penisilliini

Yhdisteen esittely

Perustiedot

Kiinalainen nimi:penisilliini

Chinesealias:penisilliini

Englanninkielinen nimi:bentsyylipenisilliin

Englishalias:cilloral;pradupen;Ursopen;bentsyylipenisilliini;kosmopen;

CASNumero: 61-33-6

Molekyylikaava: C₁₆H₁₈N₂O₄S

Molekyylipaino: 334,39000

Tarkka massa: 334.09900

PSA:112.01000

LokiP:1.18960

Fysikaaliset ja kemialliset ominaisuudet

Tiheys: 1,42 g/cm³

Kiehumispiste: 663,3 ºCat760 mmHg

Leimahduspiste: 355 ºC

Taitekerroin: 1,655

Säilytysolosuhteet: tuuletettu, matala lämpötila ja kuiva

Turvallisuustiedot

Tullikoodi:32041900

WGKSaksa:2

Vaaraluokkakoodi: R42/43

Turvaohjeet: S36/37

RTECSnumber:XH9700000

Vaarallinen tavaramerkki: 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.

Vuonna 1938 saksalainen kemisti ErnstChannsawFlemingin paperinappitaittokirjoja ja aloitti puhdistuskokeet.

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".

Vuonna 1945 brittikemisti D.C.Hodgkin käytti röntgendiffraktiota penisilliinin hemomolekyylirakenteen määrittämiseen.

5.9.1944Kiinan ensimmäinen erä kotimaisesti tuotettuja penisilliineitä syntyi, paljastaen Kiinan antibiootituotannon historian.Vuoden 2001 lopulla Kiinan penisilliinien vuosituotanto laskettiin 60-prosenttisesti vuoden 2001 lopputuloksesta.

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.

Ominaisuuksiensa mukaan se voidaan jakaa seuraaviin:

PenisilliiniG:kuten penisilliiniGnatrium,penisilliiniGnatrium,pitkävaikutteinen sillinpenisilliiniG,peilliiniG,penisilliini,penisilliini,penisilliininatrium,bentsyylipenisilliininatrium,penisilliinikalium,bentsyylipenisilliinipotkulium.

Penisilliini V:(alias:fenoksimetyylipenisilliini, 6-fenoksiasetamidopenisilliinihappo)kuten penisilliiniVkalium (mukaan lukien erilaiset annosmuodot)).

Entsyymiresistentti penisilliini:kuten kasoksasilliini (XinqingII), kloratsolepenisilliini jne.

Ampisilliini:kuten sampisilliini, amoksisilliini jne.

Anti-pseudomonaspenisilliini:kuten karbenisilliini, piperasilliini, tikarsilliini jne.

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

Metisilliinit: kuten kastamoksisilliini jne.

Valmistusmenetelmä

Luonnollisen penisilliinin ja puolisynteettisen penisilliinin valmistusmenetelmä on täysin erilainen.

[Luonnollinen penisilliini]

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).

[Puolisynteettinen penisilliini]

Using6APAasanintermediateandavarietyofchemicallysynthesizedorganicacidsforacylationreaction,varioustypesofSemi-syntheticpenicillin.

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

[Penisilliinin pitoisuusmenetelmä]

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. Penisilliiniä ei voida yhdistää samankaltaisten antibioottien kanssa

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

2. Penisilliiniä ei voida käyttää yhdessä sulfalääkkeiden ja tetrasykliinien kanssa

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

3. Penisilliiniä ei voida sekoittaa aminoglykosidilääkkeisiin infuusiolääkkeisiin

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.

⒎Keflotiini,linkomysiini,tetrasykliini,vankomysiini,erytromysiinietyylisukkinaatti,amfoterisiiniB,norepinefriini,metahydroksyyliamiini,fenytoinatrium,hydroksihydrokloridi on lisätty muut huumeet.

⒏Penisilliini voi tehostaa varfariinin vaikutusta.

⒐Aftertheproductismixedwithaminoglycosideantibiotics,theantibacterialactivityofthetwodrugsissignificantlyweakened,sothetwodrugscannotbeadministeredinthesamecontainer.

Lääkemyrkyllisyys

Penisilliiniallergia

Se imeytyynopeasti suunllisen annon jälkeen, noin 75 %～ 90 % voi imeytyä maha-suolikanavasta. Ruoalla ei ole merkittävää vaikutusta lääkkeiden imeytymiseen.Sen proteiininsitoutumisaste on 17%-20 %.20%. ism,kuuden tunnin sisällä 46-68 % annoksesta erittyy virtsaan prototyyppilääkkeenä,ja osa lääkkeistä erittyy sappiteiden kautta. Näitä potilaiden puoliintumisaikaa, joilla on vakavia vajaatoimintaa, voidaan pidentää 7 tuntiin. Seerumidialyysi voi poistaa penisilliinin, mutta vatsakalvodialyysillä ei ole vaikutusta tuotteen poistamiseen.

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.

Periaatteena kaatuminen

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.Eläinlääkintäkliiniset allergiat ovat yleensä lieviä, ilmenevät pääasiassa hikoiluna, jännittyneisyydessä, levottomuudessa, lihasvärinä, hengenahdistus, nopea sydämen syke, epävakaa seisominen, joskus väreet, silmäluomen ja kasvojen turvotus, ulvaan ja peräsuolen turvotus ja septinen selluliitti.

[Syy]

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

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

[Ensimmäiset toimenpiteet]

⒈Lääkitys on lopetettava välittömästi, makuulle ja pelastaminen paikalla, pää alas ja jalat.

⒉Ihonalainen injektio 0,1 % epinefriinihydrokloridia 0,5 ～1 ml, lapset voivat vähentää, ja sitten ihonalainen injektio 0,5 ml puolen tunnin välein, riskijaksoon asti, lisää tarvittaessa kortikosteroideja tai antihistamiinia.

⒊Patientswithcardiacarrestshouldundergocardiacchestcompressionorintracardiacinjectionof0.1%epinephrinehydrochloride1ml.

⒋Oxygeninhalation,mouth-to-mouthartificialrespirationwhenbreathingisinhibited,andintramuscularinjectionofnicotinicacidorlobelineandotherrespiratorystimulants.

Laryngealedemaaffectsthetracheotomyduringbreathing.

⒌Käytä hydrokortisonia 200 mg, ordeksametasonia 5-10 mg 50 % glukoosia 40 ml laskimoon tai 5-10 % glukoosia 500 ml laskimoon.

⒍Vasoaktiivisia lääkkeitä, kuten dopamiinia, alamiinia jne. voidaan käyttää sairaudentarpeen mukaan.

⒎Correctacidosisandtheapplicationofhistaminedrugs.

⒏Pidä lämpimänä, estä vilustuminen, pidä kirjaa ja älä liiku.

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

⒑MoxamoxibustioncanbeusedatacupointssuchasNeiguan,Hegu,Yongquan,Guanyuan,andZhongwan.

Penicinenkefalopatia

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.

Penisilliinillä ja muilla laaja-alaisten rumpenisilliinien puoliintumisaika on pidempi?Esimerkiksi suonensisäisellä penisilliinillä on puoliintumisaika0,55in-25-vuotiaan-0-7-0-7-0-7-0-ikä-0. vuotiaat;dikloksasilliini alle 30-vuotiaatThehalf-lifeis0 .88tuntia,jatulee3,97tuntia yli 65-vuotiaille;amoksisilliinin puoliintumisaika1-1,5 tuntia nuorille ja 2,67 tuntia89-vuotiaille.Samaan aikaan. Kun vanhukset käyttävät suuria annoksia penisilliinistä ja karbenisilliinistä, neurologisia ja topsykiatrisia oireita voi ilmetä, kuten hyperrefleksia, havaintohäiriöt, hallusinaatiot, kouristukset .,sekä tilapäiset mielenterveyden häiriöt,proneto"penisillinenkefalopatia".

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.

Koomastit ovat olleet pitkään ja niillä voi olla vakavia jälkitauteja. Näitä oireita ovat tylsyys, sokeus, kuurous, halvaus jne. Pieni määrä potilaita voi johtua vakavasta sairaudesta.

[Hoito]

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.

[Varotoimet]

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.

⒋On olemassa monenlaisia ​​antibiootteja, jotka voivat aiheuttaa vaurioita keskushermostolle, kuten penisilliini, kefalosporiini, taineng, aminoglykosidit, makrolidit, kloramfenikoli, polymyksiiniE, sulfonamidit, jotkin lääkkeet, kuten esimerkiksi kinolonit, syöpäsairaudet ja tuberkuloosin vastaiset lääkkeet mptoms.

Indikaatiot

Picilliiniä käytetään herkkien bakteerien tai patogeenien aiheuttamiin infektioihin.Nielutulehdus, nielurisatulehdus, tulirokko, endokardiitti, erysipelas, selluliitti ja synnytyskuume, jonka aiheuttavat hemolyyttinen streptokokki. Keuhkokuume, tulehdus.

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.Grampositiivisten basillien aiheuttamat infektiot:Jäykkäkouristus, kurkkumätä ja pernakirkko tulisi hoitaa penisilliinillä Gplusantitoksiinilla. Penisilliä käytetään pääasiassa seuraavien sairauksien hoidossa:(1)Syfilis,pymasi,solutulehdus,kivutauti.

Käyttö ja annostelu

⒈Tavallinen annos aikuisille:①Lihaksensisäinen injektio, 800 000 ~ 2 miljoonaa joka päivä, annetaan 3-4 kertaa;②Suonensisäinen tiputus, päivittäin 2-10 miljoonaa U, annetaan 2-4 annoksena.

⒉Yleinen annostus lapsille:①Lihaksensisäinen injektio, 25 000 U/kg, kerran 12 tunnin välein.②Suonensisäinen anto, 50 000 - 200 000 U/kg päivässä, jaettuna 2 - 4 kertaan.

⒊Annos vastasyntyneille: 50 000 U/kg, lihakseen tai suonensisäisesti, kerran 12 tunnin välein ensimmäisen syntymäviikon aikana, >kerran 8 tunnin välein 7 päivässä, vakava infektio 6 tunnin välein.

⒋Annos ennalta syntyneille imeväisille: 30 000 U/kg ensimmäisellä viikolla, kerran 12 tunnin välein, kerran 8 tunnin välein 2–4 viikossa ja kerran 6 tunnin välein sen jälkeen.

Valmisteet ja tekniset tiedot

1.Penisilliininatrium injektioon:①0,12g(200 000U);②0,24g(400 000U);③0,48g(800 000U)；⑑0,6 g (61 g(0,6 g); 1,6 miljoonaa U; ⑥ 2,4 g (4 miljoonaa U).

2.Penisilliinikalium injektioon:①0,125g (200 000U);②0,25g (400 000U);③0,5g (800000U);④0,625g (1 miljoonaa U).

Bacterialresistance

StaphylococcusaureusPenicillinismostlikelytoproducedrugresistance.Therearethreemainmechanismsforbacterialresistancetopenicillins:

⒈Bacteriaproduceβ-lactamasetohydrolyzeandinactivatepenicillins

⒉Thetargetsiteofpenicillininbacteria-penicillinbindingproteinchanges

⒊Thepermeabilityofthecellwalltopenicillinsisreduced.

Thefirstmechanismisthemostcommonandthemostimportant.

Picillinantibioticshavegoodwatersolubility,andtheireliminationhalf-lifeismostlylessthan2hours.Theyaremainlyexcretedthroughthekidneys.Mostvarietiescanbeeliminatedbyhemodialysis.

AccordingtotheregulationsoftheChineseMinistryofHealth,useBeforepenicillinantibiotics,apenicillinskintestisrequired.Thosewithapositivereactionareprohibited.

Varotoimet

⒈Älä sekoita alkalisten lääkkeiden kanssa, kun niitä annetaan suun kautta tai ruiskeena, jotta vältytään hajoamisesta ja epäonnistumisesta.

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.

Sen lisäksi, että teet testin ennen penisilliinin levittämistä, sinun tulee kiinnittää huomiota seuraaviin seikkoihin:

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.

Seitsemän pistettä, jotka kiinnittävät huomiota ampisilliiniin:

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.

Viidenneksi potilaat itse ovat allergisia ja niitä tulisi välttää.

Sixth,itisusuallyadministeredintravenously,whichshouldbeslowratherthanfast,andintravenousdripatarateofnomorethan60dropsperminute,soastopreventthebloodconcentrationfromincreasingtoofastandincreasingthepossibilityofdecompositionandallergies.

Seventh,beforeusing,youshouldfindtheexactevidenceofinfectionbypathogenicbacteriathataresensitivetothisdrug,andavoidblindlymisusingit,soasnottocausefloraimbalanceandmoldinfectionandincreasethedifficultyoftreatment.

Vasta-aiheet

Niille, jotka ovat allergisia ktopenisilliinia tai muita penisillilääkkeitä.

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

Lääkeinteraktiot

(1)Yhteiskäyttö probenesidin, aspiriinin, indometasiinin ja sulflääkkeiden kanssa voi vähentää penisillilääkkeiden erittymistä ja aiheuttaa penisilliinin verta.

Probenecidcaninhibitrenaltubularsecretion,thusprolongingthemaintenancetimeofpenicillinbloodconcentration,andhasasynergisticeffectonpenicillin.

(2)Combinedusewithtetracyclines,erythromycin,chloramphenicolandsulfonamidesandotherantibacterialdrugsmayreducetheantibacterialeffectofthisproduct.

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

(3)Yhdistetty käyttö sodan kanssa voi tehostaa antikoagulanttivaikutusta.

(4)Ehkäisyvälineiden ottaminen samaan aikaan voi vaikuttaa ehkäisytehoon.

(5)Penicillinsandaminoglycosideantibioticshaveasynergisticeffect,buthigh-dosepenicillinGorothersemi-syntheticpenicillinscanreducetheactivityofaminoglycosides.

Lääkestandardit

Penisilliiniin liittyvien kansallisten välttämättömien lääkkeiden vähittäismyyntihintatiedot

Kuvaus:

⒈Tuotteet, jotka on merkitty"*"merkkisarakkeessa,ovat edustavia tuotteita.

⒉Inthetable,therepresentativedosageformspecificationismarkedwith"△"intheremarkscolumn,andthepriceoftherepresentativedosageformspecificationandrelatedspecificationswithaclearpricedifferencerelationshipisatemporaryprice.

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