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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-methyldopaEplerenonemecamylamineReserpineguanethidinepropranolol1prazosin1labetalolhydral
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↑—shareReceptorblockers.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