Medications and Drugs
Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD
GENERIC NAME: estropipate
BRAND NAME: Ogen, ORTHO-EST
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.
PRESCRIPTION: Yes
GENERIC AVAILABLE: Yes
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.
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
- Drug Interactions - Learn about potential drug interactions you may be exposed to. Drug interactions can occur with prescription drugs, OTC medication, vitamins, herbs, and supplements.
- Menopause - Menopause symptoms include hot flashes, night sweats, abnormal vaginal bleeding, vaginal itching, dryness, and pain, urinary symptoms, weight gain, acne, skin texture changes, and mood changes.
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