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Antiangina Pectoris Agents 281 Brief IntroductionCoronary heart disease Teatment of Angina Pectoris:1.Dilation of blood vessels2.Reducing blood lipid level3.Reducing blood glucose level4.Antithrombosis5.Anti-painContractilityHeart RateCardiac Wall TensionPreload and Afterload1.Beta-Blockers2.Glyceryl trinitrate 3.L-CB Anti-angina pectoris AgentsCoronary heart disease prescription:Nitrate estersAntihypertensive agentsAntilipemic agents 2 Nitrate Vasodilator 1.In blood vessel wall,GTN produce NO with the help of mitochondrial aldehyde dehydrogenase(mtALDH)2.NO induce dilation of blood vessels3.Over dose/long time administration of GTN also can induce active oxygen and induce tolerance.Blood vessel dilation mechanismGTN:Glyceryl NitratePETN:pentaerythrityl tetranitrate ISDN:isosorbide dinitrate ISMN:isosorbide-5-mononitrate Soluble guanylyl cyclase(sGC)is the only known receptor for NO.It is soluble,pletely intracellular.It is most notably involved in vasodilation.In humans,it is encoded by the genes GUCY1A2,GUCY1A3,and GUCY1B3Effects of GTN1.To lower the oxygen demand of the heart2.To dilate coronary artery and increase the ischemia area blood irrigation3.To decrease the left ventricular endocardial pressure,increase the endocardial blood supply and improve the adaptability of the left ventricle4.To protect ischemic cardiac cells:NO-induced PGI2 and calcitonin gene-related peptides(CGRP)5.Anti-arrythmia and Inhibition of platelet aggregationBefore GTNAfter GTNIschemic zoneNormal zonePharmacokinetics of GTN 1.High lipophilic property2.Extensive first-pass effects for P.O.:If sublingual route,F is 80%,the onset of action is 1 to 2 minutes,and the duration of action is 20 to 30 minutes.INDICATIONS OF GTN1.Acute angina pectoris attack2.Prophylaxis of angina pectoris GTN patches,ointment 3.Acute myocardial infarction 4.Congestive heart failure Isosorbide Dinitrate(消心痛)消心痛)Isosorbide Mononitrate(异乐定)(异乐定)1.Angina Prevention2.Heart Failure TreatmentP.O.Weak Tolerance医大一院有大夫:高血压合并心绞痛,医大一院有大夫:高血压合并心绞痛,异乐定异乐定 +福新普利?福新普利?Ads of GTN1.Postural hypotension2.Reflex tachycardia3.Throbbing headache4.Flushing,Dizziness5.High Intracerebral/Intraocular Pressure6.Tolerance目前常用于心绞痛的药物:目前常用于心绞痛的药物:异乐定(欣康,硝酸酯类)异乐定(欣康,硝酸酯类)消心痛(硝酸酯类)消心痛(硝酸酯类)心痛定(硝苯地平)心痛定(硝苯地平)圣通平(硝苯地平缓释)圣通平(硝苯地平缓释)拜新同(拜新同(硝苯地平控释)硝苯地平控释)波依定(非洛地平)波依定(非洛地平)络活喜(氨氯地平)络活喜(氨氯地平)司乐平(拉西地平)司乐平(拉西地平)异搏定(维拉帕米)异搏定(维拉帕米)比索洛尔(比索洛尔(Beta1阻滞剂,选择性最高)阻滞剂,选择性最高)贝他乐克(贝他乐克(Beta1阻滞剂)阻滞剂)阿替洛尔(阿替洛尔(Beta1阻滞剂)阻滞剂)心得安(心得安(Beta阻滞剂)阻滞剂)蒙诺(蒙诺(ACEI,福新普利),诺迪康(藏药),福新普利),诺迪康(藏药)万爽力(新型药物,改变心肌代谢)万爽力(新型药物,改变心肌代谢)The current commonly used in angina medicine:Xinkang,nitratesIsosorbide dinitrate(nitrate)Nifedipine Nifedipine(slow-release)Nifedipine(controlled-release)Felodipine)AmlodipineLacidipineVerapamil Bisoprolol(Beta1 blockers,the highest selectivity)Betaloc(Beta1 blocker)Atenolol(Beta1 blocker)Propranolol(Beta blocker)Fosinopril(ACEI),Nuodikang(Medicine)Trimetazidine(changes in myocardial metabolism)Bisoprolol(Bisoprolol,Beta1 blockers,high selectivity)Metoprolol(Beta1blockers)Atenolol(Beta1 blockers)Propranolol(Beta blockers)3 Beta-R Blockers 1.To lower heart rate,V-pressure and contractility2.To slow fat decomposition3.To increase V-volume 4.To contract coronary arteries(Propranolol)-blockers is effective against the stable angina pectoris not in variant angina pectoris.和硝酸之类的区别?和硝酸之类的区别?For Angina Pectoris:Beta Blockers+GTN?Contraindications of Beta-Blockers:1.Asthma2.Heart Failure3.Bradycardia4.Hyperlipidemia5.Variant Angina4 Ca2+Channel Blockers 1.Reduction of myocardial oxygen demand?2.Dilation of coronary vessels 3.Protection of ischemic myocardial cell4.Inhibition of platelet aggregation 1.Nifidipine:variant angina2.Nifedipine+-blockers?3.Verapamil,diltiazem:variant,stable,and unstable angina pectoris.Summary 1.Acute attacks of angina are treated with:Sublingual nitrates Nifedipine 2.Acute anginal pain is treated with morphine 3.Stable angina is treated with Long-lasting nitrates -adrenergic receptor blockers Ca2+channel blockers 4.Unstable angina is treated with:Aspirin Heparin 疏血通,金纳多等疏血通,金纳多等病例病例 高血压合并心绞痛高血压合并心绞痛一一职职业业高高中中教教师师,男男7676岁岁(退退休休)。当当年年4545岁岁时时候候,患患高高血血压压,主主要要靠靠复复方方降降压压片片治治疗疗。随随着着时时间间的的推推移移,药药物物逐逐渐渐失失效效,并并患患有有冠冠心心病病。某某“地地方方小小医医院院”处处方方卡卡托托普普利利、复复方方降降压压片片(北北京京0 0号号类类似似)和和心心痛痛定定(硝硝苯苯地地平平片片)。后后来来发发生生脑脑梗梗塞塞,经经治治疗疗,基基本本恢恢复复。最最近近感感到到头头疼疼,血血压压升升高高,来来到到中中国国医医大大一一院院心心血血管管内内科科。患患者者及及其其家家属属,告告诉诉大大夫夫上上述述降降压压药药物物已已经经使使用用多多年年,效效果果不不理理想想,希希望望换换药药。大大夫夫将将如如何何处处方?方?早晨:替米沙坦(早晨:替米沙坦(35h),阿替罗尔(),阿替罗尔(24h)晚上:贝尼地平(晚上:贝尼地平(24h,抗心绞痛),小剂量阿司匹林(间隔半小时),抗心绞痛),小剂量阿司匹林(间隔半小时),饭后。你认为处方是否合理,为什么?饭后。你认为处方是否合理,为什么?复方降压片:复方降压片:本本品品为为复复方方制制剂剂,其其成成分分为为每每片片含含:利利血血平平0.032mg0.032mg,氢氢氯氯噻噻嗪嗪3.1mg3.1mg,维维生生素素B61.0mgB61.0mg,混混旋旋泛泛酸酸钙钙1.0mg1.0mg,三三 硅硅 酸酸 镁镁 30mg30mg,氯氯 化化 钾钾 30mg30mg,维维 生生 素素B11.0mgB11.0mg,硫硫酸酸双双肼肼屈屈嗪嗪4.2mg4.2mg,盐盐酸酸异异丙丙嗪嗪2.1mg2.1mg,辅料适量。辅料适量。患患者者女女性性,8282岁岁,有有典典型型的的劳劳力力型型心心绞绞痛痛发发作作史史,口口含含硝硝酸酸甘甘油油均均可可以以迅迅速速缓缓解解。患患者者于于20062006年年7 7月月1515日日5 5 pmpm呕呕血血约约400 400 mlml后后突突发发心心前前区区剧剧烈烈疼疼痛痛,经经查查是是胃胃底底静静脉脉曲曲张张破破裂裂,查查心心电电图图示示:心心房房纤纤颤颤,伴伴快快速速心心室室率率,普普遍遍导导联联STST压压低低,反反复复含含服服硝硝酸酸甘甘油油无无效效,即即刻刻输输血血800 800 mlml后后患患者者心心前前区区疼疼痛痛症症状状缓缓解解,复复查查心心电电图图示示:窦窦性性心心律律,心心肌肌缺缺血血较较前前好好转转。患患者者病病情情稳稳定定后后于于20062006年年7 7月月2727日日出出院院。出出院院后后随随访访3 3个个月月,患患者者未未再再发发呕呕血血及及出出现现持持续续剧剧烈烈心心绞绞痛痛症症 。硝酸甘油为何无效?。硝酸甘油为何无效?止止血血剂剂的的应应用用:酌酌情情选选用用安安络络血血止止血血敏敏或或止止血血芳芳酸酸,加加入入补补液液中中滴滴注注;自自胃胃管管灌灌注注浓浓度度为为80mg80mgL L去去甲甲肾肾上上腺腺素素或或凝凝血血酶酶;胃胃镜镜下下局局部部止止血血可可选选用用喷喷洒洒止止血血剂剂,如如80mg80mgL L去去甲甲肾肾上上腺腺素素或或凝凝血血酶酶;或或者者注注射射止止血血剂剂,如如1 12mg2mg肾肾上上腺腺素素加加入入1010盐盐水水10ml10ml,作分点注射;或高频电凝止血;或微波止血;或激光止血。,作分点注射;或高频电凝止血;或微波止血;或激光止血。病例病例女女,68,68岁岁.因因劳劳累累、情情绪绪波波动动等等诱诱因因致致心心绞绞痛痛发发作作入入院院.经经过过检检查查,诊诊断断为为高高血血压压病病期期、冠冠心心病病、不不稳稳定定型型心心绞绞痛痛.予予抗抗凝凝、扩扩张张冠冠状状动动脉脉、降降压压等等药药物物治治疗疗,病病情情好好转转.于于第第3 3日日晨晨患患者者进进食食油油条条时时突突然然出出现现胸胸闷闷、气气短短、心心前前区区针针刺刺样样疼疼痛痛,被被迫迫停停止止进进餐餐.急急查查心心电电图图:、aVFaVF导导联联中中T T波波压压低低,S-T,S-T段段斜斜形形下下移移,心心率率54/min54/min,确确诊诊为为心心绞绞痛痛发发作作。如何用药物治疗?如何用药物治疗?即给予吸氧、吗啡静脉注射、舌下含服速效救心丸即给予吸氧、吗啡静脉注射、舌下含服速效救心丸1010粒等粒等治疗治疗,4,4分钟后缓解分钟后缓解.之后连续之后连续2 2日均在进食馒头、馄饨过程日均在进食馒头、馄饨过程中出类似症状中出类似症状.改流质膳食配合治疗后改流质膳食配合治疗后,心绞痛未再发作心绞痛未再发作,1,1周后出院周后出院速速效效救救心心丸丸是是治治疗疗冠冠心心病病心心绞绞痛痛的的必必备备良良药药,由由川川芎芎、冰冰片片、麝麝香香,蟾蟾酥酥等等名名贵贵中中药药组组方方和和西西药药硝硝酸酸甘甘油油。独独特特的的配配方方、高高新新技技术术的的应应用用及及先先进进的的剂剂型型等等多多方方面面突突出出的的优优势势,使使速速效效救救心心丸丸既既具具备备了了西西药药高高效效、速速效效的的特特点点,又又继继承承了了中中药药标标本本兼兼治治、毒毒副副作作用用小小的的优优势势,长长期期服服用效果会更加显著。用效果会更加显著。
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