药理学导论ppt课件.pptVIP

Pharmacology,Principles,AutonomicNervousSystem,+,.,IntroductiontoPharmacology,1,.,Questions:,你是否想过新药是如何发现和研究的？你是否想过病人用药时是如何选择药物、确定给药剂量、给药途径、给药次数和给药的疗程？病人用药时应该注意些什么（副作用、毒性作用、禁忌症）？,2,WhatisthePharmacology?,研究药物和机体（包括病原体）相互作用的规律及其原理的一门科学,也是一门实践科学，主要研究药效学和药动学。,3,HistoryofPharmacology,Whataredrugs？,用于防治或诊断疾病的物质能影响机体器官生理功能和/或细胞代谢活动的化学物质与毒物没有本质的区别无药不毒!,4,Variousmixturesofplantandanimalsubstanceswereusedtotreatsickness.Bytheendofthe18thcentury,itwaspossibletoisolateactiveingredientsfromcrudedrugsandsynthesizechemicalcompoundsthatproducedpredictablebiologicresults,HistoryofPharmacology,5,HistoryofPharmacology,Morphinewasextractedfromopiumin1806AspirinwasdevelopedbyBayerCompanyin1899,6,HistoryofPharmacology,Inthe20thcentury,explosiveadvancesinthefieldofpharmacologyoccurred.InsulinANSdrugsAntibioticsandantineoplasticsGeneticallyengineereddrugs,7,DevelopmentofPharmacology,由器官水平细胞水平分子水平多学科发展：心血管药理学生殖药理学免疫药理学分子药理学肿瘤药理学时辰药理学精神神经药理学临床药理学等分支学科,8,药理学的内容,Pharmacokinatics（药代学）,Pharmacodynamics（药效学）,9,研究在药物作用下机体生命活动过程的变化规律，即药物对机体的作用,Pharmacodynamics,Pharmacokinatics,研究机体对进入体内的药物的处置规律，即药物的体内过程,10,Pharmacodynamics,药物作用：治疗效应对因治疗和对症治疗急则治其标，缓则治其本不良反应副作用毒性作用过敏反应继发反应后遗效应,11,参与或干扰细胞代谢影响生理物质转运影响酶的活性影响膜上离子通道影响核酸代谢影响免疫功能激活或阻断受体,Actingmechanismsofdrugs,12,Actingmechanismofdrugandreceptor,Receptor：细胞膜上或细胞内的特殊蛋白组分，能识别周围环境中某种微量化学物质，首先与之结合，并通过中介的信息转导与放大系统，触发相应的生理反应或药理效应.,13,Classificationofreceptors,肾上腺素受体、胆碱受体、多巴胺受体、糖皮质激素受体等。跨膜激酶活性受体、G蛋白耦联受体、离子通道受体、胞内受体（核受体）,14,ReceptorBinding“KeyinLock”Mode,15,Drug-ReceptorInteractions,k1,k2,Drug,Receptor,Effect,Drug-ReceptorComplex,Ligand-bindingdomain,Effectordomain,16,ReceptorProteins,Typesofreceptor-effectorlinkage.(R,receptor;G,G-protein;E,enzyme;ACh,acetylcholine.),17,药物的药理效应与剂量在一定范围内成正相关关系,以效应为纵坐标，药物浓度为横坐标所作的曲线如将浓度取对数值，曲线为典型的对称“S”型.,量效关系,量效曲线,18,量反应量效曲线,ECminEC50EmaxPotencyEfficacy,19,质反应量效曲线,累加量效曲线EDminED50TD50LD50频数分布曲线,20,动物：TI=LD50/ED50临床：TI=TD50/ED50,治疗指数(TherapeuticIndex,TI),安全范围(SafetyMargin,SM),动物：SMED95LD5的距离临床：SMED95TD5的距离,21,%Responding,Dose,TherapeuticandToxicEffect,22,DrugSafetyThearapeuticWindow,VERYVERYIMPORTANTCONCEPT.THISALSOAFFECTSDOSE.,23,Pharmacokinatics,AbsorptiontakenintothebodyDistributionmovedintotissuesMetabolizedchangedsocanbeexcreted(biotransformation),butnotall.Excretedremovedfromthebody,Briefly!,24,DISTRIBUTION,25,Routeofdrugadministration,AccordingtothedrugsPropertiesandthetherapeuticobjectives,therearethreetypesofrouteEnteralParenteralOther,OralSublingualRectal,IntravascularIntravenousintra-arteriallyIntramuscularSubcutaneous,InhalationIntranasalIntrathecal/IntraventricularTopicalTransdermal,26,DrugDistribution,Howdrug,onceabsorbed,getstotissuesandfluidsofthebodyDependsonseveralfactorsBloodflowSolubility(cellpermeability)BloodBrainBarrierProteinBinding(血浆蛋白结合),27,BloodBrainBarrier,http:/meds.queensu.ca/medicine/physiol/undergrad/210/210nerv/Lecture%206%202002.ppt,28,DrugMETABOLISM,ReactionofdrugmetabolisminLiver,Drugs,Enzymes,PhaseI,PhaseII,Excretion,Increasingpolarization,Oxidation,Reduction,Hydrolysis,(Active,Unchange,Inactive),Conjugation(Inactive),DirectlyUnchanged,29,Biotransformation(Metabolism),30,DrugEXCRETION,31,Time-concentrationandtime-effectrelationshipofdrugs,32,Theplasmaconcentration-timecurvefollowingasingleoraldoseofformulationA,BandC.Theextentsofabsorptionofthethreeformulationaresimilar(i.e.,theareaofAUCissimilar).Buttherateofabsorptiondiffers.TherateofabsorptionofformulationAisthefastest;therateofabsorptionofformulationCistheslowest;therateofabsorptionofformulationBisbetweenAandC.,33,传出神经药理,常用药物药理,34,传出神经对内脏器官的调节作用,35,Questions:,通过上图可见，假如迷走神经过度兴奋，出现胃部痉挛引起胃痉挛时，你如何用药物缓解？假如对支配心脏的交感神经过度兴奋时，心跳的很快（180次/分），你如何用药来治疗？,36,药物分类,拟胆碱药物抗胆碱药物拟肾上腺素药物：受体激动药受体激动药抗肾上腺素药物：受体阻断药受体阻断药,37,中枢神经药理,镇静催眠药巴比妥类苯二氮卓类抗癫痫和抗惊厥药抗精神失常药抗精神病药抗抑郁药抗躁狂药,38,中枢神经药理,抗帕金森病药拟多巴胺药中枢抗胆碱药多巴受体激动药镇痛药阿片类人工合成类解热镇痛药阿司匹林,39,内脏系统药理,抗心律失常药Na+通道阻滞药受体阻断药延长动作电位时程药Ca2+通道阻滞药治疗慢性心功能不全药强心苷类非强心苷类正性肌力药物肾素-血管紧张素抑制药,40,抗心绞痛药硝酸脂类受