Carthew P, Edwards R E, Nolan B M, Martin E A, Smith L L
MRC Toxicology Unit, University of Leicester, UK.
Carcinogenesis. 1996 Aug;17(8):1577-82. doi: 10.1093/carcin/17.8.1577.
Rats administered tamoxifen for 3 months and then returned to a basal diet developed an increase in uterine weight for up to 9 months after tamoxifen exposure. Stereological analysis of the tamoxifen exposed rat uteri showed that there was a significant increase in the amount of uterine myometrium, for a further 9 months, subsequent to the discontinuation of tamoxifen. A low incidence of myometrial proliferations (deciduomas) and uterine tumours was found at the conclusion of the study (20 months). In contrast, continuous administration of tamoxifen to mice for 24 months produced hyperplasia of the uterine endometrial epithelium and atrophy of the myometrium for the first 3 months, followed by atrophy of both the endometrium and myometrium for the remaining 21 months of the study. No uterine tumours were found in mice treated with tamoxifen for 2 years. The use of stereological analysis on interim sacrifice rodent uteri indicated that sustained uterine tissue compartment effects can occur, with either the continuous administration of tamoxifen, or after its discontinuation. Tamoxifen can have an agonist and antagonist like effect on oestrogen activity in different tissue compartments of the mouse uterus, over the same time period. The particular relevance of the finding of uterine proliferation and atrophy in the rodent studies with tamoxifen is discussed with regard to women taking this drug.
给予他莫昔芬3个月然后恢复基础饮食的大鼠,在接触他莫昔芬后长达9个月子宫重量增加。对接触他莫昔芬的大鼠子宫进行体视学分析表明,在停用他莫昔芬后的9个月里,子宫肌层数量显著增加。在研究结束时(20个月)发现子宫肌层增生(蜕膜瘤)和子宫肿瘤的发生率较低。相比之下,连续24个月给予小鼠他莫昔芬,在最初3个月会导致子宫内膜上皮增生和子宫肌层萎缩,在研究的剩余21个月里子宫内膜和子宫肌层均萎缩。用他莫昔芬治疗2年的小鼠未发现子宫肿瘤。对中期处死的啮齿动物子宫进行体视学分析表明,持续给予他莫昔芬或停药后,子宫组织隔室效应均可发生。在同一时间段内,他莫昔芬对小鼠子宫不同组织隔室的雌激素活性可产生类似激动剂和拮抗剂的作用。文中讨论了在他莫昔芬啮齿动物研究中发现的子宫增生和萎缩与服用该药物的女性的具体相关性。