Detailed Drug Information:

DRUG CLASS AND MECHANISM: Estropipate is a crystalline form ofestrone, a form of estrogen. Estrogens, when taken alone or in combinationwith a progestin, have been shown to reduce the risk for hip fracture dueto osteoporosis by 25%, the risk of heart attack (myocardial infarction)and stroke by 40-50%. Estropipate is used for numerous medical situations.Estrogens cause growth and development of female sex organs and themaintenance of sex characteristics, including growth of underarm and pubichair and shaping of body contours and skeleton. Estrogens also increasesecretions from the cervix and growth of the inner lining of the uterus(endometrium). Estrogens reduce LDL-cholesterol ("bad"cholesterol) and increase HDL-cholesterol ("good" cholesterol)concentrations in the blood.

PREPARATIONS: Tablets: 0.625mg, 1.25mg, 2.5mg.

STORAGE: Tablets should be stored between 2° (36°F) and 30°C(86°F).

PRESCRIBED FOR: Estropipate is prescribed for treatment of theusual symptoms associated with menopause (hot flashes, vaginal dryness),prevention of bone fractures associated with osteoporosis, anddysfunctional (excessive and painful) uterine bleeding.

DOSING: Estropipate is generally prescribed once daily.

DRUG INTERACTIONS: Estrogens can inhibit the metabolism ofcyclosporine, resulting in increased cyclosporine levels in blood. Suchincreased blood levels can result in kidney and/or liver damage. If thiscombination cannot be avoided, cyclosporine concentrations can bemonitored, and the dose of cyclosporine can be adjusted to assure that itsblood levels are not elevated.

Estrogens appear to increase the risk of liver disease in patientsreceiving dantrolene through an unknown mechanism. Women over 35 years ofage and those with a history of liver disease are especially at risk. Estrogensincrease the liver's ability to manufacture clotting factors. Because ofthis, patients receiving warfarin (Coumadin) need to be monitored for lossof the anticoagulant effect (blood thinning) of warfarin if estrogens likeestropipate are added.

Rifampin, barbiturates, carbamazepine (Tegretol), griseofulvin,phenytoin (Dilantin) and primidone, all can increase the elimination ofestrogens by enhancing the liver's ability to metabolize (break down) theestrogens. Thus, concurrent use of these drugs and estrogens may result inreduction of the beneficial effects of estrogens.

PREGNANCY: Estrogens are should be avoided during pregnancy dueto an increased risk of fetal abnormalities.

NURSING MOTHERS: Estrogens are secreted in milk and causeunpredictable effects in the infant. They are generally avoided duringbreast-feeding.

SIDE EFFECTS: Among the most common endocrine side arebreak-through vaginal bleeding or spotting, loss of periods or excessivelyprolonged periods, breast pain, breast enlargement, and changes insexuality (increase or decrease in libido). Abdominal pain may result fromobstruction of the gallbladder due to gallstones or hepatitis caused bythe estrogen. Migraine headaches have been associated with estrogentherapy. Estrogens can cause sodium and fluid retention leading toswelling in the legs. Melasma, tan or brown patches, may develop on theforehead, cheeks, or temples. These may persist even after the estrogen isstopped. Conjugated estrogens (estrogens attached to other chemicals) maycause an increase in the curvature of the cornea, and patients withcontact lenses may develop intolerance to their lenses.

Blood clots are occasional, serious adverse reactions of estrogentherapy and are dose-related. (The higher the dose, the more likely areclots.) Cigarette smokers are at a higher risk for developing clots whiletaking estrogens, and patients requiring estrogen therapy are stronglyencouraged to quit smoking.

Estrogens can promote a buildup of the uterine lining (endometrialhyperplasia) and increase the risk of endometrial carcinoma (cancer). Atdiagnosis, endometrial cancers in estrogen recipients are generally at anearlier stage and a lower grade making cure more likely. Survival isbetter in women exposed to estrogens than in those not exposed toestrogens. The addition of a progestin to estrogen therapy offsets therisk of endometrial carcinoma by counteracting the stimulatory effects ofestrogens on the endometrium.

Conflicting data exists on the association between estrogens and breastcancer, but there may be a small increase in risk. It is unclear ifconcomitant estrogen and progestin therapy, as with endometrial cancer,reduces the risk of estrogen-induced breast cancer.