Johansen K, Andersen A N, Kampmann J P, Mølholm Hansen J M, Mortensen H B
Eur J Clin Pharmacol. 1982 Oct;23(4):339-41. doi: 10.1007/BF00613617.
It is universally stated that antithyroid drugs are concentrated in human milk and are thus contraindicated during breast-feeding. We recently showed, however, that propylthiouracil (PTU) was not concentrated in milk and a study has now been made of the excretion of another widely used antithyroid drug carbimazole (CMI) in human milk. Methimazole (MMI) in blood and milk from five lactating women was measured after oral administration of CMI 40 mg, which is rapidly and completely transformed to the active antithyroid compound MMI. One hour after CMI, the mean serum-MMI reached 253 microgram/I and the mean concentration of MMI in milk reached 182 microgram/I. MMI was found to be unionized and not to be protein bound in serum, and it occurred in milk in the same concentration as the serum; the mean milk/serum ratio was 0.98. The mean total amount of MMI excreted in milk over 8 h was 34 microgram (SEM +/- 5, n = 5), i.e. 0.14% of the dose administered.
普遍认为抗甲状腺药物会在人乳中浓缩，因此母乳喂养期间禁用。然而，我们最近发现丙硫氧嘧啶（PTU）不会在乳汁中浓缩，现在已对另一种广泛使用的抗甲状腺药物卡比马唑（CMI）在人乳中的排泄情况进行了研究。在五名哺乳期妇女口服40毫克CMI后，测定了她们血液和乳汁中的甲巯咪唑（MMI），CMI会迅速且完全转化为活性抗甲状腺化合物MMI。服用CMI一小时后，血清MMI平均达到253微克/升，乳汁中MMI的平均浓度达到182微克/升。发现MMI在血清中呈非离子化且不与蛋白质结合，并且在乳汁中的浓度与血清相同；平均乳/血比值为0.98。8小时内乳汁中排泄的MMI总量平均为34微克（标准误±5，n = 5），即给药剂量的0.14%。
