Advanced Breast Cancer: Learn about treatment options.

estradiol oral

Pronunciation

Generic Name: estradiol oral (ess tra DYE ole)
Brand Name: Estrace, Femtrace, Gynodiol

What is estradiol oral?

Estradiol is a form of estrogen, a female sex hormone produced by the ovaries. Estrogen is necessary for many processes in the body.

Estradiol is used to treat symptoms of menopause such as hot flashes, and vaginal dryness, burning, and irritation. Other uses include prevention of osteoporosis in postmenopausal women, and replacement of estrogen in women with ovarian failure or other conditions that cause a lack of natural estrogen in the body. Estradiol is sometimes used as part of cancer treatment in women and men.

Estradiol may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about estradiol oral?

Estradiol can harm an unborn baby or cause birth defects. Do not use estradiol if you are pregnant.

You should not take estradiol if you have abnormal vaginal bleeding, liver disease, breast or uterine cancer, hormone-dependent cancer, a recent history of heart attack or stroke, if you are pregnant, if you have ever had a blood clot (especially in your lung or your lower body), or if you are allergic to any medicines or food dyes.

Slideshow: View Frightful (But Dead Serious) Drug Side Effects

Taking hormones can increase your risk of blood clots, stroke, or heart attack, especially if you have diabetes, high blood pressure, high cholesterol or triglycerides, if you smoke, or if you are overweight.

Long-term estradiol treatment may increase your risk of breast cancer, ovarian cancer, or uterine cancer. Talk with your doctor about your individual risks before using estradiol long-term. Your doctor should check your progress every 3 to 6 months to determine whether you should continue this treatment.

Taking progestin while using estradiol may lower your risk of uterine cancer. If your uterus has not been removed, your doctor may prescribe a progestin for you to take while you are using estradiol.

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medication may actually increase your risk of developing these conditions.

Have regular physical exams and mammograms, and self-examine your breasts for lumps on a monthly basis while using estradiol.

What should I discuss with my health care provider before using estradiol oral?

You should not take estradiol if you are allergic to it, or if you have:

  • liver disease;

  • abnormal vaginal bleeding that a doctor has not checked;

  • any type of breast, uterine, or hormone-dependent cancer;

  • a recent history of heart attack or stroke;

  • if you are pregnant;

  • if you have ever had a blood clot (especially in your lung or your lower body); or

  • if you are allergic to any medicines or food dyes.

Taking hormones can increase your risk of blood clots, stroke, or heart attack, especially if you have risk factors such as diabetes, high blood pressure, high cholesterol or triglycerides, smoking, or being overweight.

To make sure you can safely take estradiol, tell your doctor if you have any of these other conditions:

  • heart disease;

  • kidney disease;

  • family history of blood clots;

  • a history of jaundice caused by pregnancy or taking hormones;

  • endometriosis;

  • lupus;

  • porphyria;

  • gallbladder disease;

  • underactive thyroid;

  • asthma;

  • epilepsy or other seizure disorder;

  • migraines;

  • low levels of calcium in your blood; or

  • if you have had your uterus removed (hysterectomy).

FDA pregnancy category X. This medication can harm an unborn baby or cause birth defects. Do not use estradiol if you are pregnant. Tell your doctor right away if you become pregnant during treatment.

Estradiol can pass into breast milk and may harm a nursing baby. This medication may also slow breast milk production. You should not breast-feed while you are taking estradiol.

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medication may actually increase your risk of developing these conditions.

How should I use estradiol oral?

Take this medication exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor.

Long-term estradiol treatment may increase your risk of breast cancer, ovarian cancer, or uterine cancer. Talk with your doctor about your individual risks before using estradiol long-term.

Taking progestin while using estradiol may lower your risk of uterine cancer. If your uterus has not been removed, your doctor may prescribe a progestin for you to take while you are using estradiol.

Have regular physical exams and mammograms, and self-examine your breasts for lumps on a monthly basis while using estradiol. Your doctor should check your progress every 3 to 6 months to determine whether you should continue this treatment.

If you need medical tests or surgery, or if you will be on bed rest, you may need to stop using this medication for a short time. Any doctor or surgeon who treats you should know that you are taking estradiol.

Store at room temperature away from moisture, heat, and light.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose can cause nausea, vomiting, or vaginal bleeding.

What should I avoid while using estradiol oral?

Do not smoke while using this medication. Smoking can increase your risk of blood clots, stroke, or heart attack caused by estradiol.

Estradiol oral side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using estradiol and call your doctor at once if you have a serious side effect such as:

  • unusual vaginal bleeding (especially if you are past menopause);

  • chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;

  • sudden numbness or weakness, especially on one side of the body;

  • sudden severe headache, confusion, problems with vision, speech, or balance;

  • stabbing chest pain, sudden cough, wheezing, rapid breathing, fast heart rate;

  • pain, swelling, warmth, or redness in one or both legs;

  • nausea, vomiting, loss of appetite, increased thirst, muscle weakness, confusion, and feeling tired or restless;

  • a lump in your breast;

  • feeling like you might pass out;

  • pain, swelling, or tenderness in your stomach; or

  • jaundice (yellowing of the skin or eyes).

Less serious side effects may include:

  • mild nausea, vomiting, bloating, stomach cramps;

  • breast pain, tenderness, or swelling;

  • freckles or darkening of facial skin;

  • loss of scalp hair;

  • vaginal itching or discharge; or

  • changes in your menstrual periods, break-through bleeding.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Estradiol oral Dosing Information

Usual Adult Dose for Postmenopausal Symptoms:

Oral:
0.45 mg to 2 mg orally once a day.

Parenteral:
1 to 5 mg of estradiol cypionate IM every 3 to 4 weeks or 10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
0.05 mg/day (2 foil pouches of transdermal emulsion) applied topically to both legs each morning.
0.25 mg unit dose packet (0.1% transdermal gel) applied topically once daily to the upper right or left thigh at the same time daily.
1.25 g (one spray) EstroGel (0.75 mg/1.25 gm - 0.06% transdermal gel) applied topically to the arms at the same time daily.
1.53 mg (one spray) Evamist (1.53 mg/spray transdermal spray) applied topically to the forearm at the same time daily.
0.87 g (one spray) Elestrin (0.52 mg/1.087 g - 0.06% transdermal gel) applied topically to the upper arm at the same time daily.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

In general, the duration of hormone therapy for the treatment of postmenopausal symptoms should be limited. Treatment for one to five years is generally sufficient. However, long-term therapy (for the treatment/prophylaxis of osteoporosis and for risk reduction of cardiovascular disease) may be considered during the time in which the patient is being treated for postmenopausal symptoms.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.

Usual Adult Dose for Atrophic Urethritis:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
1.25 g/day (estradiol gel) applied topically at the same time daily. If used solely for the treatment of vulvar and vaginal atrophy, topical vaginal products should be considered.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
In general, the duration of hormone therapy for the treatment of postmenopausal symptoms like atrophic vaginitis, kraurosis vulvae, or atrophic urethritis should be limited. Treatment for one to five years is generally sufficient.

Usual Adult Dose for Atrophic Vaginitis:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
1.25 g/day (estradiol gel) applied topically at the same time daily. If used solely for the treatment of vulvar and vaginal atrophy, topical vaginal products should be considered.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
In general, the duration of hormone therapy for the treatment of postmenopausal symptoms like atrophic vaginitis, kraurosis vulvae, or atrophic urethritis should be limited. Treatment for one to five years is generally sufficient.

Usual Adult Dose for Hypoestrogenism:

Oral:
1 to 2 mg orally once a day.

Parenteral:
1.5 to 2 mg of estradiol cypionate IM once a month or 10 to 20 mg estradiol valerate IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Dosages should be titrated according to patient response. Therapy should be maintained with the minimum dosage that will achieve the desired clinical effect.

Usual Adult Dose for Oophorectomy:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate by IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Usual Adult Dose for Primary Ovarian Failure:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate by IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Usual Adult Dose for Breast Cancer--Palliative:

10 mg orally 3 times a day for at least 3 months. Estrogen therapy for breast cancer should be considered only for palliation in the treatment of metastatic disease in select patients

Usual Adult Dose for Osteoporosis:

Oral:
0.5 mg orally once a day.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Systems should not be applied to the breasts.
14 mcg/day weekly (transdermal film) applied topically once a week.

Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm.

In addition to hormonal therapy, adequate calcium intake is important for postmenopausal women who require treatment or prevention of osteoporosis. The average diet of older American women contains 400 to 600 mg of calcium per day. A suggested optimal intake is 1500 mg per day. If dietary intake is insufficient to achieve 1500 mg per day, supplementation may be useful in women who have no contraindication to calcium supplementation.

Long-term therapy (for more than 5 years) is generally necessary in order to obtain substantive benefits in reducing the risk of bone fracture. Maximal benefits are obtained if estrogen therapy is initiated as soon after menopause as possible. The optimal duration of therapy has not been definitively determined.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

When used solely for the prevention of postmenopausal osteoporosis, approved non-estrogen treatments should carefully be considered, and estrogen and combined estrogen-progestin products should only be considered for women with significant risk of osteoporosis that outweighs the risks of the drug.

Usual Adult Dose for Prostate Cancer:

Oral:
1 to 2 mg orally 3 times a day.

Parenteral:
Estradiol valerate 30 mg IM every 1 to 2 weeks.

An apparent response should be noted within 3 months of initiation of therapy. Estrogen therapy for prostate cancer should be considered only for palliation in the treatment of metastatic disease in select patients.

What other drugs will affect estradiol oral?

Tell your doctor about all other medicines you use, especially:

  • a blood thinner such as warfarin (Coumadin);

  • cimetidine (Tagamet);

  • carbamazepine (Carbatrol, Tegretol);

  • phenobarbital (Luminal, Solfoton);

  • phenytoin (Dilantin);

  • rifampin (Rifadin, Rifater, Rifamate, Rimactane); or

  • ritonavir (Norvir);

  • St. John's wort;

  • an antibiotic such as clarithromycin (Biaxin) or erythromycin (E-Mycin, E.E.S., Erythrocin, Ery-Tab); or

  • antifungal medication such as ketoconazole (Extina, Ketozole, Nizoral, Xolegal).

This list is not complete and other drugs may interact with estradiol. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

  • Your pharmacist can provide more information about estradiol.
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 10.02. Revision Date: 2010-12-15, 5:01:39 PM.

Suffering from sore knees? Assess your knee pain with our interactive tool. Click Here

Close
Hide
(web2)