抗高血压药_整理英文版课件

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Antihypertensivedrugshypertension◼Meanarterialbloodpressureishigherthanthenormalrange,inthecaseofnottakingbloodpressuredrugs:Systolicbloodpressure

≥18.7kPa(140mmHg)and(or)Diastolicbloodpressure≥12.0kPa(90mmHg)Dividedintoprimaryhypertension(90%~95%)Andsec

ondaryhypertensioncomplications◼Heartfailure◼Coronaryheartdisease(CHD)◼Cerebrovascularaccident◼RenalfailureAntihypertensivedrugsReasonab

leapplicationofantihypertensivedrugsControlofbloodpressureDelaytheformationanddevelopmentofatherosclerosisReducethecomplic

ationssuchasbrain,heartandkidneyReducethemortalityrate,prolonglifeBloodpressure-Thefactorsinfluencingbloodpressure:◼Cardiac

output:heartrate,myocardialcontractionforce,changeofbloodvolume,etc.;◼Peripheralresistance:thelengthofthebloodvesselsandbloodviscos

ity,bloodvessels,radius,etc.-Nerve-fluidsystemonbloodpressureregulation。maincentreganglionVascularsmoothmuscleclon

idine-methyldopaEplerenonemecamylamineReserpineguanethidinepropranolol1prazosin1labetalolhydral

azinesodiumnitroprussidenifedipineminoxidil1.Nervousregulation:thesympatheticnervoussystemPeripheralneurot

ransmitterreleaseThepostsynapticmembranereceptorSecond,humoralregulation:renin–angiotensinaldosteronesystemKidne

yadjacentballBesidethemachine-RblockersreninAngiotensinoriginalangiotensinⅠinvertaseACEIangiotensinⅡSmallart

erycontractionlosartanAldosteronesecretionWatersodiumretentiondiuretic(thiazides)Classification◼Diuretic◼

Thesympatheticnervousdepressants◼(1)centralbloodpressuremedication◼(2)theganglionblock◼(3)noradrenalinecannervee

ndingsblock◼(4)theadrenalinereceptorblockers◼Affecttherenin-angiotensinsystemmedicineAgleamofantihypert

ensives:diuretic,calciumantagonistmedicine,betareceptorblockersandACEIDiuretic◼Onthebasisof(aline)bloodpressuremedi

cation◼Effectinthethiazidediureticismostcommonlyused,antihypertensiveeffectismild,persistent,long-termapplicationofnosignificantresistance◼Features

:◼Antihypertensiveeffectisweak,byanaverageof10%◼2~3weeksafterthemajorityofpatientsinmedicalwork◼Canbeusedforvarioushighbloodpressur

e(basicbloodpressuremedication)◼Mild-alone,mediumandsevere-share◼Canmaketheelderlyhypertensionpatientscomplicatedwiths

troke,theincidenceofleftheartfailureandmortalityisleftHydrochlorothiazide◼Earlyantihypertensivemechanism◼Withsodiumdiuresis,reducetheextracellula

rfluidandbloodvolume◼Long-termantihypertensivemechanism◼DiureticrowsodiumtoNa+leftaorticsmoothmusclecell,cellNa+/Ca2+exchangeleft-

>intracellularCa2+left,reducevascularsmoothmuscleofnorepinephrine(NE)reactivitydisadvantages:-↓BloodK+、Na+、Mg2+-↑Bloodtotalcholesterol,triglyce

ride,lowdensitylipoproteincholesterol(hdl-c)-↑Blooduricacid-↑Bloodrenin-↓Glucosetolerance(disabled)fordiabetespatientsE

ffectivediuretic(furosemide)usedinhypertensivecrisisandpoorassociatedwithchronicrenalhypertensionpatients.◼H

ypertensivecrisis◼Patientswithhighbloodpressureintheshortterm,thebloodpressureincreasedsignificantly

,andappearhaveaheadache,beagitated,palpitation,sweating,nausea,vomiting,orpaleflush,blurredvisionandothersigns.◼Mechanism:hyperthyroidism

andcirculatingcatecholaminesincreasedsympatheticnervousactivityClinicalapplication◼Agleamofmedication◼Appl

icationofthetreatmentformildhypertensionseparately◼Withotherantihypertensivedrugtreatment,severehypertensionEf

fectofdiuresismedicineofcompoundpreparationswithotherdrugs◼Compoundantihypertensiontablet:giveupping,hydral

azine,hydrochlorothiazide◼Compoundapocynumtablet:guanidineborganism,hydralazine,hydrochlorothiazide◼Janechrysanthemumanti

hypertensiontablet:clonidine,hydrochlorothiazide◼Compoundcaptopriltablets,enalaprilandhydrochlorothiazide◼Constantdroppingpills:clonidine,hydra

lazine,hydrochlorothiazideCalciumantagonistmedicineBlockLvoltagedependentcalciumchannel->leftintracellularCa

2+diastolicsmallarteryNifedipinegroup,horizon,lacidipineflat,amlodipineNifedipine【Step-downcharacteristics】1Buckdegreewaspositivelyc

orrelatedwiththeoriginalhighbloodpressure,withnormalbloodpressurehasnoobviousantihypertensiveeffect;2Oralabsorptionisgood,workfas

t:sublingualadministering1-5minuteswork-inthetreatmentofvariantanginapectoris,hypertensivecrisis.Ora

l30to60minuteswork-treatmentofmildandmoderatehypertension;3Cancausereflectiveheartrate↑—shareReceptorblockers.Clinicalapplication◼Light,me

diumandseverehypertensiontreatmentNitrendipine◼SelectivelyACTSontheperipheralvascular,blockingitsinternalflowo

fcalciumions,relaxingsmoothmuscle,thedilatebloodvesselsandstep-down◼Warmandlastingantihypertensiveeffect,applicabletovariou

stypesofhighbloodpressureLacidipine◼Isapotentcalciumantagonists,significantlyandtheeffectofselectivecalciumionchannelsinvasculars

moothmuscle.Itsmainroleistoexpandperipheralartery,reduceperipheralvascularresistanceandtolowerbloodpressure◼Resistancetoatherosclerosis◼Us

edformildandmoderatehypertension◼Nameofcommodity:lacidipine◼Amlodipine◼Moregentle,smootheffectlasting,

convenienceofonce-dailydosage,24hoursofstabilitycontrolofhighbloodpressureandanginapectoris,goodsafetyandtolerability◼Similardrugs,onlyitcanbe

usedbypatientswithcongestiveheartfailuresafety◼AlsohastheroleofatherosclerosisAdrenalinereceptorblockers◼α1Receptorblockers:prazosin、ter

azosin、doxazosin◼βReceptorblockers:prapranolol、atenolol、labetalol、carbedilolMechanismofaction◼Nonselec

tivebetareceptorblockers,mostlyrelatedwiththebetablocker:◼Heart:myocardialcontractionforceisabate,slowheartrate,ca

rdiacoutputdecreases◼Kidney:reducereninsecretion,inhibitRASonbloodpressureregulation◼Thesympatheticnerveendingspr

esynapticmembrane:inhibitionofpositivefeedback,NAsecretiondecline◼Central(hypothalamusandmedullaoblongat

a):excitatoryneuronactivityisabate,peripheralsympatheticnervetensionby,vascularresistancedecreased◼Incre

asethetopringelementsynthesisClinicalapplication◼Suitableforvarioushighbloodpressure◼Withhighcardiacou

tputorplasmareninlevelshasgoodeffectonthehighsideofhypertensivepatients,especiallysuitableforhypertensivepatientswithcoronaryheartdisease,cereb

rovasculardisease◼Diureticorpoolingvasodilatorscanenhancecurativeeffectatenolol◼Selectivebeta1receptorblockers,lackofinternaltothesympatheti

cactivity◼Oralisusedtotreatvariousdegreeofhighbloodpressure,antihypertensiveeffectalongerdurationlabetalol◼α、βReceptorblockers◼Applicab

letovariousdegreesofhypertensionandhypertensiveemergency,gestationalhypertension,pheochromocytoma,highbloodpressurewhenanesth

esiaorsurgerycarvedilol)◼α、βReceptorblockers◼Usedinthetreatmentofmildandmoderatehypertensionwithrenalinsufficiency,diabetes,highbloodpressurepatien

tsReninangiotensinsystemdepressantsACEI:Captopriletc.AT1-resistance:Chlorinesand,valsartan,etc【Antihypertensivemechanism】1.AngI

IGenerateandfunction。-Arteriovenousdiastolic→Peripheralresistance↓→Bloodpressure↓;-Blockthereleaseofaldosteronewatersodiumretention;2.Inhibiti

onofslowexcitationpeptidedegradation↓Slowexcitationpeptideconcentrationsintheblood↑:produceNO、PG2Etc.→血管扩张→血压↓An

giotensinconvertingenzymeinhibitorsACEIcaptopril(Asulfhydrylpropionicacidpulp)【Functioncharacteristics】◼1orallyactive,workfast,

antihypertensiveeffectofmediumstrong;◼2withoutreflectiveheartrate,long-termusewithoutresistance,noteasytocausetheelectrolytedisorder

s;◼Threepairsofrenalhypertensiveeffectisgood,cantreatrefractoryheartfailure【application】Eachperiodhighbloodpressure.Importantfirst-linedrugs.E

speciallysuitableforcomplicatedwithdiabetesandinsulinresistanceandleftventricularhypertrophy,heartfailure,acutemyocardialinfarctionpatientswithh

ighbloodpressureAngiotensinⅡreceptorblockersARBAT1receptor:vascularsmoothmuscle,cardiacmuscle,brain,kidne

yandsecretionofaldosteroneAdrenalzonacells-hasregulatingeffecttothestabilityofthecardiovascularfunction.losartan【Antihyp

ertensivemechanism】SelectiveblockingAT1receptor:blockingangiotensinⅡmediatedbloodvesselsShrinkage,aldosteronereleaseandpro

motevascularsmoothmuscleproliferationandeffect→Peripheralresistance↓Promotinguricacidexcretion,inhibitingrenaltubuleofu

ricacidabsorption,short【Clinicalapplicationof】EachperiodhighbloodpressureStep-downfeatures:1.Theoralworkfast2.Theroletomaintainforalongtime:24hs

moothstep-down,3~6weeksformaximumeffect【sideeffect】relativelylessACEI:Attractedlessdrycoughandangioneur

oticoedema;Butstillcancauselowbloodpressureandhighpotassium.Forpatientswithpregnancy.Promotinguricacidexcretion,inhibitingrenaltubul

eofuricacidabsorption,shortPharmacologicaleffects◼Diastolicsmallarterysmoothmuscle,reducetheperipheralvascularresistan

ce,lowerbloodpressure◼Withheartrateslows,decreasedcardiacoutput◼Inhibitthesecretionofgastrointestinaltractandmovementandtheprot

ectionofgastricmucosa◼Buckwithsedation◼Reduceintraocularpressure,donotaffectthepupilandtheadjustmentofthelensPharmacolog

icalactionandmechanism◼ActivateI1-imidazolinereceptor,Maketheperipheralsympatheticactivitydecline,vasodilation,blo

odpressuredrops◼Theexcitedcentralpostsynapticmembranereceptoralpha2◼Lowerlevelsofplasmareninandaldoste

rone◼Inhibitthesecretionofgastrointestinaltractandmovementandtheprotectionofgastricmucosa◼Staticnoteclonidinecanproduceboosterforashortperi

odoftime(associatedwithperipheralalpha2receptorexcited),followedbyalongperiodoftimethestep-down(centralrole).Oralwithth

ecentralroleofthedominant,theboostereffectisnotobviousClonidine◼Processinthebody◼Absorption:oralabsorption◼Distribution:eas

ythroughthebloodbrainbarrier,plasmaproteincombinedrateof30%◼Metabolism:50%inintrahepaticmetabolism◼Discharg

e:metabolicproductandprototypebyrenalexcretionClinicalapplication◼First-linetreatmentinvalidmoderately

highbloodpressure,withthiazidediureticorotherantihypertensiveagentssharecanimprovethecurativeeffect◼Renalhypertension◼Patientsw

ithhighbloodpressureofpepticulcer◼Primaryopen-angleglaucomaAdversereactions◼Drymouth,sleepiness,constipation,

impotence,canhappenoccasionallybradycardia◼Watersodiumretention◼Drugwithdrawalsyndrome:along-termdrugwithdrawalmaysuddenlyappearhaveahead

ache,tremor,abdominalpain,sweating,heartpalpitationsandbloodpressuresurge.Andlong-termmedicationmadethealpha2weeksthepresynapt

icmembranereceptorsensitivity,negativefeedbackeffectisreduced,suddenwithdrawal,increasedsympatheticnerv

ousfunctionisassociatedwithincreasedNErelease.Recoveryformedicineoralphareceptorblockers(e.g.,phentolam

ine)canalleviate.WithdrawalshouldbegraduallyreducedTheothercentralbloodpressuremedication◼methyldopa◼Amedium

tostrongstep-down,cardiovascularandoutput,lessinfluencerenalbloodflow◼Suitableforrenalhypertensionandmoderatehypertensiv

epatientswithpoorkidneyfunction,oftenwiththiazidediureticshare◼moxonidine◼ForIlreceptoraffinityishigh,andt

hereceptorisstrong,biologicalt1/2longer,onceadaydosing◼Suitableforpatientswithmildandmoderatehypertension◼Onthecentralandperipheral

alpha2receptorfunctionisweak,thecalm,drymouthgreatlyreduceadversereactionsVasodilationmedicine◼Directlytorelaxvascularsmoothmuscle,de

creaseperipheralresistanceandbloodpressuretodrop◼Long-termuseantihypertensivevasodilatorshasthefollowingdisadvan

tages◼Cantheexcitedsympatheticnerve,reflectiveincreasecardiacoutput,heartratespeedup◼Increaseofreninandaldosteronesecretion,leadingt

owaterandsodiumretention◼Alongtimewitheasytolerance◼Withadiureticoradrenalinereceptorblockerssharecanenhancecurativeeffect,reduceadversereactionsS

odiumnitroprusside◼AntihypertensiveeffectsassociatedwithanincreasedNO-GC-cGMP,candilatebloodvesselsandinhibitplateletaggregation◼Ofarteriolesandvenu

lesvascularsmoothmusclewerediastolicfunction,antihypertensiveeffectstrong,rapidandshort◼Mainlyusedinthetreatmentofhyp

ertensivecrisis.Alsousedincongestiveheartfailure,acutemyocardialinfarctionandcontrollinghypertensionduringanesthesia◼Becauseo

fexcessivestep-downcancausenausea,vomiting,sweating,restlessness,palpitationsandheadacheGanglionbloc

kmedicinemecamylamine【Functioncharacteristics】1.Antihypertensiveeffectstrong,quickly;2.Hasinhibitoryeffectonbothsympatheticandparasymp

athetic,adversereactions,andtheheavier,orthostatichypotension;Theparasympatheticganglionblocksymptoms.3.Hypertensivecrisis

.Prazosin–Processinthebody◼Absorption:goodoralabsorption,firsteliminatetheobvious,bioavailabilityof60%◼Distribution

:thecombinationofplasmaproteinratewas97%◼Metabolism:livermetabolism◼Discharge:mostbileexcretion,byasmallnumberofurine

Pharmacologicaleffectsandmechanismofaction◼Alpha1receptorsonpostsynapticmembraneofvascularsmoothmusclearehighlyselectiveblockingeffect◼Step-

downfeatures:◼Amediumtostrongantihypertensiveeffect◼Don'taffectkidneyfunction,improvethelevelofrenin◼Long-termusecanimpr

ovelipidmetabolism◼Block1receptoralpha,relievedysuriaprostatepatientsClinicalapplication◼Canbeseparatelyusedtreatme

ntofmildandmoderatehypertension◼Forelderlypatientswithhypertensioncombinedprostatichypertrophy,canimprovethesymptomsofdysuria◼Severehyp

ertensionsharediureticandbetareceptorblockerscanenhancestep-downeffectAdversereactions◼Firstagentphenomenon:somepatientsforth

efirsttime0.51hourafterthetreatmentcanappearorthostatichypotension,dizziness,sweating,heartpalpitation

sandreaction◼Long-termusecancausewatersodiumretention,diuresismedicinecanmaintainitsantihypertensiveeffectreserpine【Antihyperten

sivemechanism】ReducecatecholaminetransmitterinthestorageandreleaseAndthesympatheticnerveendings(peri

pheralandcentraladrenergic)vesiclemembraneAminepumpcombination,catecholamineneurotransmitter(NA,5-HT)synthesis,storag

e,reuptakeleft,thedepletionoftheneurotransmitters,thesympatheticnerveconductionleft-vasodilation,BPlef

tCentralinhibition,composed,stableeffect.PhenylephrinecannerveendingsblockerFeatures:effectiveslow,gentleandlasting【Cli

nicalapplication】1light,moderatetohighbloodpressure,ithasbeenlessusedalone2manicpsychosis【Adversereactions】1Theparasympatheticnerveexcitemen

tsymptoms:nausea,vomiting,intestinalcrampsanddiarrhea,pepticulcer2Centralinhibition:calm,lethargy,de

pression。PotassiumchannelsareopenPromotetheKATPopen→Thecellmembranehyperpolarization→TheinflowCa↓Thenewconcept

ofhighbloodpressuremedication1.Theeffectivetreatmentandlifelongtreatment2.Protecttargetorgans3.Smoothstep-down4.CombinationtherapyThemainpoi

nts◼1.Diuretic,pharmacologicalaction,mechanismofactionandclinicalapplication◼2.Thebetablockerdrugs:ant

ihypertensiveeffectandmechanismofaction◼3.TheangiotensinIconvertingenzymeinhibitionofmedicine◼(1)thepha

rmacologicaleffectsandmechanismofaction◼(2)theclinicalapplicationof◼(3)theadversereactions◼4.Chlorinesandtemple:pharmacologicaleffectsand

mechanismofaction◼5.Calciumantagonistmedicine:pharmacologicaleffects◼THANKS

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