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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-methyldopaEplerenonemecamylamineReserpineguanethidinepropranolol1prazosin1labetalolhydralazineso
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↑—shareReceptorblockers.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◼