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%)Andsecondaryhypertensioncomplica

tions◼Heartfailure◼Coronaryheartdisease(CHD)◼Cerebrovascularaccident◼RenalfailureAntihypertensivedrugs

ReasonableapplicationofantihypertensivedrugsControlofbloodpressureDelaytheformationanddevelopmentofathero

sclerosisReducethecomplicationssuchasbrain,heartandkidneyReducethemortalityrate,prolonglifeBloodpressure-

Thefactorsinfluencingbloodpressure:◼Cardiacoutput:heartrate,myocardialcontractionforce,changeofbloodvolume,e

tc.;◼Peripheralresistance:thelengthofthebloodvesselsandbloodviscosity,bloodvessels,radius,etc.-Nerve-fluidsystemonbloodpressureregulat

ion。maincentreganglionVascularsmoothmuscleclonidine-methyldopaEplerenonemecamylamineReserpineguanethidine

propranolol1prazosin1labetalolhydralazinesodiumnitroprussidenifedipineminoxidil1.Nervousregulation:thesy

mpatheticnervoussystemPeripheralneurotransmitterreleaseThepostsynapticmembranereceptorSecond,humoralregulation:reni

n–angiotensinaldosteronesystemKidneyadjacentballBesidethemachine-RblockersreninAngiotensinoriginalangiotensinⅠinvertaseAC

EIangiotensinⅡSmallarterycontractionlosartanAldosteronesecretionWatersodiumretentiondiuretic(thiazide

s)Classification◼Diuretic◼Thesympatheticnervousdepressants◼(1)centralbloodpressuremedication◼(2)theganglionblock◼(3)noradrenalinecannerveendin

gsblock◼(4)theadrenalinereceptorblockers◼Affecttherenin-angiotensinsystemmedicineAgleamofantihypertensives:diuretic,calciumantagonistmedicine,b

etareceptorblockersandACEIDiuretic◼Onthebasisof(aline)bloodpressuremedication◼Effectinthethiazidediureticismo

stcommonlyused,antihypertensiveeffectismild,persistent,long-termapplicationofnosignificantresistance◼Features:◼Antihypertensiveeffectisweak,byanav

erageof10%◼2~3weeksafterthemajorityofpatientsinmedicalwork◼Canbeusedforvarioushighbloodpressure(basi

cbloodpressuremedication)◼Mild-alone,mediumandsevere-share◼Canmaketheelderlyhypertensionpatientscomplicatedwithstroke,theinc

idenceofleftheartfailureandmortalityisleftHydrochlorothiazide◼Earlyantihypertensivemechanism◼Withsodiumdiuresis,reducetheextracell

ularfluidandbloodvolume◼Long-termantihypertensivemechanism◼DiureticrowsodiumtoNa+leftaorticsmoothmusclecell,cellNa+/Ca2+exchangeleft->intracellularCa

2+left,reducevascularsmoothmuscleofnorepinephrine(NE)reactivitydisadvantages:-↓BloodK+、Na+、Mg2+-↑Bloodtotalcholesterol,trig

lyceride,lowdensitylipoproteincholesterol(hdl-c)-↑Blooduricacid-↑Bloodrenin-↓Glucosetolerance(disabled)fordiabetespatientsEffectivediuretic(furosem

ide)usedinhypertensivecrisisandpoorassociatedwithchronicrenalhypertensionpatients.◼Hypertensivecrisis

◼Patientswithhighbloodpressureintheshortterm,thebloodpressureincreasedsignificantly,andappearhaveaheadache,beagitated,palpitation,sweating,nausea,vom

iting,orpaleflush,blurredvisionandothersigns.◼Mechanism:hyperthyroidismandcirculatingcatecholaminesincreasedsympatheticnervousactivityClinicalappl

ication◼Agleamofmedication◼Applicationofthetreatmentformildhypertensionseparately◼Withotherantihypertensivedrugtreatment,severehypertensionEffect

ofdiuresismedicineofcompoundpreparationswithotherdrugs◼Compoundantihypertensiontablet:giveupping,hydralaz

ine,hydrochlorothiazide◼Compoundapocynumtablet:guanidineborganism,hydralazine,hydrochlorothiazide◼Janechrysanthemum

antihypertensiontablet:clonidine,hydrochlorothiazide◼Compoundcaptopriltablets,enalaprilandhydrochlorothiazide◼Constantdroppingpills:clonidi

ne,hydralazine,hydrochlorothiazideCalciumantagonistmedicineBlockLvoltagedependentcalciumchannel->leftintracellularCa2+diastolicsmallarteryNife

dipinegroup,horizon,lacidipineflat,amlodipineNifedipine【Step-downcharacteristics】1Buckdegreewaspositivelycorrelatedwiththeoriginalh

ighbloodpressure,withnormalbloodpressurehasnoobviousantihypertensiveeffect;2Oralabsorptionisgood,workfast:sublin

gualadministering1-5minuteswork-inthetreatmentofvariantanginapectoris,hypertensivecrisis.Oral30to60minuteswork-treatmentofmildandmoderatehyper

tension;3Cancausereflectiveheartrate↑—shareReceptorblockers.Clinicalapplication◼Light,mediumandseverehypert

ensiontreatmentNitrendipine◼SelectivelyACTSontheperipheralvascular,blockingitsinternalflowofcalciumions,relaxin

gsmoothmuscle,thedilatebloodvesselsandstep-down◼Warmandlastingantihypertensiveeffect,applicabletovarioustype

sofhighbloodpressureLacidipine◼Isapotentcalciumantagonists,significantlyandtheeffectofselectivecalciumion

channelsinvascularsmoothmuscle.Itsmainroleistoexpandperipheralartery,reduceperipheralvascularresistanceandtolowerbloodpressure◼Resistancetoatherosc

lerosis◼Usedformildandmoderatehypertension◼Nameofcommodity:lacidipine◼Amlodipine◼Moregentle,smootheffectlasting,convenienceofonce-dailydosa

ge,24hoursofstabilitycontrolofhighbloodpressureandanginapectoris,goodsafetyandtolerability◼Similardrugs,onlyitcanbeuse

dbypatientswithcongestiveheartfailuresafety◼AlsohastheroleofatherosclerosisAdrenalinereceptorblockers◼α1Receptorblockers:prazosin、terazosin、doxazo

sin◼βReceptorblockers:prapranolol、atenolol、labetalol、carbedilolMechanismofaction◼Nonselectivebetareceptorblockers,mostl

yrelatedwiththebetablocker:◼Heart:myocardialcontractionforceisabate,slowheartrate,cardiacoutputdecreases◼Kidney:redu

cereninsecretion,inhibitRASonbloodpressureregulation◼Thesympatheticnerveendingspresynapticmembrane:inhibitionofpositivefeedback,NAsecret

iondecline◼Central(hypothalamusandmedullaoblongata):excitatoryneuronactivityisabate,peripheralsympatheticnervetensionby,vascularresistancedecrease

d◼IncreasethetopringelementsynthesisClinicalapplication◼Suitableforvarioushighbloodpressure◼Withhighcardiacoutputorplasmare

ninlevelshasgoodeffectonthehighsideofhypertensivepatients,especiallysuitableforhypertensivepatientswithcoronaryheartdiseas

e,cerebrovasculardisease◼Diureticorpoolingvasodilatorscanenhancecurativeeffectatenolol◼Selectivebeta1r

eceptorblockers,lackofinternaltothesympatheticactivity◼Oralisusedtotreatvariousdegreeofhighbloodpressu

re,antihypertensiveeffectalongerdurationlabetalol◼α、βReceptorblockers◼Applicabletovariousdegreesofhypertensi

onandhypertensiveemergency,gestationalhypertension,pheochromocytoma,highbloodpressurewhenanesthesiaorsurgerycarvedilol)◼α、βR

eceptorblockers◼Usedinthetreatmentofmildandmoderatehypertensionwithrenalinsufficiency,diabetes,highbloodpressur

epatientsReninangiotensinsystemdepressantsACEI:Captopriletc.AT1-resistance:Chlorinesand,valsartan,etc【Antihypertensivemec

hanism】1.AngIIGenerateandfunction。-Arteriovenousdiastolic→Peripheralresistance↓→Bloodpressure↓;-Blockthe

releaseofaldosteronewatersodiumretention;2.Inhibitionofslowexcitationpeptidedegradation↓Slowexcitationpeptide

concentrationsintheblood↑:produceNO、PG2Etc.→血管扩张→血压↓AngiotensinconvertingenzymeinhibitorsACEIcaptopril(Asulfhydrylpropionicacidpulp)【Funct

ioncharacteristics】◼1orallyactive,workfast,antihypertensiveeffectofmediumstrong;◼2withoutreflectiveheartrate,long-termu

sewithoutresistance,noteasytocausetheelectrolytedisorders;◼Threepairsofrenalhypertensiveeffectisgood,cantreatrefractoryheartfailure【app

lication】Eachperiodhighbloodpressure.Importantfirst-linedrugs.Especiallysuitableforcomplicatedwithdi

abetesandinsulinresistanceandleftventricularhypertrophy,heartfailure,acutemyocardialinfarctionpatientswithhig

hbloodpressureAngiotensinⅡreceptorblockersARBAT1receptor:vascularsmoothmuscle,cardiacmuscle,brain,kidneyandsecretionofaldosteron

eAdrenalzonacells-hasregulatingeffecttothestabilityofthecardiovascularfunction.losartan【Antihypertensivemecha

nism】SelectiveblockingAT1receptor:blockingangiotensinⅡmediatedbloodvesselsShrinkage,aldosteronereleaseandpromotevasc

ularsmoothmuscleproliferationandeffect→Peripheralresistance↓Promotinguricacidexcretion,inhibitingrenaltubuleofuricacidabsor

ption,short【Clinicalapplicationof】EachperiodhighbloodpressureStep-downfeatures:1.Theoralworkfast2.Theroletomaintainforalongtime:

24hsmoothstep-down,3~6weeksformaximumeffect【sideeffect】relativelylessACEI:Attractedlessdrycoughandangioneuroticoedema

;Butstillcancauselowbloodpressureandhighpotassium.Forpatientswithpregnancy.Promotinguricacidexcretion,inhibitingrenaltubule

ofuricacidabsorption,shortPharmacologicaleffects◼Diastolicsmallarterysmoothmuscle,reducetheperipheralv

ascularresistance,lowerbloodpressure◼Withheartrateslows,decreasedcardiacoutput◼Inhibitthesecretionofgastrointestina

ltractandmovementandtheprotectionofgastricmucosa◼Buckwithsedation◼Reduceintraocularpressure,donotaffectthepupilan

dtheadjustmentofthelensPharmacologicalactionandmechanism◼ActivateI1-imidazolinereceptor,Maketheperipheralsympatheticactivitydecline,vasodilat

ion,bloodpressuredrops◼Theexcitedcentralpostsynapticmembranereceptoralpha2◼Lowerlevelsofplasmareninandaldosterone◼Inhibitthesecretionofgastrointestin

altractandmovementandtheprotectionofgastricmucosa◼Staticnoteclonidinecanproduceboosterforashortperiodoftime(associatedwithperipheralalpha2rec

eptorexcited),followedbyalongperiodoftimethestep-down(centralrole).Oralwiththecentralroleofthedominant,theboostereffectisnotobvi

ousClonidine◼Processinthebody◼Absorption:oralabsorption◼Distribution:easythroughthebloodbrainbarrier,plasmaproteincombinedrat

eof30%◼Metabolism:50%inintrahepaticmetabolism◼Discharge:metabolicproductandprototypebyrenalexcretionClinicalapp

lication◼First-linetreatmentinvalidmoderatelyhighbloodpressure,withthiazidediureticorotherantihypertensiveagentss

harecanimprovethecurativeeffect◼Renalhypertension◼Patientswithhighbloodpressureofpepticulcer◼Primaryopen-angleglaucoma

Adversereactions◼Drymouth,sleepiness,constipation,impotence,canhappenoccasionallybradycardia◼Watersodiumretention◼Dru

gwithdrawalsyndrome:along-termdrugwithdrawalmaysuddenlyappearhaveaheadache,tremor,abdominalpain,sweating,heartpalpitatio

nsandbloodpressuresurge.Andlong-termmedicationmadethealpha2weeksthepresynapticmembranereceptorsensitivity,negativefeedbacke

ffectisreduced,suddenwithdrawal,increasedsympatheticnervousfunctionisassociatedwithincreasedNErelease.Recoveryformedicineora

lphareceptorblockers(e.g.,phentolamine)canalleviate.WithdrawalshouldbegraduallyreducedTheothercentralbloodpressuremed

ication◼methyldopa◼Amediumtostrongstep-down,cardiovascularandoutput,lessinfluencerenalbloodflow◼Suitableforrenalhypertensionandmoderatehypertensiv

epatientswithpoorkidneyfunction,oftenwiththiazidediureticshare◼moxonidine◼ForIlreceptoraffinityishigh

,andthereceptorisstrong,biologicalt1/2longer,onceadaydosing◼Suitableforpatientswithmildandmoderatehypertension◼Onthecentralandperipheralalpha2rece

ptorfunctionisweak,thecalm,drymouthgreatlyreduceadversereactionsVasodilationmedicine◼Directlytorelaxvascularsmoothmuscl

e,decreaseperipheralresistanceandbloodpressuretodrop◼Long-termuseantihypertensivevasodilatorshasthefo

llowingdisadvantages◼Cantheexcitedsympatheticnerve,reflectiveincreasecardiacoutput,heartratespeedup◼Inc

reaseofreninandaldosteronesecretion,leadingtowaterandsodiumretention◼Alongtimewitheasytolerance◼Withadiureticoradrenalinerec

eptorblockerssharecanenhancecurativeeffect,reduceadversereactionsSodiumnitroprusside◼Antihypertensiveeffectsassocia

tedwithanincreasedNO-GC-cGMP,candilatebloodvesselsandinhibitplateletaggregation◼Ofarteriolesandvenulesvascularsmoothmusclewerediastolicfunctio

n,antihypertensiveeffectstrong,rapidandshort◼Mainlyusedinthetreatmentofhypertensivecrisis.Alsousedincongestiveheartfailure,acutemyocardialinfa

rctionandcontrollinghypertensionduringanesthesia◼Becauseofexcessivestep-downcancausenausea,vomiting,sweating,restlessness,palpit

ationsandheadacheGanglionblockmedicinemecamylamine【Functioncharacteristics】1.Antihypertensiveeffectstrong,quickly;2.Hasinhibitoryeffectonboth

sympatheticandparasympathetic,adversereactions,andtheheavier,orthostatichypotension;Theparasympatheti

cganglionblocksymptoms.3.Hypertensivecrisis.Prazosin–Processinthebody◼Absorption:goodoralabsorption,firsteliminatetheobvious,bioavail

abilityof60%◼Distribution:thecombinationofplasmaproteinratewas97%◼Metabolism:livermetabolism◼Discharge:mostbilee

xcretion,byasmallnumberofurinePharmacologicaleffectsandmechanismofaction◼Alpha1receptorsonpostsynapticmembraneofvascularsm

oothmusclearehighlyselectiveblockingeffect◼Step-downfeatures:◼Amediumtostrongantihypertensiveeffect◼Don'taffectkidneyfunction,improv

ethelevelofrenin◼Long-termusecanimprovelipidmetabolism◼Block1receptoralpha,relievedysuriaprostatepatientsClinicalapplication◼Canbesepar

atelyusedtreatmentofmildandmoderatehypertension◼Forelderlypatientswithhypertensioncombinedprostatichypertrophy,canimprovethesymptomsofdysuria◼Severe

hypertensionsharediureticandbetareceptorblockerscanenhancestep-downeffectAdversereactions◼Firstagentphenomenon:somepa

tientsforthefirsttime0.51hourafterthetreatmentcanappearorthostatichypotension,dizziness,sweating,heartpalpitationsandreaction◼Long-termusecan

causewatersodiumretention,diuresismedicinecanmaintainitsantihypertensiveeffectreserpine【Antihypertensivemechanism】Reducecatech

olaminetransmitterinthestorageandreleaseAndthesympatheticnerveendings(peripheralandcentraladrenergic)

vesiclemembraneAminepumpcombination,catecholamineneurotransmitter(NA,5-HT)synthesis,storage,reuptakelef

t,thedepletionoftheneurotransmitters,thesympatheticnerveconductionleft-vasodilation,BPleftCentralinhibition,compose

d,stableeffect.PhenylephrinecannerveendingsblockerFeatures:effectiveslow,gentleandlasting【Clinicalapplication】1light,moderatetohighb

loodpressure,ithasbeenlessusedalone2manicpsychosis【Adversereactions】1Theparasympatheticnerveexcitementsymptoms:nausea,vomiting,intestinalcramp

sanddiarrhea,pepticulcer2Centralinhibition:calm,lethargy,depression。PotassiumchannelsareopenPromotetheKATPopen→Thecellmembra

nehyperpolarization→TheinflowCa↓Thenewconceptofhighbloodpressuremedication1.Theeffectivetreatmentandlifelongtreatm

ent2.Protecttargetorgans3.Smoothstep-down4.CombinationtherapyThemainpoints◼1.Diuretic,pharmacologicalaction,mechanismofactionandclinicalappli

cation◼2.Thebetablockerdrugs:antihypertensiveeffectandmechanismofaction◼3.TheangiotensinIconvertingenzymeinhibitionofmedicine◼(1)thepharmacolo

gicaleffectsandmechanismofaction◼(2)theclinicalapplicationof◼(3)theadversereactions◼4.Chlorinesandtemple:pharmacologicaleffectsandmecha

nismofaction◼5.Calciumantagonistmedicine:pharmacologicaleffects◼THANKS

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