What is Estradiol: Uses, Warnings & Interactions

Medically reviewed by Karen BergerPharm.D.
Licensed Pharmacist
Updated Oct 8, 2025  •  Published Dec 30, 2020
Fact Checked

Estradiol is a female sex hormone called an estrogen. Of the three types of estrogens naturally produced by the body, estradiol is the most potent. As a generic prescription drug, estradiol is used to replace estradiol in women who are not producing enough estrogen either because of menopause or other reasons. Although estrogen replacement is successful at treating some aspects of estradiol deficiency, the use of estradiol comes with serious risks and potentially serious side effects. 

Estradiol overview

BRAND NAMES:

  • Climara, Delestrogen, Divigel, Dotti, Elestrin, Estrace, Estring, EstroGel, Evamist, Femring, Imvexxy, Menostar, Minivelle, Vagifem, Vivelle-Dot, Yuvafem

Generic Names:

  • Estradiol

Uses:

  • Treats vasomotor symptoms caused by menopause. Prevents osteoporosis or treats vulvovaginal atrophy in postmenopausal women. Treats late-stage prostate or breast cancer.

Therapeutic Classes:

  • Endocrine-metabolic agent

  • Hormone replacement therapy

Forms:

  • Oral tablet, vaginal cream, topical gel, topical spray, skin patch, vaginal ring, vaginal insert (vaginal tablet), implantable pellet, injection

How it’s taken:

  • By mouth, inside the vagina, on the skin, implanted, injected

What is Estradiol used for?

Healthcare professionals use estradiol to control or prevent menopause issues, including the vasomotor symptoms (hot flashes and night sweats) of menopause or, following menopause, degeneration of genital tissues or osteoporosis. Healthcare professionals also use estradiol to treat estrogen deficiency in women with underactive ovaries, ovarian failure, or after a hysterectomy. Healthcare professionals also use it for inoperable breast cancer or prostate cancer.

Key takeaways

  • Tell your healthcare provider about all of your medical conditions, as well as medical and family history. Tell your provider about all the medications you take, including prescription and OTC drugs, vitamins, and supplements.

  • There are many different forms of estradiol. Your healthcare provider will prescribe the one that is most suitable for your needs and tell you how to use it. 

  • Before using estradiol, read the patient information, medication guide, and instructions for use that come with your prescription. Ask your healthcare provider if you have any questions or concerns.

  • Common side effects of estradiol include headache, breast tenderness, stomach cramps, bloating, nausea, vomiting, and irregular vaginal bleeding. Call your healthcare provider if you have any side effects that bother you or do not go away.

What form(s) does Estradiol come in

  • Tablet

    • 0.5 mg

    • 1 mg

    • 2 mg

  • Vaginal cream

    • 0.01% (0.1 mg/g)

  • Vaginal insert

    • 4 mcg (0.004 mg)

    • 10 mcg (0.01 mg)

  • Vaginal ring

    • 0.05 mg/day

    • 0.0075 mg/day

    • 0.1 mg/day

  • Gel

    • 0.1% 

    • 0.06% 

  • Spray

    • 1.53 mg/spray

  • Patch

    • 0.014 mg/day

    • 0.025 mg/day

    • 0.0375 mg/day

    • 0.05 mg/day

    • 0.06 mg/day

    • 0.075 mg/day

    • 0.1 mg/day

  • Implant (pellet)

    • 25 mg

    • 50 mg

  • Injection

    • 5 mg/mL

    • 10 mg/mL

    • 20 mg/mL

    • 40 mg/mL

What are common Estradiol doses?

  • For the vasomotor symptoms of menopause: 1–2 mg tablet once per day for 21 days with a rest period of 7 days

  • For vulvovaginal atrophy in postmenopausal women: 2–4 g of 0.01% vaginal cream applied once per day for 1–2 weeks, followed by 1–2 g applied once per day for 1–2 weeks, followed by a maintenance dose of 1 g applied 1 to 3 times a week

  • For pain during sexual intercourse due to vulvovaginal atrophy in postmenopausal women: 4 mcg vaginal insert once per day for 2 weeks followed by 4 mcg vaginal insert once every 3–4 days

  • For osteoporosis prevention in postmenopausal women: 0.5 mg to 2 mg tablet once per day

  • For low estrogen levels in premenopausal women: 1–2 mg tablet once per day

  • For palliative treatment of metastatic breast cancer: 10 mg 3 times per day for 3 months or longer

  • For palliative treatment of inoperable prostate cancer: 1–2 mg tablets 3 times per day

  • Dosages will vary if other formulations are used, such as gels, creams, sprays, or vaginal rings. Find more detailed information about estradiol dosages, forms, and strengths here

Common Estradiol prescriptions

  • Estradiol
    1 box (18 vaginal tablets), 10mcg box

  • Estradiol
    1 box (30 gel packets), 0.25mg/0.25gm (0.1%) box

  • Estradiol
    1 box (30 gel packets), 0.5mg/0.5gm (0.1%) box

  • Estradiol
    1 box (30 gel packets), 0.75mg/0.75gm (0.1%) box

  • Estradiol
    1 box (30 gel packets), 1.25mg/1.25gm (0.1%) box

  • Estradiol
    1 box (30 gel packets), 1mg/1gm (0.1%) box

  • Estradiol
    1 box (4 weekly patches), 0.025mg/24 hr box

  • Estradiol
    1 box (4 weekly patches), 0.025mg/24hr box

  • Estradiol
    1 box (4 weekly patches), 0.0375mg/24hr box

  • Estradiol
    1 box (4 weekly patches), 0.05mg/24 hr box

  • Estradiol
    1 box (4 weekly patches), 0.05mg/24hr box

  • Estradiol
    1 box (4 weekly patches), 0.06mg/24 hr box

  • Estradiol
    1 box (4 weekly patches), 0.06mg/24hr box

  • Estradiol
    1 box (4 weekly patches), 0.075mg/24 hr box

  • Estradiol
    1 box (4 weekly patches), 0.075mg/24hr box

  • Estradiol
    1 box (4 weekly patches), 0.1mg/24 hr box

  • Estradiol
    1 box (4 weekly patches), 37.5mcg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.025mg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.0375mg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.0375mg/24hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.05mg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.05mg/24hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.075mg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.075mg/24hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.1mg/24 hr box

  • Estradiol
    1 box (8 twice weekly patches), 0.1mg/24hr box

  • Estradiol
    1 box (8 vaginal tablets), 10mcg box

  • Estradiol
    4 patch weekly box

  • Estradiol
    0.5mg tablet

  • Estradiol
    1mg tablet

  • Estradiol
    2mg tablet

  • Estradiol
    42.5gm of 0.1mg/gm tube of cream

How to take Estradiol

  • Your healthcare provider will tell you how much and how often to take this medicine. Do not take more medicine or take it more often than your healthcare provider tells you to.

  • How to take estradiol tablets:

    • Take as directed by your healthcare provider. 

    • Store estradiol tablets in a tightly closed, light-resistant container. Secure the container with a child-proof cap and keep it securely out of the reach of children.

  • How to use estradiol patches:

    • Estradiol patches are for use on the skin only.

    • Follow the Instructions for Use that come with this package.

    • Apply the patch to clean, dry skin only.

    • Do not apply estradiol patches to the breasts.

  • How to use estradiol gel and spray:

    • Estradiol gel and spray are for use on the skin only.

    • Follow the Instructions for Use that come with the package.

    • Do not allow other people to apply the gel.

    • Apply to clean, dry skin only.

    • Do not apply to the breasts or around the vagina or vulva.

    • Apply estradiol spray at the same time each day.

    • Immediately wash your hands after application.

  • How to use estradiol vaginal cream:

    • Estradiol cream is used in the vagina only. 

    • Use as directed by your healthcare provider. 

    • Administer each dose using the applicator.

    • Follow the Instructions for Use included with the package or follow the instructions given by a healthcare provider.

  • How to use an estradiol vaginal insert:

    • Vaginal inserts are for placement in the vagina only.

    • Follow the Instructions for Use included with the package.

  • How to use an estradiol vaginal ring:

    • Vaginal rings can be inserted and removed by either a healthcare provider or the patient.

    • Follow the Instructions for Use for inserting and removing the ring that comes with this package.

  • Estradiol injections and implants are administered by healthcare professionals.

What to do if you miss a dose of Estradiol

  • What to do if you miss a dose of estradiol?

  • If you miss a dose or forget to take your medicine, take it as soon as you can. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose.

  • Do not use extra medicine to make up for a missed dose.

Estradiol contraindications

  • Estradiol is never used in people who are pregnant or have:

    • Undiagnosed vaginal bleeding

    • A history of blood clots, stroke, or heart attack

    • Medical conditions that increase the tendency to form blood clots

    • A bleeding disorder

    • Liver disease

    • Have had uterine cancer

    • Have had certain types of breast cancer

    • Known or suspected estrogen-dependent cancer

    • Have had an allergic reaction to any ingredient in the formulation

Estradiol warnings

  • Tell any healthcare provider or other healthcare provider who treats you that you are using this medicine.

  • Your healthcare provider may need to do lab tests regularly to check on your progress and any effects of the medicine. Keep all appointments.

  • Tell your healthcare provider if you have:

    • Unusual vaginal bleeding

    • Kidney disease

    • Liver disease

    • Heart problems

    • A history of blood clot problems, including stroke

    • Bleeding disorders

    • Asthma

    • Diabetes

    • Migraines

    • Endometriosis

    • Lupus

    • Seizure disorders

    • High calcium levels

    • A history of seizures

    • A hereditary disorder that causes face and throat swelling (hereditary angioedema)

  • Tell the healthcare provider if you are:

    • Pregnant or think you’re pregnant

    • Breastfeeding

    • Going to have surgery

  • Estradiol hormone replacement treatment increases the risk of:

    • Uterine cancer (when used alone)

    • Heart attack, stroke, and other heart problems

    • Blood clots

    • Breast cancer

    • Dementia

    • Gallbladder disease

  • Estradiol can cause serious side effects, including:

    • High calcium

    • Vision changes

    • Liver problems

    • High blood pressure

    • High cholesterol and fats

    • High blood sugar

    • Underactive thyroid

    • Fluid retention

    • Enlargement of fibroids in the uterus

    • Worsening of asthma, diabetes, migraines, epilepsy, lupus, or porphyria

  • Vaginal rings can cause rare but serious problems such as:

    • Toxic shock syndrome

    • Attachment to the vaginal wall

    • Erosion of the vaginal lining

    • Ulcers of the vaginal lining

    • Bowel obstruction

    • Severe allergic reactions

  • If using topical estradiol, make sure other people and pets do not come into contact with the treated skin. It’s advisable to cover the treated area with clothing.

  • Topical estradiol may contain alcohol. Stay away from fire, flames, or other ignition sources until the gel or spray has dried.

  • Vaginal inserts can cause cuts and other abrasions on the vaginal lining. Talk to the healthcare provider if this becomes a problem.

Estradiol interactions

  • To avoid potentially hazardous drug interactions, tell the prescribing healthcare provider about all prescription drugs, over-the-counter medications, and vitamins or supplements you use before using estradiol.

  • Tell other healthcare providers you are using this medicine before they prescribe new medications.

  • Estradiol therapy can affect the results of many types of important blood tests.

Estradiol side effects

Serious side effects

Get emergency medical help right away if you notice any signs or symptoms of a possible serious side effect, including:

  • Unexplained vaginal bleeding 

  • Breast lumps (women and men)

  • Vision changes

  • Severe chest pain, shortness of breath

  • Numbness or weakness in your arm or leg, pain in your chest or leg (calf), weakness, fatigue

  • Sudden or severe headaches

  • Memory loss, confusion

  • Swelling in your hands, ankles, or feet

  • Blistering, peeling, red skin rash

  • Allergic reaction: Itching or hives, swelling in your face or hands, swelling or tingling in your mouth or throat, chest tightness, trouble breathing

Less serious side effects

  • Headache

  • Breast tenderness or pain

  • Abdominal cramps

  • Bloating

  • Nausea

  • Vomiting

  • Fluid retention

  • Irregular vaginal bleeding or spotting

  • Hair loss

  • Vaginal yeast infection

  • Skin redness or irritation at the application spot (topical estradiol or estradiol patches)

This is not a full list of side effects and others may occur. Consult your healthcare provider for more information, and find more detailed information about estradiol side effects here.

Medically reviewed by Karen BergerPharm.D.
Licensed Pharmacist

After receiving her doctorate from the University of Pittsburgh School of Pharmacy, Karen Berger, Pharm.D., has worked in both chain and independent community pharmacies. She currently works at an independent pharmacy in New Jersey. Dr. Berger enjoys helping patients understand medical conditions and medications—both in person as a pharmacist, and online as a medical writer and reviewer.

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