最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件

甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs甲狀腺激素和抗甲狀腺藥Thyroidhormonesanda1ThyroidhormonesandantithyroiddrugsSummaryThyroidhormones

Necessarytomaintainnormalmetabolism,growthanddevelopment.Hypothyroidism

CauseCretinismifithappensinembryoorneonatal

period.Causemyxedemaifithappensinadultswhenthethyroidhormonecouldbeusedinreplacementtherapy.Hyperthyroidism

Asyndromcharacterizedbythyroidoversecretionandmetabolicdisordercausedbymultiplereasons.Itcanbetreatedwithradioactiveiodine(131I)irradation,antithyroiddrugsandoperation.Thyroidhormonesandantithyro2最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件3最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件4最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件5最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件6最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件7最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件8Synthesis,storageandregulationofthyroidhormonesIodineuptakeIodineactivationandtyrosineiodationCondensationandstorageDisintegrationandreleaseRegulationSynthesis,storageandregula9Stepsofthyroidhormonessynthesis,releaseandregulationIodineuptake：I－inbloodcanbeuptakenintocellsbyiodinepumpintheadenocytemembrane.Theaminoacidscanbeusedtosynthesizethyroidglobulinincells.Iodineactivationandtyrosineiodation：I－uptakenintocellscanbeoxydizedtoactiveiodinebyperoxydase.ActiveiodinebindstotyrosineofTGandformsmonoiodotyrosine(MIT)and

diiodotyrosine(DTT).Stepsofthyroidhormonessynt10Stepsofthyroidhormonessynthesis,releaseandregulationCondensationandstorage：Inthethyroidglobulinmolecule,twoDTTsarecondensedtoT4,oneDTTandoneMITarecondensedtoT3，whichareallstoredinglandalveoluscolloid.Disintegrationandrelease：T3andT4arereleasedintobloodafterhydrolyzedbyproteases.Atthesametime,someofthemcanbeturnedbacktotyrosineandI－bydeiodinaseincellsandreused.Regulation：Bythepositiveandnegativefeedbackregulationofhypothalamus-anteriorlobe-thyroidaxis.HypothalamussecretsTRH,anteriorlobesecretsTSHandthyroidsynthesizeT3,T4.Stepsofthyroidhormonessynt11synthesis,storageandreleaseofthyroidhormone

GastrointestinalI-Blood

I-I-Peroxid-aseIoTGTyrIodat-ionMITDITCon-den-sationMIT+DITDIT+DITT3T4TGAcinarluminaStorageSynthesisReleaseActivationProteaseT3T4MIT一碘酪氨酸DIT二碘酪氨酸TG甲狀腺球蛋白血液synthesis,storageandreleas12ThyroidhormonesMechanismofactionThebindingofT3andRincreasestheuptakeofaaandglucose,resultingintheentrancetocytoplasmofT3.AfterreactingwithCBP,T3iseduced.ThefreeT3canbindRinthemitochondriaandmakeADPtoATP.Besides,itcanenterthenuclearandbindRthere,whichcanincreasethetranscriptionofDNAandthecontentofmRNA.Thenthenewproteinscanbesynthesizedandplayroles.ThyroidhormonesMechanismofa13Thyroidhormones作用機(jī)理（圖示)ItisbelievednowthatthethermogenicactionofT3andT4isduetotheincreaseofsodiumpumpsactivityonthecellmembrane.Na+,K+—ATPaseactivityATPutilizationADPconcentrationmitochondriarespirationoxideconsumptionandheatproductionThyroidhormones作用機(jī)理（圖示)14Physiologicalandpharmacologicalactions

KeepnormalgrowthanddevelopmentPromotesynthesisofproteinsaswellasgrowthanddevelopmentofskeletonandCNS.T3,T4deficientsecretion：causescretinismininfantsandyoungchildrenandmucousedemainadults.

PromotemetabolismandincreaseheatproductionPromoteoxidation,increaseoxygenconsumption，basalmetabolicrateandheatproduction.

Elevatesensitivityofsympathetic-adrenalsystem

Nervousness,trembling,heartbeatspeedup，bloodpressureincreasePhysiologicalandpharmacologi15ThyroidclinicalapplicationReplacementtherapymainlyTherapyanddiagnosisapplication

Cretinism

Treatingtheinfantsandchildrenassoonaspossiblecouldcurethemtonormal.Iftreatingtoolate,theyneedtobetreatedalifetime.

MucousedemaIncreasethedosageofthyroidpalletgradually.Toolargedosagemayaggravateheartdiseases.Patientsincomashouldbegivenafistaid,whichisinfusionofT3（40-120μg）intravenoiusly,reinjection5－15μgevery6handoraladministrationwhenawake.Hypopituitarismpatientsshouldbegivencorticalhormonefirstandfollowedbythyroidhormone.Simplegoiter ReplacementtherapycaninhibitTSHoversecretionandcontracttheglandularorgan,3-6months.T3inhibitiontestDifferentialdiagnosisforPatientswithiodinehighuptake.

ThyroidclinicalapplicationRe16AdverseeffectsadverseeffectoverdosecombinationcontraindicationhyperthyreosisoldpeopleheartdiseasebishydroxycoumarindantinaoraspirindiabeteshypertensionCoronaryheartdiseasepyknocardiathyroidcrisis：anxiety,fear,restlessness,highbodytemperature,increaseandirregularheartrate，increasepulsepressure，congestiveheartfailurewithvomit,diarrheaanddehydrationwhichleadtocomaanddeathAnginaorheartinfarctionIncreasetoxicityofthyroidhormoneAdverseeffectsadverseeffec17AntithyroidDrugsTherapiesofhyperthyrosisinclude131Iradiotherapy,exairesisormedication.Thioureahomologuesaremainlyusedclinically.Iodineandiodideareusedjustinpreparationforoperationsandthyroidcrisistherapy.βreceptorblockerscanbeusedasadjunctivetherapyforthyroidcrisis.AntithyroidDrugsTherapiesof18硫脲類(lèi)（Thiourea）硫氧嘧啶類(lèi)(thiouracil)：甲基硫氧嘧啶(methykthiouracil)丙基硫氧嘧啶(propylthiouracil)咪唑類(lèi)(imidazoles)：他巴唑(Tapazole)，甲巰咪唑(methimazole)甲亢平(卡比馬唑Carbimazole)硫脲類(lèi)（Thiourea）硫氧嘧啶類(lèi)(thiouracil)19ThioureaPhysiologicalprocessAbsorption：easytobeabsorbedwhentakenorally.Thiouracilisthemostfasttobeabsorbed.Thebioavailabilityis80％andtheplasmaproteinbindingrateis75%.20－30minafteradministration,thedrugturnstobecomeeffectivewithT1/2of2h.Imidazoleisabsorbedslowly.T1/2oftapazoleis6h.Distribution：organsgenerallyalloverthebodyandcanpasstheplacenta.Theconcentrationinlactoisabout3timesasinblood.Metabolism：Mainlyinliver,fast.60％aredestroyedinvivo，therestareeliminatedbyurineinaconjugativeform.Carbimazolefunctionsafterturningintotapazoleinvivo.ThioureaPhysiologicalprocess20ThioureaPharmacologicalactionsInhibitperoxydaseinadenocytes,whichresultsintheinhibitedoxydationofI－toI0.Then,theiodationandcoupleoftyrosinescanbestopped.SothebiosynthesisofT3andT4isinhibited.Buttheeffectoccursslowlyastheiodineuptakeandthehormonealreadysynthesizedarenoteffected.LongtimemedicationcanleadtodecreaseofT3andT4,whichfeedbackincreasesthesecretionofTSHandmakesthyroidhyperplasyandhyperemiccompensatorily.PropylthiouracilcaninhibitT4turningtoT3andcontrolT3levelinblood.Soitisthefirstchoiceinhyperthyroidismcrisis,severehyperthyroidismandpregnanthyperthyroidism.Inhibitimmuno-system(ashyperthyroidismisrelatedwithabnormalimmunoreactions).ThioureaPharmacologicalaction21EtiopathogenesisofExophthalmoshyperthyroidism

andfunctionlinkofthioureahomologuesThisdiseaseiscausedbyanautoimmuneIgGantibodyLATS(longactingthyroidstimulator),whichcanbindtothereceptorsonthyroidadenocytesandstimulateoversecretionofthyroidhormones.Thioureahomologuescannotonlyinhibitsynthesisofthyroidhormones,butalsoLATSinpatients,whichisakindofimmunoinhibition.EtiopathogenesisofExophthalm22ThioureaClinicalapplicationHyperthyroidismForwhohasmildsymptomsandisnotsuitabletohaveoperationsand131Iradiotherapy.GiveLargerdoseatthebeginning.After1~3months,symtomsdecreasedandbasalmetabolicratereturnstoalmostnormal.Reducetomaintainingdosewithaperoidof1~2years.Alsocanbeusedasadjunctivetherapyof131Iradiotherapy.Preparationbeforeoperation：Medicationbeforeoperationisgoodtodecreasebleedinginoperationandpreventthyroidcrisisafteroperation.Adjunctivemedicationofthyroidcrisis：Besidesintegratemeasures,largedoseofThioureahomologuescanbeusedasadjunctivetherapy,SoisPropranolol.ThioureaClinicalapplication23Comparisonamongcommonthioureahomologuesdrugs

drugpotency

therapeuticdosemaintenanceadverseeffects

agranulemia (mg/d) doseincidence(%)incidence(%)

mildmoderatesevere

(mg/d)

Methyl 1 200-300 400-600 13.8 0.5 thiouracil 300-400 50-100Propyl 0.75 3.3 0.4thiouracilTapazole10 20-30 40-60 7.1 0.1Carbimazole10 30-40 5-10 1.9 0.8Comparisonamongcommonthiou24ThioureaAdverseeffects

Althoughtherearelotsofadverseeffectsofthioureahomologues,incidencesofpropylthiouracilandtapazolearelower,3％and7％respectively.Commonadverseeffects：

skinrash,headache,dinus,gastrointestinaluncomfortable,fatigueandsoon.

Severeadverseeffects：bonemarrowdepression,agranulocytosisandsoon.Note：periodicinspectionofhemogram.Themedicationshoulebestoppedifthesymptomsaspharyngalgia,fever,cathaeresisoccur.Thyroidcancerpatientsareforbiddentotake.ThioureaAdverseeffects25IodineandiodideActionsandapplicationsLowdoseofiodine(physiologicaldose)couldpreventandcuresimple(endemicity)goiter.Add1/10000~1/100000potassiumiodideorsodiumiodidetosaltcouldpreventthedesease.LargedoseofiodinecouldinhibitthereleaseofT3andT4(duetotheinhibitionofTGhydratase).Usedasadjunctivetherapyforhyperthyroidism：①preparationbeforeoperation：administrationofaqueousiodinesolutiontwoweeksbeforeoperationdegeneratestheglandulartissue,decreasesvesselsandbleeding;②adjunctivetherapyforthyroidcrisis:couldbeusedcombinedwiththioureahomologues.IodineandiodideActionsanda26IodineandiodideAdverseeffectsandapplicationnotes

Acuteeffects：acutecircumscribededema，laryngealedemaandapnoeaChronictoxicity：mouthandthroatburningsensation,increasesecretionofsalivary,eyeirritationandsoon.

Inducedysthyroidandhyperthyroidismafterlongmedication.Iodinecouldpassintothemilkandthroughplacenta,leadingtoneonatgoiter.Pregnantandlactantwomenshouletakethedrugwithcausious.Allergicandactivetuberculosispatientsareforbiddentotake.IodineandiodideAdverseeffe27Radioactiveiodine（131I）

T1/2is8.04daysActions

131Icouldbeuptakenbythroid,participateinthesynthesisofT3,T4andisstoredinfollecularcolloid.131Imainlygeneratesβray（99％）withaverageandmaximumpathof0.5mmand2mmrespectively.Sotheirradiationfunctionislimitedinthethyroid.Itcandestroytheglandularorganbutcanseldomdestroythesurroundingtissues.Γraygeneratedby131Iaccountsfor1％andcanbedetectedinvitro.Itisusuallyusedintheexaminationofthyroidiodineuptakingfunction.Radioactiveiodine（131I）

T28Radioactiveiodine（131I）ClinicalapplicationThyroidiodineuptakefunctionexamination：iodineuptakeratehighwhenhyperthyroid,timeofiodineuptakepeakantelocationiodineuptakeratelowwhenhypothyroid,timeofiodineuptakepeakretropositionHyperthyroidismTraceamountcouldbeusedindiagnosisofthyroidfunctionalstatusandthyroidadenoma.Radioactiveiodine（131I）Clinic29放射性碘（131I）

AdverseeffectsandapplicationnotesHypothyroidismisthepredominantcomplication.Theadverseeffectscanbereducedbystrictdosecontrolandresistedbythyrine.PatientswithTotalwhitebloodcellslessthan3000/mm3arenotsuitabletotakeit.Soarepragnantandlactantwomen,patientsyoungerthan20yearsoldorwithsevereliverorkidneydeseases.

放射性碘（131I）Adverseeffectsand30receptorblockersValuableadjunctivetherapydrugsforhyperthyroidismandthyroidcrisis.Theycouldimprovesymptomscausedbyaugmentedsympatheticactivitysuchasspeedupheartrateandincreaseheartcontractionforce.TheycanalsoreducethethyroidhormonesecretionandT3synthesisbyinhibiting5`-deiodinase.Controlhyperthyroidismsymptomsandcanbeusedinpreparationbeforeoperation.receptorblockersValuablead31receptorblockersClinicalapplicationAdjunctivetherapyforhyperthyroidismandhyperthyroidismcrisis.MechanismofpharmacologicalactionsControlsymptomscausedbyexcitedsympathetic-adrenergicsystemβ1receptorblockage-heartratedropCentralβreceptorblockage-toreduceanxietyβ2receptoronNAenerginicperipheralnerveendingspresynapticmembraneblockagereducesthereleaseofNA.AppropriatelyreduceT3,T4secretion.receptorblockersClinicalap32Thanks!Thanks!33

結(jié)束語(yǔ)謝謝大家聆聽(tīng)?。?！34

結(jié)束語(yǔ)謝謝大家聆聽(tīng)?。。?4甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs甲狀腺激素和抗甲狀腺藥Thyroidhormonesanda35ThyroidhormonesandantithyroiddrugsSummaryThyroidhormones

Necessarytomaintainnormalmetabolism,growthanddevelopment.Hypothyroidism

CauseCretinismifithappensinembryoorneonatal

period.Causemyxedemaifithappensinadultswhenthethyroidhormonecouldbeusedinreplacementtherapy.Hyperthyroidism

Asyndromcharacterizedbythyroidoversecretionandmetabolicdisordercausedbymultiplereasons.Itcanbetreatedwithradioactiveiodine(131I)irradation,antithyroiddrugsandoperation.Thyroidhormonesandantithyro36最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件37最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件38最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件39最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件40最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件41最新甲狀腺激素和抗甲狀腺藥Thyroidhormonesandantithyroiddrugs課件42Synthesis,storageandregulationofthyroidhormonesIodineuptakeIodineactivationandtyrosineiodationCondensationandstorageDisintegrationandreleaseRegulationSynthesis,storageandregula43Stepsofthyroidhormonessynthesis,releaseandregulationIodineuptake：I－inbloodcanbeuptakenintocellsbyiodinepumpintheadenocytemembrane.Theaminoacidscanbeusedtosynthesizethyroidglobulinincells.Iodineactivationandtyrosineiodation：I－uptakenintocellscanbeoxydizedtoactiveiodinebyperoxydase.ActiveiodinebindstotyrosineofTGandformsmonoiodotyrosine(MIT)and

diiodotyrosine(DTT).Stepsofthyroidhormonessynt44Stepsofthyroidhormonessynthesis,releaseandregulationCondensationandstorage：Inthethyroidglobulinmolecule,twoDTTsarecondensedtoT4,oneDTTandoneMITarecondensedtoT3，whichareallstoredinglandalveoluscolloid.Disintegrationandrelease：T3andT4arereleasedintobloodafterhydrolyzedbyproteases.Atthesametime,someofthemcanbeturnedbacktotyrosineandI－bydeiodinaseincellsandreused.Regulation：Bythepositiveandnegativefeedbackregulationofhypothalamus-anteriorlobe-thyroidaxis.HypothalamussecretsTRH,anteriorlobesecretsTSHandthyroidsynthesizeT3,T4.Stepsofthyroidhormonessynt45synthesis,storageandreleaseofthyroidhormone

GastrointestinalI-Blood

I-I-Peroxid-aseIoTGTyrIodat-ionMITDITCon-den-sationMIT+DITDIT+DITT3T4TGAcinarluminaStorageSynthesisReleaseActivationProteaseT3T4MIT一碘酪氨酸DIT二碘酪氨酸TG甲狀腺球蛋白血液synthesis,storageandreleas46ThyroidhormonesMechanismofactionThebindingofT3andRincreasestheuptakeofaaandglucose,resultingintheentrancetocytoplasmofT3.AfterreactingwithCBP,T3iseduced.ThefreeT3canbindRinthemitochondriaandmakeADPtoATP.Besides,itcanenterthenuclearandbindRthere,whichcanincreasethetranscriptionofDNAandthecontentofmRNA.Thenthenewproteinscanbesynthesizedandplayroles.ThyroidhormonesMechanismofa47Thyroidhormones作用機(jī)理（圖示)ItisbelievednowthatthethermogenicactionofT3andT4isduetotheincreaseofsodiumpumpsactivityonthecellmembrane.Na+,K+—ATPaseactivityATPutilizationADPconcentrationmitochondriarespirationoxideconsumptionandheatproductionThyroidhormones作用機(jī)理（圖示)48Physiologicalandpharmacologicalactions

KeepnormalgrowthanddevelopmentPromotesynthesisofproteinsaswellasgrowthanddevelopmentofskeletonandCNS.T3,T4deficientsecretion：causescretinismininfantsandyoungchildrenandmucousedemainadults.

PromotemetabolismandincreaseheatproductionPromoteoxidation,increaseoxygenconsumption，basalmetabolicrateandheatproduction.

Elevatesensitivityofsympathetic-adrenalsystem

Nervousness,trembling,heartbeatspeedup，bloodpressureincreasePhysiologicalandpharmacologi49ThyroidclinicalapplicationReplacementtherapymainlyTherapyanddiagnosisapplication

Cretinism

Treatingtheinfantsandchildrenassoonaspossiblecouldcurethemtonormal.Iftreatingtoolate,theyneedtobetreatedalifetime.

MucousedemaIncreasethedosageofthyroidpalletgradually.Toolargedosagemayaggravateheartdiseases.Patientsincomashouldbegivenafistaid,whichisinfusionofT3（40-120μg）intravenoiusly,reinjection5－15μgevery6handoraladministrationwhenawake.Hypopituitarismpatientsshouldbegivencorticalhormonefirstandfollowedbythyroidhormone.Simplegoiter ReplacementtherapycaninhibitTSHoversecretionandcontracttheglandularorgan,3-6months.T3inhibitiontestDifferentialdiagnosisforPatientswithiodinehighuptake.

ThyroidclinicalapplicationRe50AdverseeffectsadverseeffectoverdosecombinationcontraindicationhyperthyreosisoldpeopleheartdiseasebishydroxycoumarindantinaoraspirindiabeteshypertensionCoronaryheartdiseasepyknocardiathyroidcrisis：anxiety,fear,restlessness,highbodytemperature,increaseandirregularheartrate，increasepulsepressure，congestiveheartfailurewithvomit,diarrheaanddehydrationwhichleadtocomaanddeathAnginaorheartinfarctionIncreasetoxicityofthyroidhormoneAdverseeffectsadverseeffec51AntithyroidDrugsTherapiesofhyperthyrosisinclude131Iradiotherapy,exairesisormedication.Thioureahomologuesaremainlyusedclinically.Iodineandiodideareusedjustinpreparationforoperationsandthyroidcrisistherapy.βreceptorblockerscanbeusedasadjunctivetherapyforthyroidcrisis.AntithyroidDrugsTherapiesof52硫脲類(lèi)（Thiourea）硫氧嘧啶類(lèi)(thiouracil)：甲基硫氧嘧啶(methykthiouracil)丙基硫氧嘧啶(propylthiouracil)咪唑類(lèi)(imidazoles)：他巴唑(Tapazole)，甲巰咪唑(methimazole)甲亢平(卡比馬唑Carbimazole)硫脲類(lèi)（Thiourea）硫氧嘧啶類(lèi)(thiouracil)53ThioureaPhysiologicalprocessAbsorption：easytobeabsorbedwhentakenorally.Thiouracilisthemostfasttobeabsorbed.Thebioavailabilityis80％andtheplasmaproteinbindingrateis75%.20－30minafteradministration,thedrugturnstobecomeeffectivewithT1/2of2h.Imidazoleisabsorbedslowly.T1/2oftapazoleis6h.Distribution：organsgenerallyalloverthebodyandcanpasstheplacenta.Theconcentrationinlactoisabout3timesasinblood.Metabolism：Mainlyinliver,fast.60％aredestroyedinvivo，therestareeliminatedbyurineinaconjugativeform.Carbimazolefunctionsafterturningintotapazoleinvivo.ThioureaPhysiologicalprocess54ThioureaPharmacologicalactionsInhibitperoxydaseinadenocytes,whichresultsintheinhibitedoxydationofI－toI0.Then,theiodationandcoupleoftyrosinescanbestopped.SothebiosynthesisofT3andT4isinhibited.Buttheeffectoccursslowlyastheiodineuptakeandthehormonealreadysynthesizedarenoteffected.LongtimemedicationcanleadtodecreaseofT3andT4,whichfeedbackincreasesthesecretionofTSHandmakesthyroidhyperplasyandhyperemiccompensatorily.PropylthiouracilcaninhibitT4turningtoT3andcontrolT3levelinblood.Soitisthefirstchoiceinhyperthyroidismcrisis,severehyperthyroidismandpregnanthyperthyroidism.Inhibitimmuno-system(ashyperthyroidismisrelatedwithabnormalimmunoreactions).ThioureaPharmacologicalaction55EtiopathogenesisofExophthalmoshyperthyroidism

andfunctionlinkofthioureahomologuesThisdiseaseiscausedbyanautoimmuneIgGantibodyLATS(longactingthyroidstimulator),whichcanbindtothereceptorsonthyroidadenocytesandstimulateoversecretionofthyroidhormones.Thioureahomologuescannotonlyinhibitsynthesisofthyroidhormones,butalsoLATSinpatients,whichisakindofimmunoinhibition.EtiopathogenesisofExophthalm56ThioureaClinicalapplicationHyperthyroidismForwhohasmildsymptomsandisnotsuitabletohaveoperationsand131Iradiotherapy.GiveLargerdoseatthebeginning.After1~3months,symtomsdecreasedandbasalmetabolicratereturnstoalmostnormal.Reducetomaintainingdosewithaperoidof1~2years.Alsocanbeusedasadjunctivetherapyof131Iradiotherapy.Preparationbeforeoperation：Medicationbeforeoperationisgoodtodecreasebleedinginoperationandpreventthyroidcrisisafteroperation.Adjunctivemedicationofthyroidcrisis：Besidesintegratemeasures,largedoseofThioureahomologuescanbeusedasadjunctivetherapy,SoisPropranolol.ThioureaClinicalapplication57Comparisonamongcommonthioureahomologuesdrugs

drugpotency

therapeuticdosemaintenanceadverseeffects

agranulemia (mg/d) doseincidence(%)incidence(%)

mildmoderatesevere

(mg/d)

Methyl 1 200-300 400-600 13.8 0.5 thiouracil 300-400 50-100Propyl 0.75 3.3 0.4thiouracilTapazole10 20-30 40-60 7.1 0.1Carbimazole10 30-40 5-10 1.9 0.8Comparisonamongcommonthiou58ThioureaAdverseeffects

Althoughtherearelotsofadverseeffectsofthioureahomologues,incidencesofpropylthiouracilandtapazolearelower,3％and7％respectively.Commonadverseeffects：

skinrash,headache,dinus,gastrointestinaluncomfortable,fatigueandsoon.

Severeadverseeffects：bonemarrowdepression,agranulocytosisandsoon.Note：periodicinspectionofhemogram.Themedicationshoulebestoppedifthesymptomsaspharyngalgia,fever,cathaeresisoccur.Thyroidcancerpatientsareforbiddentotake.ThioureaAdverseeffects59IodineandiodideActionsandapplicationsLowdoseofiodine(physiologicaldose)couldpreventandcuresimple(endemicity)goiter.Add1/10000~1/100000potassiumiodideorsodiumiodidetosaltcouldpreventthedesease.LargedoseofiodinecouldinhibitthereleaseofT3andT4(duetotheinhibitionofTGhydratase).Usedasadjunctivetherapyforhyperthyroidism：①preparationbeforeoperation：administrationofaqueousiodinesolutiontwoweeksbeforeoperationdegeneratestheglandulartissue,decreasesvesselsandbleeding;②adjunctivetherapyforthyroidcrisis:couldbeusedcombinedwiththioureahomologues.IodineandiodideActionsanda60IodineandiodideAdverseeffectsandapplicationnotes

Acuteeffects：acutecircumscribededema，laryngealedemaandapnoeaChronictoxicity：mouthandthroatburningsensation,increasesecretionofsalivary,