药理学名词解释(含英文)

药物（drug）是指能够影响机体（包括病原体）功能和（或）细胞代谢活动，用于疾病的治疗、预防和诊断，以及计划生育等方面的化学物质。Drugsarechemicalsthatalterthefunctionoflivingsystemsbyinteractionsatthemolecularlevelandcanbeusedtoprevent,diagnoseandtreatdisease.不良反应（adversedrugreactionADR）是指上市的合格药品在常规用法、用量情况下出现的，与用药目的无关，并给患者带来痛苦或危害的反应。副作用（ sideeffect）是由于药物作用选择性低，作用范围广，在治疗剂量引起的，与用药目的无关的作用。毒性反应（toxiceffect）是由于用量过大或用药时间过长引起的严重不良反应。后遗效应（residualeffect）是指在停药后，血浆药物浓度下降至阈浓度以下时残存的药理效应。变态反应（allergicreaction）是药物引起的免疫反应，反应性质与药物原有效应无关，其临床表现包括免疫反应的各种类型。致敏原可以是药物本身或药物代谢产物，亦可能是制剂中的杂质或辅剂。继发反应（secondaryreaction）是继发于药物治疗作用之后的不良反应。停药反应（withdrawalreaction）是指患者长期应用某种药物，突然停药后发生病情恶化的现象。特异质反应（idiosyncrasyreaction）是指少数患者由于遗传因素对某些药物的反应性发生了变化。特异质反应表现为对药物的反应特别敏感，或出现与在常人不同性质的反应。依赖性（dependence）是药物与机体相互作用所造成的一种状态，表现出强迫要求连续或定期使用该药的行为或其他反应，其目的是感受药物的精神效应，或避免由于停药造成身体不适应。量效关系(does-effectrelationship)药理效应的强弱与其剂量大小或浓度高低呈一定关系，称剂量-效应关系，简称量效关系。最小有效量（minimaleffectivedoes）或最小有效浓度是指引起效应的最小药量或最低药物浓度，亦称阈剂量或阈浓度。最大效应（maximaleffectEmax）在一定范围内增加药物剂量或浓度，效应强度随之增加。但当效应增强打最大时，继续增加剂量或浓度，效应不再增强。这一药理效应的极限称为最大效应，又称效能（efficacy）。效价强度（potency）用于作用性质相同的药物之间的等效剂量的比较，达到等效时所用药量较小者效价强度大，所用药量较大者效价强度小。构效关系（structure-activityrelationship,SAR）药物的结构与药理活性或毒性之间的关系称为SAR。受体（receptor）是细胞在长期进化过程中形成的，对生物活性物质具有识别和结合的能力，并具有介导细胞信号转导功能的蛋白质。与受体特异性结合的生物活性物质称为配体（ligand）。激动药（agonist）是指既有亲和力又有内在活性的药物，它能与受体结合并激动受体而产生效应。分为完全激动药和部分激动药。拮抗药（antagonist）是指具有较强的亲和力，而无内在活性，拮抗药与受体结合但不能激动受体。竞争性拮抗药（competitiveantagonist）能与激动药竞争相同受体，但其结合是可逆的，竞争性拮抗药能使激动药的量效曲线平行右移，但最大效应不变。非竞争性拮抗药指拮抗药与受体的结合是相对不可逆的，或能引起受体构象的改变，从而干扰激动药与受体的正常结合，使激动药不能竞争性对抗这种干扰。增大激动药的剂量也不能使量效曲线的最大作用强度达到原来的水平。PA2：竞争性拮抗药对相应激动药的拮抗作用强度，pA2=-log[A2],[A2]是指在拮抗药这一浓度下，可使激动药在2倍浓度使所产生的效应恰好等于未加入拮抗药时激动药引起的效应。PA2':非竞争性拮抗药的亲和力参数，又称减活指数，是指使激动药的最大效应降低一半时，非竞争性拮抗药摩尔浓度的负对数。pD2：药物-受体复合物解离常数KD的负对数（-logKD）为pD2，其值与A和R的亲和力成正比。意义是引起最大效应的一半时（即50%受体被占领时）所需的药物浓度。吸收（absorption）是指药物从给药部位进入血液循环的过程。首关效应（first-passeffect）是指某些药物首次通过肠壁或经门静脉进入肝脏时被其中的酶所代谢致使进入体循环药量减少的一种现象。分布（distribution）是指吸收入血的药物随血液转运至组织器官的过程。血脑屏障（blood-brainbarrier，BBB）指由脑毛细血管形成的血浆与脑细胞外液间的屏障以及由脉络膜形成的血浆与脑脊液间的屏障。肝肠循环（hepatoenteralcirculation）由胆汁排入十二指肠的药物有的直接随粪便排出，但较多的药物可由小肠上皮吸收，并经肝脏重新进入全身循环，这种肝脏、胆汁间、小肠的循环称为肝肠循环。生物利用度（bioavailability,F）是指药物从某制剂吸收进入血液循环的相对数量和速度。是评价药物制剂质量的一个重要指标。分为绝对生物利用度（absolutebioavailability）和相对生物利用度（relativebioavailability）。一般认为，静脉注射的生物利用度是100%，如果把静脉注射与血管外途径给药时的AUC值进行比较，并计算后者的生物利用度，即为绝对生物利用度。也可在同一给药途径下对不同制剂进行比较，这就是相对生物利用度。半衰期（half-life,t1/2）指血浆消除半衰期，是药物在体内分布达到平衡状态后血浆药物浓度降低一半所需的时间，是表述药物在体内消除快慢的重要参数。一级消除动力学（firstordereliminationkinetics）是指血中药物消除速率与血中药物浓度的一次方成正比，即血药浓度高，单位时间内消除的药量多；血药浓度低，单位时间内消除的药量少。零级消除动力学（zeroordereliminationkinetics）是指血中药物消除速率与浓度的零次方成正比，即血药浓度按恒定消除速度进行消除，与血药浓度无关。稳态血药浓度（steady-stateconcentration，Css）在一级消除动力学药物中，若按固定间隔时间给予固定药物剂量，在每次给药时体内总有前次给药的残存量，多次给药形成不断蓄积，随着给药次数的增加，体内总药量的蓄积逐渐减慢，直至在剂量间隔内药物的消除量等于给药剂量，从而达到平衡，这时的血药浓度称为稳态浓度或坪浓度。调节痉挛（regulativespasm）：毛果芸香碱激动睫状肌环形纤维上M受体，使睫状肌向虹膜中心方向收缩，悬韧带松弛，晶状体变凸，屈光度增加，使远物不能聚焦成像于视网膜上，因此模糊不清，此时，只适合于视特定近距离的物体，这种作用称为调节痉挛。调节麻痹（regulativeparalysis）阿托品阻断睫状肌上的M受体，使睫状肌松弛而退向外缘，悬韧带拉紧，晶状体变为扁平，其屈光度降低，故不能将近物清晰地成像于视网膜上，造成视近物模糊不清，只适于看远物，这一作用成为调节麻痹。胆碱能危象（cholinergicrisk）抗胆碱酯酶药如新斯的明治疗重症肌无力，因应用过量可使骨骼肌运动终板处有过多乙酰胆碱堆积，导致持久去极化，加重神经肌肉传递功能障碍，使肌无力症状加重，称为胆碱能危象。肾上腺素升压作用的翻转（adrenalinereversal）a受体阻断药酚妥拉明等可取消去氧肾上腺素的升压作用，可以部分阻断去氧肾上腺素所致升高血压作用，使肾上腺素的升压carriersandtherequirementofenergyconsumption.Absorptionistheprocessinwhichdrugstransportfromthesiteofadministrationtothebloodcirculationafterextra-vascularadministration.Firstpasselimination:Somedrugsareinactivated/metabolizedintheGItractandliverbeforeenteringintothesystemiccirculationandresultinthereductionofactualdrugquantityenteringintosystemiccirculation.ThisprocessiscalledfirstpasseliminationDistribution:drugsabsorbedinthebloodtransportfromthebloodtotissues.Tissuepartitioncoefficient:whenthedistributionreacheshomeostasis,theratioofthedrugconcentrationbetweentissuesandplasmaremainsconstant,calledtissuepartitioncoefficientofdrugsExcretion:theprocessofparentdrugsortheirmetabolitesbeingdischargedfrombodybysecretoryorgansisknownasexcretionHepato-enteralcirculation:aportionofdrugsthosebeingcarriedtoduodenumviabilecanbereabsorbedviaepitheliaofsmallintestinesandentryintosystemiccirculationbywayofliver.Thiscyclealongliver,bile,smallintestineisknowashepato-enteralcirculationApparentvolumeofdistributionmeanstheratioofinvivodrugquantityversusconcentrationinplasmawhenthedrugreachesdynamicequilibriuminthebody.Halflife:meanstheperiodoftimewhenthedrugconcentrationinplasmareducestoone-half.AUC:areaunderthecurve,indicatestheareaundertheconcentration-timecurveBioavailability:indicatestherateandextentofabsorptionintothesystemiccirculationfollowingextravascularadministrationofdrugsClearance:mansthevolumeofbodyfluidcontainingadrugthatcanbeeliminatedbythebodyinunittime.Maintenancedose:inmostclinicalsituations,drugsareadministeredinsuchawayastomaintainasteadystateofdruginthebody,i.e,justenoughdrugisgivenineachdosetoreplacethedrugeliminatedsincetheprecedingdose.Loadingdose:whenthetimetoreachsteadystateisappreciable,asitisfordrugswithlonghalf-lives,itmaybedesirabletoadministeraloadingdosethatpromptlyraisestheconcentrationofdruginplasmatothetargetconcentration.PharmacodynamicsDrugactionreferredtotheinitialinteractionbetweendrugandbody.PharmacologicaleffectsisthephysiologicaleffectsinducedbydrugactionStimulation:enhancementofthebodyfunctionisStimulationInhibition:restraintordiminutionofthebodyfunctionisInhibitionEtiologicaltherapy:EliminationoftheetiologicalfactorstocurediseasesSymptomatictherapy:ImprovementofdiseasesymptomwithouteliminatingthecauseofthediseaseSidereaction:Intherangeoftherapeuticdosage,thedrugeffects,whicharenotrelatedtothecurrenttherapeuticpurpose,aredescribedassideeffects.Toxicreactioncanhappenedwhenthedoseofthedrugishighenoughordrugsarelongtermused.Allergicreactionisakindofresponseofthepatient’simmuno-systemtotheantigen.Itisnotdoserelatedandonlyoccurinafractionofthepopulation.IdiosyncraticreactionistheresultofabnormalreactivitytoadrugcausedbygeneticdifferencesSecondaryreactionresultsfromlong-termusingofdrug.NormalflorahasbeeninhibitedandtheinsensitiveflorabecomesprominentDrugtolerancemeanstheresponsetothesamedoseofadrugdecreaseswithrepeateduses.Physicaldependenceisanadaptivephysiologicalstateproducedbyrepeateduseofadrug.Oncedrugadministrationisstopped,abstinencesyndromeswilloccur.Psychologicaldependenceisthefeelingofsatisfactionandpsychicdrivethatrequireperiodicorcontinuousadministrationofthedrugtoproduceadesiredeffectortoavoiddiscomfort.Gradedresponse:Inacertainrangeofdoses,thepharmacologicalresponseincreaseswiththeincreasingofdoses,suchasbloodpressure,musclecontraction,urinaryexcretionofsodium.Thresholddoseindicatestheleastamountofdrugneededtoexerttherapeutic,alsoasknowasminimaleffectivedoseEfficacydescribesthemaximalbiologicalresponseproducedbyadrugConcentrationfor50%ofmaximaleffect(EC50):Theconcentrationthatgiveriseto50%ofmaximaleffectPotencyisatermdescribingthecomparativeexpressionofadrugactivitymeasuredintermsofdoserequiredtoproduceaparticulareffectofgivenintensityrelatedtoagivenstandardreference.Quantalresponse:Indicatethatagivendoseofadrughasorhasnotevokedacertaineffectinthevarioussubjectsunderinvestigation.LD50:Adosethatgivesrisetothedeathof50%ofsubjectsiscalledLD50TI:therapeuticindex.TI=LD50/ED50.Itisakindofindexevaluatedthesafetyofadrug.Receptor:AreceptorcanbedefinedasanybiologictargetmacromoleculeincellsthatinteractsspecificallywithextracellularsignalandconvertsitintointracellulareffectsLigand:Aligandisacompoundthatbindstoareceptorspeciallyandproducesthebiologicalresponse.ItwasalsocalledfirstmessengersDown-regulation/Desensitization:Chronicstimulationofreceptorscancausedecreasednumbersofreceptors.Up-regulation/Hypersensitization:Incontrary,chronicblockingreceptorsmayresultinreceptorup-regulationAgonistcanbindtoreceptors,thenactivatereceptorsandproducepharmacologicaleffect.Antagonist:Apureantagonist,whichcanbindtoreceptorswithoutintrinsicactivity,antagonizesthebiologiceffectsofthecorrespondingagonist.Toleranceissaidtodevelopwhentheresponsetothesamedoseofadrugdecreaseswithrepeateduses.Dependencemeansthebodyproducephysiologicalorpsychologicaldependenceandrequirementtosomedrugsafterlong-termuseofthedrugs.WithdrawalsyndromeTerminationofsomedrugsusingafterlong-termmedicationresultsinwithdrawalsymptomsorwithdrawalsyndromeCinchonism:Itisdescribedbythesymptomscausedbytoxicityofquinidineorquinineetal,thealkaloidsextractedfromcinchona,whichinclude3majorsymptoms:gastrointestinaldisturbancelikevomiting,nausea,diarrhea;visualandauraldisturbancesasdiplopia,photophobia,altered-color,hearingloss,tinnitus;andcentralnervoussystemeffectslikeheadache,confusion,psychosis.Mycardialremodeling:ItisthemostimportantintrinsiccompensatorymechanisminCHF.Itreferstotheslowdilationandstructuralchangesoccurredinthestressedmyocardium,includingmyocyteshypertrophy,proliferationofconnectivetissuecells(fibroblasts)andmyocardialfibrosis.Afteraninitialbeneficialeffect,mycardialremodelingcanleadtoischemicchanges,impairmentofdiastolicfilling,andmyocytesapoptosis.AngiotensinIIandaldosteronecancausemycardialremodelingduringCHF.Firstdosephenomenon:Itreferstoaprecipitousdropinstandingbloodpressure,palpitationandsyncopeshortlyafterthefirstdoseofsomeantihypertensivedrugs,especiallyprazosin.Thyroidstorm(thyroidcrisis):issuddenacuteexacerbationofallofthesymptomsofthyrotoxicosis,presentingasalife-threateningsyndrome.Insulinresistance:Adiabeticrequiringmorethan200units/dayisregardedasinsulinresistant.Acuteresistantmayresultfromtheincreaseofanti-insulinfactor-corticosteroids,growthhormonethyroxine,andestrogens.Chronicresistancemaybeduetoadeclineinnumberand/oraffinityofreceptorsortodefectsinpost-receptormechanisms.Hyperadrenalism-likesyndrome:Thisiscausedbylipidmetabolism,andredistributionorwater-electrolytemetabolismdisorders.Thesyndromeincludemoonfaces,buffalohump,centralobesity,skinatrophy,acne,crinosity,edema,hypokalemia,hypertension,diabetesmellitusetc.Reboundphenomena:Discontinuingorrepidextenuationofglucocorticosteriodscanleadoriginaldiseasesrecurringordeteriorating.Superinfections:Thereisacompletemicroecosysteminhealthadult.Afterlong-termusingbroad-spectrumantibiotics,sensitivebacteriagrowthisinhibited,non-sensitivebacteriatakesthechanceofbreeding,resultinginnewinfections.Chemotherapy：Itistousechemistrydrugstreatingorpreventingthediseasescausedbypathogenicmicrobe,helminthorcancercell.Antibacterialdrugs：substancestoinhibitorkillbacteriaandtopreventandcurethebacteroidalinflammation.Antibacterialspectrum：Antibacterialspectrumofadrugmeansthespeciesofmicroorganismsthatthedrugcaninhibitorkill.antibacterialactivity：Itmeanstheabilityofadrugthatthedrugcaninhibitorkillmicroorganisms.Minimalinhibitoryconcentration(MIC)：MICisthelowestconcentrationofantimicrobialagentsthatpreventsvisiblegrowthin18-24hoursincubation.Minimalbactericidalconcentration(MBC)：MBCisthelowestconcentrationofantimicrobialagentsthatkillsbacteriainculturemedium.Chemotherapeuticindex(CI)：CIisatermusedtoevaluatethesafetyofchemotherapeuticdrugs.ThevalueisLD50/ED50orLD5/ED95Post-antibioticeffect,PAE：PAEshowstheantimicrobialeffectaftertheconcentrationdecreasedbelowMIC.Chemotherapy：Itistousechemistrydrugstreatingorpreventingthediseasescausedbypathogenicmicrobe,helminthorcancercell.Chemotherapeuticindex(CI)：CIisatermusedtoevaluatethesafetyofchemotherapeuticdrugs.ThevalueisLD50/ED50orLD5/ED95Antibacterialdrugsaresubstancestoinhibitorkillbacteriaandtopreventandcurethebacteroidalinflammation.Antibacterialspectrumofadrugmeansthespeciesofmicroorganismsthatthedrugcaninhibitorkill.antibacterialactivity：Itmeanstheabilityofadrugthatthedrugcaninhibitorkillmicroorganisms.Minimalinhibitoryconcentration(MIC)：MICisthelowestconcentrationofantimicrobialagent