哌替啶的药理作用与作用.ppt

<p>,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,Chapter 19,Analgesics,objective,1.,掌握,吗啡,、,哌替啶,的药理作用与作用,机制、临床应用,不良反应和禁忌症。,2.,熟悉,阿片生物碱类镇痛药的概念、分类,可待因、喷他佐辛、曲马朵、,罗通定、纳洛酮的药理作用和临床用途,.,3.,了解,其他镇痛药的概念与应用特点,Introduction,pain,【,definition,】,1),a common experience;,2)an essential defensive function,3)an unpleasant sensory and emotion,4)with actual or potential tissue,damage.,Pain,function disorders,shock；,Aching feature、part 、paroxysm,Diagnostic gist,（,诊断依据）,Advantage,Disadvantage,Pain,Acute,pain,锐痛,Chronic,pain,钝痛,烧伤、战伤、割伤,头痛、牙痛、关节痛、,神经肌肉痛等,传导慢、定位不明确、伴情绪反应,刺激强、传导快，,定位明确,【,Classification of pain,】,Has an effect on CNS,removes or lessens the sensation of pain.,Classification of drugs,Analgesics,镇痛药,Relieve pain,Antipyretic,(,解热,),、,Analgesic,(,镇痛),Antiinflammatory,(,抗,炎）,NSAIDs,Opioid,analgesics,Section 1,阿片生物碱类镇痛药,麻醉,药品,阿片类：鸦片、海洛因、吗啡,古柯类：可卡因、古柯叶,大麻类：大麻、大麻酚,精神,药品,镇静催眠药：巴比妥类,中枢兴奋剂：冰毒、摇头丸,致幻剂：麦角酰二乙胺,其他,烟草：,酒精：,挥发性有机溶剂：汽油,毒品的分类,名称,主要成分,鸦片,罂粟,海洛因,二乙酰吗啡,冰毒,甲基苯丙胺,摇头丸,二亚甲基双氧苯丙胺,K,粉,氯胺酮,常见毒品的主要成分,Beautiful,poppy,(,罂粟,),Blessing or disaster,？,NOTICE,！,全世界有,10%,的人口卷入了毒,品的生产和消费；,全世界每年约有,10,万人因吸毒,死亡；,全世界每年约有,1000,万人因吸,毒丧失正常智力和工作能力；,世界毒品贸易已经占到世界贸,易的,13%,，仅次于军火贸易,;,poppy,opium,heroin,morphine,morphine,吗 啡,（梦神）,Pharmacokinetics,First-pass elimination is extensive bioavailability is low.,Passes through BBB and placenta（,胎盘,）,barrier.,Excretes,：,kidney,，,secretes in milk,Pharmacological Effects,一、,CNS,1,、,Analgesia,镇痛,2,、,Sedation,镇静,3,、,Cough suppression,镇咳,4,、,Respiratory depression,抑制呼吸,Analgesia,镇痛,Stronger:,5,10mg,Extensive:,various pain,chronic,pain,acute,pain,Longer,：,4,6 hours,镇痛时,意识清醒,其他感觉不受影响,Sedation,镇静,消除焦虑、紧张、恐惧等,欣快感,Decrease anxiety,、,tension and dread.,Euphoria :,contentment,（,满足,）,well-being,（,飘飘欲仙,）,（,欣快,）,Respiratory depression,therapy dosage,:,respiratory rate,and,tid,volume .,toxic dosage,:,1,）,respiratory failure.,2,）,Sensitivity of respiratory center,to CO2.,3,）,(-)respiratory center,Inhibition of cough reflex,Others,Miosis,(,缩瞳)：,“,pinpoint pupils”,is,valuable in the diagnosis,of,opioid,overdosage,.,Cough suppression,二,.Smooth muscle,(1),Constipation,(,便秘,):,（,-,）,CNS,便意迟钝,(+),gastroenteric,smooth muscle,propulsive peristaltic waves,(,蠕动,),(2),biliary,pressure:,constricts,biliary,smooth muscle,biliary,colic,(,胆绞痛,),(3),Urinary retention,(,尿潴留),(4)bronchial SM(+),-induced asthma,(,诱发哮喘);,三,.,Cardiovascular system,(1),Hypotension,(,低血压),:,a.Cause peripheral,vasodilation,.,(,外周血管舒张,),b.,Increase histamine,（,组胺）,release,.,c.,Respiratory depression,CO,2,vasodilation,2.,Intracranial pressure,（,颅内压,）,respiratory depression,CO,2,Cerebral,vasodilation,.,3.,Protections,of,myocardiac,ischemia,simulate ischemic preconditioning,(模拟缺血性预适应),Inhibit,immunoreaction,免疫系统,(,),lymphopoiesis,(,淋巴细胞增殖),secretion of cellular factors,(,),immunoreaction,induced,by HIV.,四,.Others,Morphine,（）,Opioid,receptors,模拟内源性阿片肽作用,增强内源性镇痛系统的功能,analgesia,镇 痛,Mechanism of action,内源性镇痛系统,脑啡肽神经元,脑啡肽,阿片受体,结合,20%,Mechanism of action,morphine,阿片,-R,Opioid,receptors,(2),variety,多型性,阿片受体的亚型主要有四种：,、和 型。,(3),天然底物,内阿片样肽,：脑,啡,肽、,-内,啡,肽、强,啡,肽,confirmation,证实,1973年,三个不同的实验室用高比活性的标记阿,片物质各自证明了脑内阿片受体的存在。,1993年,阿片分子克隆成功。,Clinical Uses,1.,Analgesia,镇痛：其它镇痛药无效的急性锐痛,心梗剧痛：,前提：,BP,正常,机理：镇痛、镇静、扩血管,biliary,colic(,胆绞痛),:,with atropine,一个前提三个机理,2.Cardiogenic asthma,强心甙类,加强心肌收缩力,速尿,减轻心脏负荷,氨茶碱,强心，松弛支气管平滑肌,吗啡,心源性哮喘,治疗,吗啡,扩张外周血管,外阻 心负荷,镇静,消除焦虑恐惧心负荷,呼吸中枢对,CO,2,的敏感性缓解浅快呼吸,Diarrhea from almost any cause,can be controlled.,3.,Diarrhea,Side Effects,Dizziness,nausea,vomiting,constipation,respiratory depression,increased,biliary,tract pressure.,戒断症状,:成瘾性药物反复使用后,停药可出现兴奋、失眠、流涕、流泪、出 汗、震颤、呕吐、腹泻、虚脱、意识丧失等,重复用药后可减轻或消失。,2.,Tolerance and Physical Dependence,成瘾者为获得用吗啡后的欣快感及避免停药后引起的戒断症状,常不择手段以获得吗啡.,毁灭自己：剜骨剃髓不用刀，,请君夜吸相思膏,祸及家庭：烟瘾一来人似狼，,卖儿卖女不认娘,危害社会：,毒品的危害,因毒瘾发作疼痛难忍砍断自己手指。,吸毒瘦弱不堪,珍爱生命,远离毒品,!,Yes to life,，,no to drugs!,6.26,国际禁毒日,addiction therapy,1.,替代疗法：,使用成瘾性较轻的阿片类药物进行治疗。,-,美沙酮和二氢埃托啡联合治疗，交替使用，6-7天基本脱瘾。,2.,外科手术法：,开颅戒毒术，钻颅切断脑毒隐细胞,.,1,）又称冷火鸡法或干戒法。,2,）强制中断吸毒者的毒品供给,使其戒断症状自然消退而达到脱毒目的,.,自然戒断法,1,）是指采用针灸、理疗仪等,2,）减轻吸毒者戒断症状反应的,一种戒毒方法。,自然戒断法,morphine poisoning,cause coma,、,pinpoint pupil,、,respiratory depression,.,naloxone,纳洛酮,、,nikethamide,尼克刹米,、,artificial respiration.,Overdosage,吸,O2、,Treatment,impaired hepatic function patients,Delivery,（,分娩,）,breast-feeding women,（,哺乳,）,bronchial asthma,（,支喘,）,pulmonary heart disease,（,肺心病,）,High intracranial pressure patients,（,颅内压升高）,Contraindications:,禁忌症,P.178,codeine,可待因,1.analgesic and,antitussive,action,morphine,addiction,morphine,；,2.use：,1）,relief of mild and moderate pain;,2,）acute dry cough,.,3.side action,characteristics,Section 2,Synthetic analgesic drugs,Pethidine,哌替啶,Pethidine,哌替啶,1.Effects and addiction all,morphine;,2.Onset rapid and duration short;,3.Produces less constipation;,action and uses,度冷丁、,dolantin,1.Analgesia,a Used to trauma(,创伤),operation,late stage of cancer.,b.Used with atropine to treat visceral colic.,c.Before delivery the pregnant women should not use,meperidine,.,clinic uses,2.,Premedication,for surgical,operation,(,麻醉前给药),.,3.,Artificial hibernation,(,人工冬眠),dolantin,+,Chlorpromazine,+,promethazine,（,异丙嗪）,4.,Cardiogenic,asthma,Adverse effects,Low dose,:Sweating,、,Dry mouth,、,Nausea,、,Vomiting,、,tachycardia and postural hypotension.,Large dose,:respiratory depression.,Contraindications,同,Morphine,fentanyl,芬太尼,1,）,Analgesic potency and respiratory depressant properties,morphine.,2,）,Used for acute pain;,3,）,neuroleptanalgesia,神经组织镇痛,droperidol,(,氟哌啶醇,),+,fentanyl,Methadone,美沙酮,1),analgesic potency,almost like,morphine.,2)Used for acute pain,.,3)often substituted for other,opioids,for treatment of physical,dependence.,pentazocine,喷他佐辛(镇痛新),1,）,the analgesic potency and,inhibition of respiration,morphine,2,）,Inhibits receptor,and has less,dependence.,3,）,Used for moderate pain.,非麻醉品,dihydroetorphine,二氢埃托啡,1,）镇痛作用为吗啡的,500-1000,倍,2,）作用仅2小时.,3,）成瘾性较吗啡轻.,4,）常用于镇痛或吗啡类毒品成瘾,者的戒毒。,Section 3 Others,延胡索乙素、罗(颅)通定,(,Corydolis,ambigua,、rotundine,),1,）,analgesic effect,meperidine,.,2,）,Used for chronic dull pain,3,）,No effect on sharp pain.,No addiction.,Section 4,Opioid,Antagonists,纳洛酮、纳曲酮,(,naloxone、naltrexone,),1,）,Block,opioids,receptors.,2,）,Used for,opioid,and other analgesics,acute intoxication.,3,）,Use for diagnosis of addiction.,（,纳洛酮催瘾实验）,小结,Analgesic,mechanism,Pharmacological Effects,Clinical Uses,questions,Please describe the,effects、clinical uses and adverse reactions,of,morphine.,2.,List,the major uses of,dolantin,.,3.,心源性哮喘和支气管哮喘能否使用吗啡？简述理由。,good bye,Thank you,</p>