What is estrogens conjugated, and how does it work (mechanism of action)?
Estrogens are one of the two major classes
of female hormones. (Progestins comprise the second major class). Estrogens are
used primarily to treat the symptoms of menopause and states in which there is a
deficiency of estrogen, for example, in women who have had their ovaries
removed. Conjugated estrogens are a mixture of several different estrogens
(estrogen salts) that are derived from natural sources and blended to
approximate the composition of estrogens in the urine of pregnant horses. The
main components are sodium estrone sulphate and sodium equilin sulfate.
Estrogens have widespread effects on many tissues in the body. Estrogens cause
growth and development of the female sexual organs and maintain female sexual
characteristics such as the growth of underarm and pubic hair, body contours, and
skeleton. Estrogens also increase secretions from the cervix and growth of the
inner lining of the uterus (endometrium).
What brand names are available for estrogens conjugated?
Premarin
Is estrogens conjugated available as a generic drug?
GENERIC AVAILABLE: No.
Do I need a prescription for estrogens conjugated?
Yes.
What are the side effects of estrogens conjugated?
Common side effects of conjugated estrogens are:
- headache,
- abdominal pain,
- nervousness,
- nausea,
- back pain,
- joint pain and
- vaginal bleeding.
Other side important effects include:
- vaginal spotting,
- loss of periods or
- excessively prolonged periods,
- breast pain,
- breast enlargement and
- an increase or decrease in sexual drive.
Effects of estrogen on the skin include rash, and
melasma (tan or brown patches) that may develop on the forehead, cheeks, or
temples and may persist even after estrogens are stopped.
In the eyes,
conjugated estrogens may cause an increase in the curvature of the cornea, and,
as a result, patients with contact lenses may develop intolerance to their
lenses.
Estrogens may increase calcium levels in the blood (hypercalcemia) in
patients with breast and bone cancer.
Some patients may experience increased
blood pressure and triglyceride levels.
There is an increased risk of cholesterol gallstones among men and women taking estrogens.
Estrogens also may
inhibit the flow of bile from the liver (cholestasis) and uncommonly cause
jaundice.
Estrogens can cause salt (sodium) and water retention (edema).
Therefore, patients with heart failure or reduced function of their kidneys who
are taking estrogens should be carefully observed for retention of water and its
complications.
Blood clots in the legs or lungs occasionally occur in women
taking conjugated estrogens. This potentially serious complication of estrogen
therapy is dose-related, that is, it occurs more commonly with higher doses.
Therefore, the lowest effective doses that relieve symptoms should be used.
Cigarette smokers are at a higher risk for blood clots. Therefore, patients
requiring estrogen therapy should
quit smoking.
Estrogens can promote a build up
of the lining of the uterus (endometrial hyperplasia) and increase the risk of
endometrial cancer. (Women who have undergone surgical removal of the
uterus–hysterectomy–are not susceptible to endometrial hyperplasia.) The
addition of a progestin to estrogen therapy prevents the development of
endometrial cancer.
The Women’s Health Initiative found that postmenopausal
women (50-79 years old) taking conjugated estrogens, 0.625 mg daily, in
combination with medroxyprogesterone, 2.5 mg daily, for five years, had an
increased risk of heart attacks, stroke, breast cancer, and
blood clots, while
postmenopausal women taking conjugated estrogens without progesterone
experienced only increased strokes but not increased blood clots, heart disease,
or breast cancer.
There was an increased risk of impaired cognition and/or
dementia among women over age 65 treated with either estrogens or estrogens and
medroxyprogesterone.
What is the dosage for estrogens conjugated?
To minimize side effects, the lowest effective oral dose of
conjugated estrogens is used. The usual starting dose for treating symptoms
associated with menopause and for preventing postmenopausal osteoporosis is 0.3
mg/day. The dose should be increased based on response.
Conjugated estrogens may
be administered continuously or in a cyclical fashion (i.e., 25 days on
treatment then 5 days off treatment).
Hypogonadism is treated cyclically with
doses of 0.3 mg or 0.625 mg daily for 25 days followed by 5 days off treatment.
The dose for women who have had their ovaries removed or have ovarian failure is 1.25 mg
daily for three weeks followed by one week off treatment. In reality, most women
take estrogens continuously since during the week off treatment, symptoms return
because of the lack of estrogen.
For treatment of
breast cancer, the recommended
dose is 10 mg daily for three months. Abnormal uterine bleeding due to hormonal
imbalance is treated with one 25 mg intravenous or intramuscular injection.
Another injection may be given in 6-12 hours if needed.
The vaginal cream is
used for treating vulvar and vaginal atrophy, and the recommended dose is ½ to 2
g daily.
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Which drugs or supplements interact with estrogens conjugated?
Estrogens increase the liver’s ability to
manufacture factors that promote the clotting of blood. Because of this,
patients receiving warfarin (Coumadin), a drug that thins the blood and prevents
clotting by reducing clotting factors, need to be monitored for loss of the
blood thinning effect if treatment with an estrogen is begun.
Rifampin (Rifadin),
barbiturates, carbamazepine (Tegretol), griseofulvin (Grifulvin), phenytoin (Dilantin),
St. John’s wort, and primidone all increase the elimination of estrogen by
enhancing the liver’s ability to eliminate estrogens. Use of any of these
medications with estrogens may result in a reduction of the beneficial effects
of estrogens.
Conversely, drugs such as erythromycin, ketoconazole (Nizoral),
itraconazole (Sporanox), and ritonavir (Norvir) may reduce the elimination of
estrogens by the liver and lead to increased levels of estrogens in the blood.
Grapefruit juice also may increase levels of estrogen by increasing the
absorption of estrogens from the intestine. Increased levels of estrogens in the
blood may result in more estrogen-related side effects.
QUESTION
If menopause occurs in a woman younger than ___ years, it is considered to be premature.
See Answer
Is estrogens conjugated safe to take if I’m pregnant or breastfeeding?
Estrogens should not be given to
pregnant women due to the
risk of harm to the fetus.
Estrogens are secreted in breast milk and may cause
unpredictable effects in the infant. Estrogens may also reduce the quality of
breast milk. They should not be taken by women who are
breastfeeding.
What else should I know about estrogens conjugated?
What preparations of estrogens conjugated are available?
Tablets: 0.3, 0.45, 0.625, 0.9, and 1.25 mg. Vaginal
cream: 0.625 mg per gm of cream. Injection: 25 mg per vial
How should I keep estrogens conjugated stored?
Conjugated estrogen tablets and cream should be stored at
room temperature, between 15 C -30 C (59 F – 86 F). The injection should be stored
between 2 C – 8 C (36 F – 46 F).