胆碱受体阻断剂.pptVIP

胆碱受体阻断剂

CholinoceptorblockingdrugsCholinoceptorblockingdrugs:Bindtocholinoceptor(affinity),butcannotorhaslittleresultincholinomimeticaction(intrinsicactivity),preventingthebindingthereceptorsitetothecholinergictransmitterorcholinoceptoragonist，thereforeresultinanticholiniceffects.Onthebasisofspecificreceptoraffinities(receptorselectivityoftheseantagonists),theantagonistfallintotwomajorfamilies.

CholinoceptorblockingdrugsclassifydrugsAntimuscarinicagentsM1、M2RantagonistsatropinescopolamineanisodamineM1RantagonistspirenzepineM2RantagonistsgallamineAntinicotinicagentsN1RantagonistsmecamylamineN2Rantagonistssuccinylcholinetubocurarine

AntimuscarinicagentsplantalkaloidsAtropabelladonnaHyoscyamine(atropine)DaturastramoniumHyoscyamineDaturasp.FengqieerscopolamineHyoscyamusnigertianxianziHyoscyamineScopoliatanguticaAT3anisodamine

AntimuscarinicagentsAtropabelladonna颠茄Atropine阿托品dl-hyoscyamineScopolamine东莨菪碱Anisodamine山莨菪碱654654-2AT3樟柳碱

Antimuscarinicagents

atropine阿托品1.pharmocokineticstertiaryaminealkaloidestersAbsorption:wellabsobedfromthegutandacrosstheconjunctivalmembrane.Oraladministrationtmax1h；injectiontmax15-20min.Distribution:widely，passingacrossblood-brainbarrier

Antimuscarinicagents

atropine阿托品Metabolismandexcretion:disappearrapidlyfromtheblood,half-lifeof2-2.5hours,1/3ofthedoseisexcretedunchangedintheurine,mostoftherest(2/3)appearsintheurineashydrolysisandconjugationproducts.Theeffectofthedrugonparasympatheticfunctiondeclinerapidlyinallorgansexcepttheeye.Effectsontheirisandciliarymusclepersistfor72hoursorlonger.

Antimuscarinicagents

atropine阿托品2.pharmacodynamicsandclinicalusesMechanismofactioncompetitivelyblockmuscarinicreceptors(atropineandAchorcholinomimeticscom