Generic name: estradiol (injection) [ ESS-tra-DYE-ol ]
Brand names: Delestrogen, Depo-Estradiol
Dosage form: intramuscular solution (cypionate 5 mg/mL; valerate 10 mg/mL; valerate 20 mg/mL; valerate 40 mg/mL)
Drug class: Estrogens

Medically reviewed by Drugs.com on Mar 15, 2024. Written by Cerner Multum.

What is estradiol injection?

Estradiol injection is used to treat certain symptoms of menopause such as hot flashes and vaginal dryness, burning, or itching. It is also used to treat a lack of estrogen that is caused by ovarian failure or a condition called hypogonadism.

Some forms of estradiol injection are used in men to treat the symptoms of prostate cancer. Estradiol treats only the symptoms of prostate cancer but does not treat the cancer itself.

Estradiol injection may also be used for purposes not listed in this medication guide.

Estradiol injection side effects

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

Estradiol may cause serious side effects. Call your doctor at once if you have:

• heart attack symptoms--chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating;

• signs of a stroke--sudden numbness or weakness (especially on one side of the body), severe headache, slurred speech, problems with vision or balance;

• signs of a blood clot--sudden numbness or weakness on one side of the body, chest pain, problems with vision or speech, pain or swelling in one leg;

• high calcium levels--confusion, tiredness, nausea, vomiting, loss of appetite, constipation, increased thirst or urination, weight loss;

• swelling or tenderness in your stomach;

• jaundice (yellowing of the skin or eyes);

• memory problems, confusion, unusual behavior;

• shortness of breath;

• dizziness, or feeling light-headed;

• unusual vaginal bleeding, pelvic pain; or

• lump in your breast.

Common side effects of estradiol may include:

• changes in your menstrual periods, breakthrough bleeding;

• nausea, vomiting, bloating, stomach cramps;

• breast pain;

• headache; or

• hair loss.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Related/similar drugs

Botox, alendronate, finasteride, estradiol, oxybutynin, tamoxifen, Fosamax

Warnings

Estradiol may increase your risk of developing uterine cancer. Report any unusual vaginal bleeding right away.

Using estradiol can increase your risk of blood clots, stroke, heart attack, or cancer of the breast, uterus, or ovaries. Estrogens should not be used to prevent heart disease, stroke, or dementia.

Before taking this medicine

You should not use estradiol if you are allergic to it, or if you have:

• unusual vaginal bleeding;

• a history of heart attack, stroke, or blood clot;

• a history of hormone-related cancer, or cancer of the breast, uterus/cervix, or vagina; or

• liver disease.

Do not use estradiol if you are pregnant and tell your doctor right away if you become pregnant.

Ask a doctor if it is safe to breastfeed while using this medicine.

Using this medicine can increase your risk of blood clots, stroke, or heart attack, especially if you have high blood pressure, diabetes, high cholesterol, if you are overweight, or if you smoke.

Estradiol should not be used to prevent heart disease, stroke, or dementia. This medicine may actually increase your risk of developing these conditions.

Tell your doctor if you have or have ever had:

• asthma;

• epilepsy or other seizure disorder;

• diabetes;

• migraine headaches;

• endometriosis or uterine fibroid tumors;

• lupus;

• heart problems;

• hypertension;

• a thyroid disorder;

• high or low levels of calcium in your blood;

• gallbladder disease;

• porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);

• hereditary angioedema;

• kidney disease; or

• liver problems, or jaundice caused by pregnancy or taking hormones.

Long-term use of estradiol may increase your risk of cancer of the breast, uterus, or ovaries. Talk with your doctor about this risk.

Using this medicine can increase your risk of blood clots, stroke, or heart attack, especially if you have high blood pressure, diabetes, high cholesterol, if you are overweight, or if you smoke.

How is estradiol injection given?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

Estradiol is injected into a muscle, usually given once every 1 to 4 weeks, depending on the condition being treated. A healthcare provider may teach you how to properly use the medication by yourself.

Prepare an injection only when you are ready to give it. Call your pharmacist if the medicine looks cloudy, has changed colors or has particles in it.

Do not reuse a needle or syringe. Place them in a puncture-proof "sharps" container and dispose of it following state or local laws. Keep out of the reach of children and pets.

Estradiol may increase your risk of developing a condition that can lead to uterine cancer. To lower this risk, your doctor may also want you to take a progestin. Report any unusual vaginal bleeding right away.

If you need surgery or will be on long-term bed rest, tell the surgeon ahead of time that you are using estradiol. You may need to stop using the medicine for a short time.

Your doctor will need to check your progress on a regular basis. Self-examine your breasts for lumps on a monthly basis, and have regular mammograms while using estradiol.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Call your doctor for instructions if you miss an appointment for your estradiol injection.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while using estradiol injection?

Grapefruit may interact with estradiol and cause side effects. Avoid consuming grapefruit products.

What other drugs will affect estradiol injection?

Tell your doctor about all your current medicines. Many drugs can affect estradiol, especially:

• nefazodone;

• St. John's wort;

• an antibiotic--clarithromycin, rifabutin, rifampin, rifapentine, telithromycin;

• antifungal medicine--itraconazole, ketoconazole;

• antiviral medicine for HIV or hepatitis C--boceprevir, cobicistat, dasabuvir, elvitegravir, indinavir, lopinavir/ritonavir, nelfinavir, ombitasvir, paritaprevir saquinavir, telaprevir, tipranavir;

• cancer medicine--apalutamide, enzalutamide, mitotane;

• seizure medicine--carbamazepine, oxcarbazepine, phenytoin, primidone; or

• steroid medicine--dexamethasone, prednisone.

This list is not complete and many other drugs may affect estradiol. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

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