基础医学各论I：抗心绞痛药

1、抗心绞痛药抗心绞痛药Whats Angina pectorisCause and the classification of angina pectoris :Atheromatous obstruction of the large coronary vessels (atherosclerotic angina, classic angina); 劳累性心绞痛：稳定型，初发型，恶化型劳累性心绞痛：稳定型，初发型，恶化型Transient spasm of localized portions of the large coronary vessels (angiospastic or va

2、riant angina); 自发性心绞痛：卧位型，变异型，急性冠脉功能不全，梗死后心绞痛自发性心绞痛：卧位型，变异型，急性冠脉功能不全，梗死后心绞痛Both causes 混合性心绞痛混合性心绞痛Primary cause of angina pectoris: In classic angina, the imbalance occurs when the myocardial oxygen requirement increases; “angina of effort”In variant angina, oxygen delivery decreases as a result of

3、 reversible coronary vasospasm. “vasospastic or Prinzmetals angina变异型心绞痛变异型心绞痛”oxygen requirement oxygen supply imbalanceTreatments: Non-drug treatment:经皮冠状动脉成形术经皮冠状动脉成形术(percutaneous transluminal coronary angioplasty, PTCA), 冠脉搭桥术冠脉搭桥术 ( coronary artery bypass graft surgery, CABG ) Drug treatment A

4、nti-platelet agents ACEIs lipid-regulators, Fish oilNitrates & Nitrites (硝酸酯类硝酸酯类 和亚硝酸酯类和亚硝酸酯类) Quick tolerance and cross-tolerance Pharmacokinetic factors govern the choice of agent nitroglycerin- PharmacokineticsLow oral bioavailability (eg, 硝酸甘油硝酸甘油nitroglycerin and 硝硝酸异山梨酯酸异山梨酯isosorbide dinitra

5、te, typically 1020%).Sublingual(舌下舌下) is normally used. Transdermal (透皮透皮)and buccal (经口颊经口颊)absorption from slow release preparations.Amyl(戊基戊基) nitrite and related nitrites can be used with inhalation route.Duration of effect is very brief (unchanged nitrate t1/2=2-8 minutes, partially denitrated

6、metabolites longer t1/2= 3 hrs). So micro-pump is very common in hospital usage.硝酸酯类硝酸酯类(Nitrate esters)Intracellular Ca2+ release，extracellular Ca2+ influxIntracellular Ca2+ The production of PGE or PGI2 and membrane hyper-polarization may also be involved.(viagra) Tolerance : Other nitrates Isosor

7、bide dinitrate Isosorbide-5-mononirate Similar but weaker effect Acting slowly but lasting longer Larger individual variation and more adverse effects选用作用时间相近的，如普萘洛尔与硝酸异山梨醇酯合用- Toxicity, including cardiac arrest, bradycardia, atrioventricular block, and heart failure.Relatively short-acting calcium

8、channel blockers have the potential to enhance the risk of adverse cardiac events.Slow-release and long-acting vasoselective calcium channel blockers are usually well tolerated.Patients receiving -adrenoceptor-blocking drugs are more sensitive to the cardiodepressant effects of calcium channel blockers.Tolerable toxicity: flushing, dizziness, nausea, constipation, and peripheral e