GENERIC NAME: esterified estrogens
BRAND NAME: Estratab; Menest
DRUG CLASS AND MECHANISM:
Esterified estrogens are a
mixture of
several estrogens, a type of female hormone. Estrogens cause
growth and
development of female sex organs and the maintenance of sex
characteristics, including growth of underarm and pubic hair
and shaping
of body contours and skeleton. Estrogens also increase
secretions 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) in
the blood.
Estrogens, when taken alone or in combination with a progestin
(another
type of female hormone), have been shown to reduce the risk of
heart
attack (myocardial infarction) and stroke by 40-50%. In
addition, their
bone-promoting effects reduce the risk for hip fracture from
osteoporosis
(a bone disease that occurs primarily in women after menopause
when the
body stops producing its own estrogens) by 25%.
PRESCRIPTION: yes
GENERIC AVAILABLE: yes
PREPARATIONS: Tablets: 0.3mg, 0.625mg, 1.25mg, 2.5mg.
STORAGE: Tablets should be stored between 2°
(36°F)
and 30°C (86°F).
PRESCRIBED FOR: Esterified estrogens are prescribed
for the
treatment of the common symptoms associated with menopause
(for, example,
hot flashes and vaginal dryness), dysfunctional (excessive and
painful)
uterine bleeding, and prostate cancer, as well as for the
prevention of
bone fractures associated with osteoporosis, heart attacks, and
strokes.
DOSING: Esterified estrogens are generally prescribed
once
daily.
DRUG INTERACTIONS:
Cyclosporine levels: Estrogens can inhibit the
metabolism
(destruction) of cyclosporine, resulting in increased
cyclosporine blood
levels. Such increased blood levels can result in kidney and/or
liver
damage. If the combination of estrogens and cyclosporine cannot
be
avoided, cyclosporine concentrations in the blood can be
monitored, and
the dose of cyclosporine can be adjusted to assure that its
blood levels
are not elevated.
Liver disease: 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.
Reduced effectiveness of anticoagulants: Estrogens
increase the
liver's ability to manufacture chemicals that are required in
order for
blood to clot. Therefore, patients receiving warfarin (Coumadin), which
anticoagulates ("thins" the blood) by inhibiting the
manufacture
of the chemicals required for clotting, need to have the
ability of their
blood to clot monitored if an estrogen is added. If blood clots
too
easily, the dose of warfarin may need to be increased.
Reduced effectiveness: Rifampin, barbiturates,
carbamazepine (Tegretol), griseofulvin, phenytoin (Dilantin) and primidone,
can increase
the elimination of estrogen by enhancing the liver's ability to
metabolize
(destroy) it. Use of these drugs may result in a reduction of
the
beneficial effects of estrogens.
PREGNANCY: Estrogens should not be used during
pregnancy
because of an increased risk of fetal abnormalities.
NURSING MOTHERS: Estrogens are secreted in milk and
cause
unpredictable effects in the infant. Therefore, they generally
should not
be used during breast-feeding.
SIDE EFFECTS: Among the most
common endocrine side are breakthrough bleeding or spotting, loss of periods, or
excessively prolonged periods, breast pain, breast enlargement, and changes
in
sexuality (increase or decrease in libido). Estrogens also may
cause
gallstones, hepatitis, migraine headaches, and fluid retention
(swelling
of the lower legs). 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, therefore, patients with contact lenses may develop
intolerance to
their lenses.
Blood clots: Blood clots are occasional but serious
side
effects of estrogen therapy and are dose-related, that is,
they occur
more frequently with higher doses. Cigarette smokers are at a
higher risk
than non-smokers. Therefore, patients requiring estrogen
therapy are
strongly encouraged to quit smoking.
Uterine cancer: Estrogens can promote a build-up of
the lining
of the uterus or endometrium (endometrial hyperplasia) and
increase the
risk of endometrial cancer. At diagnosis, endometrial cancers
in estrogen
users are generally of an earlier stage and a lesser degree of
malignancy
than in non-users. Survival, therefore, is better. The addition
of a
progestin to estrogen therapy prevents endometrial cancer from
developing.
Breast cancer: Conflicting data exists on the
association
between estrogen therapy and breast cancer. There may be a
small increase
in risk. It is not clear if the addition of a progestin during
estrogen
therapy reduces the risk of breast cancer (as it does for
uterine cancer).
Last Editorial Review: 7/23/1998
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.
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