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As the crystalline form of estrone, estropipate is used to accent or substitute for natural estrogen in women. Prior to menopause, women's ovaries produce roughly 70 to 500 micrograms each day of estradiol, a type of estrogen. After the onset of menopause, the primary form of estrogen is estrone and estriol produced by the adrenal glands rather than ovaries. Estropipate acts as a supplement to treat menopausal symptoms, most notably hot flashes and vaginal dryness. It can also be used to reduce the "bad" LDL cholesterol and increase "good" HDL cholesterol within the blood. When combined with progestin, it is also highly beneficial in reducing risks of osteoporosis and bone fractures.
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Estropipate tablets must be stored below 77-degrees Fahrenheit (25-degrees Celsius). Doses are recommended by the FDA between 0.75 and 0.9 mg taken orally on a daily basis. However, this is best when cycled like a natural menstrual cycle, with 21 days on and 7 to 10 days off. During pregnancy, estropipate usage should be halted due to an increased risk of abnormal development of the fetus. In addition, nursing mothers should use estropipate with caution. Breast milk with excess estrogen can affect infants in an unpredictable manner.
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Side effects of estropipate include vaginal bleeding, lack of periods, prolonged periods, breast pain, or changes in libido. The medication can also produce gallstones, which may result in blockage of the gallbladder resulting in abdominal pain. Estrogen therapy in general can lead to increased migraines, excessive sodium levels, and general fluid retention resulting in leg swelling. Other side effects include tan patches on the face and increased curvature of the cornea.
More serious side effects include the development of blood clots, especially in smokers, and an increased risk of uterine cancer. According to the FDA, estropipate may have a small increase in the risk of breast cancer.
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Estropipate can increase the levels of cyclosporine in the blood, resulting in the need for caution in individuals using cyclosporine treatment. This increase can cause kidney and liver damage. Combination with dantrolene can increase the risk of liver disease. Users of warfarin and estropipate also suffer from blood thinning. Other drugs result in the increased metabolism of estrogen and can offset the benefits of estropipate, notably barbiturates, carbamazepine, griseofulvin, phenytoin, primidone and rifampin.