三十一章甲状腺激素及抗甲状腺药.pptVIP

第三十一章　甲状腺激素及抗甲状腺药;; 促进机体生长、发育和成熟;促进代谢;;提高机体交感-肾上腺素系统的感受性;甲状腺激素的生理作用;第一节 甲状腺激素 ;Receptors for thyroid hormones are intracellular DNA-binding proteins that function as hormone-responsive transcription factors, very similar conceptually to the steroid hormone. 特异性核内受体介导甲状腺激素作用 Thyroid hormone receptors bind to short, repeated sequences of DNA called thyroid or T3 response elements (TREs), binding of the thyroid hormone-receptor complex activates transcription. ;碘摄取减少，引起TSH分泌增加。 长时间缺碘导致TSH过度分泌，最产生甲状腺肥大。;【体内过程】 t1/2 生物利用度 蛋白质亲和力 作用强度和持续时间 T3 2天 50%～75% 低( 游离量高) 快而强, 维持时间短 T4 6-8天 90%～95% 高 慢而弱、维持时间长 口服易吸收，与血浆蛋白结合率均高达99%以上， 主要在肝、肾线粒体内脱碘，并与葡萄糖醛酸或硫酸结合而 经肾排泄。T3与葡萄糖醛酸或硫酸结合后从胆汁排出。 T3、T4甲状腺激素可通过胎盘和进入乳汁。 The hormones are metabolized through the microsomal P-450 system. ;甲状腺激素的临床应用;INDICATIONS AND USAGE:1. As replacement or supplemental therapy for hypothyroidism of any etiology: cretinism, myxedema. Hypothyroidism is treated with T4 which is given once daily because of long half-life. Steady state is achieved at 6-8 weeks. 2. treatment or prevention of various types of euthyroid goiters ADVERSE REACTIOINS : Toxicity is directly related to thyroxine levels and manifests itself as nervousness, heart palpitations and tachycardia, intolerance to heat and unexplained weight loss. ;Hyperthyroidism leads to characteristic symptoms of nervousness, weight loss, heat intolerance, and fatigue. Signs such as tachycardia, tremor, accelerated reflexes, smooth skin, hyperhidrosis, and ocular stare are common to hyperthyroidism of any cause. Proptosis, diplopia, and corneal inflammation are specific findings in Graves’ disease. TSH受体持续兴奋，T3T4合成或分泌过度，一种自身免疫性疾病;In the absence of sufficient dietary iodide the thyroid cannot produce adequate amounts of T4 and T3. The resulting lack of negative feedback inhibition causes abnormally high level of the TSH secretion, which in turn stimulate the abnormal