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Introduction

Written by Patricia Weiser, PharmD
Medically reviewed by Rosanna Sutherby, PharmD
Updated on July 28, 2023

Estradiol (es tra DYE ole) is a generic medication prescribed for symptoms related to menopause. It’s also prescribed to help prevent or treat other conditions. Estradiol belongs to a group of drugs called hormone replacement therapy (HRT).

The Food and Drug Administration (FDA) has approved estradiol to:

• manage symptoms related to menopause
• treat low estrogen levels
• ease symptoms due to some cancers or cancer treatments
• help prevent osteoporosis

These approved uses differ based on the form of estradiol your doctor prescribes.

This article doesn’t provide coupons for all forms of estradiol. To find coupons for estradiol vaginal cream, see this article.

Boxed warnings

Estradiol has boxed warnings, which are the most serious warnings from the Food and Drug Administration (FDA). These include:

• risk of certain types of cancer
• risk of dementia
• risk of serious heart and blood vessel conditions, including blood clot, heart attack, and stroke

For details, see the “Interactions and warnings for estradiol” section.

Side effects of estradiol

Estradiol may cause mild or serious side effects. More common mild side effects of estradiol and its serious side effects are listed below. This article doesn’t include all possible side effects of the drug. Side effects can vary based on your age, overall health, and any other medications you take.

To learn more about estradiol’s side effects, ask your doctor or pharmacist. You can also refer to the prescribing information for estradiol listed in the “Resources” section.

Mild side effects

More common mild side effects reported with some forms of estradiol are listed below. These side effects may differ based on the form of estradiol your doctor prescribes.

This article doesn’t include all possible mild side effects of the drug. To learn more about estradiol’s side effects based on the form, refer to the prescribing information for estradiol listed in the “Resources” section.

With many drugs, mild side effects may go away within a few days or a couple of weeks. If the side effects are bothersome, tell your doctor or pharmacist. They may be able to suggest ways to manage them.

Estradiol oral tablet’s mild side effects include:

• headache
• breast pain or tenderness
• spotting or vaginal bleeding that’s different from usual
• nausea and vomiting
• mild allergic reaction*

Estradiol vaginal cream’s mild side effects include:

• vaginal burning, irritation, or itching where cream is applied
• headache
• breast pain or tenderness
• spotting or vaginal bleeding that’s different from usual
• nausea and vomiting
• mild allergic reaction*

* For details about this side effect, see the “Interactions and warnings for estradiol” section.

Serious side effects

Serious side effects of estradiol are listed below. These side effects may differ based on the form of estradiol your doctor prescribes.

This article doesn’t include all possible serious side effects of the drug. To learn more about estradiol’s side effects based on the form, refer to the prescribing information for estradiol listed in the “Resources” section.

With many drugs, serious side effects are possible but not common. If you have serious side effects from this drug, call your doctor right away. If you’re having severe symptoms or a medical emergency, call 911 or a local emergency number.

In general, estradiol’s serious side effects include:

• high blood pressure
• increased blood sugar
• increased triglycerides (a type of fat in your blood)
• gallbladder problems
• liver problems
• changes in eyesight
• fluid retention
• boxed warning: risk of certain cancers*
• boxed warning: risk of dementia*
• boxed warning: risk of heart or blood vessel conditions, including blood clot, heart attack, and stroke*
• severe allergic reaction*

* For details about this side effect, see the “Interactions and warnings for estradiol” section.

Common questions about estradiol

Below you’ll find answers to a few commonly asked questions about estradiol.

Is there a test to check my estradiol level?

Yes, there is. An estradiol test is a blood test used to measure the amount of estradiol in your blood. Estradiol is a form of the hormone estrogen.

During estradiol treatment, your doctor may order blood work, including an estradiol test. This depends on the condition the drug is being prescribed to treat.

Talk with your doctor to determine whether you’ll need estradiol tests.

How does estradiol compare with estrogen?

Estradiol is a form of estrogen. Estrogen is important for sexual development and reproduction. The body naturally makes estradiol, but its levels drop approaching and during menopause. This may lead to bothersome symptoms, such as hot flashes and vaginal dryness.

To replace natural estradiol, doctors can prescribe synthetic (lab-made) forms of estradiol. It belongs to a group of drugs called hormone replacement therapy (HRT). HRT can help manage symptoms related to menopause. Doctors prescribe estradiol for other uses as well.

If you have questions about whether estradiol is right for you, talk with your doctor.  

Can estradiol be prescribed for men?

Yes, estradiol can be prescribed to treat certain conditions in males,* such as:

• easing symptoms due to advanced prostate cancer or its treatment
• easing symptoms due to breast cancer that’s metastatic (has spread to other areas of the body) or its treatment

Estradiol may also be prescribed for other conditions in males, including off-label uses. With off-label use, doctors prescribe a drug for a purpose other than what it’s approved for.

If you’d like to know more about using estradiol in males, talk with your doctor or pharmacist.

* Sex and gender exist on spectrums. In this article, we use the term “male” to refer to a person’s sex assigned at birth.

How does estradiol work? And how long does it take to start working?

Estradiol works by mimicking the effects of estrogen (a type of natural hormone). Estrogen is important for many functions related to sexual development and reproduction.

How long estradiol takes to work depends on the form your doctor prescribes. For example, estradiol vaginal cream may ease vaginal dryness (a symptom related to menopause) within a couple of weeks. On the other hand, it may take a few weeks to a month for estradiol oral tablet to start relieving menopause symptoms, such as hot flashes.

If you’d like to know more about how estradiol works, talk with your doctor or pharmacist.

Uses of estradiol

The Food and Drug Administration (FDA) approves prescription drugs such as estradiol for certain conditions. Approved uses for estradiol are described below. These uses differ based on the form of estradiol prescribed.

Use for symptoms related to menopause

Doctors may prescribe estradiol for managing symptoms related to menopause. It’s used for this purpose in adults. It’s usually prescribed as a short-term treatment.

Any form of estradiol may be prescribed for this purpose, including:

• oral tablet
• patch applied on the skin
• vaginal cream
• vaginal insert
• topical gel
• injection into your muscle

With menopause, you do not have menstrual periods for 12 months. Approaching and during menopause, you may start having uncomfortable symptoms. Examples include hot flashes and vaginal dryness.

Doctors may not prescribe certain forms of estradiol for some menopause symptoms until you’ve tried other forms first.

Use for low estrogen levels

Doctors may prescribe certain forms of estradiol for treating low estrogen levels. It’s used for this purpose in adults. Estradiol may be prescribed as a short-term or long-term treatment.

The following forms of estradiol may be prescribed for this purpose:

• oral tablet
• patch applied on the skin
• injection into your muscle

With low estrogen levels, your body doesn’t have enough estrogen. Specifically, estradiol is used in adult females* who have one of the following conditions or factors:

• hypogonadism (a condition in which your ovaries aren’t producing enough of the hormone estrogen)
• primary ovarian failure (a condition in which your ovaries stop working before age 40 years)
• your ovaries have been removed by surgery

* Sex and gender exist on spectrums. In this article, we use the term “female” to refer to a person’s sex assigned at birth.

Use for certain cancers

Doctors may prescribe certain forms of estradiol to ease symptoms due to some cancers or certain cancer treatments. It’s used for this purpose in adults. It may be prescribed as a short-term or long-term treatment.

The following forms of estradiol may be prescribed for this purpose:

• oral tablet
• patch applied on the skin
• injection into your muscle

With cancer, certain cells of the body grow abnormally. Estradiol (a form of estrogen) can slow tumor growth in some types of cancers. It can be given to help ease symptoms due to some cancers or certain cancer treatments. This is known as palliative care.  

Specifically, the drug is used for this purpose in people with:

• advanced prostate cancer that’s dependent on androgen (a type of hormone)
• metastatic breast cancer (breast cancer that has spread to other parts of the body)

Use for prevention of osteoporosis

Doctors may prescribe certain forms of estradiol to help prevent osteoporosis. It’s used for this purpose in adults. It’s usually prescribed as a long-term treatment.

The following forms of estradiol may be prescribed for this purpose:

• oral tablet
• transdermal patch

With osteoporosis, your bones become thin and weak. This increases your risk for certain fractures.

Estradiol is typically prescribed together with certain dietary supplements for the prevention of osteoporosis. These include calcium and vitamin D supplements.

Doctors may not prescribe estradiol by itself for preventing osteoporosis in females* after menopause in certain situations. This includes when other treatment options are available that do not contain estrogen.

* Sex and gender exist on spectrums. In this article, we use the term “female” to refer to a person’s sex assigned at birth.

Interactions and warnings for estradiol

Below, you’ll find information about estradiol’s possible interactions and warnings.

Interactions of estradiol

Certain things may affect how a drug works. These include getting vaccines, consuming alcohol or certain foods, or taking the drug with other medications. This effect is called a drug interaction.

Before you start estradiol treatment, ask your doctor to check for possible interactions. Be sure to tell them about any of the following you take or use:

• prescription or over-the-counter drugs
• vitamins, herbs, or supplements

To learn about drug-condition interactions, see the “Warnings for estradiol” section below.

Warnings for estradiol

Some people should not take or use estradiol, and others should use it cautiously.

Boxed warnings

Estradiol has boxed warnings, which are the most serious warning from the Food and Drug Administration (FDA). These include:

• risk of certain cancers
• risk of dementia
• risk of heart or blood vessel conditions, including blood clot, heart attack, and stroke

To learn more about these warnings, read below. You can also talk with your doctor or pharmacist.

Risk of certain cancers. Treatments containing estrogen (a type of hormone) alone, such as estradiol, may increase the risk of certain cancers. Estradiol is prescribed to ease symptoms due to some cancers or certain cancer treatments. But it can increase the risk of developing other cancers, such as endometrial cancer. It may also increase the risk of certain breast cancers if it’s used with progesterone (another type of hormone). This side effect was rarely reported in studies* of estradiol.

Cancer symptoms may include a lump in your breast, unusual vaginal bleeding, weight loss, night sweats, or pain in your pelvis.

If you’re concerned about your risk of breast or endometrial cancer, tell your doctor. To help lower your risk, they may suggest decreasing your estradiol treatment to the lowest effective dose for the shortest time. They may also recommend getting routine screenings during estradiol treatment. These may include breast exams, mammograms, pelvic exams, and blood tests.

For details about estradiol’s use in cancer treatment, see the “Uses of estradiol” section.

* To learn more about these studies, refer to the prescribing information for estradiol listed in the “Resources” section.

Risk of dementia. Females* ages 65 years and older who’ve gone through menopause may have an increased risk of dementia if they take or use estradiol with progesterone. Estradiol is not meant to help prevent dementia. This side effect was rarely reported in studies† of estradiol.

Doctors typically won’t prescribe estradiol if you have symptoms of dementia. Symptoms may include problems with memory, getting lost, misplacing things, trouble remembering how to complete routine tasks, and confusion.

If you experience symptoms of dementia, tell your doctor. They’ll likely have you stop estradiol treatment. They may recommend other treatment options.

* Sex and gender exist on spectrums. In this article, we use the term “female” to refer to a person’s sex assigned at birth.
† To learn more about these studies, refer to the prescribing information for estradiol listed in the “Resources” section.

Risk of serious heart and blood vessel conditions. Estradiol treatment may increase the risk of serious heart and blood vessel conditions. These may include blood clot, heart attack, and stroke. These side effects were rarely reported in studies* of estradiol.

Symptoms of heart and blood vessel conditions may include pain or pressure in your chest, swelling in your leg or arm, dizziness, sweating, or trouble speaking.

If you’re concerned about your risk of heart and blood vessel conditions, tell your doctor. They may not prescribe the drug if you already have risk factors for heart and blood vessel problems. To help lower your risk, your doctor may suggest the lowest effective dose of estradiol for the shortest possible time.

* To learn more about these studies, refer to the prescribing information for estradiol listed in the “Resources” section.

Other warnings

Estradiol could cause harm to people with certain health conditions. This effect is called a drug-condition interaction. Other factors can also affect whether estradiol is a safe option for you. These warnings may differ based on the form of estradiol your doctor prescribes.

Ask your doctor about specific warnings for estradiol, and be sure to tell your doctor about your:

• current health, including any allergies to medications
• past health conditions or surgeries

Allergic reaction

Estradiol can cause an allergic reaction in some people. Severe allergic reactions are rare but possible.

If you’ve had an allergic reaction to estradiol or any of its ingredients, your doctor will likely not prescribe estradiol. They can tell you about medications that are safer options for you.

A mild allergic reaction may cause the following symptoms:

• skin rash
• itchiness
• flushing (temporary warmth, redness, or deepening of skin color)

A severe allergic reaction may cause the following symptoms:

• swelling under your skin, usually in your hands, feet, eyelids, or lips
• swelling of your mouth, throat, or tongue, which can cause breathing problems

If you have an allergic reaction to estradiol, call your doctor right away. If you have severe symptoms, call 911 or a local emergency number.

Overdose of estradiol

You should not take or use more estradiol than your doctor prescribes. For some drugs, doing so may lead to harmful effects or overdose.

If you think you’ve taken or used too much estradiol, call your doctor or pharmacist right away. Or you could call 800-222-1222 to speak with someone at America’s Poison Centers. You can also use its online resource. If you have concerning symptoms, call 911 or a local emergency number immediately. You can also go to the closest emergency room.

Pregnancy or breastfeeding and estradiol

Information about estradiol and pregnancy and breastfeeding is described below.

Estradiol and pregnancy

It’s not known whether estradiol treatment should be received during pregnancy. That said, estradiol tablets, cream, or injection should not be used during pregnancy.

If you’re planning a pregnancy or can become pregnant, talk with your doctor before starting this medication.

To learn more about estradiol’s safety during pregnancy based on the form, refer to the prescribing information for estradiol listed in the “Resources” section.

Estradiol and breastfeeding

There are risks to using estradiol while breastfeeding. For instance, estradiol treatment may decrease the amount of breast milk your body makes. The drug can also affect the quality of your breast milk.

If you’re planning to breastfeed, talk with your doctor about your treatment options. Together, you can discuss the risks and benefits of these options and decide whether or not you should receive estradiol treatment during this time. Your doctor may recommend other healthy ways to feed your child.

What to ask your doctor

Let your doctor know if you have questions about estradiol or would like more details about it.

Here’s a list of some possible questions you may want to ask your doctor:

• Am I at high risk for side effects with estradiol?
• How long should I continue estradiol treatment?
• Are there alternative medications that you can prescribe for my condition?
• Should I keep taking my other medications and supplements during estradiol treatment?

Resources

• Estradiol tablet. (2016). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/2c209b3d-323a-4a47-9866-b7ea70346195/spl-doc
• Estradiol gel, for topical use. (2023). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/e84ad638-6768-41aa-b2b8-e2514ef63881/spl-doc
• Estradiol vaginal inserts — estradiol tablet, film coated. (2022). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/86620f6c-fd02-40df-98d5-3048dcd92c37/spl-doc
• Estradiol valerate injection. (2022). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/66f40ab0-4432-4e85-b709-a0bc076868c6/spl-doc
• Estradiol cream. (2018). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/c8a2d29c-299c-4559-b859-87b303a4af81/spl-doc
• Estradiol patch, extended release. (2023). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/23300ef2-8133-4056-9684-92b9a9192e30/spl-doc
• Food and Drug Administration. (2023). Orange Book: Approved drug products with therapeutic equivalence evaluations. https://www.accessdata.fda.gov/scripts/cder/ob/index.cfm

Disclaimer: Optum Perks has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or another healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.