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Climara ProŽ
(Estradiol/Levonorgestrel Transdermal
System)
See:
Estradiol Evista
Mircette
Activella Alora
CombiPatch Delestrogen
Esclim 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.
Climara ProŽ (Estradiol/Levonorgestrel Transdermal System) is an adhesive-based
matrix transdermal patch designed to release both estradiol and levonorgestrel,
a progestational agent, continuously upon application to intact skin.
The 22 cm2 Climara Pro system contains 4.4 mg estradiol and 1.39 mg
levo-norgestrel and provides a nominal delivery rate (mg per day) of 0.045
estradiol and 0.015 levonorgestrel.
Estradiol USP has a molecular weight of 272.39 and the molecular formula is
C18H24O2. Levonorgestrel USP has a molecular weight of 312.4 and a molecular
formula of C21H28O2.
The Climara ProŽ system comprises 3 layers. Proceeding from the visible surface
towards the surface attached to the skin, these layers are (1) a translucent
polyethylene backing film, (2) an acrylate adhesive matrix containing estradiol
and levo-norgestrel, and (3) a protective liner of either siliconized or
fluoropolymer coated polyester film. The protective liner is attached to the
adhesive surface and must be removed before the system can be used.
The active components of the system are estradiol and levonorgestrel. The
remaining components of the system (acrylate copolymer adhesive and
polyvinylpyrrolidone/vinyl acetate copolymer) are pharmacologically inactive.
WARNINGS
Estrogens and progestins should not be
used for the prevention of cardiovascular disease or dementia. (See WARNINGS,
Cardiovascular disorders and Dementia.)
The Womens Health Initiative (WHI) study reported increased risks of myocardial
infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein
thrombosis in postmenopausal women (50 to 79 years of age) during 5 years of
treatment with oral conjugated estrogens (CE 0.625 mg) combined with
medroxyproges-terone acetate (MPA 2.5 mg) relative to placebo. (See CLINICAL
STUDIES and WARNINGS, Cardiovascular disorders and Malignant neoplasms, Breast
cancer.)
The WHI study reported increased risks of stroke and deep vein thrombosis in
postmenopausal women (50 to 79 years of age) during 6.8 years of treatment with
oral conjugated estrogens (CE 0.625 mg) relative to placebo. (See CLINICAL
STUDIES and WARNINGS, Cardiovascular disorders.)
The Womens Health Initiative Memory Study (WHIMS), a substudy of WHI, reported
increased risk of developing probable dementia in postmenopausal women 65 years
of age or older during 4 years of treatment with CE 0.625 mg combined with MPA
2.5 mg and during 5.2 years of treatment with CE 0.625 mg alone, relative to
placebo. It is unknown whether this finding applies to younger postmenopausal
women. (See CLINICAL STUDIES, WARNINGS, Dementia and PRECAUTIONS, Geriatric
Use.)
Other doses of oral conjugated estrogens with medroxyprogesterone acetate, and
other combinations and dosage forms of estrogens and progestins were not studied
in the WHI clinical trials and, in the absence of comparable data, these risks
should be assumed to be similar. Because of these risks, estrogens with or
without progestins should be prescribed at the lowest effective doses and for
the shortest duration consistent with treatment goals and risks for the
individual woman.
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