第二十二章抗高血压药课件

22章 抗高血压药Antihypertensive drugs22章 抗高血压药Antihypertensive drug1Objectiven掌掌握握 氢氯噻嗪、普普萘洛洛尔、硝硝苯苯地地平平、卡卡托托普普利利、硝硝普普钠的的降降压作作用用、机机制制、临床床应用。用。n熟熟悉悉 抗抗高高血血压药的的分分类，其其它它常常用用药的作用特点，抗高血的作用特点，抗高血压药的的应用原用原则。n了解了解其它其它药物的降物的降压作用特点。作用特点。Objective掌握 氢氯噻嗪、普萘洛尔、硝苯地平、卡托普2第二十二章抗高血压药课件3第二十二章抗高血压药课件4第二十二章抗高血压药课件5第二十二章抗高血压药课件6第二十二章抗高血压药课件7第二十二章抗高血压药课件81introduction1.Hypertensionn nBp140/90mmHg(18.7/12kPa)nTheconditioncanbefatalifuntreated,asitgreatlyincreasestheriskofthrombosis（血栓症血栓症）,stroke（卒中卒中）andrenalfailure.1 introduction1.Hyperten91introductionnClassificationofhypertension1 introductionClassificat101introductionnpathophysiology(病生理病生理)ofhypertension 1).sympatheticnervoussystemdysfunction(交感神交感神经系系统功能紊乱功能紊乱)SympatheticNS（）（）arteryconstrictionperipheralresistanceheart（）（）HR,CO-R(+)reninexcreteBp1 introductionpathophysio112).RAAS3).Others2).RAAS 3).Others121introductionnAntihypertensivedrugs【definition】Theagentscanlowerbloodpressure,clinicalusedtotreathypertensionandtopreventdamagesinkidney,heartandbrain.【significance】morbidityandmortality(发病率病率）（死亡率死亡率）1 introductionAntihyperte131introductionnClassificationofantihypertensivedrugs1.DiureticsDiuretics:DCT氢氯噻嗪,furosemide呋塞米2.RAASinhibitorsACEIACEIcaptopril,enalapril AT1blockerslosartan氯沙坦,valsartan缬沙坦 Renininhibitorsenalkiren依那吉仑,remikiren雷米克林1 introductionClassificat141introduction3.Adrenergicreceptorblockers:1)1-Rblockers:prazosinterazosin2)-Rblockers:propranolol 3)、-Rblockers:labetalol4.Calciumchannelblockers:nifedipine,amlodipine1 introduction3.Adrenerg151introduction5.Sympatheticnervousinhibitors:clonidine,methyldopa,reserpine.6.Vasodilators:hydralazine,sodium nitroprusside minoxidil,diazoxide.7.others1 introduction 5.Sympa162usualdrugs-Diuretic agents I.Diureticagents【antihypertensivemechanism】earlyhypotensiveeffectdiureticeffectbloodvolumelong-termeffectPVR（外周血管阻力外周血管阻力）Bp2 usual drugs-Diureti172usualdrugs-Diuretic agentsExcretionofsodiumintracellularNa+intracellularCa2+；thesensitivityofbloodvesselresponsestoNA;producethevasodilators(BK,PGE2).2 usual drugs-Diureti182usualdrugs-Diuretic agents【clinicaluses】噻嗪类 thiazidesbasicantihypertensiveagentsmildhypertensionusedalone(25mg);moderateandseverehypertensionusedincombinationwithotherantihypertensiveagents.（-RblockersorACEI)2 usual drugs-Diureti192usualdrugs-Diuretic agents吲达帕胺达帕胺 indapamidediureticeffect,directvasodilation血管舒张Bp adversereactionssmall;forpatientwithhyperlipidemia高脂血症:replaceDCT2 usual drugs-Diureti202usualdrugs-Diuretic agents呋塞米塞米 furosemidehighefficacydiuretic,itcancausesevereelectrolyteimbalance（电解解质失衡失衡）onlyusedinseverehypertension,especiallywithchronicrenalinsufficiencyorcardiacfailure.2 usual drugs-Diureti212usualdrugs-calcium antagonistsII、CalciumantagonistsblockingcalciumchannelvasodilationBpnifedipine(硝苯地平硝苯地平)nitrendipine(尼群地平尼群地平)lacidipine(拉西地平拉西地平)amlodipine(氨氨氯地平地平)2 usual drugs-calcium222usualdrugs-calcium antagonists硝苯地平硝苯地平 nifedipine【characteristicsofaction】1.poabsorptioniscomplete;2.Ithasmoreselectivity,usedformildormoderatehypertension.3.usedaloneorincombinationwithdiureticsand-Rblockers.2 usual drugs-calcium232usualdrugs-calcium antagonists4.ReflexsympatheticactivationslighttachycardiaorCO;sustained-releasepreparations(缓释制制剂)5.Sidereaction:hypotension,rash（皮疹皮疹）,tachycardia,peripheraledema（水水肿）,flushing面红anddizziness（眩眩晕）.2 usual drugs-calcium242usualdrugs-calcium antagonistsn nClinicalchoice:hypertensionwithangina心绞痛-nifedipine硝苯地平;withcerebralvasculardisease脑血管疾病-nimoldipine尼莫地平;withtachycardia心动过速-verapamil维拉帕米(aloneorwithdiuretics、-Rdrugs)2 usual drugs-calcium252usualdrugs-R blocking agentsIII.-Rblockingagents普普萘洛洛尔 propranolol【antihypertensivemechanism】1.blocks1RCO;2.blocking1-Rlocatedinthekidneyreninsecretion,3.theactivityofRAAS2 usual drugs-R blo262usualdrugs-R blocking agents3.blocking-RlocatedintheCNSperipheralsympatheticactivity;（外周交感外周交感N活性活性）4.blockingpresynaptic(突触前膜突触前膜)-R2inhibitthepositivefeedback（正正反反馈馈）,NArelease;5.PGI2synthesis血管扩张血管扩张2 usual drugs-R blo272usualdrugs-R blocking agentspropranolol2 usual drugs-R blo282usualdrugs-R blocking agents【antihypertensivecharacteristics】1.mildness,slowness,2.longduration;2.Individualvariation（个体差异个体差异）ofdoses;2 usual drugs-R blo292usualdrugs-R blocking agents3.Firstlineagent,mostusefulinantihypertensivetherapy;especiallywithhighplasmareninactivity（高高肾素活性素活性）；）；orwithangina（心绞痛）；orwithtachycardia（心动过速）.2 usual drugs-R blo302usualdrugs-R blocking agentsOther-Rblockingagents阿替洛阿替洛尔atenolol拉拉贝洛洛尔labetalol、卡卡维洛洛尔carvedilol2 usual drugs-R blo312usualdrugs-ACEIIV.Renin-angiotensinsysteminhibitors ACEIcaptopril卡托普利 enalapril依那普利ramipril雷米普利 benazapril贝那普利cilazapril西拉普利fosinopril福森普利2 usual drugs-ACEIIV.322usualdrugs-ACEIn nBasicactions:Basicactions:1.AngII的生成及作用的生成及作用;2.保存保存BK的活性的活性;3.保保护血管内皮血管内皮细胞及抗胞及抗动脉粥脉粥样硬化硬化;4.抗心肌缺血与心肌保抗心肌缺血与心肌保护作用作用;5.对胰胰岛素的敏感性素的敏感性;6.阻止心血管病理性重构阻止心血管病理性重构.2 usual drugs-ACEIBas33【antihypertensivemechanism】AngIAngIIBloodvessel（+）NAreleaseAldosteroneVSMhyperplasiaACE（kininaseII）BKlossaliveproduceNO,PGIproduceNO,PGI2 2 plateletcongregate聚集聚集Vasodilator血管扩张血管扩张ACEI【antihypertensive mechanism】A342usualdrugs-ACEI卡托普利卡托普利captopril【antihypertensivecharacteristics】1.poabsorptioniswell，F70%;2.Vasodilatation血管扩张血管扩张PVR外周阻力外周阻力,butCOandHRarenotsignificantlychanged;2 usual drugs-ACEI卡托普352usualdrugs-ACEI3.cardiacprotectionpreventionandreversionofbloodvesselwallincrassation（增厚）增厚）andmyocardialhypertrophy（心肌肥厚）.4.UsedforalltypesofhypertensionandsevereCHF.2 usual drugs-ACEI3.362usualdrugs-ACEI【adversereactions】1)hypotension(3.3%);2)characteristiccough(5%20%);3)hyperkalaemia（高血高血钾）;4)renalfunction*;5)dizziness,skinrashesandalterationintaste.2 usual drugs-ACEI【ad372usualdrugs-ACEI【contraindications】pregnancy（妊娠妊娠）;renovascular（肾血管血管）diseaseortothosewithdoubleaorticstenosis（双双侧肾动脉狭窄脉狭窄）.2 usual drugs-ACEI【co38(二二）AT1blockersLosartan氯沙坦氯沙坦Valsartan缬沙坦缬沙坦Candesartan坎坎地沙坦地沙坦(二）AT1 blockersLosartan氯沙坦392usualdrugs-AT1 blockersAngiotensinIIreceptor（AT1）blockers氯沙坦沙坦losartancompetitiveblockAT1PVRbloodcapacitiesUsedforhypertension.sideeffectssimilartocaptopril,butcoughislesscommon.2 usual drugs-AT1 blo403otherclassicalantihypertensivedrugs.ActingonCNS可可乐定定clonidine甲基多巴甲基多巴methyldopa莫索尼定莫索尼定moxonidine3 other classical antihyp413otherclassicalantihypertensivedrugs可乐定可乐定 clonidine【characteristicsofaction】1.poabsorptioniswell,F71-82%；2.themechanismiscomplex:central 2-R&I1imidazoline-R（咪（咪唑啉受体）啉受体）(+)sympatheticactivityPVR;(+)presynaptic 2-RNArelease 3 other classical antihyp423otherclassicalantihypertensivedrugs3.Dont renalbloodflowandGFRfrequentlyuseforhypertensionwithrenalinsufficiency（肾功能不全功能不全）.gastricacidsecretionproperforhypertensionwithpepticulcer（胃潰疡）胃潰疡）.3 other classical antihyp433otherclassicalantihypertensivedrugs4.usedformoderatetoseverehypertension；5.untowardeffects:sedation,drymouth,orthostatichypotension（体位性低血体位性低血压）,reboundwithdrawal（停停药反跳反跳），），sodiumandwaterretention.Moxonidine莫索尼定3 other classical antihyp443otherclassicalantihypertensivedrugs.Vasodilators肼屈屈嗪hydralazinetheeffectonarteriolesveins;HR,CO,reninsecretion;aloneusedrarely3 other classical antihyp453otherclassicalantihypertensivedrugshydralazinesodiumnitroprusside3 other classical antihyp463otherclassicalantihypertensivedrugs硝普硝普钠 sodiumnitroprusside【characteristics】1.iv.gtttheeffectsarestrong、rapidandunabiding(短短暂的的)；2.directvasodilationonarterialandvenous;3 other classical antihyp473otherclassicalantihypertensivedrugs3.usedforhypertensivecrisis（高血高血压危象危象）;refractoryCHF（难治性心衰治性心衰）;controlledhypotension.（控制性降控制性降压）3 other classical antihyp483otherclassicalantihypertensivedrugsGanglionicBlockers神经节阻断药神经节阻断药 美卡拉明美卡拉明mecamylamine樟磺咪芬樟磺咪芬trimetaphancamsilateonlyintreatinghypertensivecrisis（高血高血压危象危象）andtoinducecontrolledhypotension（控制性降控制性降压）forneurosurgery.3 other classical antihyp493otherclassicalantihypertensivedrugs 1-Rblockersprazosin(哌唑嗪)terazosin(特拉特拉唑嗪)doxazosin(多沙多沙唑嗪)3 other classical antihyp503otherclassicalantihypertensivedrugs哌唑嗪 prazosin【characteristics】1.selectivelyblock 1-RBp;lessreflextachycardia;prazosin3 other classical antihyp513otherclassicalantihypertensivedrugs2.coronaryarterydisease冠状动脉疾病,冠心病 n LDLn VLDLn triglyceride（甘油三甘油三酯）;n HDL;3 other classical antihyp523otherclassicalantihypertensivedrugs3.Clinicaluses:i.mildtomoderatehypertension;combinationwithotheragents(diureticsandpropranolol)effects;ii.acuteCHF;4.untowardeffects:Dizziness,headache,drowsiness.3 other classical antihyp533otherclassicalantihypertensivedrugsnFirstdosephenomenon(首首剂现象象）thefirstdose1mg,posturalhypotension（体位性低血体位性低血压）andsyncope（晕厥厥）mayoccur,so,thefirstdoseshouldbesmallandshouldbeadministeredatbedtime.3 other classical antihyp543otherclassicalantihypertensivedrugsAdrenergicneuronblockingagents利血平利血平reserpine胍乙胍乙啶guanethidine causedepletion（耗竭耗竭）ofNAperipheralsympatheticactivity3 other classical antihyp55Newconceptofantihypertensivetherapy effectivelytherapyandlifetimetherapy（有效治（有效治疗与与终生治生治疗）；protecttargetorgans（保（保护靶器官）靶器官）reposefullyhypotension（平（平稳降降压）New concept of antihypertensiv56第二十二章抗高血压药课件57第二十二章抗高血压药课件58questionsn1.抗高血压药物的分类？n2.利尿药的降压机制及其应用questions1.抗高血压药物的分类？59