神经阻滞镇痛术PPT课件.ppt

Analgesics Zhang Bin 1 pain a Acutepain sharppain b Chronicpain dullpain 2 Paintransmissionpathway Noxiousstimuli Primaryafferentfibres nociceptor Spinalcord Limbicsystem Somato sensorycortex moodeffect theaffectiveaspectofpain thesensoryaspectofpain Dorsalhorn 3 Drugtreatmentofpain cholinoceptor blockingdrugs vasodilatordrugs eg Nitroglycerin Carbamazepine Localanaesthetics 4 Cortex Spinalcord Dorsalhorn PGs K H BK 5 HT NSAIDs Opioids Sitesofactionofdifferentdrugs 5 opioidanalgesics narcoticanalgesic addictiveanalgesics 6 Opium 阿片 isthedriedexudateobtainedfromunripeseedpodsofthepoppyPapaversomniferum containingmorphine codeine andotheralkaloidsubstances Opiate 阿片剂 meansthatasubstanceisextractedfromopiumorissimilarinstructuretonaturalsubstancespresentinopium Opioid 阿片样物质 isatermthatdesignatessubstancesthatarenotderivedfromopium Itrefersparticularlytoopioidpeptides i e endogenouscompoundsthatbindtoopioidreceptorsandmimictheeffectofmorphine likecompounds Widelyuseterm 7 Opium Theflowerofpapaver Opium 阿片 8 Opiate 阿片剂 MorphineCodeinePapaverine 罂粟碱 9 structure activityrelationship 海洛因 吗啡 纳洛酮 10 Opioid 阿片样物质 Endogenousopioidpeptides Enkephalins Endorphins Dynorphins Orphanin 11 1992 1973 1962 1975 analgesicsiteislaminaeIIIofperiventricularandperiaqueductalgrayarea putforward receptors foropiateanalgesicsinbrain isolatedthefirst endogenousopioidpeptide andnamedenkephalin Clonedopioidreceptors Researchhistory 12 Opioidreceptors Gprotein coupledreceptors 13 Opioidreceptors supraspinalanalgesia sedation euphoria dependence respiratorydepression miosis spinalanalgesia sedation dysphoria 烦躁不安 hallucination spinalanalgesia sedation euphoria dependence respiratorydepression 14 Spinalcord Dorsalhorn enkephalins Ca2 Ca2 Presynapticterminal Postsynapticneuron enkephalins Thecellularmechanisms 15 enkephalins Presynapticterminal Postsynapticneuron Thecellularmechanisms 16 Morphine receptors OpenK channel CloseCa2 channel 抑制冲动传导 Ach NA Glu 5 HT Prelease presynaptic postsynaptic Excitability Thecellularmechanisms 17 Thecellularmechanisms Presynapticinhibition activationofopioidreceptorsonpresynapticnerveterminals CloseCa2 channel decreaseCa2 input andtherebyreducetransmitterrelease Ach NA Glu 5 HT P Postsynapticinhibition activationofpostsynapticopioidreceptors OpenK channelsonpostsynapticneurons increaseK output andtherebycausehyperpolarizationandthusreducepostsynapticneuronalexcitability 18 Descendingpaininhibitorypathways Localinhibitoryinterneuroninspinalcord Ascendingpaintransmissionpathways Endogenousopioidpeptides 19 Pharmacologicalactions CNSSmoothmuscles3 Cardiovascularsystem 20 1 CNSeffects principaleffectsAnalgesiaSedation euphoriaRespiratorydepressionCoughsuppressionOthers miosis nausea hormone 21 1 Analgesiainsensitive musclespasmspain deafferentationpainpartiallysensitive nervepain CNScompressioninjury bonecancersensitive myocardialinfarction othertypesofcancersrelieveanxietyanddistress toleranceofpain 1 CNS 灼性神经痛 causalgia 系指在明确的神经损伤后 与损伤神经支配范围相一致的区域内出现的以剧烈灼样疼痛主要症状 表现为痛觉异常 痛觉过敏 交感神经机能障碍 血流障碍 出汗异常 骨 肌肉萎缩 有时表现出水肿性改变的慢性顽固性疼痛综合征 22 2 Sedationandeuphoria drowsinessandcloudingofmentation sleepinducedandarousedeasily Euphoria asenseofcontentmentandwell being Sedation themainreasonfordrugabuse Site limbicsystemandlocusceruleus 23 respiratoryrate tidalvolumethemostcommoncauseofdeathfromacutepoisoninginfluencedbystimulusMechanisms thesensitivityofrespiratorycentertoincreasedCO2tension 3 Respiratorydepression 24 4 Coughsuppression antitussiveeffectbyinhibitingcoughcenter codeine 5 OtherCNSeffects Miosis pinpointpupilsNauseaandvomiting CTZ musculartension 限制胸廓活动 影响呼吸Hormone LH FSH prolactin GH ADH 25 2 SmoothmusclesystemGastrointestinalsystemBiliarytractUrinarysystemgenitalsystem 26 1 Gastrointestinaltract delayspassage secretionofdigestivegland indigestion centralinhibition acallofnaturedefecationreflex GITtone GITmotility absorptionofwater 27 biliarycolic constrictbiliarysmoothmuscleconstrictOddi ssphincter pressureinthebiliarytract 2 Biliarytract 28 3 Urinarytract constrictureteralsmoothmusclebladdersphinctertone urinaryretention uterinetone prolonglabor 4 Genitaltract 29 orthostatichypotension Mechanisms releaseofhistaminevasomotorcenter 3 Cardiovascularsystem 1 peripheralarterialandvenousdilatation 2 intracranialpressure secondarytorespiratorydepression 30 Clinicaluses AnalgesiaCardiacasthmaAntidiarrheaAntitussiveCombinedanesthesia 31 Analgesiaterminalcancermyocardialinfarctionrenalandbiliarycolic atropine trauma burn operation atregulartimeandquantity 32 2020 1 7 33 Pulmonaryedema dyspnea Acuteleftventriculardysfunction shortofbreath respiratorycenter CO2retention anxietyanddistress Alveolarhypoventilation Cardiacasthmaandmorphinetherapy 2 Cardiacasthma oxygenconsumption 34 1 Mechanisms peripheralarterialandvenousdilationpreloadandafterloadpulmonaryedema sedationanxietyanddistressoxygenconsumption thesensitivityofrespiratorycentertoCO2shortnessofbreath Cardiacasthma 35 Opioidanalgesicdrugs Morphine 吗啡 Heroin 海洛因 二醋吗啡 Codeine 可待因 Pethidine 哌替啶 Methadone 美沙酮 Fentanyl 芬太尼 buprenorphine 丁丙诺啡 Tramadol 曲马多 36 Morphine 1803Serturnerisolatedapureactivealkalinesubstancefromopium Heproposedthename morphine foritafterMorpheus 37 absorption excretion distribution freedrug blood liver iv Bioavailability25 30 metabolism 38 美施康定 硫酸吗啡缓释片 1 强效 作用持续12hr 主要用于晚期癌症患者第三阶梯止痛 2 抑制呼吸 可引起恶心 呕吐 便秘及排尿困难 长期应用可产生耐受性 身体依赖性和成瘾性 39 Heroin diamorphine Semisyntheticsubstance prodrugofmorphineMorelipidsolublethanmorphineMorerapidonset 德国拜尔公司heroin在德文中意为英雄万能药药品转变为毒品白粉 40 Codeine higheroralefficacy2 lowerefficacythanmorphine3 useasantitussive severedrycough 联邦止咳露 麻黄碱 可待因 氯苯那敏 氯化铵 注意事项 不宜用于痰多粘稠者 连续应用不宜 2周 因久用可成瘾 7岁儿童禁用 41 Pethidine dolantin WeakerpotencythanMorphine noantitussiveactionMorerapidonsetandshorterduration 2 4h thanmorphineMetabolite normeperidine convulsionLyticcocktail 42 Methadone 1 syntheticcompound equalanalgesiatomorphine2 milderabstinencesyndrome3 routinelyusedindetoxificationofmorphineaddicts 43 Fentanyl 1 moreanalgesicpotentcythanmorphine 2 rapidonsetandshortdurationofaction3 fentanyl alfentanil remifentanil adjunctivedrugforgeneralanaesthesia4 Fentanyl Droperidol 氟哌利多 neuroleptanalgesia 神经阻滞镇痛术 Usedforminorsurgery 5 breakthroughcancerpain 44 口腔经粘膜芬太尼拘橼酸盐 OralTransmucosalFentanylCitrate OTFC Fentanyllollipop ACTIQ 芬太尼口腔粘膜贴片 Fentanylsublingualtablets ABSTRAL 芬太尼透皮贴剂 Fentanyltransdermalsystem 多瑞吉 highlipid soluble 45 Pentazocine agonist partialagonist increasebloodpressureandcausetachycardia NA weakactionon littleaddictiveliabilityprecipitatewithdrawalsyndromeofmorphineabuser 列入非麻醉药品 但久用仍会成瘾 analgesiaandrespiratorydepression weaker 46 Tramadol Atypicalopioid weak activation alsointeractswithmonoaminergicsystems inhibitNAand5 HTreuptake Alternativetotraditionalopioidanalgesics 2008年1月1日国家将曲马多列为精神药品进行管理 47 延胡索乙素和罗通定 罗通定为左旋体的延胡索乙素 是有效部分 镇静安定镇痛和中枢性肌肉松弛作用解热镇痛抗炎药 镇痛作用 哌替啶 镇痛作用与阿片受体及前列腺素均无关无明显成瘾性口服后10 30min起效 维持2 5h 对慢性持续性钝痛效果好不影响产程 48 1 Tolerance Adverseeffects largedosesatshortintervalsreadilycrosstolerancefullagonist moreobvious 49 2 Dependence physicaldependence withdrawalsyndromepsychologicaldenpendence compulsivedrug seekingbehavior Adverseeffects 50 身体依赖性 精神依赖性 渴求 戒断综合征 强迫性用药 依赖性 药物滥用 51 药物滥用 drugabuse 非医疗目的反复使用具有依赖性潜能的精神活性物质 体验该物质产生的特殊精神效应 药物误用 drugmisuse 用药适应证选择不当 用量过大 疗程过长等错误用药行为 52 WithdrawalsyndromeofOpioid 53 3 Generaladverseeffects 54 4 AcuteMorphinePoisoning 55 Naloxone petitivefullantagonistforopioidR 2 opioidoverdose reversescomaandrespiratorydepression3 differentialdiagnosisinmorphineabuser precipitateswithdrawalsymptom4 shortt1 2 1h repeatedinjections 56 Contraindications obstetriclabor breastingperiodobstructiveairwaydisease bronchiala