痛第23章_精品文档.ppt

1、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.Glycery

2、l 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.O

3、ver 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 i

4、s 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 ventric

5、ular 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 zoneNorma

6、l zonePharmacokinetics of GTN 1.High lipophilic property2.Extensive first-pass effects for P.O.:3.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 pat

7、ches,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.

8、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（

9、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（con

10、trolled-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,hig

11、h 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

12、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.Prote

13、ction 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

14、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

15、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

16、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