- What is estradiol, and how does it work (mechanism of action)?
- What brand names are available for estradiol?
- Is estradiol available as a generic drug?
- Do I need a prescription for estradiol?
- What are the side effects of estradiol?
- What is the dosage for estradiol?
- Which drugs or supplements interact with estradiol?
- Is estradiol safe to take if I'm pregnant or breastfeeding?
- What else should I know about estradiol?
What is estradiol, and how does it work (mechanism of action)?
Estrogen is one of the major female hormones, the other one being progesterone. Estrogens occur in nature in several chemical forms. In women with active menstrual cycles, the ovaries produce between 70 and 500 micrograms of estradiol daily. This is converted to estrone and to a lesser extent estriol. After menopause, estrone made in the adrenal glands, is the most active circulating estrogen. Estrogens cause growth and development of female sex organs and maintain sex characteristics, including underarm and pubic hair and the shape of body contours and skeleton. Estrogens also increase secretions from the cervix and growth of the inner lining of the uterus (endometrium). Estrogens reduce LDL-cholesterol ("bad" cholesterol) and increase HDL-cholesterol ("good" cholesterol) concentrations in the blood. Estrogens, when taken alone or in combination with a progestin (progesterone), have been shown to reduce the risk for hip fracture due to osteoporosis by 25%.
What brand names are available for estradiol?
Alora, Climara, Delestrogen, Depo-Estradiol, Divigel, Elestrin, Estrace, Estrasorb, Estrogel, Evamist, Femring, Menostar, Minivelle, Vivelle, Vivelle-Dot
What are the side effects of estradiol?
- Among the most common endocrine side effects are:
- Abdominal pain may indicate the development of gallstones or occasionally hepatitis.
- Migraine headaches have been associated with estrogen therapy.
- Estrogens can cause sodium and fluid retention leading to edema.
- Melasma, tan or brown patches, may develop on the forehead, cheeks, or temples. These may persist even after the estrogen is stopped.
- Conjugated estrogens may cause an increase in the curvature of the cornea. Patients with contact lenses may develop intolerance to their lenses.
- Blood clots are an occasional but serious adverse effect and are dose-related. (The higher the dose of estradiol, the more likely blood clots are to form.) Cigarette smokers are at a higher risk for clots, and, therefore, patients requiring estrogen therapy are strongly encouraged to quit smoking.
- Estrogens can increase the risk of endometrial cancer. This risk may be decreased if estrogens are combined with progestin.
- Some people also have a higher chance of developing breast cancer while taking estrogens. Sometimes people who have breast cancer when they are taking estrogens may have increased calcium in the blood. If this happens, the estrogen should be stopped.
What is the dosage for estradiol?
The dose of estradiol can vary depending on the condition that is being treated. Estradiol tablets are given daily or they can be prescribed to be taken in a cyclic regimen, wherein estradiol is given daily for 3 weeks followed by 1 week of no medication, after which the cycle resumes. The tablets can also be given more than once a day for some conditions. The topical gel or the topical emulsions are applied to the skin daily at the same time. The vaginal ring is inserted in the vagina and left without removal for 3 months at a time. The intramuscular dose and the frequency it is given can differ depending on the product.
The adhesive part of patches should be applied to a dry, hairless, clean part of the trunk, but not on the breasts. It should not be placed onto irritated or damaged skin. Sites of application should be rotated, with at least one week between repeated applications to any one site. The patch should be applied immediately after removing the protective layer, and pressure should be applied to the patch when it is attached for about 10 seconds.
Latest Menopause News
Daily Health News
Which drugs or supplements interact with estradiol?
Estrogens can inhibit the metabolism of cyclosporine, resulting in increased cyclosporine blood levels. Such increased blood levels can result in kidney and/or liver damage. If this combination cannot be avoided, cyclosporine concentrations can be monitored, and the dose of cyclosporine can be adjusted to assure that its blood levels are not elevated.
Estrogens appear to increase the risk of liver disease in patients receiving dantrolene through an unknown mechanism. Women over 35 years of age and those with a history of liver disease are especially at risk. Estrogens increase the liver's ability to manufacture clotting factors. Because of this, patients receiving warfarin (Coumadin) need to be monitored for loss of anticoagulant (blood thinning) effect if an estrogen is added when warfarin is already being taken.
Rifampin, barbiturates, carbamazepine (Tegretol), griseofulvin, phenytoin (Dilantin), primidone and St. John's wort preparations can all increase the elimination of estrogen by enhancing the liver's ability to metabolize it. Concurrent use may result in reduction of the beneficial effects of estrogens. On the other hand, drugs such as erythromycin, clarithromycin, ketoconazole (Nizoral, Extina, Xolegel, Kuric), itraconazole (Sporanox), ritonavir (Norvir) and grapefruit juice can decrease the liver's ability to metabolize and eliminate estrogens and may increase the side effects of estrogen.
Estrogens may increase the levels and effects of exogenous corticosteroids (corticosteroids used as drugs that are not produced by the body), ropinirole (Requip, Requip XL), tipranavir (Aptivus) and medications that contain theophylline (Elixophyllin, Theo-24, Theochron).
Estrogens may reduce the levels and the effects of anastrozole (Arimidex), aripiprazole (Abilify), axitinib (Inlyta), hyaluronidase (Amphadase, Hylenex, Vitrase), saxagliptin (Onglyza), somatropin (Genotropin, Humatrope, Norditropen Flexpro etc.), ibrutinib (Imbruvica), and ursodiol (Actigall, Urso 250, Urso Forte).
Estrogen levels and effects may be decreased by dabrafenib (Tafinlar), deferasirox (Exjade), peginterferon Alfa-2b (Peg-Intron, Peg-Intron Redipen, Peg-Intron Redipen Pak 4 and Sylatron), P-glycoprotein inducers, tocilizumab (Actemra) and herbs that belong to a class of medications called CYP3A4 inducers. herbs with contents similar to estrogens may increase the side effects of estrogens.
Estrogen levels and effects may be increased by dehydroepiandrosterone, P-glycoprotein inhibitors, nonsteroidal anti-inflammatory drugs called COX-2 inhibitors such as celecoxib (Celebrex) and ascorbic acid (vitamin C).
Is estradiol safe to take if I'm pregnant or breastfeeding?
Estrogens should not be used during pregnancy due to an increased risk of fetal abnormalities.
Estrogens are secreted in milk and cause unpredictable effects in the infant. Estrogens generally should not be used by women if they are breastfeeding.
What else should I know about estradiol?
What preparations of estradiol are available?
Estradiol is available in several forms.
- Tablets, micronized: 0.5mg, 1mg, 2mg;
- Vaginal cream: 0.01%;
- Continuous release skin patch: 14 mcg/day, 0.025 mg/day, 0.0375 mg/day, 0.05 mg/day, 0.1 mg/day, 0.06 mg/day, 0.075 mg/day;
- Topical emulsion: 4.35 mg/1.74 g; Topical Gel: 0.25 mg/0.25 g, 0.5 mg/0.5 g, 1 mg/g;
- Intramuscular oil: 5 mg/mL, 10 mg/mL, 20 mg/mL, 40 mg/mL; Vaginal Ring: 0.05 mg/24 hr, 0.1 mg/24 hr.
How should I keep estradiol stored?
All forms of estradiol should be stored between 15 C (59 F) and 30 C (86 F).
Estradiol (Alora; Climara; Delestrogen; Depo-Estradiol; Divigel; Elestrin; Estrace; Estrasorb; Estrogel; Evamist; Femring; Menostar; Minivelle; Vivelle; Vivelle-Dot) is a drug prescribed to treat the symptoms of menopause, prevention of bone fractures (osteoporosis), painful uterine bleeding, vaginal pain, dryness and atrophy associated with menopause. Estradiol is also prescribed for the treatment of breast cancer, and some cases of prostate cancer. Side effects, drug interactions, patient information, and dosage should be reviewed prior to taking this medication.
Multimedia: Slideshows, Images & Quizzes
Menopause & Perimenopause: Symptoms, Signs
What is menopause? What are the signs of menopause? What age does menopause start? Learn about menopause and perimenopause...
Women's Health: 25 Hormone Imbalance Symptoms and Signs
Hormone imbalance involves changes in estrogen, progesterone, and other hormone levels. Hormonal imbalance in women may cause...
What Is Osteoporosis? Treatment, Symptoms, Medication
Osteoporosis is a disease characterized by low bone mass and density. Osteoporosis causes symptoms of weak, thin, fragile bones....
Osteoporosis Super-Foods for Strong Bones With Pictures
What sweetener is loaded with calcium? These bone-building super foods can help stave off osteoporosis, and many of them will...
Menopause Quiz: Symptoms & Signs
The Menopause Quiz challenges your knowledge about the time in a woman’s life when menstruation ceases. Menopause can bring many...
Osteoporosis Quiz: What is Osteoporosis?
What are the causes, symptoms, and risk factors of osteoporosis? Quiz yourself about vitamin deficiency, maintaining bone...
Picture of Osteoporosis
Thinning of the bones with reduction in bone mass due to depletion of calcium and bone protein. See a picture of Osteoporosis and...
Picture of Osteoporosis Progression
Bone mass (bone density) is the amount of bone present in the skeletal structure. See a picture of Osteoporosis Progression and...
Women's Health: 10 Tips to Ease Menopause Symptoms
What happens during menopause? At what age do menopause symptoms start? Women in their 40s or 50s may begin to have hot flashes,...
Related Disease Conditions
Night sweats are severe hot flashes that occur at night and result in a drenching sweat. The causes of night sweats in most people are not serious, like menopause in women, sleep apnea, medications, alcohol withdrawal, and thyroid problems. However, more serious diseases like cancer and HIV also can cause night sweats. Your doctor will treat your night sweats depending upon the cause. You may experience other signs and symptoms that are associated with night sweats, which depend upon the cause, but may include, shaking, and chills with a fever caused by an infection like the flu or pneumonia; unexplained weight loss due to lymphoma; women in perimenopause or menopause may also have vaginal dryness, mood swings, and hot flashes during the day; and low blood sugar in people with diabetes. Other causes of night sweats include medications like NSAIDs (aspirin, acetaminophen, ibuprofen (Motrin, Advil), and naproxen (Aleve, Naprosyn), antidepressants, sildenafil (Viagra), and abuse of prescription or illegal drugs and drug withdrawal; hormone disorders like pheochromocytoma and carcinoid syndrome; idiopathic hyperhidrosis; infections like endocarditis, AIDs, and abscesses; alcoholism and alcohol withdrawal; drug abuse, addiction, and withdrawal; and stroke. A doctor or other health care professional can treat your night sweats after the cause has been diagnosed.
What Happens During Menopause?
Menopause is the time in a woman's life when menstrual periods permanently stop, also called the "change of life." Menopause symptoms and signs include hot flashes, night sweats, irregular vaginal bleeding, vaginal dryness, painful intercourse, urinary incontinence, weight gain, and emotional symptoms such as mood swings. Treatment of menopausal symptoms varies and should be discussed with your physician.
Normal vaginal bleeding (menorrhea) occurs through the process of menstruation. Abnormal vaginal bleeding in women who are ovulating regularly most commonly involves excessive, frequent, irregular, or decreased bleeding. Causes of abnormal may arise from a variety of conditions that may include, uterine fibroids, IUDs, hypothyroidism, hyperthyroidism, lupus, STDs, pelvic inflammatory disease, emotional stress, anorexia nervosa, polycystic ovary syndrome (PCOS), cancers, early pregnancy.
Vaginal Pain (Vulvodynia)
Vulvodynia or vaginal pain, genital pain is a condition in which women have chronic vulvar pain with no known cause. There are two types of vulvodynia, generalized vulvodynia, and vulvar vestibulitis. Researchers are trying to find the causes of vulvodynia, for example, nerve irritation, genetic factors, hypersensitivity to yeast infections, muscle spasms, and hormonal changes. The most common symptoms of vaginal pain (vulvodynia) are burning, rawness, itching, stinging, aching, soreness, and throbbing. There are a variety of treatments that can ease the symptoms of vulvodynia (vaginal pain).
Cholesterol (Lowering Your Cholesterol)
High cholesterol and triglyceride levels increase the risk of cardiovascular disease. Getting your cholesterol and triglyceride levels in an optimal range will help protect your heart and blood vessels. Cholesterol management may include lifestyle interventions (diet and exercise) as well as medications to get your total cholesterol, LDL, HDL, and triglycerides in an optimal range.
What Are the Benefits of Taking Estrogen?
Estrogen therapy, also known as hormone replacement therapy, is a treatment for alleviating the symptoms caused by menopausal transition. Estrogen therapy can alleviate symptoms like hot flashes, painful intercourse and bone loss.
Learn about osteoporosis, a condition characterized by the loss of bone density, which leads to an increased risk of bone fracture. Unless one experiences a fracture, a person may have osteoporosis for decades without knowing it. Treatment for osteoporosis may involve medications that stop bone loss and increase bone strength and bone formation, as well as quitting smoking, regular exercise, cutting back on alcohol intake, and eating a calcium- and vitamin D-rich balanced diet.
Hot flashes (or flushing) is the most common symptom experienced by a woman prior to and during the early stages of menopause, and often is described as the feeling of warmth that spreads over the body, often starting at the head accompanied by sweating. Symptoms of hot flashes include flushing, excessive sweating, anxiety, and palpitations.
Premature menopause is when menopause occurs in a woman before the age of 40. Causes of premature menopause include premature ovarian failure, treatments for cancer and other conditions, surgical removal of the ovaries, or chronic diseases of the pituitary or thyroid gland, or psychiatric disorders. Treatment is directed at menopausal symptoms.
Vaginal Dryness and Vaginal Atrophy
Vaginal dryness and vaginal atrophy occurs in women during perimenopause, menopause, and postmenopause. With vaginal atrophy, the lining of the vaginal wall becomes thinner, drier, less elastic, and light pink to bluish in color. Symptoms of vaginal atrophy include vaginal dryness, itching, irritation, and/or pain during intercourse. Treatment options for vaginal dryness and vaginal atrophy include hormone treatment and over-the-counter vaginal lubricating and moisturizing products.
Breast cancer is an invasive tumor that develops in the mammary gland. Breast cancer is detected via mammograms, breast self-examination (BSE), biopsy, and specialized testing on breast cancer tissue. Treatment of breast cancer may involve surgery, radiation, hormone therapy, chemotherapy, and targeted therapy. Breast cancer risk may be lowered by managing controllable risk factors. What you should know about breast cancer Breast cancer is the most common cancer among American women.One in every eight women in the United States develops breast cancer.There are many types of breast cancer that differ in their capability of spreading (metastasize) to other body tissues.The causes of breast cancer are unknown, although medical professionals have identified a number of risk factors.There are many different types of breast cancer.Breast cancer symptoms and signs includea lump in the breast or armpit,bloody nipple discharge,inverted nipple,orange-peel texture or dimpling of the breast's skin (peau d'orange),breast pain or sore nipple,swollen lymph nodes in the neck or armpit, anda change in the size or shape of the breast or nipple.Breast cancer can also be symptom free, which makes following national screening recommendations an important practice.Breast cancer is diagnosed during a physical exam, by a self-exam of the breasts, mammography, ultrasound testing, and biopsy.Treatment of breast cancer depends on the type of cancer and its stage (0-IV) and may involve surgery, radiation, or chemotherapy.
Natural Remedies for Hot Flashes
Hot flashes are experienced by many women, especially at night. However, not all women undergoing menopause experience hot flashes. What causes hot flashes? A hot flash is a feeling of warmth that spreads over the body. Treatment for hot flashes include hormone replacement therapy and alternative prescription medications such as: SSRIs (Effexor, Paxil, Prozac), clonidine (Catapres), megestrol (Megace), and gabapentin (Neurontin). Few natural remedies for hot flashes (for example phytoestrogens - isoflavones, black cohosh, and vitamin E) have been scientifically studied.
Sex and Menopause (What to Expect)
Menopause is often associated with a change in sexual functioning. Loss of estrogen, bladder control issues, anxiety, stress, health concerns, medications, and sleep disturbances often result in a decrease in libido. Though there are currently no good drugs for treating sexual problems in women, there are ways to increase intimacy with a partner and treat vaginal dryness.
Male menopause refers to the decline in testosterone production in men. As men age, they often experience many of the same symptoms that women experience in menopause. Testosterone replacement therapy may relieve some of these symptoms.
Sexual health information including birth control, impotence, herpes, sexually transmitted diseases, staying healthy, women's sexual health concerns, and men's sexual health concerns. Learn about the most common sexual conditions affecting men and women.
Treatment & Diagnosis
- Menopause FAQs
- Osteoporosis FAQs
- How To Reduce Your Medication Costs
- Pharmacy Visit, How To Get The Most Out of Your Visit
- Indications for Drugs: Approved vs. Non-approved
- Drugs: Buying Prescription Drugs Online Safely
- Drugs: The Most Common Medication Errors
- Medication Disposal
- Dangers of Mixing Medications
- What Are Hypercoagulable States?
- Generic Drugs, Are They as Good as Brand-Names?
Medications & Supplements
Prevention & Wellness
- AHA News: Estrogen Therapy in Early Menopause May Help Keep Arteries Clear
- Birth Control Pills Recalled Due to Danger of Unintended Pregnancy
- Obesity May Raise Girls' Risk of Asthma, Allergies
- Fat Near the Heart a Hazard for Postmenopausal Women
- More Evidence Menopause 'Brain Fog' Is Real
- Hormone Therapy Won't Help Memory After Menopause
- Illnesses, Deaths Spur FDA Warning on Hepatitis C Drugs
- Technivie Approved for Hepatitis C
- Hormone Therapy Doesn't Help Memory: Study
- Lead Exposure May Be Bigger Threat to Boys Than Girls
- Estrogen Receptor May Play a Role in Autism
- Losing Weight May Ease Hot Flashes, Study Finds
- 'Generally Reassuring' Findings on Fertility Drugs, Women's Cancers
- Antidepressant Eases Menopause-Related Symptoms, Study Finds
- Estrogen Won't Make Women Sharper After Menopause, Study Finds
- Study Compares Heart Risks for 2 Hormonal Regimens
- New Clues to How Exercise May Reduce Breast Cancer Risk
- New Method May Help Pinpoint Woman's Final Menstrual Period
- Blood Test May Help Define Breast Cancer Risk in Older Women
- Estrogen After Hysterectomy Lowers Cancer Risk?
- New Birth Control Pill Recall
- 1 Million Birth Control Pill Packs Recalled
- Tamoxifen May Cut Lung Cancer Deaths
- New Birth Control Pill Natazia Gets FDA Approval
- BPA Not Linked to Ill Effects in 2 Studies
Health Solutions From Our Sponsors
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
FDA Prescribing Information