Meet the author: Steven R. Goldstein, MD What are SERM's (selective estrogen receptor modulators) |
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Sue:One of the first SERM's to be approved by the FDA is Raloxifene. How does a SERM work and what benefits does it have over the more traditional forms of HRT? What woman would be a candidate for SERMs? Dr. GoldsteinActually the first SERM was clomiphene citrate although this has no use in postmenopausal patients. The second SERM was tamoxifen. It's use with patients with breast cancer and now as a preventative for patients at high risk for cancer are relatively well known. SERMS (selective estrogen receptor modulators) are compounds that because of their structural conformational shape can bind to estrogen receptors in some tissues and activate estrogen metabolic pathways (thus act like an estrogen) and in other tissues by binding to the estrogen receptor will effectively block the ability of estrogen (thus acting as estrogen blockers). It is essential that one understand the difference between women who take HRT for relief of symptoms (hot flashes, sleep disturbances, vaginal dryness) and those women increasingly who will take HRT for long term health maintenance benefits. Relief of symptoms requires estrogen whether it comes from a pill, a patch, or the health food store. If it relieves hot flashes you can guarantee that it is being metabolized through the first pass of the liver as an estrogen. There are no other substitutes for estrogen for treatment of symptoms. However, once treatment of symptoms is no longer an issue, health maintenance benefits for a long period of time make women excellent candidates for SERMs. Raloxifene will have a beneficial effect on bone metabolism and lipid metabolism (just like estrogen). We hope that future studies will confirm that this lipid improvement translates into protection of the heart. SERMs like Raloxifene however will actually reduce the incidence of new onset breast cancer and probably when new numbers are available endometrial cancer. It's only down side is 1.) a slight incidence of mild hot flashes which usually go away and are not overly bothersome (only 1.9% of women in trials discontinued because of hot flashes) and 2.) Raloxifene, Tamoxifen, and estrogen are all estrogens in the venous systems so there is a slight increased risk of deep vein thrombosis and pulmonary embolism that is similar for all these compounds for women who are at risk. Sue:Where do you see the future of SERMS in terms of perimenopause andmenopause? Dr. GoldsteinCurrently SERMs have no use in the perimenopause. These drugs act differently in premenopausal patients than they do in postmenopausal patients. I have seen Tamoxifen cause fibroids to grow, endometriosis to surge. Raloxifene has no use in premenopausal patients. Perhaps the future third generation SERMs may have use in premenopausal patients if through structural changes they actually cause fibroids to shrink and endometriosis to shrivel. This remains to be seen. |
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