肾上腺素受体激动药

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1、第十章肾上腺素受体激动药AdrenoceptorAgonistsdefinitionDrugsthatmimictheactionsofepinephrineornorepinephrineSympathomimeticdrugsChemistryParentcompound:phenylethylamineChangetheaffinityforαorβreceptorsChangepharmacokineticsproperties第一节构效关系及分类ChemistryandpharmacokineticsSubstitut

2、ionsOnthebenzenering:increasebioavailabilityandprolongsthedurationofaction;increasethedistributionofmoleculetoCNSOnthealphaorbetacarbons:blockoxidationbyMAOOntheterminalaminogroup:increaseβreceptorsactivityisomerClassificationDependontheaffinityfordifferentgroupsofre

3、ceptorα,β-adrenoceptoragonistsα-adrenoceptoragonistsβ-adrenoceptoragonistsα、β-RagonistAdrenalineDopamineephedrineAdrenalineAtlowconcentration,βeffectspredominate;athighconcentration,αeffectspredominate.β2-RaremoresensitivetoAdrthantheα-R.PharmacologicalEffectsBloodve

4、sselαeffects:constrict(skinvessels,renalvessels)β2effects:dilate(vesselsinskeletalmusclevessels)CoronarybloodflowpulmonarybloodflowBloodredistributionPharmacologicalEffectsHeartdirecteffectonβ1-R;increaseinheartrate,andincreasecardiacoutput;coronaryarterydilateaprope

5、nsitytowardarrhythmiasPharmacologicalEffectsbloodpressureAtlowconcentration:systolicpressureincreaseAthighconcentration:bothsystolicanddiastolicpressureincreasePharmacologicalEffectsSmoothmuscle:Bronchus:Bronchiolarsmoothmusclerelaxes(β2effects);bloodvesselconstrict;

6、Blockthereleaseofhistamine(β2effects)gastrointestinaltractbladderEye:ocularpressurereductionskeletalmusclePharmacologicalEffectsMetaboliceffectsincreaseinglucosesandlactateproductionviaglycogenolysisinhibitionofinsulinsecretion(α-R)increaseinfreefattyacidandoxygencon

7、sumption.PharmacologicalEffectsCNSAttherapeuticdosesIntoxicdoses,excitement,agitation,convulsionpharmacokineticsAdr-absorptionispoorwithoraladministrationAdr-absorptionisslowwithhyodermicadministrationcanbegivenivorimTherapeuticUsescardiacarrestanaphylacticshockAsthm

8、aandacutehypersensitivityreactionprolongthedurationoflocalanesthesiaGlaucomaAdverseEffectsPalpitation,headacheBP,arrhythmiaHyperten