抗心绞痛药课件.pptxVIP

抗心绞痛药 Antianginal DrugsAntianginals Types of Angina 1、Stable angina (稳定型） 冠脉硬化，劳累时发作 Therapeutic rationale: Decrease cardiac load and oxygen consumption 2、Variant angina（变异型） 冠脉痉挛，夜间/清晨时发作。 Therapeutic rationale: Decrease vasospasm of coronary vessels3、Unstable angina （不稳定型） 上二者兼有 Therapeutic rationale: Inhibit platelet aggregation and thrombus formation, decrease cardiac load and vasospasm of coronary arteries* 抗血小板药、溶栓药、吸O2、阿片以减轻疼痛并降低过高的交感N张力和ACEI等。 Pathophysiology of angina pectoris An imbalance between myocardial oxygen demand and oxygen suppliedEjection timeIn Common Used Drugs 硝酸酯类 Organic nitrates (Nitrate esters)?受体阻断药 ?-Blocker钙拮抗药 Calcium Antagonist硝酸酯类 Organic nitrate 硝酸甘油 nitroglycerinI. Effects：1. 扩张小V ： ? 回心血量? ? 心室容积??室壁肌张力? ? 心肌耗氧? ?改善心肌血流分布：对穿透心肌的血管压迫力? ? 心内膜下供血? 2. 扩张小A ? 外周阻力? ? 射血t? ? 耗O2?3. 扩张较大的冠状血管? 血从输送血管经侧枝血管?更多的分流到缺血区?改善缺血区血供 图1. * 无冠脉窃流 (coronary steal) 输送血管阻力血管Before nitrates administration After nitrates Mechanism of Action 硝酸酯类在SMC内 ? 被巯基还原成 ? NO 或硝基硫醇类 ? ?GC ? cGMP? ?Vessel Dilatation图2. GC：guanylate cyclase 鸟苷酸环化酶Endogenous NO produced by vascular endothelium.Ach and Bradykinin etc. are the endothelium dependent vasodilators Sodium Nitroprusside is another NO donor.Clinical Uses 1、各型心绞痛的防治2、急性心梗 （Acute myocardial infarction）3、充血心力衰竭（CHF）Variant angina This figure illustrates coronary artery vasospasm. The patient had been complaining of intermittent chest pain during at rest. In the top frame a localized narrowing of a long segment of the proximal right coronary artery is apparent. ?In the bottom frame the abnormality has been corrected by intracoronary nitroglycerin. The response to nitroglycering confirms that the narrowing resulted from coronary vasospasm or Prinzmetals angina. Adverse effects：1、血管扩张导致： 面红、头痛、眼内压↑、体位性 低血压（药物相互作用-降压药）、反射性心脏↑ 2、高铁血红蛋白血症 3、Tolerance Mechanism of Tolerance ： -SH depletion 扩血管 ? ?RAAS 对策：补充- SH供体： 甲硫氨酸、 N-乙酰半胱氨酸、卡托普利间歇用药、联合用药 硝酸异山梨酯 (消心痛) isosorbide dinitrate特点：长效硝酸酯类 作用弱、慢、久 预防发作β-B