抗心绞痛药ppt课件.ppt

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1、AntianginalDrugs抗心绞痛药ObjectivesKnowthemajorclassesofdrugsusedtotreatanginaandtheirmechanismsofaction抗心绞痛药分类、代表药及其作用机制WhatisAnginapectoris?冠脉供氧不足引起的暂时性急剧心肌缺血所致的临床综合征，表现为胸骨后疼痛，并可放射到左臂。是冠状动脉粥样硬化性心脏病（冠心病的常见症状。。ItistheprinciplesymptomofischemicheartdiseaseTheco

2、nditionischaracterizedbysudden,severesubsternalpainorpressureOxygensupply↓Oxygendemand↑coronaryatherosclerosis冠状动脉硬化，95%coronaryarteryspasm冠状动脉痉挛coronarythrombosis冠状动脉血栓形成myocardialcontractility↑心肌收缩力HR↑心率Sports,moodmodification运动、情绪改变Anginapectorispattern

3、sFactorsaffectingmyocardialoxygendemandandoxygensupplyOxygendemandOxygensupply=>Coronarybloodflow冠脉血流RegionalmyocardialDistribution网状血管区域心肌分布VentricularVolume心室容积LVpressure左室压walltension室壁张力Contractily心肌收缩力heartrate心率aorticpressure主动脉压Coronaryvascularresis

4、tance冠脉阻力normalischemiaanainalsymptomsAVoxygendifferenceAV血氧差ChemicalstructuresoftwonitratesNitroglycerine硝酸甘油Isosorbidedinitrate硝酸异山梨酯PharmacologicalmechanismOrganicnitratesNOguanylylcyclase(鸟苷酸环化酶)GTPcGMPcGMPdependentproteinkinaseintracellularCa2+↓vascul

5、arsmoothmusclerelaxationOxygendemand↓venousrelaxation静脉舒张arteryrelaxation（largedose)动脉舒张(大剂量)venousreturn回心血量↓preload前负荷↓ventricularend-diastolicvolume心室舒张末期容积↓ventricularwalltension心室壁张力↓VET↓心室射血时间afterload后负荷↓Oxygendemand耗氧量↓TPR↓总外周阻力Oxygensupply↑ventric

6、ularwalltension心室壁张力↓coronarybloodflow↑(especiallytheischemicmyocardium)冠脉供血(特别是缺血区心肌)↑coronaryarteryrelaxation冠脉舒张Oxygensupply↑ventricularwalltension心室壁张力↓subendocardialvascularresistance心内膜下血管阻力↓ventricularpressure心室内压↓bloodflowfromtheepicardialtoischemi

7、czoneofendocardial血液从心外膜流向心内膜缺血区coronarysteal冠脉窃血PharmacokineticPropertiesofNitratesPropertyNGTISDN5-ISMNHalf-life(min)310280Plasmaclearance(L/min)5040.1Oralbioavailability(%)820100RoutesofAdministrationGTNcanbeadministeredbysublingually,inhalation,transde

8、rmalorbuccal.It’snotsuitableformaintenancetherapy.IVnitrogylcerincanbeusedtotreatsevererecurrentunstableangina.GTN可吸入、颊部、透皮或舌下含服；作用时间短，不适合维持治疗;静注用于不稳定型的严重复发。bidQd5-ISMNisnotsubjecttofirst-passmetabolismandis1