GENERIC NAME: estradiol
BRAND NAME: Estrace; Climara; Estraderm; Menostar
DRUG CLASS AND MECHANISM: Estrogens occur in nature in
several
forms. In women with active menstrual cycles, the ovaries
produce between
70 and 500 micrograms of estradiol daily. This is converted to
estrone and
to a lesser extent estriol. After menopause, estrone is the
most active
circulating estrogen. (After menopause estrone is made in the
adrenal
glands.) Estrogens cause growth and development of female sex
organs and
maintain sex characteristics, including underarm and pubic hair
and the
shape 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)
concentrations in the blood. Estrogens, when taken alone or in
combination
with a progestin, have been shown to reduce the risk for hip
fracture due
to osteoporosis by 25%.
PRESCRIPTION: yes
GENERIC AVAILABLE: no
PREPARATIONS: Tablets,
micronized: 0.5mg, 1mg, 2mg; Vaginal cream:
0.01%;
Continuous release skin patch: 14 mcg/day, 0.05 mg/day, 0.1
mg/day.
STORAGE: All forms should be stored between 15°
(59°F)
and 30°C (86°F).
PRESCRIBED FOR: Estradiol is prescribed for symptomatic
treatment of the usual symptoms associated with menopause (hot
flashes,
vaginal dryness, etc.), prevention of bone fractures associated
with
osteoporosis, reduction of the risk of heart attacks and
strokes, and
dysfunctional (excessive and painful) uterine bleeding. The
vaginal cream
is prescribed for vaginal or vulvar atrophy associated with
menopause.
DOSING: Estradiol tablets are generally prescribed once
daily.
In some patients, a so-called cyclic regimen is used, wherein
estradiol is
given daily for 23 consecutive days, followed by 5 days of no
medication,
after which the cycle resumes.
The adhesive part of the patch should be applied to a dry,
hairless,
clean part of the trunk, but not on the breasts. It should not
be placed
onto irritated or damaged skin. Sites of application should be
rotated,
with at least one week between repeated applications to any one
site. The
patch should be applied immediately after removing the
protective layer,
and pressure should be applied to the patch when it is attached
for about
10 seconds.
DRUG INTERACTIONS: Estrogens can inhibit the metabolism
of
cyclosporine, resulting in increased cyclosporine blood levels.
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 anticoagulant (blood thinning) effect if
an estrogen
is added when warfarin is already being taken.
Rifampin, barbiturates, carbamazepine (Tegretol), griseofulvin,
phenytoin (Dilantin) and primidone, can all increase the
elimination of
estrogen by enhancing the liver's ability to metabolize it.
Concurrent use
may result in reduction of the beneficial effects of
estrogens.
PREGNANCY: Estrogens are contraindicated during
pregnancy due to
an increased risk of fetal abnormalities.
NURSING MOTHERS: Estrogens are secreted in milk and
cause
unpredictable effects in the infant. Estrogens generally should
not be
used by women if they are breast-feeding.
SIDE EFFECTS: Among the most
common endocrine side effects are break-through bleeding or spotting, loss of
periods or excessively prolonged periods, breast pain, breast enlargement, and changes
in
sexuality (increase or decrease in libido). Abdominal pain may
indicate
the development of gallstones or occasionally hepatitis.
Migraine
headaches have been associated with estrogen therapy. Estrogens
can cause
sodium and fluid retention. Melasma, tan or brown patches, may
develop on
the forehead, cheeks, or temples. These may persist even after
the
estrogen is stopped. Conjugated estrogens may cause an increase
in the
curvature of the cornea. Patients with contact lenses may
develop
intolerance to their lenses.
Blood clots are an occasional but serious adverse effect and
are
dose-related. (The higher the dose, the more likely the clots.)
Cigarette
smokers are at a higher risk for clots, and, therefore,
patients requiring
estrogen therapy are strongly encouraged to quit smoking.
Estrogens can promote a buildup of the uterine lining
(endometrial
hyperplasia) and increase the risk of endometrial carcinoma. At
diagnosis,
endometrial cancers in estrogen recipients are generally of an
earlier
stage and a lower grade. Survival is also is better in women
exposed to
estrogens than in those not exposed to estrogens. The addition
of a
progestin to estrogen therapy prevents endometrial
carcinoma.
Conflicting data exists on the association between
estrogens and breast cancer. There may be a small increase in risk. The effect of
concomitant
progestin therapy on the risk of estrogen-induced breast
carcinoma is
unclear.
Last Editorial Review: 12/31/1997
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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From the Doctors at MedicineNet.com  |
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- 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. Source:MedicineNet
- Cholesterol - Learn about cholesterol and how to lower LDL cholesterol. Read in-depth cholesterol information on a low cholesterol diet, normal ratio (levels), treatment for high cholesterol and more. Source:MedicineNet
- Osteoporosis - Get information on osteoporosis causes, symptoms, diagnosis, treatment (drugs), prevention (diet, weight-bearing exercise), statistics, risk factors (hereditary) and research. Source:MedicineNet
- Read 57 more estradiol related articles ...
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