estropipate, Ogen

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GENERIC NAME: estropipate


DRUG CLASS AND MECHANISM: Estropipate is a crystalline form of estrone, a form of estrogen. Estrogens occur in nature in several forms. In women with active menstrual cycles, the ovaries produce between 70 and 500 micrograms of one estrogen, estradiol, daily. The estradiol is converted to estrone and to a lesser extent estriol. After menopause, estrone is the most active circulating estrogen but is then produced by the adrenal glands. Estrogens cause growth and development of female sex organs and maintain sexual characteristics, including underarm and pubic hair and the shape of body contours and the strength of bones. They increase secretions from the cervix and growth of the inner lining of the uterus (endometrium). They also reduce LDL-cholesterol ("bad" cholesterol) and increase HDL-cholesterol ("good" cholesterol) concentrations in the blood. Estrogens, when taken alone or in combination with a progestin, have been shown to reduce the risk for hip fractures due to osteoporosis by 25%. The FDA approved estropipate in June 1977.



PREPARATIONS: Tablets: 0.625, 0.75, 1.25, 1.5, 2.5, 5, and 6 mg.

STORAGE: Tablets should be stored below 25 C (77 F).

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

DOSING: The recommended dose is 0.75-9 mg orally daily. Administration usually is cycled; 21 days on and 7-10 days off.

DRUG INTERACTIONS: Estrogens can inhibit the metabolism of cyclosporine, resulting in increased cyclosporine levels in blood. Such increased blood levels can result in kidney and/or liver damage. If this combination cannot be avoided, cyclosporine concentrations can be monitored, and the dose of cyclosporine can be adjusted to assure that its blood levels are not elevated.

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

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

PREGNANCY: Estrogens should be avoided during pregnancy due to an increased risk of fetal abnormalities.

NURSING MOTHERS: Estrogens are secreted in breast milk and cause unpredictable effects in the infant. They generally are not recommended for nursing mothers.

SIDE EFFECTS: Common side effects include break-through vaginal bleeding or spotting, loss of periods or excessively prolonged periods, breast pain, breast enlargement, and changes in sexuality (increased or decreased libido). Abdominal pain may result from obstruction of the gallbladder due to gallstones caused by the estrogen. Migraine headaches have been associated with estrogen therapy. Estrogens can cause sodium and fluid retention leading to swelling in the legs (edema). Melasma - tan or brown patches - may develop on the forehead, cheeks, or temples. These may persist even after the estrogen is stopped. Estrogens may cause an increase in the curvature of the cornea, and patients with contact lenses may develop intolerance to their lenses.

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