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Chapter28抗心絞痛藥Anti-anginaPectorisDrugsChapter28抗心絞痛藥Anti-anginaPe1Teachinggoals列舉抗心絞痛藥物分類及代表藥。簡(jiǎn)述硝酸甘油抗心絞痛作用及機(jī)理。分析硝酸酯類與-R

阻斷藥合用治療心絞痛是否合理。Teachinggoals列舉抗心絞痛藥物分類及代表藥。2I.Introduction(概述)

Anginapectoris(心絞痛)isacommonsymptomofcoronaryartery(冠狀動(dòng)脈)diseasecausedbytransient(短暫)episodes(發(fā)作)ofmyocardialischemia(缺血)andanoxia(缺氧).

Anattackofanginapectorisoccurswhentheneedofthemyocardiumforoxygenexceedstheamountdeliveredtoitbythecoronarycirculation.I.Introduction(概述)Angin3【ClassificationofAnginaPectoris】Stableanginapectoris(穩(wěn)定型、勞累型心絞痛):冠脈粥樣硬化,激動(dòng)、勞累時(shí)發(fā)作Unstableanginapectoris(不穩(wěn)定型心絞痛):(非典型性或梗死前心絞痛)冠脈粥樣硬化,血栓,可發(fā)展為心?;蜮?,也可恢復(fù)為穩(wěn)定型心絞痛。Variantanginapectoris(變異型心絞痛):冠脈痙攣所致,夜間或休息時(shí)發(fā)作?!綜lassificationofAnginaPec4【發(fā)病機(jī)理】Determinantsofmyocardialoxygenconsumption(決定心肌耗氧量主要因素

):Ventricularwalltension(室壁張力)Heartrate(心率)Ventricularcontractility(心室收縮力)Ejectiontime(射血時(shí)間)

Anginapectorisresultsfromanimbalance(失衡)betweenoxygensupply-demandrelationshipinischemic(缺血的)regionsofthemyocardium(心肌).【發(fā)病機(jī)理】Determinantsofmyocard5NormalOxygensupplyOxygendemandAngina供氧耗氧冠脈硬化痙攣栓塞射血時(shí)間↑心室容積↑收縮力↑HR↑NormalOxygensupplyOxygendem6Principlesoftreatment(治療原則):耗氧室壁張力心率心肌收縮力心臟負(fù)荷冠脈血流量側(cè)枝循環(huán)心舒張時(shí)間供氧〓

Torecoverthebalancebetweenoxygensupplyandoxygenconsumption.(恢復(fù)氧供需平衡)Principlesoftreatment(治療原則)7【Classificationofanti-anginapectoris】(抗心絞痛藥物分類)1)Organicnitrates(硝酸酯類)2)-Rblockers3)Calciumchannelblockers(鈣拮抗劑)

【Classificationofanti-angin8II.Organicnitrates(硝酸酯類)Nitroglycerin(硝酸甘油)【Pharmacokinetics】1.Becauseofmarkedfirst-passeliminationitcannotbegivenorally,andusuallygivensublingually(舌下).

(首過消除明顯,口服無效,舌下含服)

2.可透皮吸收II.Organicnitrates(硝酸酯類)Ni9【pharmacologicalactions】Reductionofmyocardialoxygenconsumption

(降低心肌耗氧量)Dilationofveins(擴(kuò)V)

myocardialoxygenconsumption心肌耗氧量cardiacpreload(心臟前負(fù)荷)Dilationofarteries(擴(kuò)A)Cardiacafterload(心臟后負(fù)荷)Note:HR↑、心肌收縮力↑→耗氧↑why【pharmacologicalactions】Reduc102.Dilatecoronaryartery,increasethebloodflowinischemicareas.(擴(kuò)張冠脈,↑缺血區(qū)血流)

Nitroglycerin→舒張側(cè)枝血管→血流重新分布→從非缺血區(qū)經(jīng)側(cè)枝流向缺血區(qū)→缺血區(qū)血供↑2.Dilatecoronaryartery,inc11抗心絞痛藥白--課件123.Increasethebloodflowinsubendocardialarea.(↑心內(nèi)膜下區(qū)域血供)Nitroglycerin

硝酸甘油擴(kuò)V→LVEDP↓擴(kuò)心外膜大血管擴(kuò)側(cè)支血管心內(nèi)膜下缺血區(qū)血供↑4.保護(hù)缺血的心肌細(xì)胞,減輕缺血損傷3.Increasethebloodflowin13mechanismmechanism14【clinicaluses】1.Alltypesofanginapectoris(各型心絞痛

):

急性發(fā)作首選,舌下(sublingually)給藥

2.Acutemyocardialinfarction(急性心肌梗死)3.Congestiveheartfailure(充血性心衰)【clinicaluses】1.Alltypesof15【Adversereactions】Vasodilation(擴(kuò)血管):面部潮紅、搏動(dòng)性頭痛、體位性低血壓、眼壓↑、顱內(nèi)壓↑2.Tolerance(耐受性):間歇給藥:間隔8小時(shí)以上補(bǔ)充含巰基藥:卡托普利等硝酸異山梨醇酯【Adversereactions】Vasodilat16

III.-RBlockersPropranolol(普萘洛爾)【Anti-anginapectoriseffects】(抗心絞痛作用)Reducethemyocardialoxygenconsumption.(降低心肌耗氧量)(-)-RHR↓forceofcontraction(心肌收縮力)↓BP↓oxygenconsumption耗氧量III.-RBlockersPropranol17Note:forceofcontraction(心肌收縮力)Ventricularejectiontime(射血時(shí)間)Ventricularvolume(心容積)耗氧2.Improvementofbloodsupplyinischemicareas

(改善心肌缺血區(qū)供血)1)HR↓→舒張期↑→血流從心外膜進(jìn)入內(nèi)膜↑

2)增加缺血區(qū)側(cè)支循環(huán)Note:forceofcontractionVentr18【Clinicaluses】1.Stableanginapectoris(穩(wěn)定型心絞痛):

Especiallyforthepatientswithhypertensionandarrhythmia.(對(duì)伴高血壓或心律失常者尤佳)2.Cardiacinfarction(心肌梗死):Note:變異型心絞痛不用why【Clinicaluses】Note:變異型心絞痛不用wh19IV.CalciumChannelBlockers(鈣通道阻斷藥)Nifedipine(硝苯地平,心痛定)Verapamil(維拉帕米,異搏定)Diltiazem(地爾硫卓,硫氮卓酮)【Mechanism】阻鈣內(nèi)流IV.CalciumChannelBlockers202.Dilationofcoronaryvessels(擴(kuò)張冠脈)3.Protectionofischemicmyocardialcell(保護(hù)缺血心肌細(xì)胞):防止C內(nèi)Ca2+超負(fù)荷4.Inhibitionofplateletaggregation(抑制血小板聚集)【Anti-anginapectoriseffects】(抗心絞痛作用)1.Reductionofoxygenconsumption(降低氧耗)

:心力↓、HR↓、血管擴(kuò)張、BP↓、心負(fù)荷↓2.Dilationofcoronaryvessel21【Clinicaluses】1.Variantangina(變異性心絞痛):首選2.Stableorunstableangina(穩(wěn)定型或不穩(wěn)定型):

【Clinicaluses】1.Variantangi22心肌收縮力Propranolol冠狀動(dòng)脈室壁張力HRNitroglycerin舒張收縮↓↑↑↑↓↓射血時(shí)間↓↑BP↓↓心肌收縮力Propranolol冠狀動(dòng)脈室壁張力HRNitr23Chapter28抗心絞痛藥Anti-anginaPectorisDrugsChapter28抗心絞痛藥Anti-anginaPe24Teachinggoals列舉抗心絞痛藥物分類及代表藥。簡(jiǎn)述硝酸甘油抗心絞痛作用及機(jī)理。分析硝酸酯類與-R

阻斷藥合用治療心絞痛是否合理。Teachinggoals列舉抗心絞痛藥物分類及代表藥。25I.Introduction(概述)

Anginapectoris(心絞痛)isacommonsymptomofcoronaryartery(冠狀動(dòng)脈)diseasecausedbytransient(短暫)episodes(發(fā)作)ofmyocardialischemia(缺血)andanoxia(缺氧).

Anattackofanginapectorisoccurswhentheneedofthemyocardiumforoxygenexceedstheamountdeliveredtoitbythecoronarycirculation.I.Introduction(概述)Angin26【ClassificationofAnginaPectoris】Stableanginapectoris(穩(wěn)定型、勞累型心絞痛):冠脈粥樣硬化,激動(dòng)、勞累時(shí)發(fā)作Unstableanginapectoris(不穩(wěn)定型心絞痛):(非典型性或梗死前心絞痛)冠脈粥樣硬化,血栓,可發(fā)展為心?;蜮?,也可恢復(fù)為穩(wěn)定型心絞痛。Variantanginapectoris(變異型心絞痛):冠脈痙攣所致,夜間或休息時(shí)發(fā)作。【ClassificationofAnginaPec27【發(fā)病機(jī)理】Determinantsofmyocardialoxygenconsumption(決定心肌耗氧量主要因素

):Ventricularwalltension(室壁張力)Heartrate(心率)Ventricularcontractility(心室收縮力)Ejectiontime(射血時(shí)間)

Anginapectorisresultsfromanimbalance(失衡)betweenoxygensupply-demandrelationshipinischemic(缺血的)regionsofthemyocardium(心肌).【發(fā)病機(jī)理】Determinantsofmyocard28NormalOxygensupplyOxygendemandAngina供氧耗氧冠脈硬化痙攣栓塞射血時(shí)間↑心室容積↑收縮力↑HR↑NormalOxygensupplyOxygendem29Principlesoftreatment(治療原則):耗氧室壁張力心率心肌收縮力心臟負(fù)荷冠脈血流量側(cè)枝循環(huán)心舒張時(shí)間供氧〓

Torecoverthebalancebetweenoxygensupplyandoxygenconsumption.(恢復(fù)氧供需平衡)Principlesoftreatment(治療原則)30【Classificationofanti-anginapectoris】(抗心絞痛藥物分類)1)Organicnitrates(硝酸酯類)2)-Rblockers3)Calciumchannelblockers(鈣拮抗劑)

【Classificationofanti-angin31II.Organicnitrates(硝酸酯類)Nitroglycerin(硝酸甘油)【Pharmacokinetics】1.Becauseofmarkedfirst-passeliminationitcannotbegivenorally,andusuallygivensublingually(舌下).

(首過消除明顯,口服無效,舌下含服)

2.可透皮吸收II.Organicnitrates(硝酸酯類)Ni32【pharmacologicalactions】Reductionofmyocardialoxygenconsumption

(降低心肌耗氧量)Dilationofveins(擴(kuò)V)

myocardialoxygenconsumption心肌耗氧量cardiacpreload(心臟前負(fù)荷)Dilationofarteries(擴(kuò)A)Cardiacafterload(心臟后負(fù)荷)Note:HR↑、心肌收縮力↑→耗氧↑why【pharmacologicalactions】Reduc332.Dilatecoronaryartery,increasethebloodflowinischemicareas.(擴(kuò)張冠脈,↑缺血區(qū)血流)

Nitroglycerin→舒張側(cè)枝血管→血流重新分布→從非缺血區(qū)經(jīng)側(cè)枝流向缺血區(qū)→缺血區(qū)血供↑2.Dilatecoronaryartery,inc34抗心絞痛藥白--課件353.Increasethebloodflowinsubendocardialarea.(↑心內(nèi)膜下區(qū)域血供)Nitroglycerin

硝酸甘油擴(kuò)V→LVEDP↓擴(kuò)心外膜大血管擴(kuò)側(cè)支血管心內(nèi)膜下缺血區(qū)血供↑4.保護(hù)缺血的心肌細(xì)胞,減輕缺血損傷3.Increasethebloodflowin36mechanismmechanism37【clinicaluses】1.Alltypesofanginapectoris(各型心絞痛

):

急性發(fā)作首選,舌下(sublingually)給藥

2.Acutemyocardialinfarction(急性心肌梗死)3.Congestiveheartfailure(充血性心衰)【clinicaluses】1.Alltypesof38【Adversereactions】Vasodilation(擴(kuò)血管):面部潮紅、搏動(dòng)性頭痛、體位性低血壓、眼壓↑、顱內(nèi)壓↑2.Tolerance(耐受性):間歇給藥:間隔8小時(shí)以上補(bǔ)充含巰基藥:卡托普利等硝酸異山梨醇酯【Adversereactions】Vasodilat39

III.-RBlockersPropranolol(普萘洛爾)【Anti-anginapectoriseffects】(抗心絞痛作用)Reducethemyocardialoxygenconsumption.(降低心肌耗氧量)(-)-RHR↓forceofcontraction(心肌收縮力)↓BP↓oxygenconsumption耗氧量III.-RBlockersPropranol40Note:forceofcontraction(心肌收縮力)Ventricularejectiontime(射血時(shí)間)Ventricularvolume(心容積)耗氧2.Improvementofbloodsupplyinischemicareas

(改善心肌缺血區(qū)供血)1)HR↓→舒張期↑→血流從心外膜進(jìn)入內(nèi)膜↑

2)增加缺血區(qū)側(cè)支循環(huán)Note:forceofcontractionVentr41【Clinicaluses】1.Stableanginapectoris(穩(wěn)定型心絞痛):

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