,bloodchemistrychanges(suchashypoglycemia,hyponatremia,acidemia),andrespiratoryfailure.8.Speed​​uptheeliminationofdrugsandreducementalsymptoms.9.Energysupporttherapy.Toxicitycanbemetabolizedwithinafewhoursortensofhours,butthepoisonednervesarestillinastateofparalyticshock.Ifthenervesinparalyticshockarenotactivatedandnourishedbyearlytreatment,theinvolvednerveswillbeprolongedduetoischemia.Delayedischemicpathologicalchanges,medicallycalleddelayedneurologicaldamage,itisdifficulttorecover.10.Theprognosisofmostpatientswiththisdiseaseisgood,andthesymptomsdisappearwithin24hoursafterpropertreatment,andthereisnosequelae.Ifthecomalastsforseveraldaystoseveralweeks,itmaycauseserioussequelaesuchasinsufficiency,blindness,deafness,rigidlimbs,inflexibility,orparalysisinchildren.Asmallnumbercandieinarelativelyshortperiodoftimeduetorespiratoryfailure.

[Предпазни мерки]

⒈Amongthesideeffectsofpenicillin,anaphylacticshockisfatal.Itoftenattractspeople’sattentionandmanifestsasencephalopathyandsurroundingTheneurotoxiceffectofnervedamageiseasilyoverlooked.Thepreviousbeliefthatpenicillinisrarelypoisonedaslongasitisnotallergicmustbedispelled.Donotabusepenicillin(includingotherantibiotics)inlargedoses.Whenyoumustuseit,useintravenousinfusionaslittleaspossible.Theelderlyandchildrenshoulduseitwithcaution;inaddition,Itshouldalsobenotedthatwhenpenicillinisusedincombinationwithampicillin,itismorelikelytocausepenicillinencephalopathy.

Whentheelderlyuseantibacterialdrugs,theeffectoftheeliminationprocessissignificantlyslower.

⒉Penicillinwasoriginallyahighlyeffectiveandlow-toxicantibiotic.Ithasmadegreatachievementsinthehistoryofhumananti-infection,anditsreputationhasnotdiminished.Probablybecauseofthis,thereisatrendthatpenicillinisusedmoreandmorewidely,andthedoseisincreasingdaybyday.Asmallnumberofmedicalstaffgivepatientsalargeamountofpenicillinintravenously,especiallytheintravenousinfusionofmorethan8millionunits,andsomeofthemhaveusedthedrugseveraltimesadayandcontinuouslyforseveraldays.Thisnotonlycausestheconcentrationofpenicillininthebloodtoremainhigh,butalsomakestheconcentrationofpenicillininthecerebrospinalfluidgraduallyincrease.Whentheconcentrationinthecerebrospinalfluidis>8units/ml,itwillstimulatethebrainnervesandthenappearhyperreflexia,sensorydisturbances,hallucinations,Convulsions,comaandotherencephalopathysymptomscanalsocausetransientmentaldisorders,especiallythosewithrenalinsufficiency,theelderlyandchildrenaremorelikelytoinducethisdisease.

⒊Duetothedeclineofrenalfunctionandthedecreaseofplasmaalbumin,bloodconcentrationandcerebrospinalfluiddrugconcentrationincrease,resultingincentralnervoussystemtoxicity.Therefore,whenantibioticsareusedintheelderly,thedosageshouldbeadjustedaccordingtorenalfunction.Inordertopreventtheoccurrenceof"penicillinencephalopathy",thedosageofsuchdrugsshouldnotbetoolarge.Ifthediseaserequiresalargedosage,thedailydosageshouldbedividedinto3times~Give4times.Bytheway,manyantibiotics,suchascephalosporins,vancomycin,tetracycline,nalidixicacid,etc.,cancauseincreasedtoxicandsideeffectsduetodecreasedrenalfunctionandincreasedserumconcentration.Somedrugscanbeusedinreduceddoses,andsomearebestnottobeused,andotherantibioticsareusedinstead.

⒋Има много видове антибиотици, които могат да причинят увреждане на централната нервна система, като спеницилин, цефалоспорин, Тайненг, аминогликозиди, макролиди, хлорамфеникол, полимиксин Е, сулфонамиди, някои лекарства като аскинолони, противотуберкулозен изониазид и антивирусни лекарства (ацикловир, използване на канцеларски продукти и вирусологичен вирус) insymptoms.

Показания

Пицилин, използван за инфекции, причинени от чувствителни бактерии или патогени. Фарингит, тонзилит, скарлатина, ендокардит, еризипел, целулит и пуерперална треска, причинени от хемолитичен стрептокок. Пневмония, отит на средното ухо, менингит и бактериемия, причинени от пневмокок от.

1.PenicillinGhasagoodeffectonpharyngitis,scarletfever,cellulitis,septicarthritis,pneumonia,puerperalfeverandsepsiscausedbygroupAβ-hemolyticstreptococcus.Thedrugofchoice.Fortheabovesevereinfections,intravenousdripadministration4timesaday,eachtime1.2millionto1.6millionU.Thetreatmentofpharyngitisshouldbeadministeredforatleast10daystoensurethatthepathogenicbacteriaareeliminatedfromthepharynxtoavoidrheumaticfeverinthefuture.Acutepurulentmeningitis(meningitis)andendocarditiscausedbyStreptococcuspyogenesshouldbeadministeredintravenouslywithhigh-dosepenicillinG(10millionto20millionUperday).

2.Infectionscausedbyotherstreptococci:includingrespiratorytractinfectionscausedbygroupBβ-hemolyticstreptococcus,viridisstreptococcusandfaecalisstreptococcus,acutepurulentmeningitis(meningitis),heartInfectionssuchasendometritisandsepsis.StreptococcuspneumoniaeishighlysensitivetopenicillinG,andpenicillinGtreatmentisthefirstchoice.

3.Meningitiscausedbymeningococcusorothersensitivebacteria:PenicillinGdoesnoteasilypenetratethenormalblood-cerebrospinalfluidbarrierandentersthecerebrospinalfluidinasmallamount,butitispermeabilitywhenthemeningesaredamagedbyinflammationIncrease,sohigh-dosetreatmentiseffective.Thestartingdoseforadultsis10to20millionUperday,dividedinto4intravenousdrips.

4.GonorrhoeacausedbyNeisseriagonorrhoeae:NeisseriagonorrhoeaeissensitivetopenicillinG,butdrug-resistantbacteriahaveincreasedsignificantlyinrecentyears,andsomearehighlyresistant.Therefore,itisnecessarytodecidewhethertousepenicillinGaccordingtotheresultsofthesensitivitytest.Theamountoftreatmentshouldalsobedeterminedbasedonthedegreeofsensitivity.

5.SyphiliscausedbyTreponemapallidum:PenicillinGisstillthemaintreatmentdrug.Forsecondaryandtertiarysyphilisorseverecasesofthefirststage,especiallythosewithearlycentralnervoussystemsymptoms,high-dosepenicillinGshouldbeusedfortreatment,5to20millionUperday,intravenousdrip,3to4weeksoftreatmentStableefficacy.

6. Инфекции, причинени от грам-положителни бацили: Инфекциите, причинени от тетанус, дифтерия и антрацис, трябва да се лекуват с пеницилин G плюс антитоксин.

Употреба и дозировка

⒈Обичайна доза за възрастни:①Интрамускулно инжектиране,800 000~2 милиона на ден, приложено от 3 до 4 пъти;②Интравенозно капково, дневно от 2 до 10 милиона U, приложено в 2 до 4 дози.

⒉Обща доза за деца:①Интрамускулно инжектиране, 25 000 U/kg, веднъж на всеки 12 часа.②Интравенозно приложение, 50 000 до 200 000 U/kg дневно, разделено на 2 до 4 пъти.

⒊Доза за новородени: 50 000 U/kg веднъж, интрамускулно или интравенозно, веднъж на всеки 12 часа през първата седмица на раждането, > веднъж на всеки 8 часа през 7 дни, тежка инфекция на всеки 6 часа.

⒋Доза за недоносени бебета: 30 000 U/kg през първата седмица, веднъж на всеки 12 часа, веднъж на всеки 8 часа в рамките на 2 до 4 седмици и веднъж на всеки 6 часа след това.

Препарати и спецификации

1. Пеницилиннатрий за инжектиране: ①0,12 g (200 000 U); ②0,24 g (400 000 U); 1,6 милиона U; ⑥2,4 g (4 милиона U).

2.Калиев пеницилин за инжектиране:①0,125g (200 000U);②0,25g(400 000U);③0,5g(800 000U);④0,625g(1 милионU).

Bacterialresistance

StaphylococcusaureusPenicillinismostlikelytoproducedrugresistance.Therearethreemainmechanismsforbacterialresistancetopenicillins:

⒈Bacteriaproduceβ-lactamasetohydrolyzeandinactivatepenicillins

⒉Thetargetsiteofpenicillininbacteria-penicillinbindingproteinchanges

⒊Thepermeabilityofthecellwalltopenicillinsisreduced.

Thefirstmechanismisthemostcommonandthemostimportant.

Picillinantibioticshavegoodwatersolubility,andtheireliminationhalf-lifeismostlylessthan2hours.Theyaremainlyexcretedthroughthekidneys.Mostvarietiescanbeeliminatedbyhemodialysis.

AccordingtotheregulationsoftheChineseMinistryofHealth,useBeforepenicillinantibiotics,apenicillinskintestisrequired.Thosewithapositivereactionareprohibited.

Предпазни мерки

⒈Не смесвайте с алкални лекарства, когато се прилагат перорално или чрез инжектиране, за да избегнете разлагане и неуспех.

⒉Thisproductshouldnotbemixedintravenouslywithtetracyclinehydrochloride,kanamycin,polymyxinE,sulfadiazinesodium,adenosinetriphosphate,coenzymeA,etc.toavoidprecipitationorloweringtheeffect.

⒊Chloramphenicolandpenicillinaregenerallynotusedincombination,becausechloramphenicolisabacteriostaticagent,andpenicillinisabactericideinthebreedingperiod,thecombinedusecanaffecttheantibacterialactivityofpenicillinandreducetheeffect.However,thisissueisstillcontroversial.Opinionsdiffer,becausethecombinationofthetwohasagoodclinicaleffectongram-positiveandnegativebacteriamixedinfectionsandintracranialinfections.Thesolution,ifcombineduse,isrecommendedtousepenicillinfor2to3hoursbeforeusingchloramphenicol

⒋Becausetheproductcaninhibittheactivityofcertainliverenzymes,itcaninterferewiththebiotransformationoftolbutamide,phenytoinanddicoumarininthehumanbody,andcanenhancetolsicarbTheeffectofphenytoinsodiumcanenhancetheanticoagulanteffectofdicoumarinandwarfarin.

⒌Usewithcautionininfants,patientswithimpairedliverandkidneyfunction,usewithcautioninlate-pregnancywomen,andbreastfeedingNotforwomen.

Освен да направите тест на кожата, преди да приложите пеницилин, трябва да обърнете внимание и на следните точки:

⒈GotoformalmedicalcarewithrescueequipmentTheunitinjectspenicillin,incaseofanallergicreaction,timelyandeffectiverescuetreatmentcanbeobtained.Ifdizziness,palpitation,sweating,breathingdifficultiesandotherdiscomfortoccuratanytimeduringtheinjectionprocess,pleasetellthedoctorandnurseimmediately.

⒉Afterthepenicillininjection,observeinthehospitalforatleast20minutesbeforeleavingwithoutanydiscomfort.

⒊Don’tbeextremelyhungryPenicillinshouldbeusedatthesametimetopreventthebody'stolerancetothedrugfrombeingreducedwhenfasting,whichmayinduceadversereactionssuchasfainting.

⒋Thetwoinjectionsshouldnotbetooclosetoeachother,4-6hoursisbetter.Whenintravenouspenicillinisinstilled,thestartingspeedshouldnotbetoofast.Itisadvisablenottoexceed40dropsperminute.Observethatthereisnoadversereactionfor10-20minutesandthenadjusttheinfusionspeed.

⒌Ifthereisahistoryofpenicillininjectiononthesameday,dizziness,palpitation,sweating,difficultybreathingandotherdiscomfortathome,youshouldbesenttothehospitalfordiagnosisandtreatmentintime.

Седем точки спрете да обръщате внимание на ампицилин:

Ampicillin(includingampicillincontainingampicillin,etc.)isthefastestdecomposingandallergicofpenicillindrugsTheonewiththehighestreactionrate,especiallyintheacidicenvironmentandhighbloodconcentration,ismorepronetoallergicdrugeruptionandanaphylacticshockcausedbyampicillindecompositionproductsandstacks,andevenlife-threatening.Whenusingampicillinclinically,notonlydoaskintest,butalsopayattentiontothefollowingpoints:First,anegativeskintestdoesnotmeanthatyouarenotallergic.Allergicreactionstoampicillinaremostlydelayed,andallergicdrugeruptionscanoccurafterseveraldaysofcontinuousmedication,causinganaphylacticshock.Forallergicdrugeruptions,theuseofastemizole,diphenhydramine,anddexamethasonecanberesolvedafterstoppingthedrug.Suddendyspnea,chillsandfever,decreasedbloodpressure,increasedheartrateandothersymptomsshouldbestoppedimmediately,givenoxygen,andrescuedwithepinephrine,dexamethasone,calciumgluconateandotherdrugs.

Second,itissuitableforshort-termuseandavoidlong-termlarge-scaleadministration,soastoavoidthecontinuousincreaseofbloodconcentration,leadingtotheformationandaccumulationofallergensandcausingallergicreactions.

Thirdly,itshouldbeinjectedintravenouslyafterbeingfullydissolvedinasufficientamountofnormalsaline.Generallyspeaking,4gramsofampicillinneedstobedissolvedinabout300mlofnormalsaline(0.9%sodiumchlorideinjection).Itmustnotbedissolvedinsugar,especiallyhypertonicsugar(glucoseinjectionwithaconcentrationgreaterthan5%)forintravenousdrip.Becausesugarisacidic,itcannotonlyreducetheantibacterialandbactericidalabilityofampicillin,butalsopromoteself-decompositionandincreasethechanceofsensitization.

Fourth,patientswithgout,uremia,diabeticketoacidosisandlacticacidosisshoulduseaslittleornoampicillinaspossible.Thereasonisalsothatampicillincanpromoteself-decompositioninacidicenvironmentandincreasethepossibilityofsensitization.

Пето, самите пациенти са алергични и трябва да се избягват.

Sixth,itisusuallyadministeredintravenously,whichshouldbeslowratherthanfast,andintravenousdripatarateofnomorethan60dropsperminute,soastopreventthebloodconcentrationfromincreasingtoofastandincreasingthepossibilityofdecompositionandallergies.

Seventh,beforeusing,youshouldfindtheexactevidenceofinfectionbypathogenicbacteriathataresensitivetothisdrug,andavoidblindlymisusingit,soasnottocausefloraimbalanceandmoldinfectionandincreasethedifficultyoftreatment.

Противопоказания

За тези, които са алергични към топеницилиноротерпеницилинови лекарства.

Beforemedication,thepatientshouldbeaskedwhetherthereisanyhistoryofallergy.Forthosewhohavenotusedpenicillinfor24hours,anintradermalsensitivitytestshouldbeperformed.Thosewithapositivetestresultshouldbedisabled.Peoplewhoareallergictopenicillinorotherpenicillindrugs,andthosewithallergicdiseasesandallergicconditionsshouldnotbeused.

Лекарствени взаимодействия

(1) Комбинираната употреба с пробенецид, аспирин, индометацин и сулфатни лекарства може да намали отделянето на пеницилинови лекарства и да направи пеницилин в кръвта.

Probenecidcaninhibitrenaltubularsecretion,thusprolongingthemaintenancetimeofpenicillinbloodconcentration,andhasasynergisticeffectonpenicillin.

(2)Combinedusewithtetracyclines,erythromycin,chloramphenicolandsulfonamidesandotherantibacterialdrugsmayreducetheantibacterialeffectofthisproduct.

Picillinshaveantagonisticeffectswithtetracycline,chloramphenicol,macrolidesandotherantibacterialdrugs.Becausepenicillinisabactericidaldrugduringthereproductionperiod,undertheactionofbacteriostaticdrugs,bacterialreproductionisinhibited,whichmaymaketheeffectofpenicillindrugsinsufficient.

(3) Комбинираната употреба с warfarin може да засили антикоагулантния ефект.

(4) Приемането на контрацептиви по едно и също време може да повлияе на контрацептивния ефект.

(5)Penicillinsandaminoglycosideantibioticshaveasynergisticeffect,buthigh-dosepenicillinGorothersemi-syntheticpenicillinscanreducetheactivityofaminoglycosides.

Стандарти за лекарства

Информация за цените на дребно на национални основни лекарства, свързани с пеницилин

Описание:

⒈Продуктите, маркирани с "*" в колоната за бележки на таблицата, са представителни продукти.

⒉Inthetable,therepresentativedosageformspecificationismarkedwith"△"intheremarkscolumn,andthepriceoftherepresentativedosageformspecificationandrelatedspecificationswithaclearpricedifferencerelationshipisatemporaryprice.

⒌Doseforpatientswithimpairedrenalfunction:Whentheglomerularfiltrationrate(GFR)is10-15ml/min,thedosingintervalisextendedfrom8hoursto8-12hoursorthedoseisreducedby25%.WhenGFRislessthan10ml/min,theintermittentadministrationis12-18hoursorthedoseisreducedto25%-50%ofthenormaldose.Generallyspeaking,patientswithmildtomoderaterenaldamageshoulduseconventionaldoseswithoutreducingthedose.Forsevererenaldamage,adjustthedoseorextendtheadministrationtime.