藥學(xué)英語藥理學(xué)的課件

Unit2Pharmacologyassesstheeffectofdifferentdosesontherapeuticeffectuseanimalmodelstoscreenchemicalswithanti-tumoractivitymeasureplasmahalflifeofadruginbodyevaluatetoxicityofacandidatedruginmendeterminetheminimuminhibitoryconcentrationofanantibioticevaluatetheinhibitoryeffectofacandidatedrugonanenzymeHistory1.Pharmacologystudiestheeffectsofdrugsandhowtheyexerttheireffects.E.g.penicillinkillssusceptiblebacteriabyspecificallyinhibitingthetranspeptidase(轉(zhuǎn)肽酶)thatcatalyzesthefinalstepincellwallbiosynthesis,thecross-linkingofpeptidoglycan（肽聚糖）.

E.g.acetylsalicylicacid（aspirin）

Phospholipidsphospholipasearachidonicacid(花生四烯酸）

cyclooxygenase(環(huán)氧化酶)prostaglandin(前列腺素)

inflammation

InhibittheactivityofCOXEnzymeinhibitor32.4%Transportproteininhibitor16.0%Receptoragonist9.1%Receptorantagonist10.7%Drugsactingonionchannels9.1%DNA,RNA/ribosomeTypicallyadrugtargetisakeymoleculeinvolvedinaparticularmetabolicorsignalingpathwaythatisspecifictoadiseaseconditionorpathology,ortotheinfectivityorsurvivalofamicrobialpathogen.Asurveyin2000indicatedthat:2.ImportantfiguresinthedevelopmentofpharmacologyFriedrichWohlerSynthesisofurea(尿素):organiccompoundscanbesynthesizedfrominorganicmaterialsOswaldSchmiedebergHisworkprimarilydealtwithfindingthecorrelationbetweenthechemicalstructureofsubstancesandtheireffectiveness.athesisonthemeasurementofchloroform（氯仿）inbloodstudiedthepharmacologyofchloroformandchloral

hydrate（水合氯醛）

publicationofOutlineofPharmacologytrainedanumberofpreeminentscientistsJacobAbel

foundedandchairedthefirstdepartmentofpharmacologyintheUnitedStatesattheUniversityofMichiganisolationofepinephrine（腎上腺素）fromadrenalglandisolationofhistamine（組胺）frompituitaryextractpreparationofcrystallineinsulin（胰島素）WilliamWithering

discovererofdigitalis（洋地黃）forthetreatmentofcongestiveheartfailure（充血性心力衰竭）

DefinitionsPharmacologyhasbeendefinedasanexperimentalsciencethatstudieschangesbroughtaboutinvivoandinvitrobychemicallyactingsubstances,whetherusedfortherapeuticpurposeornot.Inthebroadestsense,pharmacologyisthescienceofstudyingtheeffectofdrugsonlivingorganisms.Itattemptstodescribethebiologicalresponseproducedbydrugsandtodefinetheunderlyingmechanismsbywhichtheresponsesaregenerated.Drugs:Broadlydefined,adrugisachemicalsubstancethatcanalterorinfluencetheresponsivenessofabiologicalsystem.Theactionofadrugismediatedbyanaturallyoccurringprocessofthebody.Adrugeithermimics,facilitate,orantagonizesanormallyoccurringphenomenon.Classificationofdrugs:DrugsusedtocombatinfectionSelectivetoxicityistheabilityofachemicalordrugtokillamicroorganismwithoutharmingitshostChemotherapy,initsmostgeneralsense,isthetreatmentofadiseasebychemicalsespeciallybykillingmicro-organismsorcancerouscells.

bacteriaHumanspenicillincellwallbiosynthesiswithoutcellwallsulfadrugs(磺胺藥物)folicacidsynthesisthesyntheticpathwayisnotneededDrugsusedtoreplaceinadequaciesofnaturallyoccurringsubstance

insulin:isahormonethatiscentraltoregulatingenergyandglucosemetabolisminthebody.Wheninsulinisabsent,glucoseisnottakenupbybodycellsandaccumulate,diabetesmellitus（糖尿病）willresult.

L-dopa:Afterpassingthoughthebloodbrainbarrier（血腦屏障）,itisenzymaticallytransformedintodopamine,theinsufficiencyofwhichwillcauseparkinsonism(帕金森癥)Drugsthatchangeregulationantihypertensives,antianginals,diuretics,anticoagulants,analgesics,antipyretic,sedatives,birthcontrlpills(contraceptives)Drugstoaltermoodorbehavior(psychoactivedrug，精神藥物)achemicalsubstancethatcrossestheblood-brainbarrierandactsprimarilyuponthecentralnervoussystemwhereitaltersbrainfunction,resultinginchangesinperception,mood,consciousness,cognition,andbehavior。DrugatsiteofadministrationDruginplasmaDrug/metabolitesinurine,feces,bileDrug/metabolitesintissuesAbsorptionDistributionExcretionBiotransformation1.Pharmacokinetics(藥物代謝動力學(xué)):Scope2.Pharmacodynamics（藥物效應(yīng)動力學(xué)）:isthestudyofthephysiologicaleffectsofdrugsonthebodyoronmicroorganismsorparasiteswithinoronthebodyandthemechanismsofdrugaction，includingthecorrelationoftheiractionswithconcentrationsaswellastherelationshipbetweentheactivityandthechemicalstructure.Dose-responsecurve(量效曲線)minimumeffectivedosemaximumefficacy（最大效能）

medianeffectivedoseslope（斜率）Structure-activityrelationship:therelationshipbetweenthechemicalorthree-dimensionalstructureofamoleculeanditsbiologicalactivity.TheanalysisofSARenablesthedeterminationofthechemicalgroupsresponsibleforevokingatargetbiologicaleffectintheorganism.ThisallowstomodifytheeffectorthepotencyofadrugbychangingitschemicalstructurePreclinicalpharmacology(animalpharmacologyorcomparativepharmacology)Pharmacologicalstudiesofcandidatedrugsinanimalsystemstoprovideevidenceoftheirpotentialactivity,servingaspredictorsofhumanresponseswiththegoalsofassuringsafetyandeffectivenessinhumansClinicalpharmacology:isthescienceofdrugsandtheirclinicaluse.Itisunderpinnedbythebasicscienceofpharmacology,withaddedfocusontheapplicationofpharmacologicalprinciplesandmethodsintherealworld.Itconnectsthegapbetweenmedicalpracticeandlaboratoryscience.Themainobjectiveistopromotethesafetyofprescription,maximizethedrugeffectsandminimizethesideeffectsPharmacotherapeutics（藥物治療學(xué)）:theuseofdrugsinthepreventionandtreatmentofdisease.Toxicology:theaspectofpharmacologythatdealswiththeadverseeffectsofdrugsTranslation1.Whilethemedicinal/organicchemistmaycreatethecandidatecompound(sometimesreferredtoasanewchemicalentity,NCE),itisthepharmacologistwhoisresponsiblefortestingitforpharmacologicalac