Estradiol acetate ( EA), sold under the brand names Femtrace, Femring, and Menoring, is an estrogen medication which is used in hormone therapy for the treatment of menopause in women.
of estradiol acetate include breast tenderness, breast enlargement, nausea, headache, and fluid retention.
Estradiol acetate was introduced for medical use in 2001.
Medical uses
Estradiol acetate is used as a component of menopausal hormone therapy to treat and prevent
menopause such as
and
osteoporosis in women.
The Women's Health Initiative studies report increased health risks for menopausal women when using unopposed estrogens.
Available forms
Estradiol acetate comes in the form of 0.45, 0.9, and 1.8 mg oral tablets (Femtrace) and in the form of 12.4 or 24.8 mg
that release 50 or 100 μg/day estradiol for 3 months (Femring, Menoring).
However, the Femtrace product was discontinued in the
United States.
Contraindications
of estrogens include
coagulation problems, cardiovascular diseases,
liver disease, and certain hormone-sensitive cancers such as
breast cancer and endometrial cancer, among others.
Side effects
The
of estradiol acetate are the same as those of estradiol. Examples of such side effects include breast tenderness and enlargement,
nausea,
bloating,
edema,
headache, and
melasma.
Overdose
of estrogen
overdose may include
nausea,
vomiting,
bloating,
weight gain, water retention, breast tenderness, vaginal discharge,
heavy legs, and
leg cramps.
These side effects can be diminished by reducing the estrogen dosage.
Interactions
Enzyme inhibitor and
enzyme inducer of cytochrome P450 may influence the
metabolism of estradiol and by extension circulating estradiol levels.
Pharmacology
Pharmacodynamics
Estradiol acetate is an
estradiol ester, or a
prodrug of estradiol.
As such, it is an estrogen, or an
agonist of the estrogen receptors.
Estradiol acetate is of about 15% higher
molecular weight than estradiol due to the presence of its C3
acetic acid ester.
Because estradiol acetate is a prodrug of estradiol, it is considered to be a
natural product and bioidentical form of estrogen.
Pharmacokinetics
Estradiol acetate is converted into estradiol in the body.
Chemistry
Estradiol acetate is a synthetic
estrane steroid and the C3
acetic acid ester of estradiol.
It is also known as estradiol 3-acetate or as estra-1,3,5(10)-triene-3,17β-diol 3-acetate.
Another common ester of estradiol in use for oral administration is estradiol valerate, which is a C17β ester of estradiol.
The experimental octanol/water partition coefficient (logP) of estradiol acetate is 4.2.
History
Estradiol acetate is relatively recent to the market, having been first approved in a
vaginal ring drug formulation as Menoring in the
United Kingdom in 2001,
followed by a vaginal ring formulation as Femring in the
United States in 2002,
and finally as an oral preparation as Femtrace in the United States in 2004.
Society and culture
Generic names
Estradiol acetate is the
generic term of the drug and its .
Brand names
Estradiol acetate is marketed under the brand names Femtrace, Femring, and Menoring.
Availability
Estradiol acetate is available in the
United States and the
United Kingdom.
