Thiourea derivatives 2. Clinical uses (1)Non-operative therapy of hyperthyroidism: latent period (2)Preoperative therapy of hyperthyroidism: combined with iodide (3)Thyrotoxic crisis: combined with larger dose of iodide, propylthiouracil 3. Adverse effects (1) Agranulocytosis(0.2%) (2)Hypersensitivity (3 Gl reactions (5)Goitrogenic action (goiter): TSHT
2. Clinical uses (1) Non-operative therapy of hyperthyroidism: latent period (2) Preoperative therapy of hyperthyroidism: combined with iodide (3) Thyrotoxic crisis: combined with larger dose of iodide, propylthiouracil 3. Adverse effects (1) Agranulocytosis (0.2%) (2) Hypersensitivity (3) GI reactions (5) Goitrogenic action (goiter): TSH↑ Thiourea derivatives
Antithyroid drugs lodine and iodides 1. Pharmacological effects (1)Small doses: simple goiter (2) Larger doses: inhibiting the release of thyroid hormones(proteolysis l )and synthesis After iodide use, the thyroid vascularity is reduced, and the gland becomes much firmer, the cells become smaller
Iodine and iodides 1. Pharmacological effects (1) Small doses: simple goiter (2) Larger doses: inhibiting the release of thyroid hormones (proteolysis ) and synthesis After iodide use, the thyroid vascularity is reduced, and the gland becomes much firmer, the cells become smaller. Antithyroid drugs
TPO TPO |+ INHIBITOR H2O2 or Tg DIT H20, fDI METABOLIC STEP L HOI MIT A lodide transport CIO, SCN- lumen I iodination PTU MMI EOI C Coupling PTU, MMI D Colloid resorption Colchicine, Li2+,I- Cytochalasin B E Proteolysis F Deiodination of DIT MIT Dinitrotyrosine PTU apical membrane G Deiodination of T4 cell E MIT DIT. 5 de iodinate 4 G 3 上: ECF A basement membrane Mechanism of iodides
Mechanism of iodides
Antithyroid drugs 2. Clinical uses (1) Simple goiter (2)Preoperative therapy of hyperthyroidism combined with thiourea derivatives (2)Thyrotoxic crisis: combined with thiourea derivatives(propylthiouracil) Lugol's solution卢戈氏液:5% iodine and 10% potassium iodide
2. Clinical uses (1) Simple goiter (2) Preoperative therapy of hyperthyroidism: combined with thiourea derivatives (2) Thyrotoxic crisis: combined with thiourea derivatives (propylthiouracil) Lugol’s solution 卢戈氏液: 5% iodine and 10% potassium iodide Antithyroid drugs
Antithyroid drugs 3. Adverse effects (1)Acute effects: hypersensitivity, angioedema, swelling of the larynx 2 Chronic intoxication(iodism) (3) Thyroid dysfunction: exacerbation of hyperthyroidism, goiter
3. Adverse effects (1) Acute effects: hypersensitivity, angioedema, swelling of the larynx (2) Chronic intoxication (iodism) (3) Thyroid dysfunction: exacerbation of hyperthyroidism, goiter Antithyroid drugs