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Overview: Estradiol is available as a tablet and an injection to increase estrogen levels. It is used after menopause to reduce vaginal dryness, pain during sex, hot flashes, night sweats, prevent osteoporosis, and to treat advanced prostate cancer. The tablets are also used to treat some types of breast cancer. The most common side effects are headache and breast pain or tenderness. Talk with your healthcare provider right away about any unusual vaginal bleeding or vaginal discharge.

Uses

What is estradiol used for?

Estradiol is commonly used for the following.

  • To help reduce postmenopausal vaginal dryness or pain during sex 
  • To help reduce hot flashes and night sweats (vasomotor menopause symptoms)
  • To help prevent osteoporosis after menopause
  • To increase estrogen levels in people when they are not making enough on their own
  • To treat certain types of prostate cancer and breast cancer

Estradiol may also be used for other conditions as determined by your healthcare provider.

How does estradiol work (mechanism of action)?

Estrogen is an important hormone for the health of the vagina and bones. It also plays a role in temperature regulation and reduces levels of androgens (male hormones). During menopause or when your body does not make enough natural estrogen, levels go down. When this happens, the vagina can become dry and irritated, bones can become weak and fragile, and you may have hot flashes or night sweats. Estradiol raises estrogen levels to reduce symptoms of menopause by improving vaginal health, reducing bone loss, and helping regulate body temperature. Certain breast and prostate cancers are fed by male hormones. Estradiol can reduce male hormone levels and may limit growth and spread of these cancers.

How is estradiol supplied (dosage forms)?

Brands and other names

  • Estrace
  • Delestrogen
  • Depo-Estradiol

Dosage forms and strengths 

  • 0.5 mg, 1 mg, 2 mg oral tablets
  • 5 mg/mL, 10 mg/mL, 20 mg/mL, 40 mg/mL intramuscular injection

How should I store estradiol?

Oral Tablets. Estradiol tablets should be stored at room temperature, between 68 F to 77 F (20 C to 25 C). It can be exposed to temperatures between 59 F to 86 F (15 C to 30 C), for shorter periods of time, such as when transporting it. Store in a cool, dry place.

Injection. Estradiol injection is usually given by a healthcare provider in a hospital or clinic. If you will store estradiol injection at home, follow the instructions given by your healthcare provider.

Side Effects

What are the most common side effects of estradiol?

The most common side effects of estradiol are listed below. Tell your healthcare provider if you have any of these side effects that bother you.

  • Headache
  • Breast pain
  • Irregular vaginal bleeding or spotting
  • Stomach cramps, bloating, nausea, or vomiting
  • Hair loss

There may be other side effects of estradiol that are not listed here. Contact your healthcare provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088. In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of estradiol?

While less common, the most serious side effects of estradiol are described below, along with what to do if they happen.

Blood Clots. Estradiol may cause blood clots in your arteries or veins and could cause a stroke, heart attack, or venous thromboembolism, including a blood clot in the back of the eye (retinal vein occlusion), in the lungs (pulmonary embolism), or deep venous thrombosis (DVT). Stop using estradiol and get emergency help if you have any of the following signs of blood clots.

  • Chest pain or pressure
  • Fast or abnormal heartbeat
  • Trouble breathing
  • Pain in your back, jaw, throat, or arm
  • Sweating, upset stomach, vomiting, or dizziness
  • Sudden weakness on one side of your body
  • Sudden and severe headache
  • Slurred speech or trouble understanding speech
  • Pain, swelling, or tenderness in your arm or leg
  • Vision loss
  • Bulging eyes 
  • Double vision

Endometrial Cancer. You may be at higher risk for cancer in the lining of your uterus (endometrial cancer) if you use estradiol. Call your healthcare provider right away if you have any abnormal vaginal bleeding.

Breast Cancer. You may be at higher risk for breast cancer if you use estradiol. Call your healthcare provider right away if you have any of the following symptoms.

  • New lump in your breast or armpit
  • Changes in the size, shape, texture, or temperature of your breast
  • Nipple changes

Ovarian Cancer. You may be at higher risk for cancer in your ovaries (ovarian cancer) if you use estradiol. Call your healthcare provider right away if you have any of the following symptoms.

  • Unusual vaginal discharge
  • Belly or back pain
  • Need to pee more often or urgently

Gallbladder Problems. Using estradiol may cause gallbladder problems, including cholecystitis and cholelithiasis (also known as gallstones). Call your healthcare provider right away if you have any of the following symptoms.

  • Your skin or the whites of your eyes turning yellowish in color (also called jaundice)
  • Fever
  • Pain in your upper stomach area
  • Stool (poop) that is clay-colored

Memory Problems. Using estradiol may increase your risk for memory problems (dementia), especially if you are 65 or older. Call your healthcare provider if you or friends or family notice that you are having trouble with your memory.

Increased Blood Pressure (Hypertension). Estradiol may increase your blood pressure or worsen it if you have a history of high blood pressure. Call your healthcare provider if your blood pressure increases while using this medicine.

If you measure your blood pressure and the top number (systolic) is 180 mm Hg or higher or the bottom number (diastolic) is 120 mm Hg or higher, get medical attention right away. Increases in blood pressure may not be noticeable but look out for any of the following symptoms of severely high blood pressure.

  • Sudden severe headache
  • Chest pain
  • Dizziness or confusion
  • Trouble breathing
  • Nausea or vomiting
  • Blurry or other changes to vision
  • Anxiety
  • Buzzing in the ears
  • Nosebleed
  • Feeling of skipped heart beats

Fluid Retention (Edema). Estradiol can cause fluid retention, also called edema. Fluid retention can cause serious issues in people with certain conditions, such as heart failure or kidney disease. Call your healthcare provider right away if you have any of the following symptoms. 

  • Chest pain
  • Irregular heartbeat
  • Shortness of breath
  • Stretched or shiny skin
  • Swollen body parts, such as the belly or ankles

Severe Allergic Reactions. Estradiol may cause allergic reactions, which can be serious. Stop using estradiol and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat (angioedema)
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

Warnings & Precautions

Who should not use estradiol?

Allergies to Ingredients. People who are allergic to any of the following should not use estradiol products.

  • Estradiol
  • Delestrogen
  • Depo-Estradiol
  • Estrace
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in the specific estradiol products they stock.

Blood Clots. Estradiol should not be used if you have now or have a history of blood clots in your veins, such as a deep venous thrombosis (DVT), or your lungs, such as a pulmonary embolism (PE).

Breast Cancer. Depending on why you are using it, estradiol should not be used if you have, are being evaluated to see if you have, or have previously had breast cancer.

Estrogen Dependent Cancer. Estradiol should not be used if you have cancer that needs estrogen to grow. Examples of these cancers include ovarian cancer and endometrial or uterine cancer. 

Stroke or Heart Attack. Estradiol should not be used if you have had a stroke or heart attack within the last year.

Unusual Vaginal Bleeding. Estradiol should not be used if you have abnormal bleeding from your vagina that has not been diagnosed by a healthcare provider.

Thrombophilia. Estradiol should not be used if you have low blood levels of protein C, protein S, or antithrombin, or if you have a condition that increases your risk of developing a blood clot.

Liver Problems. Estradiol should not be used if your liver is not working as well as it should be. If there is a concern about the health of your liver, your healthcare provider may do tests to determine if it is working well enough to use this medicine.

Pregnancy. Do not use estradiol if you are pregnant. If you become pregnant, contact your healthcare provider right away. See the Pregnancy section for more details.

What should I know about estradiol before using it?

If you have a uterus, talk to your healthcare provider about whether adding a progestin is right for you.

Do not use estradiol unless it has been prescribed to you by a healthcare provider. Use it as prescribed.

Do not share estradiol with other people, even if they have the same condition as you. It may harm them.

Keep estradiol out of the reach of children.

It is best to use the lowest dose of estrogen that works for the shortest length of time. Ask your healthcare provider how much and for how long you should use estradiol. 

Keep all scheduled appointments for breast exams, vaginal exams, and mammograms while using estradiol. 

People who are aged 65 or older can be at greater risk for some side effects from estradiol. Talk to your healthcare provider about your risks if you are in this age group.

What should I tell my healthcare provider before using estradiol?

Tell your healthcare provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them determine if estradiol is right for you.

In particular, make sure that you discuss any of the following.

Surgery or Bedrest. Tell your healthcare provider about any bedrest or upcoming surgery that will require you to be immobile or not be able to get up and walk around normally. Follow any instructions from your healthcare provider about when to stop and restart using estradiol. 

Current and Past Health Conditions. Tell your healthcare provider if you have any of the following. 

  • Aspirin allergy
  • Unusual vaginal bleeding or spotting after menopause
  • Cancer
  • Heart problems
  • Stroke
  • Blood clots
  • High blood pressure
  • Liver problems, including growth of abnormal blood vessels in the liver (hemangioma)
  • Asthma
  • Diabetes
  • Seizures
  • Migraines
  • Endometriosis
  • Systemic lupus erythematosus
  • Porphyria
  • Thyroid or parathyroid problems
  • Kidney problems
  • High blood calcium levels
  • Hereditary angioedema
  • Smoking
  • Gallbladder problems with estrogen use or during pregnancy

Other Medicines and Supplements. Estradiol may interact with other medicines and supplements. Before using estradiol, tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

High Triglyceride Levels. If you have high triglyceride levels, estradiol may make your triglycerides even higher. Very high triglyceride levels can lead to inflammation of the pancreas, which is called pancreatitis. Tell your healthcare provider if you have high triglyceride levels.

Pregnancy. People who can become pregnant are not usually prescribed estradiol, unless it is a method of birth control. Estradiol should not be used in pregnancy. Tell your healthcare provider if you are, think you are, or plan to become pregnant. 

Breastfeeding. Estradiol may pass into breast milk. Using estradiol can reduce the quality and quantity of milk your body makes. Tell your healthcare provider if you are breastfeeding or plan to breastfeed. Your healthcare provider will advise you if you should use estradiol while breastfeeding. 

Interactions

Does estradiol interact with foods or drinks?

Do not eat or drink things with grapefruit or grapefruit juice in them while using estradiol. This could increase the estradiol levels in your blood and may cause serious side effects. 

Limit the amount of alcohol you drink while using estradiol. The risk for liver damage may increase if you drink large amounts of alcohol while using estradiol.

Does estradiol interact with other medicines (drug interactions)?

Always tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.

In particular, make sure that you discuss if you are using any of the following before using estradiol.

  • St. John’s wort, which is a supplement that may be used to treat depression
  • Phenobarbital or carbamazepine (Carbatrol, Tegretol, and others), which is a medicine to control seizures
  • Rifampin, which is a medicine commonly used to treat an infection called tuberculosis
  • Erythromycin (Ery-Tab and others) or clarithromycin, which is a medicine used for bacterial infections
  • Ketoconazole or itraconazole (Sporanox, Tolsura), which is a medicine used for fungal infections
  • Ritonavir, which is a medicine commonly used to treat HIV

Some other medicines may alter the blood levels of estradiol. Tell your healthcare provider about all medicines that you take or have recently taken.

This may not be a complete list of medicines that can interact with estradiol. Always check with your healthcare provider.

Does interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much estradiol?

If you or someone else has used too much estradiol, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of estradiol?

If you miss a dose of an estradiol tablet, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and only take the next dose. Do not take double or extra doses. 

The estradiol injection is usually given by a healthcare provider in a hospital or clinic. Your healthcare provider will make sure you are receiving estradiol as scheduled. If you miss an appointment to get your estradiol injection, call to make another appointment as soon as possible.