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estradiol (injection)

Pronunciation

Generic Name: estradiol (injection) (ESS tra DYE ol)
Brand Name: Depo-Estradiol

What is estradiol injection?

Estradiol is a form of estrogen, a female sex hormone that regulates many processes in the body.

Estradiol injection is used to treat certain symptoms of menopause such as hot flashes and vaginal dryness, burning, or irritation. 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 injection may also be used for purposes not listed in this medication guide.

What is the most important information I should know about estradiol injection?

You should not use estradiol if you have any of the following conditions: liver disease, a bleeding disorder, unusual vaginal bleeding, a history of breast or uterine cancer, or if you have ever had a heart attack, stroke, or a blood clot.

Do not use if you are pregnant.

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions. Long-term use may increase your risk of breast cancer, uterine cancer, heart attack, stroke, or blood clot.

Call your doctor at once if you have any unusual vaginal bleeding while using this medicine.

What should I discuss with my health care provider before using estradiol injection?

You should not use this medicine if you are allergic to estradiol, if you are pregnant, or if you have:

  • liver disease;

  • a bleeding or blood-clotting disorder;

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

  • unusual vaginal bleeding that a doctor has not checked; or

  • any type of breast, uterine, or hormone-dependent cancer.

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

To make sure estradiol is safe for you, tell your doctor if you have:

  • heart disease;

  • risk factors for coronary artery disease (such as diabetes, lupus, smoking, being overweight, having high blood pressure or high cholesterol, having a family history of coronary artery disease, or if you have had a hysterectomy);

  • hereditary angioedema (an immune system disorder);

  • a history of jaundice caused by pregnancy or birth control pills;

  • a thyroid disorder;

  • kidney disease;

  • asthma;

  • epilepsy or other seizure disorder;

  • migraines;

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

  • endometriosis or uterine fibroid tumors;

  • gallbladder disease; or

  • high or low levels of calcium in your blood.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Your doctor may prescribe a progestin to take while you are using estradiol, to help lower this risk. Report any unusual vaginal bleeding right away.

Long-term use of estradiol may increase your risk of breast cancer, heart attack, stroke, or blood clot. Talk with your doctor about your individual risks before using estradiol long term.

FDA pregnancy category X. Do not use estradiol if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use effective birth control while you are using this medicine.

Estradiol can pass into breast milk. This medication may slow breast milk production. Tell your doctor if you are breast-feeding a baby.

How should I use estradiol injection?

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Estradiol is injected into a muscle. You may be shown how to use injections at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles and syringes.

This medicine is usually given once every 2 to 4 weeks, depending on the condition being treated. Follow your doctor's instructions.

Prepare your dose only when you are ready to give an injection. Do not use if the medicine has changed colors or has particles in it. Call your pharmacist for new medicine.

Use a disposable needle only once. Follow any state or local laws about throwing away used needles and syringes. Use a puncture-proof "sharps" disposal container (ask your pharmacist where to get one and how to throw it away). Keep this container out of the reach of children and pets.

If you need surgery or medical tests or if you will be on bed rest, you may need to stop using this medicine for a short time. Any doctor or surgeon who treats you should know that you are using estradiol.

Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. Self-examine your breasts for lumps on a monthly basis 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 and grapefruit juice may interact with estradiol and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.

Estradiol injection side effects

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

Call your doctor at once if you have:

  • chest pain or heavy feeling, pain spreading to the jaw or shoulder, nausea, sweating, general ill feeling;

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

  • sudden cough, wheezing, rapid breathing, coughing up blood;

  • pain, swelling, warmth, or redness in one or both legs;

  • swelling or tenderness in your stomach;

  • jaundice (yellowing of the skin or eyes);

  • unusual vaginal bleeding;

  • a lump in your breast;

  • fluid retention (swelling, rapid weight gain);

  • high levels of calcium in your blood--numbness or tingly feeling around your mouth, fast or slow heart rate, muscle tightness or contraction, overactive reflexes; or

  • dangerously high blood pressure--severe headache, blurred vision, buzzing in your ears, anxiety, confusion, chest pain, shortness of breath, uneven heartbeats, seizure.

Common side effects may include:

  • breast pain;

  • headache;

  • vaginal itching or discharge, changes in your menstrual periods, light vaginal bleeding or spotting;

  • thinning scalp hair; or

  • nausea, vomiting, bloating, stomach cramps.

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.

See also: Side effects (in more detail)

Estradiol dosing information

Usual Adult Dose for Postmenopausal Symptoms:

Oral:
0.45 mg to 2 mg orally once a day.

Parenteral:
1 to 5 mg of estradiol cypionate IM every 3 to 4 weeks or 10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
0.05 mg/day (2 foil pouches of transdermal emulsion) applied topically to both legs each morning.
0.25 mg unit dose packet (0.1% transdermal gel) applied topically once daily to the upper right or left thigh at the same time daily.
1.25 g (one spray) EstroGel (0.75 mg/1.25 gm - 0.06% transdermal gel) applied topically to the arms at the same time daily.
1.53 mg (one spray) Evamist (1.53 mg/spray transdermal spray) applied topically to the forearm at the same time daily.
0.87 g (one spray) Elestrin (0.52 mg/1.087 g - 0.06% transdermal gel) applied topically to the upper arm at the same time daily.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

In general, the duration of hormone therapy for the treatment of postmenopausal symptoms should be limited. Treatment for one to five years is generally sufficient. However, long-term therapy (for the treatment/prophylaxis of osteoporosis and for risk reduction of cardiovascular disease) may be considered during the time in which the patient is being treated for postmenopausal symptoms.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.

Usual Adult Dose for Atrophic Urethritis:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
1.25 g/day (estradiol gel) applied topically at the same time daily. If used solely for the treatment of vulvar and vaginal atrophy, topical vaginal products should be considered.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
In general, the duration of hormone therapy for the treatment of postmenopausal symptoms like atrophic vaginitis, kraurosis vulvae, or atrophic urethritis should be limited. Treatment for one to five years is generally sufficient.

Usual Adult Dose for Atrophic Vaginitis:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate IM every 4 weeks.

Vaginal Ring:
0.05 mg/day or 0.1 mg/day vaginal ring. The ring should remain in place for 3 months and then be replaced by a new ring if therapy is to continue.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.
1.25 g/day (estradiol gel) applied topically at the same time daily. If used solely for the treatment of vulvar and vaginal atrophy, topical vaginal products should be considered.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Because of the potential increased risks of cardiovascular events, breast cancer and venous thromboembolic events, use should be limited to the shortest duration consistent with treatment goals and risks for the individual woman, and should be periodically reevaluated. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
In general, the duration of hormone therapy for the treatment of postmenopausal symptoms like atrophic vaginitis, kraurosis vulvae, or atrophic urethritis should be limited. Treatment for one to five years is generally sufficient.

Usual Adult Dose for Hypoestrogenism:

Oral:
1 to 2 mg orally once a day.

Parenteral:
1.5 to 2 mg of estradiol cypionate IM once a month or 10 to 20 mg estradiol valerate IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Dosages should be titrated according to patient response. Therapy should be maintained with the minimum dosage that will achieve the desired clinical effect.

Usual Adult Dose for Oophorectomy:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate by IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Usual Adult Dose for Primary Ovarian Failure:

Oral:
1 to 2 mg orally once a day.

Parenteral:
10 to 20 mg of estradiol valerate by IM every 4 weeks.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm. Systems should not be applied to the breasts.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

Usual Adult Dose for Breast Cancer--Palliative:

10 mg orally 3 times a day for at least 3 months. Estrogen therapy for breast cancer should be considered only for palliation in the treatment of metastatic disease in select patients

Usual Adult Dose for Osteoporosis:

Oral:
0.5 mg orally once a day.

Topical:
0.025 to 0.1 mg/day (transdermal film) applied topically 1 or 2 times a week. Systems should not be applied to the breasts.
14 mcg/day weekly (transdermal film) applied topically once a week.

Application sites vary according to manufacturer formulation and include the lower abdomen, upper thigh, buttocks, or upper arm.

In addition to hormonal therapy, adequate calcium intake is important for postmenopausal women who require treatment or prevention of osteoporosis. The average diet of older American women contains 400 to 600 mg of calcium per day. A suggested optimal intake is 1500 mg per day. If dietary intake is insufficient to achieve 1500 mg per day, supplementation may be useful in women who have no contraindication to calcium supplementation.

Long-term therapy (for more than 5 years) is generally necessary in order to obtain substantive benefits in reducing the risk of bone fracture. Maximal benefits are obtained if estrogen therapy is initiated as soon after menopause as possible. The optimal duration of therapy has not been definitively determined.

Women currently on oral estrogen therapy and changing to a transdermal estradiol system should initiate transdermal therapy 1 week following discontinuation of oral estrogens (sooner if menopausal symptoms reappear). Changes between transdermal systems may be initiated without interruption of therapy.

When used solely for the prevention of postmenopausal osteoporosis, approved non-estrogen treatments should carefully be considered, and estrogen and combined estrogen-progestin products should only be considered for women with significant risk of osteoporosis that outweighs the risks of the drug.

Usual Adult Dose for Prostate Cancer:

Oral:
1 to 2 mg orally 3 times a day.

Parenteral:
Estradiol valerate 30 mg IM every 1 to 2 weeks.

An apparent response should be noted within 3 months of initiation of therapy. Estrogen therapy for prostate cancer should be considered only for palliation in the treatment of metastatic disease in select patients.

What other drugs will affect estradiol injection?

Other drugs may interact with estradiol, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Where can I get more information?

  • Your pharmacist can provide more information about estradiol injection.
  • 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.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 3.02. Revision Date: 2014-11-26, 12:37:33 PM.

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