神经系统药理-魏尔清镇痛药

Part12

AnalgesicsOpioidanalgesicsSyntheticopioidanalgesicsOtheranalgesics1精品pptGeneralConsiderationsPain(疼痛)：躯体痛－快痛，慢痛内脏痛情绪反应Analgesia(镇痛)：选择性抑制疼痛感觉，不影响意识和其他感觉2精品pptPainClassificationHeadache(migraine)AcuteChronicPainNociceptiveMixedNeuropathicVisceralDiabeticneuropathy

(DN)Post-herpeticneuralgia

(PHN)Radiculopathy

(RADIC)CancerpainLowbackpainOsteoarthritisRheumatoid

arthritisFibromyalgiaIBSPancreatitisBladderpainNoncardiacchestpainAbdominalpainsyndromeInjuryPostoperativeFlareAnadverseorunpleasantreactionplusthereactionsevokedbyit3精品ppt4精品ppt5精品pptPaingenerationandreactions6精品pptStimulationanddepolarizationofsensorynerveendings7精品pptPain:

peripheralsensoryreflex

8精品pptPeripheralmechanismsofpain9精品pptPeripheralmechanismsofpain10精品pptPrimary&secondaryhyperalgesia11精品pptTheperceptionofsomaticpain12精品pptTheperceptionandconductionofsomaticpain13精品pptConductionpathwaysofpain14精品pptCorticallocationsofpain15精品pptThefMRIimagingofpain16精品pptClassificationofanalgesics：Opioidanalgesics(centrallyacting)

opiates

syntheticagentsAntipyretic,analgesic,andanti-inflammatorydrugs(peripherallyacting)

aspirin,indomethacinOtherdrugs(forspecialtypesofpain)

carbamazepine,atropine,nitroglycerin,etc.GeneralConsiderations17精品pptMorphine吗啡Morphine吗啡Heroin海洛因A.

OpioidAnalgesics18精品pptOpium19精品pptMorphine:Morphus,

theGreekgodofdreams20精品ppt1.Pharmacologicaleffects(1)MechanismsofactionsActingoncentralopioidreceptorsreceptorsreceptorsδreceptorsA.

OpioidAnalgesics21精品pptATPcAMPGiACOpioidReceptorsandEndogenousLigandsδEndorphinEnkephalinDynorphinK+abgabgGi=22精品ppt23精品pptMechanismsofmorphineactions24精品pptPeripheralmechanismsofmorphineactions25精品pptCentralmechanismsofmorphineactions:Paininhibitorysystem26精品ppt(2)CentralnervoussystemeffectsA.Analgesia：maximalanalgesicefficacy；relievingunpleasantsensation;

euphoniaandpotentialofdependenceB.Depressionofrespiration:

reducingthesensitivityofrespiratorycentertoCO2C.DepressionofcoughreflexD.Othercentraleffects:miosis,emesisA.

OpioidAnalgesics27精品ppt(3)CardiovasculareffectsA.Posturalhypotension：Releasinghistamine;depressingCVScentersB.Increaseofintracranialpressures：RespiratorydepressionbrainCO2increase

vasodilatationinthebrainA.

OpioidAnalgesics28精品ppt(4)EffectsonsmoothmusclesA.GItract：Contispation:increasingrestingtoneofsmoothmusclesandsphincters,decreasingpropulsiveperistalsisandsecretions;Biliarytract：Oddi’ssphinctercontraction,increasingthepressureinthebiliarytractB.Respiratorytract：bronchoconstrictionC.Urinarytract：increasingvesicalsphinctertoneurinaryretentionD.UterusA.

OpioidAnalgesics29精品ppt(5)OthereffectsA.ImmunedepressionB.EndocrineeffectsA.

OpioidAnalgesics30精品ppt2.Clinicaluses(1)AnalgesiathepainofhighintensityandthepainofterminalillnessCautions:

a)obscurethesymptomsandtheprogressofthedisease;b)dependenceoraddiction;c)biliarycolic:combinedwithatropined)notusedforlong-termifnoclearindicationsA.

OpioidAnalgesics31精品ppt(2)Cardiacasthma(acuteleftventricularfailure)

Asanadjuvanttreatment

A.Vasodilatation:afterload

B.Sedation:anxiety

C.Respiratorydepression:breathingslowlyanddeeply(3)DiarrheaMixturecontainingopiate

A.

OpioidAnalgesics32精品ppt3.Adverseeffects(1)Sideeffects(2)Toleranceanddependence

psychologicalandphysicdependence:addiction

withdrawalsyndromesorabstinancesyndromesA.

OpioidAnalgesics33精品ppt(3)Acuteintoxication

coma,respiratorydepression,hypotension,pinpointpupils

reversedbynaloxone,anopioidreceptorantagonist(4)Contraindicationslaborandlactation;bronchialasthmaandcorpulmonal;increasedintracranialpressures;severehepaticdamageA.

OpioidAnalgesics34精品ppt35精品pptMorphinetoxicitycanbereversedbyopioidreceptorantagonist(naloxone)36精品pptAnalgesia;centralantitussiveCodeine可待因A.

OpioidAnalgesics37精品pptB.

SyntheticAnalgesicsPethidine哌替啶Dolantin度冷丁38精品pptPethidineMorphineStructuresofnaturalopioid(morphine)andsyntheticanalgesics(pethidine)哌啶环中的叔氮与叔氮相隔两个碳原子的季碳与季碳相连的苯环39精品pptB.

SyntheticAnalgesicsPethidine1.PharmacologicaleffectsSimilartomorphinebutineffectiveforcoughanddiarrhea,anditsmetabolitenormeperidinehascentralstimulanteffects.2.Clinicalusesanalgesia;cardiacasthma;

preanestheticmedicationorartificialhibernation;

3.Adverseeffects

similartomorphine,convulsion(overdose)40精品pptFentanyl（芬太尼）highefficacycombinedwithdroperidol:neuroleptanalgesiaMethadone（美沙酮）orallyeffectivelong-actingalsousedfordisplacementinheroinormorphinedetoxicationB.

SyntheticAnalgesics41精品pptPentazocine（喷他佐辛,镇痛新）receptoragonist/receptorpartialagonist;low-narcoticanalgesicdrugpsychotomimeticeffects:anxiety,nightmare,hallucinationsTramadol（曲马朵）

RelativelyweakefficacyanddependenceB.

SyntheticAnalgesics42精品pptSummaryofopioidreceptorli