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Estradiol (hormone replacement therapy)

Know the basics|Know the precautions & warnings|Know the side effects|Know the interactions|Understand the dosage

Estradiol is a hormone naturally produced in the body. Synthetic forms of this hormone are used in hormone replacement therapies.

Know the basics

What is estradiol used for?

It is used by women to help reduce symptoms of menopause (such as hot flashes, vaginal dryness). These symptoms are caused by the body making less estrogen.

If you are using estradiol to treat symptoms only in and around the vagina, products applied directly inside the vagina should be considered before medications that are taken by mouth, absorbed through the skin, or injected.

Certain estrogen products may also be used by women after menopause to prevent bone loss (osteoporosis). However, there are other medications (such as raloxifene, bisphosphonates including alendronate) that are also effective in preventing bone loss and may be safer. These medications should be considered for use before estrogen treatment.

Certain estrogen products may also be used by men and women to treat cancers (certain types of prostate cancer, breast cancer that has spread to other parts of the body) and by women who are not able to produce enough estrogen (for example, due to hypogonadism, primary ovarian failure).

How should I take estradiol?

Take estradiol by mouth with or without food as directed by your doctor. You may take it with food or right after a meal to prevent stomach upset.

If you are taking the extended-release tablets, do not crush, chew, or dissolve them. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split extended-release tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.

If you are using a transdermal patch, do not cut it or touch the adhesive side. Place the patch on a clean, hairless area of skin. The best areas to place the patch is on the upper chest, upper outer arm, lower abdomen, and the hip. Shave the area if needed. Once the patch is used up, dispose of it properly by folding the adhesive side onto itself and throwing it in the trash or biological wastes container.

The dosage is based on your medical condition and response to treatment.

Take estradiol regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day as directed. Follow your dosing schedule carefully. Do not increase your dose or take estradiol more often or for a longer time than directed.

Tell your doctor if your condition does not improve or if it worsens.

How do I store estradiol?

Estradiol is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store estradiol in the bathroom or the freezer. There may be different brands of estradiol that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush estradiol down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Know the precautions & warnings

What should I know before using estradiol?

Before taking estradiol, inform your doctor if you are/have:

  • Allergic to any brand of oral estrogen, any other estrogen products, any other medications, or any of the ingredients in estrogen tablets. If you will be taking estradiol, tell your doctor and pharmacist if you are allergic to aspirin or tartrazine (a food color additive). Ask your pharmacist or check the manufacturer’s patient information for a list of the inactive ingredients in the brand of estrogen tablets you plan to take.
  • Taking prescription or nonprescription medications, vitamins, or nutritional supplements.
  • Pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking estrogen, call your doctor immediately.
  • Over the age of 65 years.
  • Other underlying conditions or comorbidites.

Is it safe to take estradiol during pregnancy or breast-feeding?

This drug is contraindicated (not allowed) during pregnancy. There is data that shows it can cause harm to a fetus.

Estradiol is pregnancy risk category X according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

If you become pregnant or plan to become pregnant, you should stop taking this drug. Consult with your doctor if you become pregnant or plan to become pregnant.

Know the side effects

What are the side effects of estradiol?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using estradiol and call your doctor at once if you have a serious side effect such as:

  • Unusual vaginal bleeding (especially if you are past menopause);
  • Chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;
  • Sudden numbness or weakness, especially on one side of the body;
  • Sudden severe headache, confusion, problems with vision, speech, or balance;
  • Stabbing chest pain, sudden cough, wheezing, rapid breathing, fast heart rate;
  • Pain, swelling, warmth, or redness in one or both legs;
  • Nausea, vomiting, loss of appetite, increased thirst, muscle weakness, confusion, and feeling tired or restless;
  • A lump in your breast;
  • Feeling like you might pass out;
  • Pain, swelling, or tenderness in your stomach;
  • Jaundice (yellowing of the skin or eyes).

Less serious side effects may include: mild nausea, vomiting, bloating, stomach cramps; breast pain, tenderness, or swelling; freckles or darkening of facial skin; loss of scalp hair; vaginal itching or discharge; changes in your menstrual periods, break-through bleeding.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Know the interactions

What drugs may interact with estradiol?

Estradiol may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval, especially: a blood thinner such as warfarin (Coumadin); cimetidine (Tagamet);; carbamazepine (Carbatrol, Tegretol); phenobarbital (Luminal, Solfoton);; phenytoin (Dilantin); rifampin (Rifadin, Rifater, Rifamate, Rimactane); or ritonavir (Norvir); St. John’s wort; an antibiotic such as clarithromycin (Biaxin) or erythromycin (E-Mycin, E.E.S., Erythrocin, Ery-Tab); or antifungal estradiol such as ketoconazole (Extina, Ketozole, Nizoral, Xolegal).

This list is not complete and other drugs may interact with estradiol. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Does food or alcohol interact with estradiol?

Estradiol may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Avoid taking this drug with alcohol or grapefruit juice as these can affect the efficacy of the drug and increase the chance of side effects. The risk of becoming pregnant may also increase. .Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with estradiol?

Estradiol may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Abnormal or unusual vaginal bleeding;
  • Blood clots (eg, deep vein thrombosis, pulmonary embolism), active or history of;
  • Breast cancer, known or suspected, or history of;
  • Heart attack, active or recent (within the past 12 months);
  • Liver disease;
  • Protein C or protein S deficiency, or other known blood clotting disorders;
  • Stroke, active or recent (within the past 12 months);
  • Surgery with a long period of inactivity;
  • Tumors (estrogen-dependent), known or suspected—Should not be used in patients with these conditions.
  • Asthma;
  • Cancer, history of;
  • Diabetes;
  • Edema (fluid retention or body swelling);
  • Endometriosis;
  • Epilepsy (seizures);
  • Gallbladder disease;
  • Heart disease;
  • Hereditary angioedema (swelling of the face, lips, tongue, or throat);
  • Hypercalcemia (high calcium in the blood);
  • Hypertension (high blood pressure);
  • Hypertriglyceridemia (high triglycerides or fats in the blood);
  • Hypocalcemia (low calcium in the blood), severe;
  • Hypothyroidism (an underactive thyroid);
  • Jaundice during pregnancy or from using hormonal therapy in the past;
  • Liver tumors;
  • Migraine headache;
  • Porphyria (an enzyme problem);
  • Systemic lupus erythematosus (SLE)—Use with caution. May make these conditions worse

Understand the dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using estradiol.

What is the dose for an adult?


  • Prostate cancer:For androgen-dependent, inoperable and progressing cancer: 10 mg three times a day, two times a day for at least 3 months.
  • Moderate to severe vasomotor symptoms associated with menopause: Adult: 1-2 mg/day adjusted as necessary; admin can be cyclical (3 weeks on, 1 week off) or continuous. In conjunction with a progestogen in women with uterus.
  • Prophylaxis of osteoporosis in postmenopausal women: Adult: 5 mg/day in cyclic regimen (23 days on and 5 days off).
  • Hypogonadism: Adult:1-2 mg/day in a cyclic regimen for 3 weeks on drug, followed by 1 week drug-free.


  • Prostate cancer: As valerate: ≥30 mg every 1-2 week.
  • Moderate to severe vasomotor symptoms associated withmenopause: As cypionate: 1-5 mg every 3-4 weeks; as valerate: 10-20 mg every 4 weeks. In conjunction with a progestogen in women with uterus.
  • Hypogonadism: As valerate: 10-20 mg every 4 weeks. As cypionate: 1.5-2 mg monthly;


  • Moderate to severe vasomotor symptoms associated with menopause: Each patch delivers 0.025 mg/day: Initially, apply once per week, adjust dose as necessary to control symptoms. Attempt to taper or discontinue treatment at 3-6 mth intervals. In conjunction with a progestogen in women with uterus.
  • Prophylaxis of osteoporosis in postmenopausal women: Each patch delivers 14 mcg/day. Apply patch once or twice per week. Adjust dose by monitoring biochemical markers and bone mineral density. A 14-day course of progestogen is required in women with an intact uterus once every 6-12 mth.


  • Vulvular and vaginal atrophy:Insert 2-4 g/day of vag cream intravaginally for 2 weeks, then reduce gradually to half the initial dose for 2 weeks followed by a maintenance dose of 1 g; 1-3 times/week.
  • Postmenopausal vaginal atrophy:Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days.
  • Urogenital symptoms:Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days.
  • Atrophic vaginitis: Initial: Insert 1 tab (20 mcg) once daily for 2 wk. Maintenance: Insert 1 tab twice weekly. Attempt to discontinue or taper estradiol at 3-6 monthly intervals.

What is the dose for a child?

The dosage has not been established in pediatric patients. It may be unsafe for your child. It is always important to fully understand the safety of the drug before using. Please consult with your doctor or pharmacist for more information.

How is estradiol available?

Estradiol is available in the following dosage forms and strengths:

  • Transdermal gel, topical: 600 mcg/g
  • Transdermal patch system, dermal: 0.025, 0.05, 0.075, 0.1 mg/day
  • Tablet, Oral: 35 mcg, 0.5 mg, 1 mg, 2 mg.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of estradiol, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.


Estradiol https://www.hormone.org/your-health-and-hormones/glands-and-hormones-a-to-z/hormones/estradiol Accessed June 14, 2021

Estradiol https://pubchem.ncbi.nlm.nih.gov/compound/Estradiol Accessed June 14, 2021

Estradiol (oral)  https://www.uofmhealth.org/health-library/d00537a1 Accessed June 14, 2021

EstradiolMenopause: Medicines to Help You https://www.fda.gov/consumers/free-publications-women/menopause-medicines-help-you Accessed June 14, 2021

Estradiol https://m.pdr.net/Mobile/Pages/drug-summary/Estradiol-estradiol-1966.1610 Accessed June 14, 2021

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Written by Stephanie Nicole Nera, RPh, PharmD Updated Jun 14