estradiol

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.

Important information

You should not use estradiol if you have: liver disease, a bleeding disorder, unusual vaginal bleeding, history of a hormone-dependent cancer (such as breast, uterine, ovarian, or thyroid cancer), or if you have ever had a heart attack, stroke, or a blood clot.

Do not use if you are pregnant.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Call your doctor at once if you have any unusual vaginal bleeding while using this medicine.

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions. Long-term use may also increase your risk of breast cancer or blood clot.

Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment.

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. 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.

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

Before taking this medicine

You should not use this medicine if you are allergic to estradiol, if you are pregnant, or if you have:

• unusual vaginal bleeding that a doctor has not checked;

• liver disease;

• a bleeding or blood-clotting disorder;

• a recent history of heart attack or stroke;

• a history of hormone-dependent cancer (such as breast, uterine, ovarian, or thyroid cancer);

• 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.

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

To make sure estradiol is safe for you, tell your doctor if you have:

• heart disease;

• risk factors for coronary artery disease (such as diabetes, lupus, smoking, being overweight, having high blood pressure or high cholesterol, having a family history of coronary artery disease, or if you have had a hysterectomy);

• a history of jaundice caused by pregnancy or birth control pills;

• a thyroid disorder;

• kidney disease;

• asthma;

• epilepsy or other seizure disorder;

• migraines;

• porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);

• endometriosis or uterine fibroid tumors;

• gallbladder disease;

• high or low levels of calcium in your blood; or

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

Long-term use of estradiol may increase your risk of breast cancer, heart attack, stroke, or blood clot. Talk with your doctor about your individual risks before using estradiol long term.

FDA pregnancy category X. Do not use estradiol if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use effective birth control while you are using this medicine.

See also: Pregnancy and breastfeeding warnings (in more detail)

Estradiol can pass into breast milk. This medication may slow breast milk production. Tell your doctor if you are breast-feeding a baby.

How should I take estradiol?

Take estradiol exactly as it was prescribed for you. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Your doctor may prescribe a progestin to take while you are using estradiol, to help lower this risk. Report any unusual vaginal bleeding right away.

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

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

Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

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?

Grapefruit and grapefruit juice may interact with estradiol and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.

Estradiol side effects

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

Call your doctor at once if you have:

• heart attack symptoms - chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating;

• signs of a stroke - sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance;

• signs of a blood clot in the lung - chest pain, sudden cough, wheezing, rapid breathing, coughing up blood;

• signs of a blood clot in your leg - pain, swelling, warmth, or redness in one or both legs;

• swelling or tenderness in your stomach;

• jaundice (yellowing of the skin or eyes);

• unusual vaginal bleeding;

• a lump in your breast;

• fluid retention (swelling, rapid weight gain); or

• high levels of calcium in your blood - nausea, vomiting, stomach pain, loss of appetite, constipation, increased thirst or urination, muscle pain or weakness, joint pain, confusion, and feeling tired or restless.

Common estradiol side effects may include:

• breast pain;

• headache;

• vaginal itching or discharge, changes in your menstrual periods, light vaginal bleeding or spotting;

• thinning scalp hair; or

• nausea, vomiting, bloating, stomach cramps.

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 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?

Other drugs may interact with estradiol, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

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.