抗高血压药_英文版-课件

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Antihypertensivedrugshypertension◼Meanarterialbloodpressureishigherthanthenormalrange,inthecaseofnottakingbloodpressuredrugs:Systolicbloodp

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

ations◼Heartfailure◼Coronaryheartdisease(CHD)◼Cerebrovascularaccident◼RenalfailureAntihypertensivedrug

sReasonableapplicationofantihypertensivedrugsControlofbloodpressureDelaytheformationanddevelopmentofatherosclerosisReducethecom

plicationssuchasbrain,heartandkidneyReducethemortalityrate,prolonglifeBloodpressure-Thefactorsinfluencingbloodpressure:◼Cardiacoutput:heartrate,myoc

ardialcontractionforce,changeofbloodvolume,etc.;◼Peripheralresistance:thelengthofthebloodvesselsandbloodviscosity,bloodves

sels,radius,etc.-Nerve-fluidsystemonbloodpressureregulation。maincentreganglionVascularsmoothmusclecl

onidine-methyldopaEplerenonemecamylamineReserpineguanethidinepropranolol1prazosin1labetalolhydralazineso

diumnitroprussidenifedipineminoxidil1.Nervousregulation:thesympatheticnervoussystemPeripheralneurotransmitterreleaseThepostsyna

pticmembranereceptorSecond,humoralregulation:renin–angiotensinaldosteronesystemKidneyadjacentballBesidethem

achine-RblockersreninAngiotensinoriginalangiotensinⅠinvertaseACEIangiotensinⅡSmallarterycontractionlosartanAldosteronesecretionWatersodi

umretentiondiuretic(thiazides)Classification◼Diuretic◼Thesympatheticnervousdepressants◼(1)centralbloodpressuremedic

ation◼(2)theganglionblock◼(3)noradrenalinecannerveendingsblock◼(4)theadrenalinereceptorblockers◼Affectthe

renin-angiotensinsystemmedicineAgleamofantihypertensives:diuretic,calciumantagonistmedicine,betarecep

torblockersandACEIDiuretic◼Onthebasisof(aline)bloodpressuremedication◼Effectinthethiazidediureticismostcommonlyused,antihyper

tensiveeffectismild,persistent,long-termapplicationofnosignificantresistance◼Features:◼Antihypertensiveeffectisweak,bya

naverageof10%◼2~3weeksafterthemajorityofpatientsinmedicalwork◼Canbeusedforvarioushighbloodpressure(basicbloodpressuremedication)◼Mild-alone,

mediumandsevere-share◼Canmaketheelderlyhypertensionpatientscomplicatedwithstroke,theincidenceofleftheartfailureandmortalityisleftHydrochlorothiazi

de◼Earlyantihypertensivemechanism◼Withsodiumdiuresis,reducetheextracellularfluidandbloodvolume◼Long-termantihypertensivemechan

ism◼DiureticrowsodiumtoNa+leftaorticsmoothmusclecell,cellNa+/Ca2+exchangeleft->intracellularCa2+left,reducevascularsmooth

muscleofnorepinephrine(NE)reactivitydisadvantages:-↓BloodK+、Na+、Mg2+-↑Bloodtotalcholesterol,triglyceride,lowdensitylipoproteincho

lesterol(hdl-c)-↑Blooduricacid-↑Bloodrenin-↓Glucosetolerance(disabled)fordiabetespatientsEffectivediuretic(furo

semide)usedinhypertensivecrisisandpoorassociatedwithchronicrenalhypertensionpatients.◼Hypertensivecri

sis◼Patientswithhighbloodpressureintheshortterm,thebloodpressureincreasedsignificantly,andappearhaveaheadache,beagitated,palpitation,

sweating,nausea,vomiting,orpaleflush,blurredvisionandothersigns.◼Mechanism:hyperthyroidismandcirculatingcate

cholaminesincreasedsympatheticnervousactivityClinicalapplication◼Agleamofmedication◼Applicationofthetreatmen

tformildhypertensionseparately◼Withotherantihypertensivedrugtreatment,severehypertensionEffectofdiuresismedicineo

fcompoundpreparationswithotherdrugs◼Compoundantihypertensiontablet:giveupping,hydralazine,hydrochlor

othiazide◼Compoundapocynumtablet:guanidineborganism,hydralazine,hydrochlorothiazide◼Janechrysanthemumantihypertensiontablet:clonidine,hyd

rochlorothiazide◼Compoundcaptopriltablets,enalaprilandhydrochlorothiazide◼Constantdroppingpills:clonidine,hydralazine,hydr

ochlorothiazideCalciumantagonistmedicineBlockLvoltagedependentcalciumchannel->leftintracellularCa2+diastolicsma

llarteryNifedipinegroup,horizon,lacidipineflat,amlodipineNifedipine【Step-downcharacteristics】1Buckdegreewaspositivelycorrelatedwiththeoriginalhighbl

oodpressure,withnormalbloodpressurehasnoobviousantihypertensiveeffect;2Oralabsorptionisgood,workfast:sublingualadministering1-5minuteswork-inthetreat

mentofvariantanginapectoris,hypertensivecrisis.Oral30to60minuteswork-treatmentofmildandmoderatehypertension;

3Cancausereflectiveheartrate↑—shareReceptorblockers.Clinicalapplication◼Light,mediumandseverehypertensiontreatmentNitrend

ipine◼SelectivelyACTSontheperipheralvascular,blockingitsinternalflowofcalciumions,relaxingsmoothmuscle,thedilatebloodvess

elsandstep-down◼Warmandlastingantihypertensiveeffect,applicabletovarioustypesofhighbloodpressureLacidipine◼Isapotent

calciumantagonists,significantlyandtheeffectofselectivecalciumionchannelsinvascularsmoothmuscle.Itsmainroleistoexpandperipheralarter

y,reduceperipheralvascularresistanceandtolowerbloodpressure◼Resistancetoatherosclerosis◼Usedformildandmoderatehypertension◼Nameofcommodity:la

cidipine◼Amlodipine◼Moregentle,smootheffectlasting,convenienceofonce-dailydosage,24hoursofstabilitycontrolofhighbloodpressureandangi

napectoris,goodsafetyandtolerability◼Similardrugs,onlyitcanbeusedbypatientswithcongestiveheartfailuresafet

y◼AlsohastheroleofatherosclerosisAdrenalinereceptorblockers◼α1Receptorblockers:prazosin、terazosin、doxazosin◼βReceptorblockers:praprano

lol、atenolol、labetalol、carbedilolMechanismofaction◼Nonselectivebetareceptorblockers,mostlyrelatedwiththebetablocker:◼Heart:myocardia

lcontractionforceisabate,slowheartrate,cardiacoutputdecreases◼Kidney:reducereninsecretion,inhibitRASonbl

oodpressureregulation◼Thesympatheticnerveendingspresynapticmembrane:inhibitionofpositivefeedback,NAsecretiondecline◼Central(hypothalamu

sandmedullaoblongata):excitatoryneuronactivityisabate,peripheralsympatheticnervetensionby,vascularresis

tancedecreased◼IncreasethetopringelementsynthesisClinicalapplication◼Suitableforvarioushighbloodpressure◼Withhighcardiacoutput

orplasmareninlevelshasgoodeffectonthehighsideofhypertensivepatients,especiallysuitableforhypertensivepatie

ntswithcoronaryheartdisease,cerebrovasculardisease◼Diureticorpoolingvasodilatorscanenhancecurativeeffectatenolol◼Selectiveb

eta1receptorblockers,lackofinternaltothesympatheticactivity◼Oralisusedtotreatvariousdegreeofhighbloodpressure,antihypertensiveeff

ectalongerdurationlabetalol◼α、βReceptorblockers◼Applicabletovariousdegreesofhypertensionandhypertensiveemergency,gestationa

lhypertension,pheochromocytoma,highbloodpressurewhenanesthesiaorsurgerycarvedilol)◼α、βReceptorblockers◼Usedinthetr

eatmentofmildandmoderatehypertensionwithrenalinsufficiency,diabetes,highbloodpressurepatientsReninangiotensinsys

temdepressantsACEI:Captopriletc.AT1-resistance:Chlorinesand,valsartan,etc【Antihypertensivemechanism】1.AngIIGenerateandfunction。-Arterio

venousdiastolic→Peripheralresistance↓→Bloodpressure↓;-Blockthereleaseofaldosteronewatersodiumretention;2.Inhibiti

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

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

antihypertensiveeffectofmediumstrong;◼2withoutreflectiveheartrate,long-termusewithoutresistance,noteasytocausetheelectrolytedisorder

s;◼Threepairsofrenalhypertensiveeffectisgood,cantreatrefractoryheartfailure【application】Eachperiodhighbloodpressure.I

mportantfirst-linedrugs.Especiallysuitableforcomplicatedwithdiabetesandinsulinresistanceandleftventricularhypertrophy,heartfailure,acute

myocardialinfarctionpatientswithhighbloodpressureAngiotensinⅡreceptorblockersARBAT1receptor:vascularsmoothmuscle,cardiacmuscle,brain,kidneyandsecr

etionofaldosteroneAdrenalzonacells-hasregulatingeffecttothestabilityofthecardiovascularfunction.losartan【Antihypertensiveme

chanism】SelectiveblockingAT1receptor:blockingangiotensinⅡmediatedbloodvesselsShrinkage,aldosteronereleaseandpromotevascularsmoot

hmuscleproliferationandeffect→Peripheralresistance↓Promotinguricacidexcretion,inhibitingrenaltubuleofuricacidabsorption,short【Clinicalapplic

ationof】EachperiodhighbloodpressureStep-downfeatures:1.Theoralworkfast2.Theroletomaintainforalongtime:24hsmoothstep-down,3~6weeksformaximume

ffect【sideeffect】relativelylessACEI:Attractedlessdrycoughandangioneuroticoedema;Butstillcancauselowbloodpressureandhighpotassium.Forpa

tientswithpregnancy.Promotinguricacidexcretion,inhibitingrenaltubuleofuricacidabsorption,shortPharmacologicaleffects◼Diastolicsmallart

erysmoothmuscle,reducetheperipheralvascularresistance,lowerbloodpressure◼Withheartrateslows,decreasedcardiacoutput◼Inhibitthesecretionofg

astrointestinaltractandmovementandtheprotectionofgastricmucosa◼Buckwithsedation◼Reduceintraocularpressure,donotaffect

thepupilandtheadjustmentofthelensPharmacologicalactionandmechanism◼ActivateI1-imidazolinereceptor,Maketheperip

heralsympatheticactivitydecline,vasodilation,bloodpressuredrops◼Theexcitedcentralpostsynapticmembranereceptor

alpha2◼Lowerlevelsofplasmareninandaldosterone◼Inhibitthesecretionofgastrointestinaltractandmovementandthepr

otectionofgastricmucosa◼Staticnoteclonidinecanproduceboosterforashortperiodoftime(associatedwithperipheralalpha2receptor

excited),followedbyalongperiodoftimethestep-down(centralrole).Oralwiththecentralroleofthedominant,theboostereffect

isnotobviousClonidine◼Processinthebody◼Absorption:oralabsorption◼Distribution:easythroughthebloodbrainbarrier,plasmaproteincombinedra

teof30%◼Metabolism:50%inintrahepaticmetabolism◼Discharge:metabolicproductandprototypebyrenalexcretionClinicalapplication◼First-li

netreatmentinvalidmoderatelyhighbloodpressure,withthiazidediureticorotherantihypertensiveagentssharecanimprovethecurativeeffect◼Renalhypertensi

on◼Patientswithhighbloodpressureofpepticulcer◼Primaryopen-angleglaucomaAdversereactions◼Drymouth,sleepiness,constip

ation,impotence,canhappenoccasionallybradycardia◼Watersodiumretention◼Drugwithdrawalsyndrome:along-termd

rugwithdrawalmaysuddenlyappearhaveaheadache,tremor,abdominalpain,sweating,heartpalpitationsandbloodpressuresurge.Andlong-termm

edicationmadethealpha2weeksthepresynapticmembranereceptorsensitivity,negativefeedbackeffectisreduced,suddenwithdrawal,increasedsympatheticn

ervousfunctionisassociatedwithincreasedNErelease.Recoveryformedicineoralphareceptorblockers(e.g.,phentol

amine)canalleviate.WithdrawalshouldbegraduallyreducedTheothercentralbloodpressuremedication◼methyldopa◼Amediumtostrongstep-down,

cardiovascularandoutput,lessinfluencerenalbloodflow◼Suitableforrenalhypertensionandmoderatehypertensivepa

tientswithpoorkidneyfunction,oftenwiththiazidediureticshare◼moxonidine◼ForIlreceptoraffinityishigh,andthereceptorisstrong,biologicalt1/2longer,

onceadaydosing◼Suitableforpatientswithmildandmoderatehypertension◼Onthecentralandperipheralalpha2recep

torfunctionisweak,thecalm,drymouthgreatlyreduceadversereactionsVasodilationmedicine◼Directlytorelaxvascular

smoothmuscle,decreaseperipheralresistanceandbloodpressuretodrop◼Long-termuseantihypertensivevasodilatorshasthefollowingdisad

vantages◼Cantheexcitedsympatheticnerve,reflectiveincreasecardiacoutput,heartratespeedup◼Increaseofreninandaldosteronesecretion,leading

towaterandsodiumretention◼Alongtimewitheasytolerance◼Withadiureticoradrenalinereceptorblockerssharecanenhancecurativeeffect,reduce

adversereactionsSodiumnitroprusside◼AntihypertensiveeffectsassociatedwithanincreasedNO-GC-cGMP,candilatebloodvesselsandinhibitplateletaggregatio

n◼Ofarteriolesandvenulesvascularsmoothmusclewerediastolicfunction,antihypertensiveeffectstrong,rapidandshort◼Mainlyu

sedinthetreatmentofhypertensivecrisis.Alsousedincongestiveheartfailure,acutemyocardialinfarctionandcontrollinghypertensio

nduringanesthesia◼Becauseofexcessivestep-downcancausenausea,vomiting,sweating,restlessness,palpitationsandheadacheGanglio

nblockmedicinemecamylamine【Functioncharacteristics】1.Antihypertensiveeffectstrong,quickly;2.Hasinhibitoryeffectonbothsympatheticandparasym

pathetic,adversereactions,andtheheavier,orthostatichypotension;Theparasympatheticganglionblocksymptoms.3.Hypertensivecrisis.Prazosin–Processinthe

body◼Absorption:goodoralabsorption,firsteliminatetheobvious,bioavailabilityof60%◼Distribution:thecombinat

ionofplasmaproteinratewas97%◼Metabolism:livermetabolism◼Discharge:mostbileexcretion,byasmallnumberofurinePharmacologicaleffectsandmecha

nismofaction◼Alpha1receptorsonpostsynapticmembraneofvascularsmoothmusclearehighlyselectiveblockingeffect◼Step-dow

nfeatures:◼Amediumtostrongantihypertensiveeffect◼Don'taffectkidneyfunction,improvethelevelofrenin◼Long-termusecanimprovelip

idmetabolism◼Block1receptoralpha,relievedysuriaprostatepatientsClinicalapplication◼Canbeseparatelyusedt

reatmentofmildandmoderatehypertension◼Forelderlypatientswithhypertensioncombinedprostatichypertrophy,canimp

rovethesymptomsofdysuria◼Severehypertensionsharediureticandbetareceptorblockerscanenhancestep-downeffectAdversereactions◼Firstagentphenomenon:somep

atientsforthefirsttime0.51hourafterthetreatmentcanappearorthostatichypotension,dizziness,sweating,heartpalpitatio

nsandreaction◼Long-termusecancausewatersodiumretention,diuresismedicinecanmaintainitsantihypertensiveeffectres

erpine【Antihypertensivemechanism】ReducecatecholaminetransmitterinthestorageandreleaseAndthesympatheticnerv

eendings(peripheralandcentraladrenergic)vesiclemembraneAminepumpcombination,catecholamineneurotransmitter(NA,5-HT)synthesis,storage,reuptak

eleft,thedepletionoftheneurotransmitters,thesympatheticnerveconductionleft-vasodilation,BPleftCentralinhibition,composed,stableeffec

t.PhenylephrinecannerveendingsblockerFeatures:effectiveslow,gentleandlasting【Clinicalapplication】1light,moderatetohi

ghbloodpressure,ithasbeenlessusedalone2manicpsychosis【Adversereactions】1Theparasympatheticnerveexcitementsymptoms:nausea,vomiting,intestinalcrampsan

ddiarrhea,pepticulcer2Centralinhibition:calm,lethargy,depression。PotassiumchannelsareopenPromotetheKATPopen→Thecellmembranehyperpo

larization→TheinflowCa↓Thenewconceptofhighbloodpressuremedication1.Theeffectivetreatmentandlifelongtreatment2.

Protecttargetorgans3.Smoothstep-down4.CombinationtherapyThemainpoints◼1.Diuretic,pharmacologicalaction,mechanis

mofactionandclinicalapplication◼2.Thebetablockerdrugs:antihypertensiveeffectandmechanismofaction◼3.Theangiotensin

Iconvertingenzymeinhibitionofmedicine◼(1)thepharmacologicaleffectsandmechanismofaction◼(2)theclinicalapplicationof◼(3)theadversereac

tions◼4.Chlorinesandtemple:pharmacologicaleffectsandmechanismofaction◼5.Calciumantagonistmedicine:pharmacologicaleffects◼

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