【医学ppt课件】 甲状腺激素和抗甲状腺药

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1、甲状腺激素和抗甲状腺药Thyroidhormonesandantithyroiddrugs北京协和医学院基础医学院药理学系叶菜英SummaryThyroidhormonesNecessarytomaintainnormalmetabolism,growthanddevelopment.HypothyroidismCauseCretinismifithappensinembryoorneonatalperiod.Causemyxedemaifithappensinadultswhenthethyroid

2、hormonecouldbeusedinreplacementtherapy.HyperthyroidismAsyndromcharacterizedbythyroidoversecretionandmetabolicdisordercausedbymultiplereasons.Itcanbetreatedwithradioactiveiodine(131I)irradation,antithyroiddrugsandoperation.ThyroidhormonesThyroxine,T4Trii

3、odothyreninumnatricum,T3Synthesizedandsecretedbythyroid抗甲状腺药分为4类：硫脲类Thiourea碘和碘化物（复方碘溶液，lugol’ssolution））放射性碘（131I）β受体阻断药（心得安等从略）硫脲类硫氧嘧啶类（thiouracil）：甲基硫氧嘧啶（methykthiouracil）丙基硫氧嘧啶（propylthiouracil）咪唑类（imidazoles）他巴唑（Tapazole，甲巯咪唑methimazole）甲亢平（卡比马唑Car

4、bimazole）ThyroidhormonesareiodicaminoacidsActivecomponentsThyroxine,T4Triiodothyreninumnatricum,T3ChemicalconstitutionThyroidhormones甲状腺激素的化学结构PhysiologicaldispositionofthyroidhormonesAbsorbedrapidlywhentakeorally,activityT3>T4，maintainingtimeT4>T3.T1/2

5、ofT4andT3are6－7daysand1－2days,respectively.Deiodinationinmitochondriaofliverandkidney,eliminatedbykidneyafferconjugatedwithglucuronicacidandsulfuricacid.T3,T4canalsopasstheplacentaandentermilk.Figure:theamountofnormaladults’thyroidhormonesproducedandmet

6、abolizeddaily.Synthesis,storageandregulationofthyroidhormonesIodineuptakeIodineactivationandtyrosineiodationCondensationandstorageDisintegrationandreleaseRegulationStepsofthyroidhormonessynthesis,releaseandregulation(Ⅰ)Iodineuptake:I－inbloodcanbeuptaken

7、intocellsbyiodinepumpintheadenocytemembrane.Theaminoacidscanbeusedtosynthesizethyroidglobulinincells.Iodineactivationandtyrosineiodation:I－uptakenintocellscanbeoxydizedtoactiveiodinebyperoxydase.ActiveiodinebindstotyrosineofTGandformsmonoiodotyrosine(MI

8、T)anddiiodotyrosine(DTT).Condensationandstorage:Inthethyroidglobulinmolecule,twoDTTsarecondensedtoT4,oneDTTandoneMITarecondensedtoT3，whichareallstoredinglandalveoluscolloid.Disintegrationandrelease:T3andT4arereleasedintobloodafte