作用于血液系统地药物——山东大学药理学英文教学教案.ppt

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1、welcome!AnJieInstituteofPharmacologyChapter29AgentsaffectingbloodandhematopoieticorganThrombosis–theformationofanunwantedclotwithinthebloodvesslsorheartBleedingdisorders–duetofailureofhemostasisandincludehemophiliaandvitaminKdeficiencyAnemia--causedbynutritionaldefici

2、encyDysfunctionsofbloodAnticoagulantsAntiplateletdrugsantithrombolicdrugsFibrinolyticdrugsHemostaticsAgentsUsedinAnemiaHematopoieticgrowthfactorsPlasmavolumeexpandersClotformationrequiresplateletactivationandaggregation(whiteclotorplateletclot),followedbyformationofafi

3、brinclot(redclot).ⅫⅫaⅪaⅨaⅩaⅢa,ⅦaⅪⅨⅩⅢ,ⅦⅩ+++++Prothrombin(Ⅱ)Thrombin(Ⅱa)Fibrin(Insoluble)Fibrin(soluble)fibrinogen++ⅩIIIⅩIIIa+Fibrinclotprocessofnormalbloodcoagulationextrinsicpathwayintrinsicpathway§1anticoagulantsAnticoagulantsaredrugsemployedinpreventingbloodcoagulati

4、on.Theyinhibitcertainclottingfactorsintheliver.Thefunctionofthemisto:1)preventtheformationofnewbloodclots.2)keepexistingbloodclotsfromgrowinglarger.ClassificationofanticoagulantsⅠAnticoagulantsbothinvivoandvitro:e.g.HeparinⅡAnticoagulantsinvivo:dicoumarolⅢAnticoagulant

5、sinvitro:Sodiumcitrate1.Heparin1.1sourceandchemistry(1)largeamountofnegativecharge(2)strongaciditypharmacokineticsAbsorptionAdministeredbyi.vors.cMetabolismExcretion1.2Pharmacologicaleffects1.AnticoagulativeeffectMechanism:accelerateinactivationofclottingfactors.(Ⅱa,Ⅸa

6、,Ⅹa,Ⅺa,Ⅻa)byenhancingtheanticoagulativeactivityofATⅢ(antithrombinⅢ).ⅫⅫaⅪaⅨaⅩaⅦaⅪⅨⅩⅦⅩ+++++Prothrombin(Ⅱ)Thrombin(Ⅱa)FibrininsolubleFibrinsolublefibrinogen++ⅩIIIⅩIIIa+FibrinclotATⅢ:aplasmaproteaseinhibitorMechanismofheparinThisreactionhappensinnormalphysiologicalstate,bu

7、tit’sveryslowandweak.Inthepresenceofheparin(whichactsasancatalyst),itwillbeacceleratedbymorethan1,000timesCharacteristicsofanticoagulativeeffecteffectivebothinvivoandinvitroquickonsetandpotenteffectsefficacypositivelyrelativetomocularweight1.2Pharmacologicaleffects2.Ot

8、hereffectsadjustingbloodlipidanti-inflammatoryeffectanti-proliferativeeffectonvascularsmoothmusclecellinhibitingplete