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Pharmac和ologyChapter颜光美药理学抗心绞痛药
第 26 章 抗心绞痛药 Key concepts Angina pectoris is characterized by chest pain caused by insufficient coronary blood flow to meet the oxygen demands of the myocardium. The hallmark symptom of angina is a sudden, severely pressing substernal pain radiating to the left arm. The imbalance between the oxygen demand and oxygen utilization may result from the obstruction of blood vessels caused by atherosclerotic lesions or from a spasm of the vascular smooth muscle. All the antianginal drugs exert their effects by decreasing the demand of O2 of the myocardium and/or increasing the supply of O2 to the ischemic region of myocardium through different mechanisms. Key concepts In treating patients with stable angina, three classes of drugs (nitrates, β-receptor blockers, and calcium channel blockers) are equally effective for relief of anginal symptoms. Variant angina (also called Prinzmetals angina) caused by spontaneous coronary spasm rather than by increases in myocardial O2 requirements, is able to be controlled by organic nitrates or calcium channel blockers, but β-receptor blockers are contraindicated. Nitrates decrease coronary vasoconstriction or spasm and increase perfusion of the myocardium by relaxing coronary arteries. β-receptor blockers decrease the O2 demands of the heart. Calcium channel blockers reduce cardiac contractility and cause vasodilatation. Nitrates are often used in combination with β-receptor blockers in order to decrease adverse reactions and increase treatment efficacy. 决定心肌供O2与需的因素O2 心绞痛 抗心绞痛药物 1.硝酸酯及亚硝酸酯类:如硝酸甘油等。 2.β受体阻断药:如普萘洛尔等。 3.钙转运阻断药:如硝苯吡啶、硫氮草酮、心可定等。 一、硝酸酯和亚硝酸类 硝酸甘油(Nitroglycerin) 药理作用: 基本作用:直接松弛各种平滑肌。松弛血管平滑肌最显著,所松弛 的节段与剂量有关 二、β受体阻断药 普萘洛尔(Propranolol) [作用] 本药主要通过阻滞过多的儿茶酚胺兴奋β受体,减慢心率,减弱收缩力,从而减少心作功和心耗氧达到抗心绞痛作用。 β受体阻断药抑制心收缩力,使心室容积增大,射血时间延长,从而增加心肌耗氧量。这是不利的方面,但综合作用是有利因素占优势。 普萘洛尔(Propranolol) [用途] 抗心绞痛、降血压、抗心律失常、抗甲亢(一药多效。硝酸甘油和β受体阻断药合用抗心绞痛优点!)。 [不良反应] 心动过缓、低血压及诱发或加重心力衰竭。对心传导阻滞和支气管哮喘一般禁用。 三、钙拮抗药
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