General
Description & Use
A powerful and effective female hormone used as Hormone replacement
Therapy (HRT) for symptoms associated with menopause: hot flashes,
sweating, sleep disturbance, vaginal discomfort (dryness and itchiness),
poor concentration, and irritability. Used in the treatment of
breast cancer in post menopausal women and breast and prostate
cancer.
Note:
Premarin 1.25mg tablets have now been discontinued. We are advising
customers who were taking the 1.25mg dosage to now order the 0.625mg
Tablets and take two tablets at your scheduled dosage time.
PREMARIN®
is also a popular female hormone for M2F transsexuals in gender
reassignment
PREMARIN®
is the commercial name for compound drug consisting primarily
of conjugated estrogens. Isolated from mare's urine (PREgnant
MARes' urINe), it is manufactured by Wyeth Pharmaceuticals and
has been marketed since 1942. It is available in oral (0.3/ 0.45/
0.625/ 1.25mg), IV, and topical form.
The
major forms of estrogen in PREMARIN® are estrone (>50%),
equilin (15-25%) and equilenin. The estrogens in Premarin are
often called "conjugated equine estrogens" (CEE) because
the estrogen molecules are generally present with hydrophilic
side-groups attached such as sulfate. Thus, estrone sulfate is
actually the major molecule in PREMARIN®. Estrone sulfate
is easily absorbed into the blood after PREMARIN® tablets
are taken by women. Estrone sulfate is converted to estradiol,
an active estrogen normally found in women. It is not clear if
estrogens such as equilin that are foreign to the human body have
effects in women that are significantly different from the estrogens
like estradiol that are normally made in the human body.
As PREMARIN® is not a single compound, but
a mixture of many naturally derived compounds, the structural
diagram above does not show PREMARIN® but its primary ingredient,
Estrone in its sulfated form. Thus, PREMARIN® cannot be characterized
by the structure of just one of its many compounds.
PREMARIN® (conjugated estrogens tablets,
USP) is used after menopause to reduce moderate to severe hot
flashes; to treat moderate to severe dryness, itching, and burning,
in and around the vagina; and to help reduce your chances of getting
osteoporosis (thin weak bones).
PREMPRO®
(conjugated estrogens/ medroxyprogesterone acetate tablets) is
used after menopause in women with a uterus to reduce moderate
to severe hot flashes; to treat moderate to severe dryness, itching,
and burning, in and around the vagina; and to help reduce your
chances of getting osteoporosis (thin weak bones).
PREMARIN®
(conjugated estrogens) Vaginal Cream is used after menopause to
treat dryness, itching, and burning, in and around the vagina.
PREMARIN® and PREMPRO should be used at the lowest effective
dose and for the shortest duration consistent with your treatment
goals and risks. If using PREMARIN® or PREMPRO only to treat
your symptoms of vaginal dryness, consider topical therapies first.
If you do not have symptoms, non-estrogen treatments should be
carefully considered before taking PREMARIN® and PREMPRO solely
for the prevention of postmenopausal osteoporosis.
In
a clinical trial, the most commonly reported (=5%) side effects
that occurred more frequently with PREMARIN than with placebo
were vaginitis due to yeast or other causes, vaginal bleeding,
painful menstruation, and leg cramps.
In a clinical trial, the most commonly reported
(=5%) side effects that occurred more frequently with PREMPRO
0.45 mg/1.5 mg and PREMPRO 0.625 mg/2.5 mg than with placebo were
breast pain/enlargement, vaginitis due to yeast or other causes,
leg cramps, vaginal spotting/bleeding, and painful menstruation.
In a clinical trial, there was no difference in the commonly reported
(=5%) side effects for women taking PREMPRO 0.3 mg/1.5 mg compared
to those taking placebo.
The
most commonly reported side effects of PREMARIN® Vaginal Cream
include vaginal discomfort or pain, breast pain, vaginitis, and
itching.
PREMARIN®,
PREMPRO, and PREMARIN® Vaginal Cream should not be used if
you have unusual vaginal bleeding, have or had cancer of the breast
or uterus, had a stroke or heart attack in the past year, have
or had blood clots, have liver problems, are allergic to any of
the ingredients in PREMARIN®, PREMPRO, or PREMARIN® Vaginal
Cream, or think you may be pregnant. In general, the addition
of a progestin is recommended for women with a uterus to reduce
the chance of getting cancer of the uterus.
Hormone
replacement therapy (HRT)
If severe side effects of low levels of estradiol in a woman's
blood are experienced (commonly at the beginning of menopause
or after oophorectomy), hormone replacement therapy may be prescribed.
Often such therapy is combined with a progestin.
Estrogen
therapy may be used in treatment of infertility in women when
there is a need to develop sperm-friendly cervical mucus or an
appropriate uterine lining. Estrogen therapy is also used to maintain
female hormone levels in male-to-female
transsexuals.
Some
further suggested female hormone medications supplied by NPD
The following are marketed versions of estradiol:
Oral
versions: Estrace, Activella (also contains a progestin), estradiol
acetate, Progynova,
Estrofem®,
Zumenon,
Ethinylestradiol,
Lynoral,
Estinyl
Transdermal preparation: Alora, Climara,
Vivelle, Vivelle-Dot, Menostar, Estraderm
TTS
Ointments: Estrasorb Topical, Estrogel, Elestrin
Injection: Estradiol cyprionate: Lunelle monthly injection, Estradiol
valerate
Also
see a list of all hormones
available from NPD here.
