Estradiol Valerate

Last Reviewed: Nov 21, 2024

Drug Details


Generic Name:

Estradiol valerate

Common Brands:

Delestrogen

Availability:

Prescription only

Therapeutic Class:

Estrogen replacement therapy

Forms:

Injection solution

Administration:

By intramuscular injections

Therapeutic Uses:

  • Moderate to severe vasomotor symptoms of menopause in women, such as hot flashes and night sweats.
  • Moderate to severe symptoms of vaginal and vulvar atrophy in menopausal women, such as vaginal atrophy and vaginal dryness.
  • Hypoestrogenism due to hypogonadism, castration, or primary ovarian failure in women.
  • Palliative treatment of advanced androgen-dependent prostate cancer in men.

Controlled Status:

Not a controlled substance


Estradiol Valerate Drug Class

Estradiol valerate (ess-trah-dee-ohl vah-luh-rate) belongs to a group of medications called estrogens, which are a synthetic (lab-made) form of the hormone estrogen which the body makes naturally.

Estradiol Valerate Age Range

Estradiol valerate is approved for use in adult women and adult men with advanced prostate cancer that grows in response to androgens (sex steroids). This drug should not be used in children because its estrogenic effects can affect bone growth.

Uses


Estradiol Valerate Uses

Estrogen therapy with estradiol valerate is used to treat moderate to severe vasomotor symptoms, such as hot flashes and night sweats, in postmenopausal women. It is also used to treat moderate to severe symptoms of vulvar and vaginal atrophy, such as vaginal dryness and irritation, in postmenopausal women. In addition, estradiol valerate is prescribed to women with hypoestrogenism (low estrogen levels) or lack of natural estrogen production due to hypogonadism, castration, or primary ovarian failure. Estradiol valerate is also used for palliation of advanced androgen-dependent carcinoma of the prostate in men.

There may be other uses of estradiol valerate—your doctor or pharmacist can give you further drug information.

Estradiol Valerate Mechanism of Action

Estradiol valerate is a type of hormonal therapy that replaces natural estrogen in the body. Falling estrogen levels are responsible for symptoms in menopausal women. Estrogen therapy also replaces the hormone in women whose bodies do not make enough estrogen naturally. In men with advanced androgen-dependent carcinoma of the prostate, it provides palliative treatment by lowering androgen (male sex hormone) levels.

Estradiol Valerate Doses

Estradiol valerate is available as a 5 milliliter (mL) multi-dose vial of injection solution. It comes in strengths of 10 mg/mL, 20 mg/mL, and 40 mg/mL. It is given by intramuscular injections (injection into your buttock muscle) by a healthcare provider. 

The usual dose of estrogen therapy with estradiol valerate for menopausal symptoms like hot flashes and vaginal dryness, and hypoestrogenism (low estrogen levels) is 10 mg to 20 mg every 4 weeks. The usual dosage for advanced androgen-dependent prostate cancer in men is 30 mg or higher doses every 1-2 weeks.

Directions


How To Use Estradiol Valerate

Estradiol valerate (also spelled oestradiol valerate) comes in the form of an injection solution for intramuscular injection into your buttock muscle. Your healthcare provider will give you this long-acting injectable estrogen therapy in their office every 4 weeks for menopausal symptoms and low estrogen and every 1-2 weeks for advanced prostate cancer. 

In women who have a uterus, progestin is given with estradiol valerate to lower the risk of endometrial cancer. Women who do not have a uterus do not need to take the progestin.

Your doctor will prescribe the lowest dose of estradiol valerate for the shortest duration necessary to control your symptoms. They will reevaluate you every 3-6 months to assess whether you need to continue treatment. Ask your provider and read the patient information leaflet to understand the benefits versus risks of hormone replacement therapy with estradiol valerate.

Tell your doctor if you don’t notice an improvement in menopausal symptoms within 1-5 days of receiving estrogen treatment with estradiol valerate.

Missed dose: If you miss an appointment for your dose of estradiol valerate, call your doctor for further instructions.

Storage: Your healthcare provider will store the injection solution of estradiol valerate in their office.

Unused medicine: Your healthcare provider will dispose of unused or expired estradiol valerate appropriately. The best way to dispose of expired or unneeded medications that you take at home is through your local waste disposal company or a drug take-back program. Learn more about proper medication disposal

NOTEThis medication guide is a summary and may not contain all possible drug information on estradiol valerate. The information contained here may not be up-to-date. This sheet is for information purposes only. If you have questions about estradiol valerate, talk to your healthcare professionals for medical advice.


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Side Effects


Estradiol Valerate Side Effects

Possible side effects of estradiol valerate are listed below. Call your doctor for medical advice about side effects if they are severe or do not go away in a few days.

  • Breast tenderness or breast pain
  • Nausea
  • Vomiting
  • Stomach upset
  • Weight changes
  • Lightheadedness or dizziness
  • Anxiety, depression, or mood changes such as nervousness or irritability
  • Changes in libido (sexual desire)
  • Unwanted hair growth or hair loss
  • Dark spots on facial skin
  • Leg cramps
  • Vaginal itching, redness, burning, swelling, and irritation
  • Vaginal discharge
  • Problems with wearing contact lenses

Estradiol valerate can also cause more serious side effects. Call your doctor immediately or seek emergency medical care if you develop the following serious symptoms:

  • Skin rash, hives, itching, blistering
  • Swelling of the face, eyes, lips, tongue, throat, arms, hands, lower legs, ankles, or feet
  • Hoarseness
  • Trouble breathing or swallowing 
  • Bulging of the eyes
  • Stomach pain, tenderness, or swelling
  • Yellowing of the eyes or skin
  • Loss of appetite
  • Tiredness or weakness
  • Uncontrolled movements
  • Joint pain

The above list may not include all the potential adverse effects of estradiol valerate. Contact your healthcare professional if your side effects are unusual or severe or they do not get better over time. You can also report unusual side effects to the Food and Drug Administration at 1-800-FDA-1088.

Estradiol valerate Overdose: In case of symptoms of an overdose of estradiol valerate, call your doctor immediately. You can also call your local poison control center, provincial poison control center, or the national poison control center at 1-800-222-1222. If a person cannot be awakened, has trouble breathing, has collapsed, or has had a seizure, call 911. Signs and symptoms of an overdose may include stomach upset, vomiting, and vaginal bleeding.

Source: FDA


Warnings


Estradiol Valerate Risks, Warnings, and Complications


Estradiol valerate can cause serious adverse effects in certain high-risk individuals. Talk to your doctor about other treatment options for your condition if you are at a high risk of complications from this medication. Some of the risks of taking estradiol valerate include:

  • INCREASED RISK OF CERTAIN CANCERS: Estrogen therapy, including estradiol valerate, is associated with an increased risk of endometrial cancer (cancer of the lining of the uterus). If you have a uterus in place, your doctor will prescribe a progestin along with estradiol valerate to lower this risk. Tell your doctor without delay if you develop persistent or recurrent abnormal vaginal bleeding while on estrogen therapy.

    Estrogen replacement therapy is also linked to an increased risk of invasive breast cancer. Tell your doctor if you have a personal or family history of breast cancer before starting treatment. Talk to your provider about getting yearly breast examinations in your doctor’s office and mammograms (imaging studies of the breasts) for early detection of breast cancer. Seek immediate medical care for any breast changes such as a lump or bump, nipple discharge, or other breast changes. Breast tenderness and discomfort are, however, common side effects of estrogen treatment.

    Estradiol valerate and other estrogen therapies can increase the risk of ovarian cancer. Seek immediate medical care for fatigue, unexplained weight loss, any pain or swelling in the abdomen or pelvic area, urinary problems, or abnormal vaginal bleeding after menopause.

  • CARDIOVASCULAR RISKS: Hormonal therapy with estradiol valerate can increase cardiovascular risks, including the risk of myocardial infarction (heart attack), stroke, and blood clots (deep vein thrombosis (DVT) and pulmonary embolism (PE)). 

    To lower these risks, your healthcare provider will prescribe estradiol valerate with or without progestins at the lowest dose for the shortest time period necessary to control your symptoms. Talk to your doctor about lowering other risk factors of cardiovascular disease, such as smoking, obesity, high blood pressure, high blood glucose, and high cholesterol levels.

    Seek emergency medical help if you develop chest pain, trouble breathing, weakness on one side of the body, trouble speaking or walking, sudden severe headache, sudden vision changes, or leg pain or swelling.

  • RISK OF OTHER HEALTH PROBLEMS: Women treated with estrogen replacement therapy are at an increased risk of health problems such as dementia, gallbladder disease, hypercalcemia (high blood calcium levels) in patients with breast cancer that has spread to the bones, and vision abnormalities. Seek immediate medical care for any unusual symptoms.


Precautions Before Starting Estradiol Valerate

Tell your doctor if you have ever had an allergic reaction to estradiol valerate injection, oral estradiol valerate, other estrogen products, oral contraceptives, or any other drugs. Your pharmacy can give you a list of active and inactive ingredients in estradiol valerate injections.

Give your doctor or pharmacist a complete list of your other medications, including prescription drugs, nonprescription drugs, vitamins, supplements, and herbal products, especially St. John’s Wort. This can help avoid possible drug interactions between estradiol valerate and your other medications.

Give your doctor a complete medical history. Hormone replacement therapy with estradiol valerate may not be safe for people with certain medical conditions, such as jaundice (yellowing of the eyes or skin) after treatment with estrogen or during pregnancy, endometriosis, uterine fibroids, migraine, asthma, seizures, porphyria (a rare genetic disorder), high or low calcium levels, thyroid disorders, impaired liver function, kidney disease, pancreatic disease, gallbladder problems, cancer, heart disease, heart attack, stroke, or blood clots.

Tell your doctor if you are pregnant, could be pregnant, are planning a pregnancy, or are nursing an infant with breast milk.

Precautions During Use of Estradiol Valerate

Keep all your medical and lab appointments while taking estradiol valerate. Your healthcare provider will periodically review the need for continuing treatment with this drug every 3-6 months.

Tell your doctor if you become pregnant while on this medicine.

Tell all your healthcare providers and lab personnel that you are on estradiol valerate.

Estradiol Valerate Drug Interactions

Certain medicines can affect serum levels of estradiol valerate. This can affect how the medicine works and make it less effective. Concomitant use with certain medicines can increase the risk of severe adverse effects. Your doctor may change the doses of your medications, switch you to a different medicine, and/or monitor you carefully for adverse effects if there are known interactions between estradiol valerate and your other medicines.

The following medications can have possible interactions with estradiol valerate:

  • Anticonvulsants such as phenobarbital and carbamazepine
  • Tuberculosis medicines such as rifampin 
  • Antibiotics such as erythromycin and clarithromycin
  • Antifungal drugs such as ketoconazole and itraconazole
  • HIV medicines such as ritonavir 
  • St. John's Wort (Hypericum perforatum)
  • Grapefruit juice

The above list may not include all the possible interactions of estradiol valerate. Give your doctor or pharmacist a complete list of your medications, including prescription drugs, over-the-counter medicines, dietary supplements, and herbal remedies. Also, tell your healthcare provider if you smoke, drink alcohol, or use recreational drugs because some of these substances can cause serious health complications when used with prescription and over-the-counter medicines.

Pros & Cons


Estradiol Valerate Pros and Cons

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  • Estradiol valerate can relieve many symptoms in postmenopausal women, including hot flashes, night sweats, vaginal atrophy, vaginal dryness, and vaginal irritation.
  • You only need to take a single intramuscular injection of estradiol valerate once every 4 weeks.
  • There is a lower-cost generic available.

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  • You need to go to a doctor’s office for an estradiol valerate injection.
  • Hormone therapy with estradiol valerate is linked to an increased risk of blood clots, heart attack, and stroke.

Pharmacist Tips


Estradiol Valerate Tips from Pharmacists

  • Keep all your medical and laboratory appointments during estrogen therapy with estradiol valerate. Your doctor will reevaluate you every 3-6 months to assess whether you need to continue treatment.

  • Seek immediate medical help for chest pain, difficulty breathing, or sudden changes in the ability to walk or talk. These can be signs of a heart attack or stroke. 

  • Tell your healthcare provider without delay if you notice any breast lumps or develop abnormal vaginal bleeding while on this medicine.

Rx Savings Tips


Estradiol Valerate Rx Savings Tips

Estradiol valerate is a generic medication and is available at significantly lower prices than the brand name drug. Brand name Delestrogen and generic estradiol valerate contain the same medicine and are equally effective and safe. Like with most medications, the generic drug offers better value. A BuzzRx estradiol valerate coupon can result in big savings on the brand name and generic forms of the drug. With a BuzzRx discount card, savings card, or discount coupons, the medication could cost you a fraction of retail prices. Estradiol valerate may be under $102.50 for one vial of the 5 ml of 20 mg/ml dose at Walmart, Walgreens, Rite Aid, CVS Pharmacy, and other participating pharmacies with a BuzzRx discount card or free coupon. For the biggest discounts on estradiol valerate, give the checkout clerk your BuzzRx estradiol valerate discount coupon when you drop off your prescriptions at the pharmacy counter.


Lowest Price for Estradiol Valerate
Brand
$154.49
Generic
$102.00

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Common Questions


Common Questions about Estradiol Valerate


Can you get pregnant on estradiol valerate?

Yes, you can get pregnant on estradiol valerate. It is not a contraceptive. It is a type of hormone therapy to relieve menopausal symptoms. The American College of Obstetricians and Gynecologists does not advise hormone replacement therapy for women who are pregnant or planning to get pregnant.

Note: Oral estradiol valerate (an estrogen) and dienogest (a progestin) combination is available for oral administration (in pill form to take by mouth). It belongs to a group of birth control pills called combined oral contraceptives and is used to prevent pregnancy and control heavy menstrual bleeding.



Does estradiol valerate stop periods?

If you have had your uterus removed, you won’t have menstrual periods. If you have your uterus in place, your doctor will prescribe estradiol valerate injection along with progesterone to lower the risk of endometrial cancer. In this case, you may have no menstrual bleeding, irregular bleeding, or spotting (breakthrough bleeding).



Is estradiol valerate used during in vitro fertilization (IVF)?

Estradiol valerate may be used off-label during ovulation induction and IVF to thicken the uterine lining and prepare it for embryo transfer. It is not FDA approved for this purpose.



Is estradiol valerate used in gender-affirming hormone therapy?

Estradiol valerate injection may be used off-label in people undergoing gender-affirming feminizing hormone therapy. It is not FDA-approved for this purpose.



Do estradiol valerate injections hurt?

Most people report minor discomfort from an estrogen valerate injection. However, if you find the injections painful, you can ask your healthcare provider to use a numbing cream and/or take an over-the-counter pain reliever.



How long can you stay on estradiol valerate injection?

Because of the serious risks associated with hormone replacement therapy, your doctor will reevaluate you every 3-6 months to see if you need to continue treatment with estradiol valerate injection. If you only have local symptoms, such as vaginal dryness, your provider may recommend topical vaginal products.



What is the price of estradiol valerate without insurance?

Without insurance, estradiol valerate can be as high as $178.46, but with a free BuzzRx prescription discount coupon, you could pay as low as $102.00 for the most common version of this medication. Use the BuzzRx drug price look-up tool to find the lowest discounted price, and be sure to enter the correct dosage, form, and quantity for the most accurate pricing. While generics tend to have the best savings, you can also use your BuzzRx card and coupons to purchase brand-name versions. It never hurts to ask your pharmacist to try BuzzRx when filling or refilling any of your prescription drugs—whether you have insurance or not.



What is the price of estradiol valerate with insurance?

Ask your pharmacist or insurance provider for your copay price on estradiol valerate—Copay amounts vary depending on the type of insurance plan you have and if there is a deductible to reach before prescription drug coverage begins.

You could save up to 80% on your prescription medication with a free BuzzRx discount coupon for estradiol valerate. When using the BuzzRx lookup tool to find the price of your medicine, be sure to enter the correct dosage, form, and quantity to receive the most accurate discounted pricing. It never hurts to ask your pharmacist to try BuzzRx when filling or refilling any of your prescriptions—whether you have insurance or not.