Estradiol is a prescription medication used to treat symptoms of menopause including hot flashes and vaginal dryness. It is also used to treat conditions in which a woman's ovaries do not produce enough estrogen naturally (hypoestrogenism).

Estradiol is a form of the hormone estrogen. It replaces estrogen that is not naturally produced by the ovaries.

This medication comes is available as a topical cream, a transdermal patch, a transdermal gel, a transdermal spray, a vaginal insert, and an oral tablet. It is usually taken once a day.

This medication is available in an injectable form to be given directly into a muscle (IM) by a healthcare professional.

Estradiol is also available in several combination products and hormonal contraceptives. This medication page only refers to the single-ingredient preparations.

Common side effects of estradiol include headache, breast pain, nausea, and bloating.

Estradiol is a prescription medication used to treat symptoms of menopause including hot flashes and vaginal dryness. It is also used to treat conditions in which a woman's ovaries do not produce enough estrogen naturally (hypoestrogenism).

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with topical, oral, and injectable forms of estradiol. See the “Estradiol Precautions” section.

Common side effects of estradiol include the following:

• headache
• breast pain or tenderness
• nausea
• vomiting
• constipation
• gas
• heartburn
• weight gain or loss
• hair loss
• redness or irritation of the skin that was covered by the estradiol patch, cream, or gel
• swelling, redness, burning, irritation or itching of the vagina
• vaginal discharge
• painful menstrual periods
• anxiety
• depression
• changes in mood
• change in sexual desire
• back, neck, or muscle pain
• runny nose or congestion
• cough
• darkening of skin on face (may not go away even after you stop using transdermal estradiol)
• unwanted hair growth
• difficulty wearing contact lenses

This is not a complete list of estradiol side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• Amiodarone (Cordarone, Pacerone)
• Antifungals such as itraconazole (Sporanox) and ketoconazole (Nizoral)
• Aprepitant (Emend)
• Carbamazepine (Carbatrol, Epitol, Tegretol)
• Cimetidine (Tagamet)
• Clarithromycin (Biaxin)
• Cyclosporine (Neoral, Sandimmune)
• Dexamethasone (Decadron, Dexpak)
• Diltiazem (Cardizem, Dilacor, Tiazac, others)
• Erythromycin (E.E.S, Erythrocin)
• Fluoxetine (Prozac, Sarafem)
• Fluvoxamine (Luvox)
• Griseofulvin (Fulvicin, Grifulvin, Gris-PEG)
• Lovastatin (Altocor, Mevacor)
• Medications for human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS) such as atazanavir (Reyataz), delaviridine (Rescriptor), efavirenz (Sustiva), indinavir (Crixivan), lopinavir (in Kaletra),nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir, in Kaletra), and saquinavir (Fortovase, Invirase)
• Medications for thyroid disease
• Nefazodone
• Other medications that contain estrogen
• Phenobarbital
• Phenytoin (Dilantin, Phenytek); rifabutin (Mycobutin)
• Rifampin (Rifadin, Rimactane, in Rifamate)
• Sertraline (Zoloft)
• Troleandomycin (TAO)
• Verapamil (Calan, Covera, Isoptin, Verelan)
• Zafirlukast (Accolate)
• St. John's Wort

This is not a complete list of estradiol drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with topical, oral, and injectable forms of estradiol including the following:

• bulging eyes
• yellowing of the skin or eyes
• itching
• loss of appetite
• fever
• joint pain
• stomach tenderness, pain, or swelling
• movements that are difficult to control
• hives
• rash or blisters on the skin
• swelling, of the eyes, face, lips, tongue, throat, hands, feet, ankles, or lower legs
• hoarseness
• wheezing
• difficulty breathing or swallowing

Do not take estradiol if you:

• are allergic to estradiol or to any of its ingredients
• have abnormal vaginal bleeding
• have a known or suspected history of breast cancer
• have a known or suspected estrogen-dependent cancer
• have a history of blood clots
• have liver disease
• are pregnant or possibly pregnant

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

Before taking estradiol, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to estradiol or to any of its ingredients
• have or have ever had asthma
• have seizures
• have migraine headaches
• have endometriosis (a condition in which the type of tissue that lines the uterus [womb] grows in other areas of the body)
• have uterine fibroids (growths in the uterus that are not cancer)
• have or have had yellowing of the skin or eyes, especially during pregnancy or while you were using an estrogen product
• have very high or very low levels of calcium in your blood
• have porphyria (condition in which abnormal substances build up in the blood and cause problems with the skin or nervous system) or gallbladder, thyroid, pancreas, liver or kidney disease
• are pregnant or breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Estradiol falls into category X. Estradiol should now be used during pregnancy. There appears to be little or no increased risk of birth defects in children born to women who inadvertently used estrogens during early pregnancy. Talk to your doctor right away if you become pregnant while taking estradiol.

Tell your doctor if you are breastfeeding or plan to breastfeed.

Estradiol has been detected in human breast milk. Estradiol can decrease the quality or quantity of breast milk. A choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

Take estradiol exactly as prescribed.

Topical:

This medication is available as a vaginal cream, a transdermal patch, a transdermal gel, a transdermal spray, and vaginal insert. It is usually applied once a day.

Oral:

This medication is available as an oral tablet. It is usually taken once a day, with food.

Injectable:

This medication is also available in an injectable form to be given directly into a muscle (IM) by a healthcare professional.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of estradiol at the same time.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication

Topical:

The recommended starting dose of estradiol transdermal patches for the treatment of menopause symptoms or hypoestrogenism is 0.025 mg daily applied to the skin once weekly.

The recommended starting dose of estradiol transdermal spray for the treatment of menopause symptoms is 1.53 mg daily applied to the skin of the forearm once daily.

The recommended starting dose of estradiol transdermal gel for the treatment of menopause symptoms is 0.25 g daily applied to the skin of the upper thigh once daily.

The recommended starting dose of estradiol vaginal cream for the treatment of menopause symptoms is 2 to 4 g daily applied to the skin of the upper thigh once daily.

The recommended starting dose of estradiol vaginal insert for the treatment of menopause symptoms is 0.05 or 0.10 mg daily inserted into the vagina every 3 months.

Oral:

The recommended dose range of estradiol oral tablets for the treatment of menopause symptoms is 1 to 2 mg daily by mouth.

Injectable:

The recommended dose range of estradiol cypionate intramuscular injection for the treatment of menopause symptoms is 1 to 5 mg injected every 3 to 4 weeks.

The recommended dose range of estradiol valerate intramuscular injection for the treatment of menopause symptoms is 10 to 20 mg injected every 4 weeks.

If you take too much estradiol, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If estradiol is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Store estradiol at room temperature.

Keep this and all medicines out of the reach of children.

WARNING: ESTROGENS INCREASE THE RISK OF ENDOMETRIAL CANCER.

CLOSE CLINICAL SURVEILLANCE OF ALL WOMEN TAKING ESTROGENS IS IMPORTANT. ADEQUATE DIAGNOSTIC MEASURES, INCLUDING ENDOMETRIAL SAMPLING WHEN INDICATED, SHOULD BE UNDERTAKEN TO RULE OUT MALIGNANCY IN ALL CASES OF UNDIAGNOSED PERSISTENT OR RECURRING ABNORMAL VAGINAL BLEEDING. THERE IS CURRENTLY NO EVIDENCE THAT THE USE OF “NATURAL” ESTROGENS RESULTS IN A DIFFERENT ENDOMETRIAL RISK PROFILE THAN SYNTHETIC ESTROGENS OF EQUIVALENT ESTROGEN DOSE.

CARDIOVASCULAR AND OTHER RISKS 

ESTROGENS WITH AND WITHOUT PROGESTINS SHOULD NOT BE USED FOR THE PREVENTION OF CARDIOVASCULAR DISEASE OR DEMENTIA.

THE WOMEN’S HEALTH INITIATIVE (WHI) STUDY REPORTED INCREASED RISKS OF MYOCARDIAL INFARCTION, STROKE, INVASIVE BREAST CANCER, PULMONARY EMBOLI, AND DEEP VEIN THROMBOSIS IN POSTMENOPAUSAL WOMEN (50 TO 79 YEARS OF AGE) DURING 5 YEARS OF TREATMENT WITH ORAL CONJUGATED ESTROGENS (CE 0.625 MG) COMBINED WITH MEDROXYPROGESTERONE ACETATE (MPA 2.5 MG) RELATIVE TO PLACEBO.

THE WOMEN’S HEALTH INITIATIVE MEMORY STUDY (WHIMS), A SUBSTUDY OF WHI, REPORTED INCREASED RISK OF DEVELOPING PROBABLE DEMENTIA IN POSTMENOPAUSAL WOMEN 65 YEARS OF AGE OR OLDER DURING 4 YEARS OF TREATMENT WITH ORAL CONJUGATED ESTROGENS PLUS MEDROXYPROGESTERONE ACETATE RELATIVE TO PLACEBO. IT IS UNKNOWN WHETHER THIS FINDING APPLIES TO YOUNGER POSTMENOPAUSAL WOMEN.

OTHER DOSES OF ORAL CONJUGATED ESTROGENS WITH MEDROXYPROGESTERONE ACETATE, AND OTHER COMBINATIONS AND DOSAGE FORMS OF ESTROGENS AND PROGESTINS WERE NOT STUDIED IN THE WHI CLINICAL TRIALS AND, IN THE ABSENCE OF COMPARABLE DATA, THESE RISKS SHOULD BE ASSUMED TO BE SIMILAR. BECAUSE OF THESE RISKS, ESTROGENS WITH OR WITHOUT PROGESTINS SHOULD BE PRESCRIBED AT THE LOWEST EFFECTIVE DOSES AND FOR THE SHORTEST DURATION CONSISTENT WITH TREATMENT GOALS AND RISKS FOR THE INDIVIDUAL WOMAN.