THYROID GLAND ransport Peroxidase Thyroglobulin MIT-DIT-T3-Ta Proteolysis lodides thioamides SCN, CIA TT PERIPHERAL BLOOD TISSUES T3 ipodate B-blockers corticosteroids T3 Biosynthesis of thyroid hormones. The sites of action of various drugs that interfere with thyroid hormone biosynthesis are shown
Antithyroid drugs N CaHy Thiourea Propylthiouracil Methimazole derivatives丙硫氧嘧啶 甲巯咪唑 C-0-2 Carbimazole比马唑
丙硫氧嘧啶 卡比马唑 甲巯咪唑 Thiourea derivatives Antithyroid drugs
Antithyroid drugs Thiourea derivatives 1. Pharmacological effects (1)Inhibiting the formation of thyroid hormones by interfering with iodination: inhibiting peroxidation, then the iodination and coupling Symptom relieving: 2-3 weeks Basic metabolic rate returning 1-2 months (2)Inhibiting peripheral deiodination of T4: T4> T3t ( propylthiouracil丙硫氧嘧啶)
Thiourea derivatives 1. Pharmacological effects (1) Inhibiting the formation of thyroid hormones by interfering with iodination: inhibiting peroxidation, then the iodination and coupling Symptom relieving: 2-3 weeks Basic metabolic rate returning: 1-2 months (2) Inhibiting peripheral deiodination of T4 : T4 → T3 (propylthiouracil 丙硫氧嘧啶) Antithyroid drugs
Antithyroid drugs Thiourea derivatives 1. Pharmacological effects (3)Inhibiting glucose metabolism by down regulatingβ receptor (4)Immunosuppression: TSI
Thiourea derivatives 1. Pharmacological effects (3) Inhibiting glucose metabolism by downregulating βreceptor (4) Immunosuppression: TSI↓ Antithyroid drugs
H2o H2O drug TPO TPo。x TPO-drug H今ro,oda ②目+ TPo」 TPO+ xidized⑤ Drug-I MIT-Tg PO Oxidation steps Drug +Tyr-Tg Mechanism of inhibition of thyroid hormone synthesis by thioureas: Thioureas are oxidized by oxidized thyroid peroxidase(TPO)
Mechanism of inhibition of thyroid hormone synthesis by thioureas: Thioureas are oxidized by oxidized thyroid peroxidase (TPO)