What is/are Estrace Oral Tablets?
ESTRADIOL is an estrogen. It is mostly used as hormone replacement in menopausal women. It helps to treat hot flashes and prevent osteoporosis. It is also used to treat women with low estrogen levels or those who have had their ovaries removed. This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care providers before I take this medicine?
They need to know if you have or ever had any of these conditions:
- abnormal vaginal bleeding
- blood vessel disease or blood clots
- breast, cervical, endometrial, ovarian, liver, or uterine cancer
- gallbladder disease
- heart disease or recent heart attack
- high blood pressure
- high cholesterol
- high level of calcium in the blood
- kidney disease
- liver disease
- migraine headaches
- systemic lupus erythematosus (SLE)
- tobacco smoker
- an unusual or allergic reaction to estrogens, other hormones, medicines, foods, dyes, or preservatives
- pregnant or trying to get pregnant
How should I use this medicine?
Take this medicine by mouth. To reduce nausea, this medicine may be taken with food. Follow the directions on the prescription label. Take this medicine at the same time each day and in the order directed on the package. Do not take your medicine more often than directed.
Contact your pediatrician regarding the use of this medicine in children. Special care may be needed.
A patient information sheet will be given with each prescription and refill. Read this sheet carefully each time. The sheet may change frequently.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
Note: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What may interact with this medicine?
Do not take this medicine with any of the following:
- aromatase inhibitors like aminoglutethimide, anastrozole, exemestane, letrozole, testolactone
This medicine may also interact with the following:
- certain antibiotics used to treat infections
- certain barbiturates or benzodiazepines used for inducing sleep or treating seizures
- grapefruit juice
- medicines for fungus infections like itraconazole and ketoconazole
- raloxifene or tamoxifen
- rifabutin, rifampin, or rifapentine
- St. John's Wort
This list may not describe all possible interactions. Give your health care providers a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What side effects may I notice from this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
- allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
- breast tissue changes or discharge
- changes in vision
- chest pain
- confusion, trouble speaking or understanding
- dark urine
- general ill feeling or flu-like symptoms
- light-colored stools
- nausea, vomiting
- pain, swelling, warmth in the leg
- right upper belly pain
- severe headaches
- shortness of breath
- sudden numbness or weakness of the face, arm or leg
- trouble walking, dizziness, loss of balance or coordination
- unusual vaginal bleeding
- yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
- hair loss
- increased hunger or thirst
- increased urination
- symptoms of vaginal infection like itching, irritation or unusual discharge
- unusually weak or tired
This list may not describe all possible side effects.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. You will need a regular breast and pelvic exam and Pap smear while on this medicine. You should also discuss the need for regular mammograms with your health care professional, and follow his or her guidelines for these tests.
This medicine can make your body retain fluid, making your fingers, hands, or ankles swell. Your blood pressure can go up. Contact your doctor or health care professional if you feel you are retaining fluid.
If you have any reason to think you are pregnant, stop taking this medicine right away and contact your doctor or health care professional.
Smoking increases the risk of getting a blood clot or having a stroke while you are taking this medicine, especially if you are more than 35 years old. You are strongly advised not to smoke.
If you wear contact lenses and notice visual changes, or if the lenses begin to feel uncomfortable, consult your eye doctor or health care professional.
This medicine can increase the risk of developing a condition (endometrial hyperplasia) that may lead to cancer of the lining of the uterus. Taking progestins, another hormone drug, with this medicine lowers the risk of developing this condition. Therefore, if your uterus has not been removed (by a hysterectomy), your doctor may prescribe a progestin for you to take together with your estrogen. You should know, however, that taking estrogens with progestins may have additional health risks. You should discuss the use of estrogens and progestins with your health care professional to determine the benefits and risks for you.
If you are going to have surgery, you may need to stop taking this medicine. Consult your health care professional for advice before you schedule the surgery.
Where should I keep this medicine?
Keep out of the reach of children.
Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Keep container tightly closed. Protect from light. Throw away any unused medicine after the expiration date.
Mechanism of action
Estradiol enters cells freely and interacts with a cytoplasmic target cell receptor. After the estrogen receptor has bound its ligand, estradiol can enter the nucleus of the target cell, and regulate gene transcription, which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell.
Estradiol binds well to both estrogen receptors, ERα, and ERβ, in contrast to certain other estrogens, notably medications that preferentially act on one of these receptors. These medications are called selective estrogen receptor modulators, or SERMs.
Estradiol is the most potent naturally occurring estrogen.
Adverse effects, which may occur as a result of use of estradiol and have been associated with estrogen and/or progestin therapy, include changes in vaginal bleeding, dysmenorrhea, increase in size of uterine leiomyomata, vaginitis including vaginal candidiasis, changes in cervical secretion and cervical ectropion, ovarian cancer, endometrial hyperplasia, endometrial cancer, nipple discharge, galactorrhea, fibrocystic breast changes and breast cancer. Cardiovascular effects include chest pain, deep and superficial venous thrombosis, pulmonary embolism, thrombophlebitis, myocardial infarction, stroke, and increased blood pressure. Gastrointestinal effects include nausea and vomiting, abdominal cramps, bloating, diarrhea, dyspepsia, dysuria, gastritis, cholestatic jaundice, increased incidence of gallbladder disease, pancreatitis, or enlargement of hepatic hemangiomas. Skin adverse effects include chloasma or melasma that may continue despite discontinuation of the drug. Other effects on the skin include erythema multiforme, erythema nodosum, otitis media, hemorrhagic eruption, loss of scalp hair, hirsutism, pruritus, or rash. Adverse effects on the eyes include retinal vascular thrombosis, steepening of corneal curvature or intolerance to contact lenses. Adverse central nervous system effects include headache, migraine, dizziness, mental depression, chorea, nervousness/anxiety, mood disturbances, irritability, and worsening of epilepsy. Other adverse effects include changes in weight, reduced carbohydrate tolerance, worsening of porphyria, edema, arthralgias, bronchitis, leg cramps, hemorrhoids, changes in libido, urticaria, angioedema, anaphylactic reactions, syncope, toothache, tooth disorder, urinary incontinence, hypocalcemia, exacerbation of asthma, and increased triglycerides.
Estrogen combined with medroxyprogesterone is associated with an increased risk of dementia. It is not known whether estradiol taken alone is associated with an increased risk of dementia. Estrogens should only be used for the shortest possible time and at the lowest effective dose due to these risks. Attempts to gradually reduce the medication via a dose taper should be made every three to six months.
St John's wort, phenobarbital, carbamazepine and rifampicin decrease the levels of estrogens, such as estradiol, by speeding up its metabolism, whereas erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice may slow down metabolism, leading to increased levels in the blood plasma.
Estradiol should be avoided when there is undiagnosed abnormal genital bleeding, known, suspected or a history of breast cancer, current treatment for metastatic disease, known or suspected estrogen-dependent neoplasia, deep vein thrombosis, pulmonary embolism or history of these conditions, active or recent arterial thromboembolic disease such as stroke, myocardial infarction, liver dysfunction or disease. Estradiol should not be taken by people with a hypersensitivity/allergy or those who are pregnant or are suspected pregnancy.
This article uses material from the Wikipedia article Estradiol, which is released under the Creative Commons Attribution-Share-Alike License 3.0.