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All about: Estradiol

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Generic Name: Estradiol Oral Tablets (ES-tra-DYE-ol)
Brand Name: Examples include Estrace and Gynodiol

Estradiol should not be used to prevent heart disease, heart attacks, strokes, or dementia. Estrogens have been shown to increase the risk of heart disease (including heart attack), stroke, dementia, serious blood clots (eg, in the lungs or legs), cancer of the uterus, and breast cancer in some women. Tell your doctor right away if you have unusual vaginal bleeding while you use Estradiol . Talk with your doctor if you have questions about the benefits and risks of using Estradiol .

Estradiol should be used for the shortest possible time at the lowest effective dose to minimize the risk of these side effects. Talk with your doctor regularly about your need to use Estradiol .


Estradiol is used for:

Treating conditions due to menopause (eg, hot flashes; vaginal itching, burning, or dryness), treating vulval or vaginal atrophy, and preventing osteoporosis (brittle bones). It is also used for estrogen replacement therapy after failure of the ovaries and to relieve the symptoms of breast cancer.

Treating advanced prostate cancer. It is also used to relieve symptoms of breast cancer.

Estradiol is a female estrogen hormone. It works by replacing natural estrogens in a woman who can no longer produce enough estrogen.It works for advanced prostate cancer by antagonizing male hormones.

Do NOT use Estradiol if:

  • you are allergic to any ingredient in Estradiol
  • you are pregnant or suspect you may be pregnant, have recently given birth or are breast-feeding, or have vaginal bleeding of abnormal or unknown cause
  • you have known or suspected breast cancer (unless directed by your doctor) or you have cancers that are estrogen-dependent
  • you have blood clots, vein inflammation, or liver disease
  • you have had a recent stroke or heart attack

Contact your doctor or health care provider right away if any of these apply to you.

Before using Estradiol :

Some medical conditions may interact with Estradiol . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

  • if you are planning to become pregnant
  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
  • if you have allergies to medicines, foods, or other substances
  • if you have a family history of breast cancer, or you have breast lumps or disease, or an abnormal mammogram
  • if you have yellowing of the whites of the eyes or skin during pregnancy or with past estrogen use, or high blood pressure during pregnancy (toxemia)
  • if you have a vaginal infection or womb problems (eg, uterine fibroids/endometriosis, abnormal vaginal bleeding, other uterine problems)
  • if you have abnormal calcium levels in the blood, asthma, cancer, certain blood disorder (porphyria), cholesterol or lipid problems, depression, diabetes, epilepsy, excessive weight gain, gallbladder disease, heart disease or other heart problems, high blood pressure, kidney or liver disease, low thyroid hormone levels, lupus, migraine headaches, pancreas disease, seizures, or yellowing of the skin or eyes
  • if you smoke or will be having surgery

Some MEDICINES MAY INTERACT with Estradiol . Tell your health care provider if you are taking any other medicines, especially any of the following:

  • Blood thinners (eg, warfarin), corticosteroids (eg, prednisone), succinylcholine, or tacrine because their actions and the risk of their side effects may be increased by Estradiol
  • Blood thinners (eg, warfarin) because their effectiveness may be decreased by Estradiol
  • Barbiturates (eg, phenobarbital), hydantoins (eg, phenytoin), or rifampin because they may decrease Estradiol 's effectiveness

This may not be a complete list of all interactions that may occur. Ask your health care provider if Estradiol may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Estradiol :

Use Estradiol as directed by your doctor. Check the label on the medicine for exact dosing instructions.

  • An extra patient leaflet is available with Estradiol . Talk to your pharmacist if you have questions about this information.
  • Take Estradiol by mouth with or without food. If stomach upset occurs, take with food to reduce stomach irritation.
  • Grapefruit and grapefruit juice may increase the risk of Estradiol 's side effects. Talk to your doctor before including grapefruit or grapefruit juice in your diet while you are taking Estradiol .
  • If you miss a dose of Estradiol , take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Estradiol .

Important safety information:

  • Estradiol may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Estradiol with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
  • Limit alcoholic beverages while you are taking Estradiol .
  • Estradiol may cause dark skin patches on your face (melasma). Exposure to the sun may make these patches darker and you may need to avoid prolonged sun exposure and sunlamps. Consult your doctor regarding the use of sunscreens and protective clothing.
  • Estradiol may increase the risk of blood clots. The risk may be greater if you smoke (especially in women older than 35 years of age).
  • Contact your doctor if vaginal bleeding of unknown cause occurs. This could be a sign of a serious condition requiring immediate medical attention.
  • Contact your doctor if vaginal discomfort occurs or if you suspect you have developed an infection while taking Estradiol .
  • Follow your doctor's instructions for examining your breasts and report any lumps immediately.
  • Additional monitoring of your dose or condition may be necessary if you are presently taking an azole antifungal (eg, itraconazole), carbamazepine, a macrolide antibiotic (eg, erythromycin), ritonavir, cimetidine, or St. John's wort.
  • If you wear contact lenses and you develop problems with them, contact your doctor.
  • If you will be having surgery or will be confined to a chair or bed for a long period of time (eg, a long plane flight), notify your doctor beforehand. Special precautions may need to be taken in these circumstances while you are taking Estradiol .
  • Nonprescription therapy to help prevent bone loss includes a weight-bearing exercise plan, as well as adequate daily calcium and vitamin D intake. Consult your doctor or pharmacist for more details.
  • Some of these products may contain the dye tartrazine (FD&C Yellow No. 5), which can cause allergic reactions in certain patients. Consult your doctor or pharmacist. If you previously had allergic reactions to the dye tartrazine, contact your doctor or pharmacist to determine if the product you are taking contains the dye tartrazine.
  • Estradiol may interfere with certain lab tests. Be sure your doctor and lab personnel know you are taking Estradiol .
  • Diabetes patients - Estradiol may affect your blood sugar. Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.
  • Lab tests, including physical exams and blood pressure, may be performed while you use Estradiol . You should have breast and pelvic exams, and a Pap test at least once a year. You should also have periodic mammograms as determined by your doctor. Be sure to keep all doctor and lab appointments.
  • Estradiol should not be used in CHILDREN; safety and effectiveness in children have not been confirmed.
  • PREGNANCY and BREAST-FEEDING: Do not use Estradiol if you are pregnant. Avoid becoming pregnant while you are taking it. If you think you may be pregnant, contact your doctor right away. Estradiol may be found in breast milk. If you are or will be breast-feeding while you use Estradiol , check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Estradiol :

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Breast pain or tenderness; headache; hair loss; mild nausea or vomiting; spotting or breakthrough bleeding; stomach cramps or bloating.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); back pain;breast discharge or lump in the breast; calf or leg pain or swelling; chest pain; coughing up blood; dark urine; depression; dizziness; fainting; fever; memory problems; mental or mood changes; muscle pain; one-sided weakness; painful or difficult urination; persistent or severe breast pain or tenderness; persistent or severe headache, nausea, or vomiting; severe stomach pain or swelling; slurred speech; sudden shortness of breath; sunburn-like rash; swelling of hands, legs, or feet; unusual vaginal bleeding, discharge, itching, or odor; vision changes; vomiting; weakness or numbness of an arm or leg; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions or need medical advice about side effects, contact your doctor or health care provider. You may report side effects to the FDA at 1-800-FDA-1088 (1-800-332-1088) or at http://www.fda.gov/medwatch.

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center (http://www.aapcc.org/findyour.htm), or emergency room immediately. Symptoms may include excessive vaginal bleeding; severe nausea; vomiting.

Proper storage of Estradiol :

Store Estradiol at room temperature, 59 to 86 degrees F (15 to 30 degrees C), in a tight, light-resistant container. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Estradiol out of the reach of children and away from pets.

General information:

  • If you have any questions about Estradiol , please talk with your doctor, pharmacist, or other health care provider.
  • Estradiol is to be used only by the patient for whom it is prescribed. Do not share it with other people.
  • If your symptoms do not improve or if they become worse, check with your doctor.

This information is a summary only. It does not contain all information about Estradiol . If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: September 5, 2007
Database Edition 07.3.1.003
Copyright © 2007 Wolters Kluwer Health, Inc.

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