primary cause – 主因，原发性原因
iodide – n. 碘化物
ionic inhibitor – 离子抑制剂
radioactive – a. 放射性的
isotope – n. 同位素
radioactive isotopes – 放射性同位素
iodine – n. 碘
underlying cause – 基础原因，潜在原因
thioamide – n. 硫代酰胺
derivative –n. a. 衍生的，衍生物
methimazole – n. 甲巯咪唑
propylthiouracil – n. 丙硫氧嘧啶
iodine-131 – 碘-131
potassium iodide – 碘化钾
ablation – n. 消融
prophylaxis – n. 预防
incorporation – n. 结合
tyrosine – n. 酪氨酸
precursor – n. 前体，先驱者
impede – v. 妨碍，阻止
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Antithyroid Drugs 抗甲状腺药
Treatment of hyperthyroidism is aimed at treating either the primary cause or the symptoms of the disease. Antithyroid drugs, iodides, ionic inhibitors, surgery, and radioactive isotopes of iodine are used to treat the underlying cause, and beta blockers are used to treat the symptoms. The focus of this discussion is on the antithyroid drugs called thioamide derivatives, namely methimazole and propylthiouracil. In addition to the thioamides, radioactive iodine (iodine-131) and potassium iodide may be used to treat hyperthyroidism. Radioactive iodine works by destroying the thyroid gland, in a process known as ablation. It is a commonly used treatment for both hyperthyroidism and thyroid cancer. Potassium iodide is also used as prophylaxis for radiation exposure.
Methimazole and propylthiouracil act by inhibiting the incorporation of iodine molecules into the amino acid tyrosine, a process required to make the precursors of T3 and T4. By doing so, these drugs impede the formation of thyroid hormone. Propylthiouracil has the added ability to inhibit the conversion of T4 to T3 in the peripheral circulation. Neither drug can inactivate already existing thyroid hormone, however.
The drug effects of methimazole and propylthiouracil are primarily limited to the thyroid gland, and their overall effect is a decrease in the thyroid hormone level. Administration of these medications lowers the high levels of thyroid hormone, thereby normalizing the overall metabolic rate.
Antithyroid drugs are used to treat hyperthyroidism and to prevent the surge in thyroid hormones that occurs after the surgical treatment of or during radioactive iodine therapy for hyperthyroidism or thyroid cancer. In some types of hyperthyroidism, such as that seen in Graves’ disease, the long-term administration of these drugs (for several years) may induce a spontaneous remission. Surgical resection of the thyroid gland (thyroidectomy) is often used both in patients who are intolerant of antithyroid drug therapy and in pregnant women, in whom both antithyroid drugs and radioactive iodine therapy are usually contraindicated.
抗甲状腺药用于治疗甲状腺功能亢进，防止手术治疗后或放射性碘治疗甲状腺功能亢进或甲状腺癌期间出现的甲状腺激素激增。对于某些类型的甲状腺功能亢进来说，如见于格雷夫斯病者，长期（几年）这些药物可能诱发自行缓解。甲状腺手术切除（甲状腺切除术）经常用于甲状腺激素疗法不耐受患者和妊娠妇女患者，因为这些患者通常禁忌使用抗甲状腺药和放射性碘疗法。
Contraindications 禁忌症
The only usual contraindications to the use of the two antithyroid drugs are known drug allergy. Their use in pregnancy, although necessary, is somewhat controversial. Per the U.S. Food and Drug Administration (FDA), propylthiouracil is to be used during the first trimester only, and then methimazole is used for the remainder of the pregnancy. However, there are case reports of scalp abnormalities in the fetus when methimazole is used. The choice of how to treat pregnant patients is physician specific. Both drugs are classified as pregnancy category D drugs.
这两种抗甲状腺药使用的唯一禁忌是已知药物过敏。其妊娠使用尽管有必要，但在某种程度上，仍然存在争议。根据FDA，丙硫氧嘧啶只用于妊娠前三个月，剩余妊娠期则使用甲巯咪唑。不过，有病历报告显示，使用甲巯咪唑时，胎儿可出现头皮异常。选择如何治疗妊娠患者，要根据医师而定。这两种药物均归类为妊娠D类药。
Adverse Effects 不良效应
The most damaging or serious adverse effects of the antithyroid medications are liver and bone marrow toxicity.
抗甲状腺药的最破坏性或最严重不良效应是肝和骨髓毒性。
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Antithyroid Agents
★Tests ★
1. A patient who is in her first trimester of pregnancy is diagnosed with hyperthyroidism. Which medication do you suspect the patient will be started on?
A. Propylthiouracil (PTU)
B. Radioactive Iodine
C. Tapazole
D. Synthroid 2. A patient is receiving radioactive iodine treatment for hyperthyroidism. What will you include in your patient education to this patient about this type of treatment?
A. Taste changes and swollen salivary glands
B. Constipation
C. Excessive thirst
D. Sun protection
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答案 Answers
1. A. Propylthiouracil (PTU) Rationale: Propylthiouracil (PTU) is the only anti-thyroid medication that can be used during the 1st trimester of pregnancy. 2. A. Taste changes and swollen salivary glands Rationale: Taste changes and swollen salivary glands
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