抗心絞痛藥課件

抗心絞痛藥Teachinggoals列舉抗心絞痛藥物分類及代表藥。簡述硝酸甘油抗心絞痛作用及機理。分析硝酸酯類與－R

阻斷藥合用治療心絞痛是否合理。I.Introduction(概述)

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

Anattackofanginapectorisoccurswhentheneedofthemyocardiumforoxygenexceedstheamountdeliveredtoitbythecoronarycirculation.【ClassificationofAnginaPectoris】Stableanginapectoris(穩(wěn)定型、勞累型心絞痛)：冠脈粥樣硬化，激動、勞累時發(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，夜間或休息時發(fā)作?！景l(fā)病機理】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(射血時間)

Anginapectorisresultsfromanimbalance(失衡)betweenoxygensupply-demandrelationshipinischemic(缺血的)regionsofthemyocardium(心肌).NormalOxygensupplyOxygendemandAngina供氧耗氧冠脈硬化痙攣栓塞射血時間↑心室容積↑收縮力↑HR↑Principlesoftreatment(治療原則)：耗氧室壁張力心率心肌收縮力心臟負荷冠脈血流量側枝循環(huán)心舒張時間供氧〓

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

II.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【pharmacologicalactions】Reductionofmyocardialoxygenconsumption

（降低心肌耗氧量）Dilationofveins(擴V)

myocardialoxygenconsumption心肌耗氧量cardiacpreload(心臟前負荷)Dilationofarteries(擴A)Cardiacafterload(心臟后負荷)Note:HR↑、心肌收縮力↑→耗氧↑why2.Dilatecoronaryartery,increasethebloodflowinischemicareas.(擴張冠脈，↑缺血區(qū)血流)

Nitroglycerin→舒張側枝血管→血流重新分布→從非缺血區(qū)經(jīng)側枝流向缺血區(qū)→缺血區(qū)血供↑3.Increasethebloodflowinsubendocardialarea.(↑心內(nèi)膜下區(qū)域血供)Nitroglycerin

硝酸甘油擴V→LVEDP↓擴心外膜大血管擴側支血管心內(nèi)膜下缺血區(qū)血供↑4.保護缺血的心肌細胞，減輕缺血損傷mechanism【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)【Adversereactions】Vasodilation(擴血管)：面部潮紅、搏動性頭痛、體位性低血壓、眼壓↑、顱內(nèi)壓↑2.Tolerance(耐受性)：間歇給藥：間隔8小時以上補充含巰基藥：卡托普利等硝酸異山梨醇酯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Note：forceofcontraction(心肌收縮力)Ventricularejectiontime(射血時間)Ventricularvolume(心容積)耗氧2.Improvementofbloodsupplyinischemicareas

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

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

Especiallyforthepatientswithhypertensionandarrhythmia.(對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whyIV.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2.Dilationofcoronaryvessels(擴張冠脈)3.Protectionofischemicmyocardialcell(保護缺血心肌細胞)：防止C內(nèi)Ca2+超負荷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↓、血管擴張、