新型抗过敏药英文版 ppt课件

抗过敏药Antiallergicdrug我在花粉的刺激下脓包成堆Flower?你在春天的花朵里自拍纷飞Content:1.Allergydiseaseandhistamine2.Thedevelopmentofantiallergicdrug3.Newallergymedicine--OlopatadineHydrochloride4.Thechemicalstructure5.Structure-activityrelationship(SAR)6.Studyontoxicityandsideeffect7.Indications8.Syntheticroute9.Prospects10.Howtochoosetheallergymedicine?1.AllergydiseaseandhistamineWhenbodyhasbeenstimulatedbytheantigenicsubstances,itmaybecausethetissuedamageorphysicaldisorders,namelypathologicalimmuneresponsetodiseases.Histamineininflammationandallergicdiseasesplayanimportantroleinphysi-ological,histamineofproinflammatoryandimmuneadjustmentisbythreekind-sofhistamineH1,H2,H3.Histamineisthemostimportantmediumallergicdisease.2.ThedevelopmentofantiallergicdrugAntiallergicdrugsarealsocalledantihistamines,withthecontinuousdevelopmentofpharmacology,antihistamineshavebeendevelopedtosixcategoriesnearlyhundredkindsofvarieties.ThefirstgenerationofantiallergicdrugThefirstgenerationofhistamineH1receptorantagonisthasstrongcentralnervouscalmingandcholinefightingeffects.ThesecondgenerationofantiallergicdrugTheadvantagesofsecondgenerationantiallergic:(1)betterclinicalcurativeeffect(2)long-termeffect(3)nosideeffecttocentralnervoussystem(4)noresistingcholineeffect(5)eutherapeutictoasthma(6)goodtolerabilitySlightlyCNSeffect:①Sleepiness②headache③whettheappetiteandsideeffecttocardiovascularsystem3.Newallergymedicine--OlopatadineHydrochlorideOlopatadineasanewkindofrelativelyhighselectivityantiallergic,ConcordeFermentationbyJapanlistedcompanydevelopmentandantiallergic,successivelyonthemarketinEurope,America,Japanandothercountries.4.Thechemicalstructure11-[(反)-3-二甲胺基丙烯]-6,11-二氢苯骈[b,e]氧杂卓-2-乙酸盐酸Structure-activityrelationship(SAR):1.烯基碳和氮原子间相隔2个碳原子最佳,延长或缩短碳链对H1受体的亲和力减弱;氮原子上以二甲基取代抑制支气管哮喘作用最强,以二乙基取代抑制作用减弱,以吗琳和哌啶取代活性消失。2.分子中梭基是必要的官能团,梭基和二苯骈氧卓环之间以亚甲基相连,抗过敏活性最强,但适当延长或缩短连接基团对H1受体的亲和力变化影响不大。3.二苯骈氧卓环也是必要的,开环化合物失去所有的活性。4.反式异构体比顺式体对H1受体的亲和力强,但它对M1受体亲和力也强,副作用多。6.Studyontoxicityandsideeffect:Preclinicalandclinicalstudieshaveshown:noanticholinergicsideeffects;doesnotleadtocataractsandeyesymptomsofnervedamage;noantigenicityandallergicreaction,butlar-gedoses;pregnantwomenwithfetaldevelopmentorafterthebirthofababy'sgrowthandleadtoweightlossordevelopmentaldelays,sopregnantwomenandnursingmothersban.7.Indications:Oraltreatment:Allergicrhinitis,skinirritations,pleomorphicexudativeerythemaandurticariaEyedrops:AllergicconjunctivitisDosageform:Tablets:5mg/tabletEyedrops:1%eyedrops8.Syntheticroute:Accordingtothechemicalstructuralformulaandinversesyntheticanalysis,areasonablemodeoffractureinthedoublebond,bycarbonylbuilddoublebond.OlopatadineHydrochloridehavecertaineffecttocommonvarietyofallergicconjunctivitis,atthesametimehavelessadversereaction.9.Prospects:OlopatadineHydrochloridehavestrongantagonismeffecttoH1receptor,alsoinhibitmastcellsreleaseofinflammatorymediators.Inrecentyears,somenewusagesjustlikenasalsprayandsoonareundertheresearching.Therefore,theresearchanddevelopmenttheloshewillproducegoodeconomicbenefitandsocialbenefit.10.Howtochoosetheallergymedicine?Antiallergicselectionprinciple:1.Consultaphysicianbeforeusingthisdrug.2.Findtheallergen.3.Payattentiontomedicinetakingtime.4.Moderatedrugdosage.5.Unfavorablecombinationintakeallergydrugsatthesametime.6.BecarefulofcombiningwithChinesemedicineandwesternmedicine.References:[1]薛建英.新型抗过敏药盐酸奥洛他定的合成研究[M][2]王金龙,陈孝治.H1受体拮抗剂及其研究的新进展[J],中国药房,1999,10(3):140[3]李莹,张潇等.过敏性结膜炎的流行病学及奥洛他定滴眼液开放性多中心治疗的初步效果[J]OphthalmolCHN,2008(17):166-170[4]博恩.如何选用抗过敏药[J]中国中医药报2010(5)[5]KyosukeSatake,JunichiIkedaet.Olopatadinehydrochloridesuppresseshotflashesinducedbytopicaltreatmentwithtacrolimusointmentinrats[J]EuropeanJournalofPharmacology,Volume765,2015(10):402-405[6]B.Mortemousque,T.Bourcier,M.Khairallahet.Comparisonofpreservative-freeketotifenfumarateandpreservedolopatadinehydrochlorideeyedropsinthetreatmentofmoderatetosevereseasonalallergicconjunctivitis[J]JournalFrançaisd'Ophtalmologie,2014(1):1-8[7]SakiMatsui,HiroyukiMurota,EmiOnoet.Olopatadinehydrochloriderestoreshistamine-inducedimpairedsweating[J]JournalofDermatologicalScience,2014(6):260-261Thankyou!