药物化学研究案例.docx
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药物化学研究案例.docx
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药物化学研究案例
CASESTUDY
MedicinalChemistry
Case1
Adentistcallsyourpharmacyandasksyouprepareanantisepticmouthwashforapatientwithapainfulbacterialinfectionoftheoralcavity.Youaskyoursecond-yearpharmacyinterntoresearchtheproject,andshesuggestscombiningbupivacainehydrochloride(localanesthetic)withcetylpyridiniumbromide(antiinfective)
Case1-Q1Identifytheacidic,basic,orneutralcharacterofthetwodrugmoleculesinthecasebasedonsaltname.
Case1-Q2Arethesespeciesionizedorunionizedinsaltform?
Case1-Q3Fromanacid-basestandpoint,isthemouthwashsuggestionsound?
Case3
Adistraughtmothercallsthepoisoncontrolcenterwhereyouwork.Her6-year-oldsonjustarehalfabottleofNH4Cltabletsmeantforthefamilycat.Asacomplicationofmorbidobesity,Heishypertensive(thesonnotthecat),andhasbeenontimololmaleate(blockadren)for6months.Asignificantfractionoftimololisexcretedunchangedintheurine,andanoverdosecanresultinbradycardiaandhypotension.
Case3-1QFromanacid-basestandpoint,isthisapotentialmedicalemergency?
Why,orwhynot?
Case5
ZT,a26-year-oldsinglemotheroffourwithahistoryofdepression,isrushedunconscioustotheemergencyroomofthehospitalwhereyouwork.Theattendanthandsyouanemptybottlethathadcontained10tabletsofamobarbitalsodium(pKa=8.0)Afterstabilizingrespirationandperforminggastriclavage,youdecidetoenhancetherenaleliminationofthedrug.ZThasaurinarypHof6.0.
pKa=8.0
Case5–Q1Whatistheacid-basecharacterofamobarbitalsodium?
Case5–Q2Whatwouldbetheratioofionizedtounionizeddrugformsinthispatient’surine?
Case5–Q3WouldyourecommendtheIVadministrationofNH4ClorNaHCO3?
Case5–Q4TheERnurseispreparingtoaddphenterminehydrochloridetotheIVbagcontainingthepHmodifieryouhavejustelected.Wouldyoustophim?
Why,orwhynot?
Case17
YouareanM.D./Ph.D.(inmedicinalchemistry,ofcourse)practicinggeneralmedicineintheearly1930s.Themedicalcommunityisallatwitteraboutanewanti-infective,sodiumsulfanilamide,whichhasshownvalueinthetreatmentofurinarytractinfectionsandinfectionsecondarytoburns.Youareconcerned,however,aboutthetendencyofthisagenttocausecrystalluria,whichcanresultinsevere,life-threateningkidneydamage.ThepKaofsulfanilamide(17.1)is10.4.
Case17-Q1DrawthestructureofSodiumSulfanilamide.
Case17-Q2WhywouldapatientwithaurinarypHof5.4beatgreaterriskforthedevelopmentofcrystalluriathanonewithaurinarypHof6.4?
WhatwouldbetheratioofionizedtounionizedsulfanilamidedrugformsateachurinarypH?
Case17-Q3WhichurinarypHmodifierwouldyouprescribeforapatientwhobegantoshowsymptomsofcrystalluria,NH4ClorNaHCO3?
Case17-Q4Asamedicinalchemist,youunderstandtheimpactofstructureonthetherapeuticprofileofdrugmolecules,anddrugdesignvisionsarenowdancinginyourhead.Whichofthethreemodifiedsulfanilamidestructures(17.3~17.5)wouldhaveahighertherapeuticindexwithregardtocrystalluria?
Whatisthestructuralbasisforyouranswer?
Case28
LP,aprepharmacystudentattendingalocaljuniorcollege,hasbeentakingorganicchemistry(herfavoriteclass)andhasbeenstartingtoreallyunderstandorganicstructures.Shehasbeenseeingherphysicianregularlyforallergyproblemsthatareparticularlytroublesomeinthefall(ragweedseason).Shehasbeentakingdiphenhydramine(28.1)formorethanayearnow,butitisreallybotheredbythedrymouthandsleepinessthatshehascometoassociatewithtakingthisdrug.Lately,shehasbeendrinkinglotsofcolastostayawakeinorganicchemistryandcombatthedrymouth.Shenowthinksthatsheisdependentoncaffeine.YouarethepharmacistondutyatthedrugstorewhenLP’sphysiciancallstoaskforadviceregardinganalternativemedication.
Case28-Q1Explainthereasonsforthesideeffectsthathavebeenobservedwithdiphenhydramine(28.1).
Case28-Q2Recommendoneofthefollowingdrugsasanappropriatechoiceforthispatient.Justifyyourchoiceanddiscussbrieflywhytheotherchoicesareinappropriate.
28.2Ranitidine
28.3chlorpheniramine
28.4cetirizine
28.5Bethanechol
Case46
Imagineyourselfasdruginformationspecialistatapoisoncontrolcenter.Atechnicianfromthecoroner’sofficeisinvestigatingacaseandrequiresassistanceinidentifyingthepossiblesourcesofbenzodiazepines(BZDs)inthetoxicologyprofileofaparticularcorpse.ThetechnicianhasidentifiedfourdistinctBZDsinthebloodsample.Shebelievesthatthemajorcomponentisdiazepam(46.1)(72%oftheidentifiedBZDs)andthattheremainingthreecompoundsaremetabolites(NOTE:
theassayidentifiesonlyactivecompounds).
Case46–Q1WhatarethethreestructuresofpotentialACTIVEmetabolitesfordiazepam(46.1)?
Case50
SAisa20-year-olduniversitycoedwhopresentstothestudenthealthservicecomplainingofextremenervousness,irritability,anddifficultyconcentrating.Forthepastyear,SAhasconstantlyworriedaboutachievingsufficientlyhighgradesinherprepharmacycoursestoqualifyforentryintotheDoctorofpharmacyprogram.Sheisalsoconcernedaboutherskincondition,whichhasworsenedsincesheenteredtheuniversity2yearsage’shassufferedfromatomicdermatitissincehighschool,aconditionwhichuntilrecentlyhadbeenkeptundercontrolusingtopicalhydrocortisone(0.5%cream).AsthetimeforherinterviewwiththeCollegeofPharmacyadmissionscommitteeapproaches,SA’sworryincrease,andshehasbecomeincreasinglyagitated,isunabletoconcentrateonherstudies,andhasshortnessofbreathandpalpitations.Tomakemattersworse,theitchingrashonherfaceandarmshasworsened.
Thestudenthealthphysician,inconsultationwithSA’sfamilydoctor,decidesonadiagnosisofgeneralizedanxietydisorder(GAD).Thetwophysiciansagreethatabenzodiazepineisindicated.
Case50-Q1Selectabenzodiazepinefromthestructures(50.1-50.5)providedthatwouldbethemostappropriatefortreatingSA’sanxiety.Justifyyourchoiceonthebasisofstructure/potencyanddurationofaction/relationships.Eliminateinappropriatechoicesonthesamebasis.
Case50-Q2HowlongshouldSAmaintainedonanti-anxietymedication?
Explainfully.
Case50-Q3Whatareyougoingtodoforthepatient’satopicdermatitis?
Case83
FPisa62-year-oldmalevintnerwithhypertensionthatisnotwellcontrolledonhydrochlorothiazide50mgdailyandcaptopril50mgtid.Bloodpressuresontreatmentrangesfrom160to170systolicand95to105diastolic.Tendaysago,FPdevelopedacoldthatinitiallygotsomewhatbetter,buttheworsenedoverthelast3days,withthedevelopmentoffacialpainbelowtheeyes,whichismadeworsewhenhebendsover;apurulentnasaldischargethat“tastesandsmellsfoul”;andafeverof101F.Thedoctorplanstotreatthesinusitiswithamoxicillin500mgtidfor3weeksandwantsdecongestanttreatmentforthefirst3to5days,butisconcernedaboutitseffectonFP’sbloodpressure.FPusedDristannasalsprayforhiscold,butstoppedbecause“itmademejittery”.Thedoctorcallsaskingforarecommendationforadecongestantthatwillexertminimaleffectonbloodpressureandwon’tmakeFPfeeljittery.
Case83-Q1Selectadecongestantfromthestructures(83.1~83.5)providedthatyouwouldrecommendforFP.Explainyourrationalonastructure/activitybasis.
Case84
AstheinpatientpharmacistatBigshotsUniversityHospital,youhavereceivedacallfromamedicalstudentforsomedruginformation.ThismedicalstudentisworkingonacasepresentationforapatientwhohasbeenorderedAldomet500mgIVq6h.Hisquestionforyouis:
whywouldanIVsolutionbepreparedwithα-methyldopatehydrochloride(AldometIV[84.1])ratherthanα-methyldopate(Aldomet[84.2])?
Case84-Q1WhywouldanIVsolutionbepreparedwithα-methyldopatehydrochloride(AldometIV[84.1])ratherthanα-methyldopate(Aldomet[84.2])
Case86
HS,awesternNebraskafarmer,isbroughtbyhiswifetotheemergencyroomofyourlocalhospitalwithabrokenleg.Hisalsocomplainingofweaknessanddizziness,whichheisattributingtothepainofhisbreak.Youalsonotethatheissalivatingandsweatingexcessively,hasalowheartrate,andisbreathingwithsomedifficulty.Youdiscoverthat,inthefarmaccidentwhichcausedthebrokenleg,hecameincontactwithlargequantitiesoftheinsecticideParathion(硝苯硫磷酯)(86.1).
Case86-Q1Explainthecauseofthefarmer’ssymptoms.
Case86-Q2Whichofstructures(86.2~86.5)shouldbeimmediatelyadministered?
Why?
Case88
LNisa74-year-oldwomanwhopresentstoherHMOwithmalaise,shortnessofbreath,andfatigue.Shealsocomplainsofweightgainandswollenhandsandfeet.LNhasa6-monthhistoryofcongestiveheartfailure(CHF),a3-yearhistoryofhypercholesterolemia,anda6-yearhistoryofadultonset(typeII)diabetesmellitus.Twoweeksago,LNsufferedamildstrokeandwashospitalizedfor3days.Shewasthendischargedwithaprescriptionfororalwarfarin(5mgdaily)for3weeks.Herothercurrentmedicationsinclude:
digoxin(0.125mgdaily),lovastatin(20mgatnight),andtolazamide(250mgdaily).Thepatient’screatinineclearanceis35mL/min.ThecardiologistdeterminesthatthedigoxinaloneisinsufficienttocontrolLN’scongestiveheartfailure.Becausepreviousattemptstouseangiotensin-convertingenzymeinhibitorscausedintolerablehypotension,itisdecidedtoemploydiuretictherapy.
Case88-Q1Whichdiuretic(s),ofthestructures(88.
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