Estradiol (Page 4 of 5)
I. Geriatric Use
The safety and efficacy of estradiol tablets in geriatric patients has not been established. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greatest frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.
In the Women’s Health Initiative Memory Study, including 4,532 women 65 years of age and older, followed for an average of 4 years, 82% (n = 3,729) were 65 to 74 while 18% (n = 803) were 75 and over. Most women (80%) had no prior hormone therapy use. Women treated with conjugated estrogens plus medroxyprogesterone acetate were reported to have a two-fold increase in the risk of developing probable dementia. Alzheimer’s disease was the most common classification of probable dementia in both the conjugated estrogens plus medroxyprogesterone acetate group and the placebo group. Ninety percent of the cases of probable dementia occurred in the 54% of women that were older than 70. (See WARNINGS, Dementia.)
It is unknown whether these findings apply to estrogen alone therapy.
ADVERSE REACTIONS
See BOXED WARNINGS, WARNINGS , and PRECAUTIONS.
The following additional adverse reactions have been reported with estrogen and/or progestin therapy.
1. Genitourinary system
Changes in vaginal bleeding pattern and abnormal withdrawal bleeding or flow; breakthrough bleeding, spotting, dysmenorrhea
Increase in size of uterine leiomyomata
Vaginitis, including vaginal candidiasis
Change in amount of cervical secretion
Changes in cervical ectropion
Ovarian cancer; endometrial hyperplasia; endometrial cancer
2. Breasts
Tenderness, enlargement, pain, nipple discharge, galactorrhea; fibrocystic breast changes; breast cancer
3. Cardiovascular
Deep and superficial venous thrombosis; pulmonary embolism; thrombophlebitis; myocardial infarction; stroke; increase in blood pressure
4. Gastrointestinal
Nausea, vomiting
Abdominal cramps, bloating
Cholestatic jaundice
Increased incidence of gallbladder disease
Pancreatitis
Enlargement of hepatic hemangiomas
5. Skin
Chloasma or melasma that may persist when drug is discontinued
Erythema multiforme
Erythema nodosum
Hemorrhagic eruption
Loss of scalp hair
Hirsutism
Pruritus, rash
6. Eyes
Retinal vascular thrombosis
Steepening of corneal curvature
Intolerance to contact lenses
7. Central Nervous System
Headache, migraine, dizziness
Mental depression
Chorea
Nervousness, mood disturbances, irritability
Exacerbation of epilepsy
Dementia
8. Miscellaneous
Increase or decrease in weight
Reduced carbohydrate tolerance
Aggravation of porphyria
Edema
Arthralgias; leg cramps
Changes in libido
Urticaria
Angioedema
Anaphylactoid/anaphylactic reactions
Hypocalcemia
Exacerbation of asthma
Increased triglycerides
OVERDOSAGE
Serious ill effects have not been reported following acute ingestion of large doses of estrogen-containing oral contraceptives by young children. Overdosage of estrogen may cause nausea and vomiting, and withdrawal bleeding may occur in females.
DOSAGE AND ADMINISTRATION
When estrogen is prescribed for a postmenopausal woman with a uterus, a progestin should also be initiated to reduce the risk of endometrial cancer. A woman without a uterus does not need progestin. Use of estrogen, alone or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Patients should be reevaluated periodically as clinically appropriate (e.g., 3-month to 6-month intervals) to determine if treatment is still necessary (see BOXED WARNINGS and WARNINGS). For women who have a uterus, adequate diagnostic measures, such as endometrial sampling, when indicated, should be undertaken to rule out malignancy in cases of undiagnosed persistent or recurring abnormal vaginal bleeding.
Patients should be started at the lowest dose for the indication.
1. For treatment of moderate to severe vasomotor symptoms, vulval and vaginal atrophy associated with the menopause, the lowest dose and regimen that will control symptoms should be chosen and medication should be discontinued as promptly as possible.
Attempts to discontinue or taper medication should be made at 3-month to 6-month intervals. The usual initial dosage range is 1 to 2 mg daily of estradiol adjusted as necessary to control presenting symptoms. The minimal effective dose for maintenance therapy should be determined by titration. Administration should be cyclic (e.g., 3 weeks on and 1 week off).
2. For treatment of female hypoestrogenism due to hypogonadism, castration, or primary ovarian failure.
Treatment is usually initiated with a dose of 1 to 2 mg daily of estradiol, adjusted as necessary to control presenting symptoms; the minimal effective dose for maintenance therapy should be determined by titration.
3. For treatment of breast cancer, for palliation only, in appropriately selected women and men with metastatic disease.
Suggested dosage is 10 mg three times daily for a period of at least three months.
4. For treatment of advanced androgen-dependent carcinoma of the prostate, for palliation only.
Suggested dosage is 1 to 2 mg three times daily. The effectiveness of therapy can be judged by phosphatase determinations as well as by symptomatic improvement of the patient.
5. For prevention of osteoporosis.
When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should be considered only for women at significant risk of osteoporosis and for whom non-estrogen medications are not considered to be appropriate.
The lowest effective dose of estradiol has not been determined.
HOW SUPPLIED
Estradiol Tablets USP are available as:
| 1 mg: | Light purple, oval, flat-faced, beveled-edge, scored tablet. Debossed with 886 / 1 on the scored side and stylized b on the other side, Packaged in bottles of 30 (NDC 68788-8063-3) Packaged in bottles of 60 (NDC 68788-8063-6) Packaged in bottles of 90 (NDC 68788-8063-9) Packaged in bottles of 100 (NDC 68788-8063-1) |
Store at 20° to 25° C (68° to 77°F) [See USP Controlled Room Temperature].
Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).
KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN
Manufactured by:
TEVA PHARMACEUTICALS USA, INC.
North Wales, PA 19454
Distributed by:
Mayne Pharma
Greenville, NC 27834
Rev. B 5/2018
Repackaged By: Preferred Pharmaceuticals Inc.
PATIENT INFORMATION
Read this PATIENT INFORMATION before you start taking estradiol and read what you get each time you refill estradiol tablets. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.
|
WHAT IS THE MOST IMPORTANT INFORMATION I SHOULD KNOW ABOUT ESTRADIOL TABLETS (AN ESTROGEN HORMONE)?
Report any unusual vaginal bleeding right away while you are taking estrogens. Vaginal bleeding after menopause may be a warning sign of cancer of the uterus (womb). Your healthcare provider should check any unusual vaginal bleeding to find out the cause.
Using estrogens with or without progestins may increase your chances of getting heart attacks, strokes, breast cancer, and blood clots. Using estrogens with progestins may increase your risk of dementia. You and your healthcare provider should talk regularly about whether you still need treatment with estradiol tablets. |
WHAT IS ESTRADIOL TABLETS?
Estradiol is a medicine that contains estrogen hormones.
WHAT IS ESTRADIOL USED FOR?
Estradiol is used to:
- •
- reduce moderate to severe hot flashes
Estrogens are hormones made by a woman’s ovaries. Between ages 45 and 55, the ovaries normally stop making estrogens. This leads to a drop in body estrogen levels which causes the “change of life” or menopause (the end of monthly menstrual periods). Sometimes, both ovaries are removed during an operation before natural menopause takes place. The sudden drop in estrogen levels causes “surgical menopause.”
When the estrogen levels begin dropping, some women develop very uncomfortable symptoms, such as feelings of warmth in the face, neck, and chest, or sudden strong feelings of heat and sweating (“hot flashes” or “hot flushes”). In some women, the symptoms are mild, and they will not need estrogens. In other women, symptoms can be more severe. You and your healthcare provider should talk regularly about whether you still need treatment with estradiol.
Weight-bearing exercise, like walking or running, and taking calcium with vitamin D supplements may also lower your chances for getting postmenopausal osteoporosis. It is important to talk about exercise and supplements with your healthcare provider before starting them.
- •
- treat dryness , itching, and burning in or around the vagina, difficulty or burning on urination associated with menopause
You and your healthcare provider should talk regularly about whether you still need treatment with estradiol to control these problems. If you use estradiol only to treat your dryness, itching, and burning in and around your vagina, talk with your healthcare provider about whether a topical vaginal product would be better for you.
- •
- treat certain conditions in which a young woman’s ovaries do not produce enough estrogen naturally
- •
- treat certain types of abnormal vaginal bleeding due to hormonal imbalance when your doctor has found no serious cause of the bleeding
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- treat certain cancers in special situations, in men and women
- •
- prevent thinning of bones
Osteoporosis from menopause is a thinning of the bones that makes them weaker and easier to break. If you use estradiol only to prevent osteoporosis from menopause, talk with your healthcare provider about whether a different treatment or medicine without estrogens might be better for you. You and your healthcare provider should talk regularly about whether you should continue with estradiol.
WHO SHOULD NOT USE ESTRADIOL?
Do not start taking estradiol if you:
- •
- have unusual vaginal bleeding which has not been evaluated by your doctor (see BOXED WARNINGS)
Unusual vaginal bleeding can be a warning sign of cancer of the uterus, especially if it happens after menopause. Your doctor must find out the cause of the bleeding so that he or she can recommend the proper treatment. Taking estrogens without visiting your doctor can cause you serious harm if your vaginal bleeding is caused by cancer of the uterus.
- •
- currently have or have had certain cancers
Estrogens may increase the risk of certain types of cancer, including cancer of the breast or uterus. If you have or had cancer, talk with your healthcare provider about whether you should take estradiol.
(For certain patients with breast or prostate cancer, estrogens may help.)
- •
- had a stroke or heart attack in the past year
- •
- currently have or have had blood clots
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- have or have had liver problems
- •
- are allergic to estradiol tablets or any of its ingredients
See the end of this leaflet for a list of ingredients in Estradiol Tablets.
Estradiol Tablets USP 2 mg tablets contain tartrazine which may cause allergic-type reactions (including bronchial asthma) in certain susceptible individuals. Although the overall incidence of FD&C Yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity.
- •
- think you may be pregnant
Tell your healthcare provider:
- •
- if you are breast feeding
The hormone in estradiol can pass into your milk
- •
- about all of your medical problems
Your healthcare provider may need to check you more carefully if you have certain conditions, such as asthma (wheezing), epilepsy (seizures), migraine, endometriosis, lupus, problems with your heart, liver, thyroid, kidneys, or have high calcium levels in your blood.
- •
- about all the medicines you take
This includes prescription and nonprescription medicines, vitamins, and herbal supplements. Some medicines may affect how estradiol tablets work. Estradiol tablets may also affect how your other medicines work.
- •
- if you are going to have surgery or will be on bed rest
You may need to stop taking estrogens.
HOW SHOULD I TAKE ESTRADIOL?
1. Start at the lowest dose and talk to your healthcare provider about how well that dose is working for you.
2. Estrogens should be used at the lowest dose possible for your treatment only as long as needed. You and your healthcare provider should talk regularly (for example, every 3 to 6 months) about the dose you are taking and whether you still need treatment with estradiol.
WHAT ARE THE POSSIBLE SIDE EFFECTS OF ESTROGENS?
Less common but serious side effects include:
- •
- Breast cancer
- •
- Cancer of the uterus
- •
- Stroke
- •
- Heart attack
- •
- Blood clots
- •
- Dementia
- •
- Gallbladder disease
- •
- Ovarian cancer
These are some of the warning signs of the serious side effects:
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- Breast lumps
- •
- Unusual vaginal bleeding
- •
- Dizziness and faintness
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- Changes in speech
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- Severe headaches
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- Chest pain
- •
- Shortness of breath
- •
- Pains in your legs
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- Changes in vision
- •
- Vomiting
Call your healthcare provider right away if you get any of these warning signs, or any other unusual symptom that concerns you.
Common side effects include:
- •
- Headache
- •
- Breast pain
- •
- Irregular vaginal bleeding or spotting
- •
- Stomach/abdominal cramps, bloating
- •
- Nausea and vomiting
- •
- Hair loss
Other side effects include:
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- High blood pressure
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- Liver problems
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- High blood sugar
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- Fluid retention
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- Enlargement of benign tumors (“fibroids”) of the uterus
- •
- A spotty darkening of the skin, particularly on the face
- •
- Vaginal yeast infection
These are not all the possible side effects of estradiol tablets. For more information, ask your healthcare provider or pharmacist.
WHAT CAN I DO TO LOWER MY CHANCES OF A SERIOUS SIDE EFFECT WITH ESTRADIOL?
If you use estrogens, you can reduce your risks by doing these things:
- •
- Talk with your healthcare provider:
1. While you are using estrogens, it is important to visit your doctor at least once a year for a check-up.
2. If you have a uterus, talk to your healthcare provider about whether the addition of a progestin is right for you.
3. See your healthcare provider right away if you have vaginal bleeding while taking estradiol tablets.
4. Have a breast exam and mammogram (breast x-ray) every year unless your healthcare provider tells you something else. If members of your family have had breast cancer or if you have ever had breast lumps or an abnormal mammogram (breast x-ray), you may need to have more frequent breast examinations.
5. If you have high blood pressure, high cholesterol (fat in the blood), diabetes, are overweight, or if you use tobacco, you may have higher chances for getting heart disease. Ask your healthcare provider for ways to lower your chances for getting heart disease.
6. Talk with your healthcare provider regularly about whether you should continue taking estradiol tablets. You and your doctor should reevaluate whether or not you still need estrogens at least every six months.
- •
- Be alert for signs of trouble
If any of these warning signals (or any other unusual symptoms) happen while you are using estrogens, call your doctor immediately:
Abnormal bleeding from the vagina (possible uterine cancer)
Pains in the calves or chest, sudden shortness of breath, or coughing blood (possible clot in the legs, or lungs)
Severe headache or vomiting, dizziness, faintness, changes in vision or speech, weakness or numbness of an arm or leg (possible clot in the brain or eye)
Breast lumps (possible breast cancer; ask your doctor or health professional to show you how to examine your breasts monthly)
Yellowing of the skin or eyes (possible liver problem)
Pain, swelling, or tenderness in the abdomen (possible gallbladder problem)
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
GENERAL INFORMATION ABOUT SAFE AND EFFECTIVE USE OF ESTRADIOL
Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets.
Do not take estradiol for conditions for which it was not prescribed. Do not give estradiol to other people, even if they have the same symptoms you have. It may harm them.
KEEP ESTRADIOL OUT OF THE REACH OF CHILDREN
This leaflet provides a summary of the most important information about estradiol. If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about estradiol tablets that is written for health professionals. For more information about estradiol, please contact TEVA USA, PHARMACOVIGILANCE at 1-888-838-2872, X6351.
WHAT ARE THE INGREDIENTS IN ESTRADIOL TABLETS?
Inactive Ingredients: Colloidal silicon dioxide, corn starch, dibasic calcium phosphate, lactose monohydrate, magnesium stearate, and sodium starch glycolate. In addition, the 1 mg also contains FD&C blue no. 1 aluminum lake and D&C red no. 27 aluminum lake. The 2 mg also contains FD&C blue no. 1 aluminum lake and FD&C yellow no. 5 (tartrazine) aluminum lake.
Manufactured by:
TEVA PHARMACEUTICALS USA, INC.
North Wales, PA 19454
Distributed by:
Mayne Pharma
Greenville, NC 27834
Rev. A 1/2016
Repackaged By: Preferred Pharmaceuticals Inc.
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