Karras Spiros, Tzotzas Themistoklis, Kaltsas Themistoklis, Krassas Gerasimos E
Department of Endocrinology, Diabetes and Metabolism, Panagia General Hospital, Thessaloniki, Greece.
Pediatr Endocrinol Rev. 2010 Sep;8(1):25-33.
Antithyroid drugs (ATD) are used as a first line treatment in thyrotoxicosis. Propylthiouracil (PTU), carbimazole (CMZ) and methimazole (MMI) are available. During absorption CMZ is bioactivated to MMI. Initially, mothers were not allowed to breastfeed during treatment with ATD. Newer studies minimized the risk for mother and infant. PTU should be preferred over MMI due to its lower milk concentration. Recent studies have shown severe hepatic dysfunction for both ATD, but especially for PTU, in hyperthyroid patients. Most of those cases were idiosyncratic, not-dose related and presented a latent period of occurrence. No biomarkers could predict hepatic damage. The American Thyroid Association (ATA) has recommended that PTU should not be prescribed as the first line agent in children and adolescents. Its use might be accepted in the first trimester of pregnancy for severe thyrotoxicosis or for patients with previous MMI adverse reactions. Considering the potential harmful effects of PTU, MMI should be used instead during lactation.
抗甲状腺药物（ATD）被用作甲状腺毒症的一线治疗药物。有丙硫氧嘧啶（PTU）、卡比马唑（CMZ）和甲巯咪唑（MMI）可供使用。在吸收过程中，CMZ被生物激活为MMI。最初，母亲在接受ATD治疗期间不被允许母乳喂养。最新研究将母婴风险降至最低。由于PTU在乳汁中的浓度较低，应优先于MMI使用。最近的研究表明，甲状腺功能亢进患者使用这两种ATD均会出现严重肝功能障碍，但PTU尤为明显。这些病例大多是特异质性的，与剂量无关，且有一段发生潜伏期。没有生物标志物能够预测肝损伤。美国甲状腺协会（ATA）建议，PTU不应作为儿童和青少年的一线用药。在妊娠早期，对于严重甲状腺毒症或既往有MMI不良反应的患者，PTU的使用可能会被接受。考虑到PTU的潜在有害影响，哺乳期应改用MMI。
