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ANTIANGINAL DRUGS抗心绞痛药 Angina Pectoris Symptom: radiating chest pain Pathophysiology: transient episodes of myocardial ischemia and anoxia coronary flow does not meet the metabolic needs of the heart increase in myocardial oxygen demand, or decrease in myocardial oxygen supply, or by both Factors affecting myocardial oxygen demand and oxygen supply Types of angina (1)Stable angina 稳定性心绞痛 (2)Unstable angina 不稳定性心绞痛 (3)Variant (Prinzmetal’s) angina 变异性心绞痛 Stable Angina Pectoris Angina symptom that recurs under similar circumstances and with similar frequency over time. Symptom usually begins at low intensity, increases over 2-3 minutes, lasts a total of 15 minutes. Unstable Angina Angina of increasing severity, duration or frequency; occurring at rest. may be a precursor of myocardial infartion. Prinzmetal’s (variant) Angina变异型心绞痛 Resulted from transient coronary spasm Usually associated with fixed atherosclerotic lesion, but not always. Usually occurs at rest (often at night). Mechanism of antianginal drugs (1) Decease myocardial oxygen consumption (2) Increase myocardial blood and oxygen supply (3) Antiplatelet, antithrombosis, antiatherosclrosis Nitrate esters硝酸酯类 1.Drugs: Short action Nitroglycerin (硝酸甘油) Long action Isosorbide dinitrate(硝酸异山梨酯) Isosorbide mononitrate(单硝酸异山梨酯) 2. Pharmacological mechanism Nitrate esters NO guanylyl cyclase(鸟苷酸环化酶) cGMP cGMP dependent protein kinase intracellular Ca2+ vascular smooth muscle relaxation 3. Pharmacological actions (1) Decrease myocardiac oxygen consumption Dilate venous decrease blood returning to heart decrease ventricular end-diastolic volume and pressure decrease preload (large dose) Dilate arterial decrease peripheral resistance decrease afterload Disadvantage: compensatory sympathetic reflexes (2) Increase blood supply to ischemia area Dilate large vessels without impairing autoregu
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