Cohen H N, Fyffe J A, Ratcliffe W A, McNicol A M, McIntyre H, Kennedy J S, Thomson J A
J Endocrinol. 1981 Nov;91(2):299-303. doi: 10.1677/joe.0.0910299.
The effects on pituitary-thyroid function of the commonly prescribed anti-bacterial preparations co-trimoxazole and co-trifamole, and their component drugs, have been studied in the rat and compared to the changes caused by propylthiouracil. Co-trimoxazole and co-trifamole, in doses 20-fold in excess of a pharmacological dose administered for 10 days, produced marked changes in hormone levels consistent with blocking of hyperplastic goitre formation, were also demonstrated. Propylthiouracil produced less marked changes of thyroid hormone levels but higher levels of thyroid-stimulating hormone. Pharmacological doses of co-trimoxazole and co-trifamole and sulphamoxole, the sulphonamide component of co-trifamole, caused significant changes in thyroid hormone levels consistent with anti-thyroidal activity. In contrast, there was no evidence that trimethoprim, which is common to both preparations, or sulphamethoxazole, the sulphonamide component of co-trimoxazole, had an anti-thyroidal action, indeed, serum thyroxine levels were significantly increased at pharmacological dosage. We have concluded that the new commonly prescribed combination preparations retain the goitrogenic properties of the earlier sulphonamides.
已在大鼠中研究了常用抗菌制剂复方新诺明和复方三嗪磺胺及其成分药物对垂体 - 甲状腺功能的影响,并与丙硫氧嘧啶引起的变化进行了比较。复方新诺明和复方三嗪磺胺以超过药理剂量20倍的剂量给药10天,导致激素水平发生显著变化,这与增生性甲状腺肿形成的阻断一致。丙硫氧嘧啶引起的甲状腺激素水平变化较小,但促甲状腺激素水平较高。复方新诺明、复方三嗪磺胺和复方三嗪磺胺的磺胺成分磺胺异恶唑的药理剂量导致甲状腺激素水平发生显著变化,与抗甲状腺活性一致。相比之下,没有证据表明两种制剂共有的甲氧苄啶或复方新诺明的磺胺成分磺胺甲恶唑具有抗甲状腺作用,事实上,在药理剂量下血清甲状腺素水平显著升高。我们得出结论,新的常用复方制剂保留了早期磺胺类药物的致甲状腺肿特性。