Abdi Hengameh, Amouzegar Atieh, Azizi Fereidoun
Endocrine Research Center, Research Institute for Endocrine Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Iran J Pharm Res. 2019 Fall;18(Suppl1):1-12. doi: 10.22037/ijpr.2020.112892.14005.
The thionamide drugs, carbimazole and its metabolite methimazole (MMI), and propylthiouracil (PTU) have extensively been used in the management of various forms of hyperthyroidism over the past eight decades. This review aims to summarize different aspects of these outstanding medications. Thionamides have shown their own acceptable efficacy and even safety profiles in treatment of hyperthyroidism, especially GD in both children and adults and also during pregnancy and lactation. Of the antithyroid drugs (ATDs) available, MMI is the preferred choice in most situations taking into account its better efficacy and less adverse effects accompanied by once-daily dose prescription because of a long half-life and similar cost. Considering the more severe teratogenic effects of MMI, PTU would be the selected ATD for treatment of hyperthyroidism during pre-pregnancy months and the first 16 weeks of gestation. Recent studies have confirmed the efficacy and safety of long-term MMI therapy with low maintenance doses for GD and toxic multinodular goiter. Despite the long-term history of ATD use, there is still ongoing debate regarding their pharmacology and diverse mechanisms of action, viz. their immunomodulatory effects, and mechanisms and susceptibility factors to their adverse reactions.
硫酰胺类药物，如卡比马唑及其代谢产物甲巯咪唑（MMI）和丙硫氧嘧啶（PTU），在过去八十年中被广泛用于治疗各种类型的甲状腺功能亢进症。本综述旨在总结这些优秀药物的不同方面。硫酰胺类药物在治疗甲状腺功能亢进症，特别是儿童和成人以及妊娠和哺乳期的格雷夫斯病（GD）方面，已显示出其可接受的疗效和安全性。在现有的抗甲状腺药物（ATD）中，考虑到MMI疗效更好、不良反应更少，且由于其半衰期长且成本相似，每日只需服用一次，因此在大多数情况下是首选。鉴于MMI有更严重的致畸作用，PTU将是孕前数月和妊娠前16周治疗甲状腺功能亢进症的首选ATD。最近的研究证实了低维持剂量的MMI长期治疗GD和毒性多结节性甲状腺肿的疗效和安全性。尽管ATD有长期使用历史，但关于其药理学和多种作用机制，即免疫调节作用、不良反应的机制和易感因素，仍存在持续的争论。
