药理1(1)

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ReasonsforstudypharmacologyA.compulsoryforveterinarymedicinemajorstudents;B.R&Dofpharmaceuticals;C.commonsense,e.g.usingaspirintopreventarteryclotting;introduction1)Definitionofadrug2)originsofdrugs3)dosageform4)objectivesofstudent5)historyofpharmacology(一)药物的概念(definitionofadrug)•药物(ADrug)isasubstanceusedtodiagnose,preventortreatdisease(用于诊断、预防或治疗疾病的物质).兽药还包括能促进动物生长繁殖和提高生产性能的物质。•毒物(poison):对动物机体能产生损害作用的物质。药物超过一定的剂量也能产生毒害作用,因此药物和毒物的区别仅在于剂量的差别。药物长期使用或剂量过大有可能成为毒物。(二)药物的来源1.天然药物:1)Plant(botanical):theactivecomponentsofplantsthatareusefulasdrugsincludealkaloids(生物碱),glycoside(糖苷),gums(树胶),resins(树脂),andoils.生物碱的英文名以-ine结尾,糖苷以-in结尾。例如,生物碱有:atropine(阿托品),caffeine,nicotine;糖苷有digi’toxin(洋地黄毒苷),di’goxin(地高辛)。2)矿物质(mineral):includetheelectrolytes(sodiumchloride),iron,selenium,andothers3)动物:insects,4)微生物发酵产物:Fermentationproductsofbacteriaandmolds,includingmanyantibiotics(抗生素)andanthelmintics(抗蠕虫药),suchaspenicillins,ivermectins.•2.合成药物:人工合成的化学药物、抗菌药物等.Aspirin,enrofloxacin•3.生物技术药物:usingrecombinantDNAtechnologytoproduceanimalandhumanproducts,suchasinterferon,insulin,andsoon.Nuclearacids(dsDNA)(三)药物剂型1.将药物的原料加工制成安全、稳定和便于应用的形式,这种药物的形式称之为药物剂型(dosageform),简称剂型,如pills、片剂(tablets)、粉剂(powders)、注射剂(injectionsolutions)等。2.剂型是一个集合名词,任何一种具体的剂型如安定片、葡萄糖氯化钠注射液,则称为制剂(preparation)。3.药剂学(pharmaceutics)主要是研究药物合适的制剂的科学。合理的制剂有利于药物的储存、运输和使用,提高药物的生物利用度,降低不良反应,发挥最大的疗效。4.新型制剂的进展1)长效制剂(缓释制剂)(long-releasedpreparations)2)喷雾剂(兽用疫苗)3)浇泼剂4)靶向制剂(targetdelivery)单抗、磁疗制剂(四)兽医药理学的性质和任务1.Scopeofpharmacology.Pharmacologyisanexperimentsciencedealingwiththepropertiesofdrugsandtheireffectsonlivingsystems.2.任务(目标):通过药理学的学习,熟悉和掌握各类药物的基本作用原理,主要适用症(indication)和禁忌症(contraindication),从而能正确的选药、合理用药。也为将来开发新药和新制剂打下基础。(五)兽医药理学的发展简史1.Humanemployeddrugsfortreatingdiseaseandforsocialandreligiouspurpose.Discoveryofdrugswerethroughtheprocessoftrialsanderrors.2700BC,ChineseEmperorShenNung→Pentsao→1550BCEberspapyrusrecorded829prescriptionsformedicamentsempoyedinEgyptianmedicine→Greekcivilization:Hippocrates(460-375BC),Hippocraticschoolpromotedtheuseofinorganicsaltsasmedicine→Galen(131-201),Gelenicmedicineconsistsofpreparationofplantsbysoakingorboiling→Renaissance:duetothedevelopmentofprinting,the1stpharmacopeiawascompiledbyValeriusCordus(1514-1544).1540opiumwasintroducedintoclinicaluse2.The17thand18thCenturies:Drugssuchascinchona(quinine),coffee,tea,cocoa,curare,digitaliswerediscovered3.the19thcentury:FriedrichSerturner(1783-1841),aGermanpharmacist,isolatedthespecificnarcoticsubstancefromopiumandnameditMorphineafterMorpheus,theRomangodofsleep.strychine,atropineandmanyotherchemicalswereisolatedfrommedicinalplants.ThefirstlaboratoryofstudyofpharmacologywasestablishedinEstonia(1820-1879).Sincethen,pharmacologygraduallyseparatelyfrompharmacy.4.20世纪:药理学分支1)Molecularpharmacology2)Biochemicalpharmacology3)geneticalpharmacology4)Immuno-pharmacology5)pharmacodanamics6)pharmacokineticsChapter1Generalpharmacology•第一节药物对机体的作用-药效学Pharmacodynamics•第二节机体对药物的作用-药动学pharmacokinetics•第三节影响药物作用的因素及合理用药第一节药物对机体的作用—PharmacodynamicsPharmacodynamicsisthestudyofPhysiological&biochemicaleffectsofdrugsandhowtheseeffectsrelatetoadrug’sMechanismsofactionItfocuseson:Actionandeffectsofdrugsinbody•Pharmacodynamicscharacterizes:whatadrugsdoestothepatient•Pharmacokinetics:whatthepatient’sbodydoestoadrugPharmacodynamics一、pharmacodynamicterms二、structure-responserelationshipanddose-responserelationship(药物的构效关系和量效关系)三、药物作用机理(mechanismsofaction)一、pharmacodynamicterms1.Drugaction:drugmoleculescombinewithcomponentsofcellmembranetoinitiatereactions2.Pharmacologicaleffect:theresultsofdrugactionse.g.药物→心肌细胞膜受体→心肌细胞收缩增加(drugaction)→心输出量和外周组织血流量增加→patientwithcongestiveheartfailure的症状改善(药理效应)3.Stimulants:enhancetheactivityofcells,tissues,organsofbodye.g.caffeine4.Depressants:diazapine5.localfunction(局部作用)6.absorptiveaction(吸收作用),alsocalledgeneralorsystemicaction(全身作用)7.directactionorprimaryaction:digitoxin加强心肌收缩力8.Indirectactionorsecondaryaction:digitoxin使水肿减轻9.Selectivity:preferentiallyproduceaparticulareffectinacertaintissuee.g.clenbuterol:highselectivityforβ2receptorinairways,lessselectivityincardiacβ1原因:组织亲和力(affinity)药物在组织的代谢率10.therapeuticaction(治疗作用):对防治疾病有利的作用etiologicaltreatment(对因治疗):symptomatictreatment(对症治疗)11.adversereaction:anundesirableresponsetoadrug;itmayvaryinseverityfrommildtofatal(与用药目的无关作用,称为不良反应)。(1)sideeffect(副作用):在治疗剂量时产生的与治疗无关的作用或危害不大的不良作用。如Atropine麻醉前给药时对胃肠道平滑肌的抑制作用(2)toxiceffect(毒性反应):用药剂量过大或用药时间过长引起的不良反应。少数药物在常用剂量时也能产生毒性反应,如chloramphenicol,aminoglycosides.(3)Allergy(变态反应):青霉素(4)Secondreaction(继发反应):由治疗作用引起的不良后果。如二重感染。(5)Residualeffect(后遗效应):停药后的残存药理效应二、structure-responserelationshipanddose-responserelationship(一)structure-responserelationship(二)dose-responserelationship(一)structure-responserelationship•structure-responserelationship:药物的药理作用与特定的化学结构的关系•结构相似的化合物:相似或相反的反应。•光学异构体影响药理作用:多数药物的左旋体有药理活性,右旋体无活性,如左旋氯霉素、左旋咪唑。•研究构效关系的意义:了解药物的作用机理、寻找和合成新药(二)dose-responserelationship•establishingandmaintainingforacertaintimeaneffectiveconcentrationofthedrugintheimmediatevicinityofactionsite.•dose-responsere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