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Esclim™
estradiol transdermal system
Continuous delivery for twice-weekly application
See:
Estradiol Evista
Mircette
Activella Alora
Climara Pro
CombiPatch Delestrogen
Estraderm
Estring Estrace Tablets
Evamist Vagifem Vivelle-Dot
All of these products are used to reduce symptoms
of menopause, including feelings of warmth in the face, neck, and chest; the
sudden intense episodes of heat and sweating known as "hot flashes"; dry, itchy
external genitals; and vaginal irritation. They are also prescribed for other
conditions that cause low levels of estrogen, and some doctors prescribe them
for teenagers who fail to mature at the usual rate.
Along with diet, calcium supplements, and exercise, Alora, Estraderm, Climara,
Vivelle, and Vivelle-Dot are prescribed to prevent osteoporosis, a condition in
which the bones become brittle and easily broken.
The Esclim™ estradiol transdermal system contains estradiol in a polymeric
adhesive. The system is designed to release 17̉²estradiol continuously upon
application to intact skin.
Five systems are available to provide nominal in vivo delivery of 0.025, 0.0375,
0.05, 0.075, or 0.1 mg of estradiol per day via skin of average permeability.
Each corresponding system having an active surface area of 11, 16.5, 22, 33, or
44 cm2 contains 5, 7.5, 10, 15, or 20 mg of estradiol USP, respectively.
The composition of the systems per unit area is identical.
Estradiol USP (17̉²estradiol) is a white, crystalline powder, chemically
described as estra-1, 3, 5 (10)triene3, 17̉²diol.
The molecular formula of estradiol is C18 H24 O2. The molecular weight is
272.39.
Esclim transdermal systems are composed of a soft, flexible, rectangular foam
backing material with rounded corners, covered on 1 side with a self-adhesive
polymer matrix which contains estradiol and pharmacologically inactive
components. The adhesive surface is covered by a transparent protective release
liner.
The active component of the system is estradiol. The remaining components of the
system (EVA copolymers, ethylcellulose, octyldodecanol, dipropylene glycol,
polyester protective release liner) are pharmacologically inactive.
WARNING
1. ESTROGENS HAVE BEEN REPORTED TO INCREASE THE
RISK OF ENDOMETRIAL CARCINOMA IN POSTMENOPAUSAL WOMEN.
Close clinical surveillance of all women taking estrogens is important. Adequate
diagnostic measures, including endometrial sampling when indicated, should be
undertaken to rule out malignancy in all cases of undiagnosed persistent or
recurring abnormal vaginal bleeding. There is no evidence that "natural"
estrogens are more or less hazardous than "synthetic" estrogens at
equiestrogenic doses.
2. ESTROGENS SHOULD NOT BE USED DURING
PREGNANCY.
There is no indication for estrogen therapy during pregnancy or during the
immediate postpartum period. Estrogens are ineffective for the prevention or
treatment of threatened or habitual abortion. Estrogens are not indicated for
the prevention of postpartum breast engorgement.
Estrogen therapy during pregnancy is associated with an increased risk of
congenital defects in the reproductive organs of the fetus and possibly other
birth defects. Studies of women who received diethylstilbestrol (DES) during
pregnancy have shown that female offspring have an increased risk of vaginal
adenosis, squamous cell dysplasia of the uterine cervix, and clear cell vaginal
cancer later in life; male offspring have an increased risk of urogenital
abnormalities and possibly testicular cancer later in life. The 1985 DES Task
Force concluded that use of DES during pregnancy is associated with a subsequent
increased risk of breast cancer in the mothers, although a causal relationship
remains unproven, and the observed level of excess risk is similar to that for a
number of other breast cancer risk factors.
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