Designer oestrogens -Pt II

 

Designer estrogens or  SERMS, are two terms currently being used to describe the actions of a medication that acts as an estrogen on one tissue and an anti-estrogen on others in a same woman . The ideal estrogen medication would switch of or off the effects of estrogen at different sites in the woman's body.

Designer estrogen is an in fact an engineered drug that possesses some, but not all, of the actions of estrogen. also known as selective estrogen-receptor modulator (SERM). For example, raloxifene (brand name: Sevista) is classified as a designer estrogen because, like estrogen, it A) prevents bone loss and B)  lowers serum cholesterol; however,C)  it does not stimulate the endometrial lining of the uterus.

. Tamoxifen is the first SERM used by mainly breast cancer patients and has been shown to block the recurrence of breast cancer in the other breast by 40 percent.

But risks of Tamoxifene ??  The risk associated with Tamoxifen is that it may increase risk of developing blood clots and uterine cancer. Hormone-replacement therapy (HRT) is effective in relieving menopausal symptoms and reduces the risk of osteoporotic fracture, coronary heart disease  

and probably also Alzheimer's disease.But  

^., Long-term use of HRT(Combined HRT)  is associated with adverse effects, of which the most serious is an increased risk of breast cancer. 

Other unwanted effects of long-term HRT include venous thromboembolism 

and endometrial cancer. 

·        For many women, monthly vaginal bleeds are a considerable inconvenience and an important cause of non-compliance, although this problem may be obviated by the use of continuous combined preparations.

 

 

Adv of TMX? Ans: Tamoxifen in postmenopausal womenmay be better Than combined HRT

Osteoporosis Drug Might Replace HRT for Disease Prevention-- Evidence is mounting that a class of drugs known as "designer estrogens" may fulfill the broken promises of hormone replacement therapy, but experts warn that it is too soon to know for sure.

Selective estrogen receptor modulators (SERMs) have been proved to be effective in preventing bone loss in older women, and early studies suggest they may also protect against stroke, heart disease, breast cancer, and even Alzheimer's.

The downside? SERMs like the drug Evista (raloxifene), which is widely prescribed for the prevention and treatment of osteoporosis, do nothing to lessen the symptoms associated with menopause, and may even bring on hot flashes and mood swings, especially when given close to the menopausal transition period. But Evista appears to be an increasingly popular choice for women who once took hormones to prevent the diseases of aging.

"Although SERMs already are in clinical use, the preventive and therapeutic potential of this class of drugs has only begun to be unraveled," researcher Evanthia Diamanti-Kandarakis, MD, and colleagues wrote in the Jan. 1 issue of the American Cancer Society publication Cancer.

SERM researcher Elizabeth Barrett-Connor, MD, agrees, but says the definitive study assessing the benefits of Evista(RLX)  is ongoing. The trial involves just over 10,000 women who are at increased risk for heart disease, and findings are expected in 2006.

"Women and their doctors got a big surprise a few months ago with regard to hormone replacement therapy (HRT)," Barrett-Connor tells WebMD. "We have to be very careful at this point not to recommend [SERMs] for unproven indications so they don't get another one."

Barrett-Connor is referring to the large government study, halted early last July, which showed HRT to be associated with an increased risk for breast cancer, heart attack, stroke, and blood clots.

Raloxifen ( Sevista)  has been approved for the prevention and treatment of osteoporosis, but not for other diseases. In a trial involving 7,000 women, Barrett-Connor and colleagues found that the drug is not associated with an increased risk of cardiovascular disease. Although the results suggest the drug can lower "bad" LDL cholesterol, it had no effect on "good" HDL cholesterol. RLX   significantly reduced the risk of stroke in the same study population, and earlier findings showed a dramatic reduction in breast cancer risk.