硫代酰胺硫脲类丙硫氧嘧啶PTU卡比马唑.PPT

* 甲亢病人在甲状腺次全切除或甲状腺切除后，因为手术的刺激，机体对甲状腺激素的反应大大增强，出现甲亢症状，严重者可出现甲状腺危象。 * 碘中毒：铜腥味、口咽烧灼感，牙和牙龈疼痛，唾液分泌增多，眼刺激症状 * Normal：FT3 4~10 pmol/L； FT4 10-31pmol/L TSI: 甲状腺刺激性免疫球蛋白 Thyroid hormones and antithyroid drugs Shi-Hong Zhang (张世红) shzhang713@zju.edu.cn Front view Thyroid gland Biosynthesis of thyroid hormones 1. Uptake of iodide 2. Oxidation of iodide (peroxidase) and iodination and coupling of tyrosine 3. Formation of thyroxine (T4) and triiodothyronine (T3) from iodotyrosine (peroxidase) 4. Secretion of thyroid hormones (proteolytic enzymes) 5. Regulation by thyroid stimulating hormone (TSH), T4, T3 三碘甲状腺原氨酸 四碘甲状腺原氨酸 甲状腺素的生理及药理作用 1．维持生长发育 2．促进代谢和产热 3．提高交感神经系统的敏感性 Hypothyroidism cretinism (呆小症) 瘿 simple goiter (单纯性甲状 腺肿) Hypothyroidism After treatment Hyperthyroidism 颤抖 腱反射亢进 心慌，心脏肥大 甲状腺肿大，突眼，情绪激动 多食、腹泻、消瘦 Hypothyroidism: iodine and iodides (small doses); thyroid hormone Therapeutic drugs on thyroid dysfunction 1 甲状腺功能低下：呆小病；黏液性水肿（甲状腺功能减退）；不典型及亚临床型甲状腺功能减退；甲状腺切除术后 2 单纯性甲状腺肿 3 T3抑制试验（服用T3后摄碘率下降50%者为单纯性甲状腺肿， 50%者为甲亢） 甲状腺素的临床应用 Hypothyroidism: thyroid hormones iodine and iodides (小剂量) Hyperthyroidism: antithyroid drugs: thiourea derivatives 硫脲类 iodine and iodides 碘和碘化物 （大剂量） ? receptor antagonists Radioiodines 放射性碘: 131I Therapeutic drugs on thyroid dysfunction (硫代酰胺；硫脲类) 丙硫氧嘧啶 PTU 卡比马唑，甲亢平 甲巯咪唑，他巴唑 MMI Thiourea derivatives Antithyroid drugs 硫脲类 Thiourea derivatives 1. Pharmacological effects (1) Inhibit the formation of thyroid hormones by interfering with iodination: competing peroxidation, then the iodination and coupling Symptom relieving: 2-3 weeks Basic metabolic rate returning: 1-2 months (2) Inhibit peripheral deiodination of T4: T4 ? T3 ? (propylthiouracil 丙硫氧嘧啶), rapid remission of hyperthyroidism due to T3 upregulation. Antithyroid drugs Thiourea derivatives 1. Pharmacological effects (3) Inhibit glucose metabolism by down-regulating β receptor (4) Immunosuppression: TSI↓ Antithyroid drugs 2. Clinical