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China Medical University Chapter 32 Antianginal drugs Cardiovascular pharmacology Angina Angina is a specific type of pain in the chest caused by inadequate blood flow through the blood vessels (coronary vessels) of the heart muscle (myocardium). So coronary flow does not meet the metabolic needs of the heart, a radiating chest pain --anginal pain –results . The heart as pump Left anterior descending pathology Contractility Coronary Oxygen Oxygen Blood Flow Supply Demand Heart Rate LV Wall Tension Systolic LV BP Volume Ischemia LV Dysfunction Chest Pain Arrhythmias Causes of angina • Coronary atherosclerosis • Coronary artery spasm • Transient platelet aggregation and coronary thrombosis • Endothelial injury causing the accumulation of vasoconstrictor substances. • Coronary vasoconstriction following adrenergic stimulation Classification of angina : Stable or classical angina is due to fixed stenosis 狭窄of the coronary arteries, and is brought on by exercise and stress. Unstable angina can occur suddenly at rest, and becomes progressively worse, with a increase in the number and severity of attacks. Variant angina occurs at rest, at the same time each day, and usually due to coronary artery spasm . Classifications of treatment medicine • Nitrate esters : Nitroglycerin Isosorbide dinitrate (IDN) 硝酸异山梨酯 • receptor blocker : Propranolol Atenolol Metoprolol • Calcium channel blockers: Verapamil Diltiazem Nifedipne Unstable angina is treated with: • Aspirin (reduces platelet aggregation) Nitrate esters Nitroglycerin 硝酸甘油 CH 2 O NO 2 CH O NO 2 CH 2 O NO 2 O Isosorbide Dinitrate 硝酸异山梨酯 CH2 Isosorbide -5-Mononitrate 5’-单硝酸异山梨酯 CH2 O NO2 CH CH CH CH O O O O NO 2 CH CH CH CH2 CH O O H CH2 NO2 Nitroglycerin 硝酸甘油 Pharmacological Function: CH2 O Dilatation of the veins CH O and artery decreases preload O and afterload thus the oxygen CH2 demand of the heart Dilatation of the coronary arteries increases blood flow and oxygen delivery to the myocardium. Increase the heart rate NO2 NO2 NO2 Mechanism of action: Nitrate Nitroglycerin are prodrugs, esters NO decomposing to form nitric active oxide (NO), which activates SMC or EC(GC) guanylyl cyclase (GC) ,thereby increasing the levels of cyclic cGMP active guanosine monophosphate cGMP dependent PK(cGMP). Protein kinase G is PKG activated and contractile 2+ inner cell Ca proteins are phosphorylated. Inhibit platelet aggregation and adhesion VSM dilation Route of administration: Nitroglycerin is administered sublingually , and can be given by intravenous infusion or from patches. Indication: Nitroglycerin is given for the prophylaxis预 防 and treatment of angina- Stable angina Adverse effects: The side effects of nitroglycerin include postural hypotension, tachycardia, headache ,flushing and dizziness. Therapeutic notes: To avoid nitrate tolerance, a drug-free period of approximately 8 hours is needed. -receptor blocker • Propranolol 普奈洛尔 • Pindolol 吲哚洛尔 • Timolol 噻吗洛尔 Metoprolol 美托洛尔 Atenolol 阿替洛尔 Pharmacological Function: -blockers block 1- adrenoreceptors in the heart. this causes a decrease in heart rate (slowing of phase 4) in systolic blood pressure in cardiac contractile activity and in myocardial oxygen demand. 1 2) Improve the myocardial metabolism 3) Increases blood flow and oxygen of The ischemia region 4) Promote the oxygen release from the Hb Inhibit platelet aggregation To • Clinical utilization: Stable or classical angina (specially to patient who concurring the fast heart rate and hypertension ) • Unstable angina not suitable to Variant angina receptor (一) α receptor will be predominate coronary artery spasm Contraindications and notes • Related to heart: Bradycardia, hypotention, AV block, and CHF • Asthmatic 哮喘 •β1 receptor up-regulation So slowly reduce the doses Calcium-channel blockers Examples of calcium-channel blockers include Verapamil Diltiazem Nifedipine block L-type calcium channels, thereby reducing calcium entry into cardiac and vascular cells block L-type calcium channels in vascular cells, Pharmacological Function: This decrease in intracellular calcium →reduces cardiac contractility and causes vasodilatation, which results in several effects: Reduced preload due to the reduced venous pressure; Reduced afterload due to the reduced arteriolar pressure; Increased coronary blood flow; Reduced cardioc contractility decreased heart rate anti-sympathetic activity reduced myocardial oxygen consumption Coronary vascular dilatation promote the opening of side branch Inhibit platelet aggregation Increase the supply of blood Protect the ischemic myocardial Clinical uses Treatment of angina Variant angina Verapamil is given for supraventricular arrhythmias others Dipyridamole 双嘧达莫 潘生丁 Nicorandil 尼可地尔 Dipyridamol causes inhibition of adenosine uptake, resulting in the accumulation of adenosine within the tissue. Adenosine is an endogenous vasodilator--the effect is pronounced on arterioles Nicorandil increase the cGMP,active the channel of potassium ,dilate the coronary vessels conjunction use Nitrate esters + Calcium-channel blockers Amlodipine 氨氯地平 络活喜 -receptor blocker + Calcium-channel blockers Nitrate esters+ -receptor blocker N- Nitrate esters B -β -receptor blocker Notes:↑= increase,↓=decrease,→= no change,↓↑= unsure Factor Nitrate esters -receptor blocker Calcium-channel blockers Wall Tenson室壁张力 ↓ ± ↓ LV volume ↓ ↑ ± Ventricular pressure心室压力 ↓ ↓ ↓ rate心 率 ↑ ↓ ± contractility收缩性 ↑ ↓ ± 心内膜/心外膜blood ratio ↑ ↑ ↑ ↑ → ↑ 心室容量 血流比率 the flow of side branch侧枝血流 end