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Estradiol is a form of estrogen, a female sex hormone that regulates many processes in the body. It is available as an oral tablet, a topical gel or patch, vaginal cream, or as an injection.
Estradiol is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent osteoporosis (bone loss) in menopausal women. Estradiol is also used to treat low estrogen levels in women with ovarian failure. It is also indicated to treat certain types of breast cancer and prostate cancer.
Estradiol may also be used for purposes not listed in this medication guide.
You should not use estradiol if you have: undiagnosed vaginal bleeding, liver disease, a bleeding disorder, or if you have ever had a heart attack, a stroke, a blood clot, or cancer of the breast, uterus/cervix, or vagina.
Do not use estradiol if you are pregnant.
Estradiol may increase your risk of developing uterine cancer. Report any unusual vaginal bleeding right away.
Using this medicine can increase your risk of blood clots, stroke, or heart attack, or cancer of the breast, uterus, or ovaries. Estradiol should not be used to prevent heart disease, stroke, or dementia.
Have regular physical exams and mammograms, and self-examine your breasts for lumps on a monthly basis while using this medicine.
You should not use this medicine if you are allergic to estradiol, or if you have:
unusual vaginal bleeding that has not been checked by a doctor;
liver disease;
a history of heart attack, stroke, or blood clot;
an increased risk of having blood clots due to a heart problem or a hereditary blood disorder; or
a history of hormone-related cancer, or cancer of the breast, uterus/cervix, or vagina.
Do not use estradiol if you are pregnant. Tell your doctor right away if you become pregnant during treatment.
Using this medicine can increase your risk of blood clots, stroke, or heart attack. You are even more at risk 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, because this medicine may actually increase your risk of developing these conditions.
To make sure this medicine is safe for you, tell your doctor if you have ever had:
heart disease;
liver problems, or prior jaundice caused by pregnancy or taking hormones;
kidney disease;
cancer;
gallbladder disease;
asthma;
epilepsy or other seizure disorder;
migraines;
lupus;
endometriosis or uterine fibroid tumors;
hereditary angioedema;
porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);
a thyroid disorder; or
high levels of calcium in your blood.
Using estradiol may increase your risk of cancer of the breast, uterus, or ovaries. Talk with your doctor about this risk.
Estradiol lowers the hormone needed to produce breast milk and can slow breast milk production. Tell your doctor if you are breast-feeding.
Take estradiol exactly as it was prescribed for you. Follow all directions on your prescription label. Do not take this medicine in larger amounts or for longer than recommended.
Estradiol may increase your risk of developing uterine cancer. To help lower this risk, your doctor may also want you to take a progestin. Report any unusual vaginal bleeding to your doctor immediately.
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 and have a mammogram every year while using estradiol.
If you need major surgery or will be on long-term 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 this medicine.
Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.
If you are taking injectable estrogen, dispose of any needles and syringes in an appropriate sharps container per your state laws. Do not throw away used needles into the garbage.
If you are using estradiol spray, avoid fire, flame, or smoking until the spray has dried. Do not apply lotion or sunscreen over the area for at least one hour.
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Overdose can result in nausea, vomiting and vaginal bleeding.
Avoid smoking. It can greatly increase your risk of blood clots, stroke, or heart attack while using this medicine.
Grapefruit and grapefruit juice may interact with estradiol and lead to unwanted side effects. Avoid the use of grapefruit products.
Get emergency medical help if you have signs of an allergic reaction to estradiol: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
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), sudden severe headache, slurred speech, problems with vision or balance;
signs of a blood clot - sudden vision loss, stabbing chest pain, feeling short of breath, coughing up blood, pain or warmth in one or both legs;
swelling or tenderness in your stomach;
jaundice (yellowing of the skin or eyes);
memory problems, confusion, unusual behavior;
unusual vaginal bleeding, pelvic pain;
a lump in your breast; or
nausea, vomiting, constipation, increased thirst or urination, muscle weakness, bone pain, lack of energy.
Common estradiol side effects may include:
nausea, vomiting, diarrhea, stomach cramps;
mood changes, sleep problems (insomnia);
cold symptoms such as stuffy nose, sinus pain, sore throat;
weight gain;
headache, back pain, dizziness;
breast pain;
darkening of the skin or skin rash;
thinning scalp hair; or
vaginal itching or discharge, changes in your menstrual periods, breakthrough bleeding.
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.
Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.
Many drugs can interact with estradiol. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all your current medicines and any medicine you start or stop using.
Further informationRemember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use estradiol only for the indication prescribed.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Medically reviewed by USARx EDITORIAL TEAM Last updated on 1/27/2021.
Source: Drugs.com Estradiol Valerate (www.drugs.com/estradiol.html).
Commonly reported side effects of estradiol include: cerebrovascular accident, infection, malignant neoplasm of breast, endometrium disease, headache, and mastalgia. Other side effects include: abdominal pain, limb pain, pruritus, sinusitis, nausea, skin rash, and vaginitis. See below for a comprehensive list of adverse effects.
For the ConsumerApplies to estradiol: vaginal capsule liquid filled, vaginal cream, vaginal insert extended release, vaginal tablet
Other dosage forms:
Vaginal route (Insert, Extended Release; Cream)
Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years of age or older has also been reported in women receiving estrogen alone or estrogen combined with progestins. Risks should be assumed to be similar for other doses, combinations, and dosage forms of estrogens and progestins. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible.
Vaginal route (Insert, Extended Release)
Use of unopposed estrogens increases the risk of endometrial cancer, while addition of a progestin decreases the risk of endometrial hyperplasia. Rule out malignancy if abnormal vaginal bleeding develops. Do not use estrogen alone or in combination with progestin to prevent cardiovascular disease or dementia. There is an increased risk of cardiovascular disorders (ie, DVT, pulmonary embolism, stroke, myocardial infarction) with combination therapy in women 50 years or older, and an increased risk of dementia in women 65 years or older with estrogen monotherapy or combination therapy. Combination therapy also increases the risk of invasive breast cancer. Prescribe estrogens with or without progestins at the lowest effective dose and for the shortest duration consistent with risks and treatment goals.
Along with its needed effects, estradiol may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur while taking estradiol:
Less common
Incidence not known
Get emergency help immediately if any of the following symptoms of overdose occur while taking estradiol:
Symptoms of overdose
Some side effects of estradiol may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common
Less common
Incidence not known
For Healthcare Professionals
Applies to estradiol: compounding powder, intramuscular solution, oral tablet, transdermal emulsion, transdermal film extended release, transdermal gel, transdermal spray, vaginal ring
GenitourinaryVery common (10% or more): Breast pain (29%)
Common (1% to 10%): Vulvovaginal pruritus, leukorrhea, vaginal hemorrhage, vaginal discharge, vaginal discomfort, menopause symptoms, breakthrough bleeding or spotting, dysmenorrhea, breast swelling, menorrhagia, metrorrhagia, endometrial hyperplasia
Uncommon (0.1% to 1%): Urinary problems
Rare (less than 0.1%): Galactorrhea
Postmarketing reports: Vaginal irritation, vaginal pain, genital pruritus, changes in bleeding pattern, pelvic pain, breast tenderness, vaginal ulceration, uterine fibroids
GastrointestinalVery common (10% or more): Abdominal pain (16%),
Common (1% to 10%): Flatulence, nausea, diarrhea
Uncommon (0.1% to 1%): Vomiting
Postmarketing reports: Abdominal distension
MusculoskeletalVery common (10% or more): Back pain (11%), arthralgia (11%)
Common (1% to 10%): Leg cramps
CardiovascularCommon (1% to 10%): Varicose veins, cardiac symptoms (e.g. palpitations)
Uncommon (0.1% to 1%): Hot flush, hypertension, venous thromboembolic disease
Rare (less than 0.1%): Arterial hypertension
Postmarketing reports: Deep vein thrombosis, changes in blood pressure
Nervous systemVery common (10% or more): Headache (18%)
Uncommon (0.1% to 1%): Vertigo, migraine
Rare (less than 0.1%): Aggravation of epilepsy
Postmarketing reports: Migraine aggravated, paresthesia, dizziness
OncologicUncommon (0.1% to 1%): Benign breast neoplasm, increased volume of uterine leiomyoma
Postmarketing reports: Endometrial cancer, breast cancer
OtherVery common (10% or more): Pain (11%)
Common (1% to 10%): Edema
Uncommon (0.1% to 1%): Weight increased, asthenia
Postmarketing reports: Drug ineffectiveness, blood estrogen increase, fatigue, exacerbation of hereditary angioedema
PsychiatricCommon (1% to 10%): Depression
Uncommon (0.1% to 1%): Sleep disorders, nervousness, mood swings
Rare (less than 0.1%): Change in libido
Postmarketing reports: Vaginismus, insomnia, anxiety, irritability
DermatologicCommon (1% to 10%): Pruritus
Uncommon (0.1% to 1%): Rash
Rare (less than 0.1%): Skin discoloration, acne
Postmarketing reports: Urticaria, erythematous or pruritic rash, alopecia, hyperhidrosis, night sweats, contact dermatitis, eczema
OcularUncommon (0.1% to 1%): Vision abnormal NOS
Postmarketing reports: Visual disturbances, contact lens intolerance
HepaticRare (less than 0.1%): Liver function tests abnormalities
Postmarketing reports: Cholestatic jaundice
MetabolicRare (less than 0.1%): Glucose intolerance
Postmarketing reports: Fluid retention
HypersensitivityRare (less than 0.1%): Anaphylactic reaction (with a past history of allergic reaction)
Postmarketing reports: Anaphylactic reactions, hypersensitivity
ImmunologicVery common (10% or more): Upper respiratory tract infection (17%)
Common (1% to 10%): Vulvovaginal mycotic infection, pharyngitis, rhinitis, sinusitis, moniliasis genital
Uncommon (0.1% to 1%): Vaginitis/vaginal candidosis
LocalCommon (1% to 10%): Skin irritation (topical gel)
Postmarketing reports: Application site reaction
Medically reviewed by USARx EDITORIAL TEAM Last updated on 1/27/2021.
Source: Drugs.com Estradiol Valerate (www.drugs.com/estradiol.html).
May 9, 2021
March 31, 2021
March 29, 2021
March 27, 2021
January 25, 2021
February 23, 2021
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