版權(quán)說明:本文檔由用戶提供并上傳,收益歸屬內(nèi)容提供方,若內(nèi)容存在侵權(quán),請進行舉報或認(rèn)領(lǐng)
文檔簡介
1
Chapter20Antipyretic-analgesicandAnti-inflammatoryDrugs
(
Non-SteroidalAnti-InflammatoryDrugs,NSAIDs)Thesedrugsrelievethepainassociatedwithinflammation,includingthatfromarthritisandgout.Theyproducetheiranti-inflammatoryactionthroughadifferentmechanism,notasglucocorticoid.Classedintonon-steroidalanti-inflammatorydrugs(NSAIDs)in1974.23Introduction
Non-SteroidalAnti-InflammatoryDrugs,NSAIDsAAntipyretic
(一)PGSynthetase(Cyclooxygenase)inthehypothalamicthermoregulatorycenter
Characteristics:MakingcoolingofbodytempratureoffeverBAnalgesic(一)PGSynthetase(Cyclooxygenase)intheperipheralpainpositionCAnti-Inflammatory(一)PGSynthetase(Cyclooxygenase)intheperipheralinflammatoryposition4AntipyreticActionFebrile:Endogenouspyrogen→CNS→ReleasePG↑→Thermoregulatorycenter→FebrileAntipyretic:
InhibitPGsynthetase,DecreasesynthesisofPG→Hypothermy5
depress
bradykininpain
sensorantipyreticanalgesicpainstimulus
PGsynthesis
sensitization
depress
Mechanisms:Inhibitthesynthesisofprostaglandinsandpreventbradykininfromstimulatingpainreceptors,alsoinhibittherecognitionofpainimpulsesperipherally.AnalgesicAction6Anti-InflammatoryActionMechanisms:
InhibitaprimarypathwayinPGsynthesis.
Summary:ByinhibitingthePGsynthesistoshowantipyretic,analgesicandanti-inflammatoryeffects.78NSAIDsshowdifferenteffectstoCOX-1andCOX-2:ThestrongertheinhibitingeffectstoCOX-1,themoreadversereactionthedrughas;
ThestrongertheinhibitingeffectstoCOX-2,themoreobvioustheantipyretic-analgesicandanti-inflammatoryeffectsthedrughas.9NonSelectivelyCyclooxygenaseInhibitingDrugsASalicylicAcidBAnilineCIndoleDArylAceticAcidEArylPropionicAcidFEnolicAcidGPyrazoleKetonesHAlkylKetonesIIbufenac(Yidingfensuan)
10ISalicylates1838,ExtractedfromPlant,1860,Synthesized,1875,Usedinclinic1899,Aspirinwasused.
Aspirin11【TheInVivoProcess】Absorption
MostabsorbedinsmallintestinebyP.O.,andhydrolyzedassalicylicacidquickly.DistributionPlasmaproteinbindingrateofsalicylatesis80~90%,
Distributedquicklytothewholebody,includearticularcavity、cerebro-spinalfluid、placentaMetabolismIntrahepaticoxidativemetabolism,Smalldoseofaspirin(below
1g)byP.O.willbeeliminatedasfirst-ordereliminationkinetics.12【PharmacologicalActionandUses】
Antipyretic
andAnalgesic
Mediumintensity
Temperaturedropqiuckly
Usedinheadache,toothache,
arthralgia,algomenorrhea,fever,musclepainetc.
Anti-rheumatic
Mediumintensity
Inhibitantigen-antibodyreaction,
Usedinacuterheumatism,rheumatoidarthritis,
13AnticoagulantEffect
Inhibitingplateletaggregation,
Preventingthrombosis。
Usedinthepreventationofcerebralthrombosisandmyocardialinfarction
14【AdverseReaction】AGastrointestinaltractreaction
Seenmostoften
nausea、vomitingetc.BBlockbloodcoagulation
VitKmaypreventCSalicylicacidreaction:
nausea,vomiting
dizziness
、tinnitus、acouesthesia
↓
severe→acid-basedisorders、insanityDAllergicResponse
Urticaria、Aspirinasthma、AllergicshockEReyeSyndrome→SevereliverdysfunctionFNephrotoxicity(ie:kidneytoxicity)15【DrugInteractions】
Competitivelycombinedwithplasmaprotein:
Dicoumarol(shuangxiangdousu)
Tolbutamide
(jiahuangdinniao)etc.
Competitivelyinsecretion:
Furosemide(promoteurine)16IIAniline
Phenacetin20~30%→Aminobenzeneether→
High-IronHband
Hemolyticpoisoningcompound70~80%→acetaminophen→60%combinedwithglucuronicacid→35%combined
withsulfuricacid→less→liverpoisoning
hydroxylcompound17
Acetaminophen
1949,F(xiàn)oundthatthedrughadobviousanti-pyreticandanalgesiceffects.Mostwidelyused.
Medicationforalongtime,maycauseliverandkidneydisorder.18IIIIndole
IndomethacinStronganti-pyreticandanalgesiceffects.Butmostadversereaction.19IVArylAceticAcid
Diclofenac
Strongeranti-pyretic、analgesicandanti-inflammatoryeffectsthanindomethacin.
Adversereactionissimilartoaspirin.RarelyseenliverfunctiondysorderandWBCreduced.
VArylPropionicAcid
Ibuprofen
Adversereactionofgastrointestinaltractislessthanaspirin.Widelyusedintreatingrheumatoidarthritisandosteoarthritis(bonearthritis)
20VIEnolicAcid
Piroxicam
Showeffectsquicklyandlasting.
Usedintreatingrheumatismandrheumatoidarthritis.21VIIPyrazoleKetones
Phenylbutazone
【PharmacologicAction】Stronganti-inflammatory,anti-rheumaticeffects,butweakatipyretic,analgesiceffects.Prototypeusedtorheumatismandrheumatoidarthritis.22【AdverseEffects】StomachintestinereactionWater-sodiumretentionAllergicresponseLiver&kidneydamageEtc.23VIIIAlkylKetones
NabumetoneIXIbufenacAcids
Sulindac
Effectintensityandadversereactionarelowerthanindomethacin.24SelectivelyInhibitingdrugsofCyclooxygenase
Nimesulide
ANewtypeofNSAID,higherselectivitytoinhibitCOX2.BStronganti-inflammaryeffects,lessadversereaction.CUse
溫馨提示
- 1. 本站所有資源如無特殊說明,都需要本地電腦安裝OFFICE2007和PDF閱讀器。圖紙軟件為CAD,CAXA,PROE,UG,SolidWorks等.壓縮文件請下載最新的WinRAR軟件解壓。
- 2. 本站的文檔不包含任何第三方提供的附件圖紙等,如果需要附件,請聯(lián)系上傳者。文件的所有權(quán)益歸上傳用戶所有。
- 3. 本站RAR壓縮包中若帶圖紙,網(wǎng)頁內(nèi)容里面會有圖紙預(yù)覽,若沒有圖紙預(yù)覽就沒有圖紙。
- 4. 未經(jīng)權(quán)益所有人同意不得將文件中的內(nèi)容挪作商業(yè)或盈利用途。
- 5. 人人文庫網(wǎng)僅提供信息存儲空間,僅對用戶上傳內(nèi)容的表現(xiàn)方式做保護處理,對用戶上傳分享的文檔內(nèi)容本身不做任何修改或編輯,并不能對任何下載內(nèi)容負(fù)責(zé)。
- 6. 下載文件中如有侵權(quán)或不適當(dāng)內(nèi)容,請與我們聯(lián)系,我們立即糾正。
- 7. 本站不保證下載資源的準(zhǔn)確性、安全性和完整性, 同時也不承擔(dān)用戶因使用這些下載資源對自己和他人造成任何形式的傷害或損失。
最新文檔
- 2024-2030年中國調(diào)味醬行業(yè)市場發(fā)展分析及投資前景與戰(zhàn)略研究報告
- 2024-2030年中國衣服柔順劑市場消費狀況及競爭趨勢預(yù)測研究報告
- 2024-2030年中國螃蟹飼料行業(yè)前景展望分析及運行態(tài)勢建議研究報告
- 2024-2030年中國藻酸鹽敷料行業(yè)現(xiàn)狀規(guī)模及產(chǎn)銷需求預(yù)測報告
- 2024-2030年中國薯類食品市場全景深度調(diào)研與運行態(tài)勢剖析研究報告
- 2024-2030年中國薄層色譜掃描儀行業(yè)運營動態(tài)及應(yīng)用前景預(yù)測報告
- 2024-2030年中國蓄能器充氣閥行業(yè)市場發(fā)展趨勢與前景展望戰(zhàn)略分析報告
- 2024-2030年中國落水手環(huán)行業(yè)發(fā)展態(tài)勢與未來前景預(yù)測分析研究報告
- 2024-2030年中國營養(yǎng)飲品市場發(fā)展態(tài)勢與未來行情監(jiān)測趨勢研究報告
- 公司搬遷員工安置方案
- 公路工程勞務(wù)分包參考價格
- 食品安全檢測新技術(shù)的研究
- 醫(yī)院綜合介入診療技術(shù)臨床應(yīng)用管理規(guī)范
- 檔案信息管理系統(tǒng)使用手冊
- 貨車駕駛員交通培訓(xùn)課件
- 冠心病診斷與治療指南課件
- 《玻璃知識培訓(xùn)》課件
- 骨巨細(xì)胞瘤學(xué)習(xí)課件
- 心律失常門診工作制度
- 國際貨物獨家代理協(xié)議書
評論
0/150
提交評論