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Wednesday, 02 November 2011 08:48

Estrace Vaginal Cream


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Estrace Vaginal Cream Drug Description


ESTRACE® CREAM
(estradiol) Vaginal Cream, USP, 0.01%

ESTROGENS INCREASE THE RISK OF ENDOMETRIAL CANCER

Close clinical surveillance of all women taking estrogens is important. Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding. There is no evidence that the use of “natural” estrogens results in a different endometrial risk profile than synthetic estrogens at equivalent estrogen doses. (See WARNINGS, Malignant neoplasms, Endometrial cancer.)

CARDIOVASCULAR AND OTHER RISKS

Estrogens with or without progestins should not be used for the prevention of cardiovascular disease. (See WARNINGS, Cardiovascular disorders.)

The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) during 5 years of treatment with oral conjugated estrogens (CE 0.625 mg) combined with medroxyprogesterone acetate (MPA 2.5 mg) relative to placebo. (See CLINICAL PHARMACOLOGY, Clinical Studies.)

The Women's Health Initiative Memory Study (WHIMS), a substudy of WHI, reported increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with oral conjugated estrogens-plus-medroxyprogesterone acetate relative to placebo. It is unknown whether this finding applies to younger postmenopausal women or to women taking estrogen-alone therapy. (See CLINICAL PHARMACOLOGY, Clinical Studies.)

Other doses of oral conjugated estrogens with medroxyprogesterone acetate, and other combinations and dosage forms of estrogens and progestins were not studied in the WHI clinical trials and, in the absence of comparable data, these risks should be assumed to be similar. Because of these risks, estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.

DRUG DESCRIPTION

Each gram of ESTRACE® (estradiol vaginal cream, USP, 0.01%) contains 0.1 mg estradiol in a nonliquefying base containing purified water, propylene glycol, stearyl alcohol, white ceresin wax, mono- and di-glycerides, hypromellose 2208 (4000 cps), sodium lauryl sulfate, methylparaben, edetate di-sodium and tertiary-butylhydroquinone. Estradiol is chemically described as estra-1,3,5(10)-triene-3,17β-diol. It has an empirical formula of C18H24O2 and molecular weight of 272.37. The structural formula is:

 

ESTRACE® (estradiol) Structural Formula Illustration

 

What are the possible side effects of estradiol (Estrace Vaginal Cream, Estring)?

Estradiol increases the risk of developing a condition (endometrial hyperplasia) that may lead to cancer of the lining of the uterus. Taking progestins, another hormone drug, while using estradiol lowers the risk of developing this condition. Therefore, if your uterus has not been removed, your doctor may prescribe a progestin for you to take together while using estradiol. Visit your doctor regularly and report any unusual vaginal bleeding right away.

Treatment with estradiol long-term may increase the risk of stroke....

Read All Potential Side Effects and See Pictures of Estrace Vaginal Cream »

 

What are the precautions when taking estradiol vaginal cream (Estrace Vaginal Cream)?

Before using this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: vaginal bleeding of unknown cause, certain cancers (such as breast cancer, cancer of the uterus/ovaries), blood clots, stroke, heart disease (such as heart attack), liver disease, kidney disease, family medical history (especially breast lumps, cancer, blood clots, angioedema), blood clotting disorders (such as protein C or protein S deficiency), high blood pressure, diabetes, high cholesterol/triglyceride levels,...

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Indications & Dosage


INDICATIONS

ESTRACE (estradiol vaginal cream, USP, 0.01%) is indicated in the treatment of vulvar and vaginal atrophy.

DOSAGE AND ADMINISTRATION

Use of ESTRACE (estradiol vaginal cream, USP, 0.01%), alone or in combination with a progestin, should be limited to the shortest duration consistent with treatment goals and risks for the individual woman. Patients should reevaluate 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 treatment of vulvar 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. 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.

Attempts to discontinue or taper medication should be made at 3-month to 6-month intervals.

Usual Dosage: The usual dosage range is 2 to 4 g (marked on the applicator) daily for one or two weeks, then gradually reduced to one half initial dosage for a similar period. A maintenance dosage of 1 g, one to three times a week, may be used after restoration of the vaginal mucosa has been achieved.

NOTE: The number of doses per tube will vary with dosage requirements and patient handling.

HOW SUPPLIED

ESTRACE® (estradiol vaginal cream, USP, 0.01%).

N 0430-3754-14: Tube containing 1 ½ oz (42.5 g) with a calibrated plastic applicator for delivery of 1, 2, 3, or 4 g.

Store at room temperature. Protect from temperatures in excess of 40° C (104° F).

Keep ESTRACE Vaginal Cream (estradiol vaginal cream) out of the reach of children.

Manufactured by: Contract Pharmaceuticals Limited, Buffalo, NY 14213-1091 for Warner Chilcott (US), LLC, Rockaway, NJ 07866. Marketed by: Warner Chilcott (US), LLC Rockaway, NJ 07866 1-800-521-8813. Revised: August 2008.

 

Estrace Vaginal Cream


Estrace Vaginal Cream Side Effects & Drug Interactions


SIDE EFFECTS

See BOXED WARNINGS, WARNINGS and PRECAUTIONS.

Systemic absorption may occur with the use of ESTRACE (estradiol vaginal cream, USP, 0.01%). The warnings, precautions, and adverse reactions associated with oral estrogen treatment should be taken into account.

The following additional adverse reactions have been reported with estrogen and/or progestin therapy.

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; application site reactions of vulvovaginal discomfort including burning and irritation; genital pruritus; ovarian cancer; endometrial hyperplasia; endometrial cancer.

Breasts

Tenderness, enlargement, pain, nipple discharge, galactorrhea; fibrocystic breast changes; breast cancer.

Cardiovascular

Deep and superficial venous thrombosis; pulmonary embolism; thrombophlebitis; myocardial infarction; stroke; increase in blood pressure.

Gastrointestinal

Nausea, vomiting; abdominal cramps, bloating; cholestatic jaundice; increased incidence of gallbladder disease; pancreatitis, enlargement of hepatic hemangiomas.

Skin

Chloasma or melasma, that may persist when drug is discontinued; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism; pruritus, rash.

Eyes

Retinal vascular thrombosis, intolerance to contact lenses.

Central nervous system

Headache; migraine; dizziness; mental depression; chorea; nervousness; mood disturbances; irritability; exacerbation of epilepsy, dementia.

Miscellaneous

Increase or decrease in weight; reduced carbohydrate tolerance; aggravation of porphyria; edema; arthralgias; leg cramps; changes in libido; urticaria, angioedema, hypersensitivity, anaphylactoid/anaplylactic reactions; hypocalcemia; exacerbation of asthma; increased triglycerides.

DRUG INTERACTIONS

Drug/Laboratory Test Interactions

  1. Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, II-VII-X complex, and beta-thromboglobulin; decreased levels of anti-factor Xa and antithrombin III, decreased antithrombin III activity; increased levels of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.
  2. Increased thyroid-binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by protein-bound iodine (PBI), T4 levels (by column or by radioimmunoassay) or T3 levels by radioimmunoassay. Patients on thyroid replacement therapy may require higher doses of thyroid hormone. T3 resin uptake is decreased, reflecting the elevated TBG. Free T4 and free T3 concentrations are unaltered.
  3. Other binding proteins may be elevated in serum, i.e., corticosteroid binding globulin (CBG), sex hormone-binding globulin (SHBG), leading to increased circulating corticosteroids and sex steroids, respectively. Free or biologically active hormone concentrations are unchanged. Other plasma proteins may be increased (angiotensinogen/renin substrate, alpha-1-antitrypsin, ceruloplasmin).
  4. Increased plasma HDL and HDL2 subfraction concentrations, reduced LDL cholesterol concentration, increased triglycerides levels.
  5. Impaired glucose tolerance.
  6. Reduced response to metyrapone test.
  7. Reduced serum folate concentration.

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Warnings & Precautions


WARNINGS

See BOXED WARNINGS.

Systemic absorption may occur with the use of ESTRACE (estradiol vaginal cream, USP, 0.01%). The warnings, precautions, and adverse reactions associated with oral estrogen treatment should be taken into account.

Cardiovascular disorders

Estrogen and estrogen/progestin therapy has been associated with an increased risk of cardiovascular events such as myocardial infarction and stroke, as well as venous thrombosis and pulmonary embolism (venous thromboembolism or VTE). Should any of these occur or be suspected, estrogens should be discontinued immediately.

Risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus) should be managed appropriately.

Coronary heart disease and stroke

In the Women's Health Initiative (WHI) study, an increase in the number of myocardial infarctions and strokes has been observed in women receiving CE compared to placebo. These observations are preliminary, and the study is continuing. (See CLINICAL PHARMACOLOGY, Clinical Studies.)

In the CE/MPA substudy of WHI, an increased risk of coronary heart disease (CHD) events (defined as nonfatal myocardial infarction and CHD death) was observed in women receiving CE/MPA compared to women receiving placebo (37 vs 30 per 10,000 women-years). The increase in risk was observed in year one and persisted.

In the same substudy of WHI, an increased risk of stroke was observed in women receiving CE/MPA compared to women receiving placebo (29 vs 21 per 10,000 women-years). The increase in risk was observed after the first year and persisted.

In postmenopausal women with documented heart disease (n = 2,763, average age 66.7 years) a controlled clinical trial of secondary prevention of cardiovascular disease (Heart and Estrogen/Progestin Replacement Study; HERS) treatment with CE/MPA (0.625 mg/2.5 mg per day) demonstrated no cardiovascular benefit. During an average follow-up of 4.1 years, treatment with CE/MPA did not reduce the overall rate of CHD events in postmenopausal women with established coronary heart disease. There were more CHD events in the CE/MPA-treated group than in the placebo group in year 1, but not during the subsequent years. Two thousand three hundred and twenty one women from the original HERS trial agreed to participate in an open label extension of HERS, HERS II. Average follow-up in HERS II was an additional 2.7 years, for a total of 6.8 years overall. Rates of CHD events were comparable among women in the CE/MPA group and the placebo group in HERS, HERS II, and overall.

Large doses of estrogen (5 mg conjugated estrogens per day), comparable to those used to treat cancer of the prostate and breast, have been shown in a large prospective clinical trial in men to increase the risks of nonfatal myocardial infarction, pulmonary embolism, and thrombophlebitis.

Venous thromboembolism (VTE)

In the Women's Health Initiative (WHI) study, an increase in VTE has been observed in women receiving CE compared to placebo. These observations are preliminary, and the study is continuing. (See CLINICAL PHARMACOLOGY, Clinical Studies.)

In the CE/MPA substudy of WHI, a 2-fold greater rate of VTE, including deep venous thrombosis and pulmonary embolism, was observed in women receiving CE/MPA compared to women receiving placebo. The rate of VTE was 34 per 10,000 women-years in the CE/MPA group compared to 16 per 10,000 women-years in the placebo group.

The increase in VTE risk was observed during the first year and persisted.

If feasible, estrogens should be discontinued at least 4 to 6 weeks before surgery of the type associated with an increased risk of thromboembolism, or during periods of prolonged immobilization.

Malignant neoplasms

Endometrial cancer

The use of unopposed estrogens in women with intact uteri has been associated with an increased risk of endometrial cancer. The reported endometrial cancer risk among unopposed estrogen users is about 2- to 12-fold greater than in non-users, and appears dependent on duration of treatment and on estrogen dose. Most studies show no significant increased risk associated with use of estrogens for less than one year. The greatest risk appears associated with prolonged use, with increased risks of 15- to 24-fold for five to ten years or more and this risk has been shown to persist for at least 8 to 15 years after estrogen therapy is discontinued.

Clinical surveillance of all women taking estrogen/progestin combinations is important. Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding. There is no evidence that the use of natural estrogens results in a different endometrial risk profile than synthetic estrogens of equivalent estrogen dose. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer.

Breast cancer

The use of estrogens and progestins by postmenopausal women has been reported to increase the risk of breast cancer. The most important randomized clinical trial providing information about this issue is the Women's Health Initiative (WHI) substudy of CE/MPA (see CLINICAL PHARMACOLOGY, Clinical Studies). The results from observational studies are generally consistent with those of the WHI clinical trial and report no significant variation in the risk of breast cancer among different estrogens or progestins, doses, or routes of administration.

The CE/MPA substudy of WHI reported an increased risk of breast cancer in women who took CE/MPA for a mean follow-up of 5.6 years. Observational studies have also reported an increased risk for estrogen/progestin combination therapy, and a smaller increased risk for estrogen-alone therapy, after several years of use. In the WHI trial and from observational studies, the excess risk increased with duration of use. From observational studies, the risk appeared to return to baseline in about five years after stopping treatment. In addition, observational studies suggest that the risk of breast cancer was greater, and became apparent earlier, with estrogen/progestin combination therapy as compared to estrogen-alone therapy.

In the CE/MPA substudy, 26% of the women reported prior use of estrogen-alone and/or estrogen/progestin combination hormone therapy. After a mean follow-up of 5.6 years during the clinical trial, the overall relative risk of invasive breast cancer was 1.24 (95% confidence interval 1.01 - 1.54), and the overall absolute risk was 41 vs 33 cases per 10,000 women-years for CE/MPA compared with placebo. Among women who reported prior use of hormone therapy, the relative risk of invasive breast cancer was 1.86, and the absolute risk was 46 vs 25 cases per 10,000 women-years for CE/MPA compared with placebo. Among women who reported no prior use of hormone therapy, the relative risk of invasive breast cancer was 1.09, and the absolute risk was 40 vs 36 cases per 10,000 women-years for CE/MPA compared with placebo. In the same substudy, invasive breast cancers were larger and diagnosed at a more advanced stage in the CE/MPA group compared with the placebo group. Metastatic disease was rare with no apparent difference between the two groups. Other prognostic factors such as histologic subtype, grade and hormone receptor status did not differ between the groups.

The use of estrogen-plus-progestin has been reported to result in an increase in abnormal mammograms requiring further evaluation. All women should receive yearly breast examinations by a healthcare provider and perform monthly breast self-examinations. In addition, mammography examinations should be scheduled based on patient age, risk factors, and prior mammogram results.

Dementia

In the Women's Health Initiative Memory Study (WHIMS), 4,532 generally healthy postmenopausal women 65 years of age and older were studied, of whom 35% were 70 to 74 years of age and 18% were 75 or older. After an average follow-up of 4 years, 40 women being treated with CE/MPA (1.8%, n = 2,229) and 21 women in the placebo group (0.9%, n = 2,303) received diagnoses of probable dementia. The relative risk for CE/MPA versus placebo was 2.05 (95% confidence interval 1.21 – 3.48), and was similar for women with and without histories of menopausal hormone use before WHIMS. The absolute risk of probable dementia for CE/MPA versus placebo was 45 versus 22 cases per 10,000 women-years, and the absolute excess risk for CE/MPA was 23 cases per 10,000 women-years. It is unknown whether these findings apply to younger postmenopausal women. (See CLINICAL PHARMACOLOGY, Clinical Studies and PRECAUTIONS, Geriatric Use.)

It is unknown whether these findings apply to estrogen-alone therapy.

Gallbladder disease

A 2- to 4-fold increase in the risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens has been reported.

Hypercalcemia

Estrogen administration may lead to severe hypercalcemia in patients with breast cancer and bone metastases. If hypercalcemia occurs, use of the drug should be stopped and appropriate measures taken to reduce the serum calcium level.

Visual abnormalities

Retinal vascular thrombosis has been reported in patients receiving estrogens. Discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine. If examination reveals papilledema or retinal vascular lesions, estrogens should be permanently discontinued.

PRECAUTIONS

General

Addition of a progestin when a woman has not had a hysterectomy

Studies of the addition of a progestin for 10 or more days of a cycle of estrogen administration, or daily with estrogen in a continuous regimen, have reported a lowered incidence of endometrial hyperplasia than would be induced by estrogen treatment alone. Endometrial hyperplasia may be a precursor to endometrial cancer.

There are, however, possible risks that may be associated with the use of progestins with estrogens compared to estrogen-alone regimens. These include a possible increased risk of breast cancer.

Elevated blood pressure

In a small number of case reports, substantial increases in blood pressure have been attributed to idiosyncratic reactions to estrogens. In a large, randomized, placebo-controlled clinical trial, a generalized effect of estrogens on blood pressure was not seen. Blood pressure should be monitored at regular intervals with estrogen use.

Hypertriglyceridemia

In patients with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis and other complications.

Impaired liver function and past history of cholestatic jaundice

Estrogens may be poorly metabolized in patients with impaired liver function. For patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy, caution should be exercised and in the case of recurrence, medication should be discontinued.

Hypothyroidism

Estrogen administration leads to increased thyroid-binding globulin (TBG) levels. Patients with normal thyroid function can compensate for the increased TBG by making more thyroid hormone, thus maintaining free T4 and T3 serum concentrations in the normal range. Patients dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of their thyroid replacement therapy. These patients should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range.

Fluid retention

Because estrogens may cause some degree of fluid retention, patients with conditions that might be influenced by this factor, such as a cardiac or renal dysfunction, warrant careful observation when estrogens are prescribed.

Hypocalcemia

Estrogens should be used with caution in individuals with severe hypocalcemia.

Ovarian cancer

The CE/MPA substudy of WHI reported that estrogen-plus-progestin increased the risk of ovarian cancer. After an average follow-up of 5.6 years, the relative risk for ovarian cancer for CE/MPA versus placebo was 1.58 (95% confidence interval 0.77 – 3.24) but was not statistically significant. The absolute risk for CE/MPA versus placebo was 4.2 versus 2.7 cases per 10,000 women-years. In some epidemiologic studies, the use of estrogen alone, in particular for ten or more years, has been associated with an increased risk of ovarian cancer. Other epidemiologic studies have not found these associations.

Exacerbation of endometriosis

Endometriosis may be exacerbated with administration of estrogens. A few cases of malignant transformation of residual endometrial implants have been reported in women treated post-hysterectomy with estrogen-alone therapy. For patients known to have residual endometriosis post-hysterectomy, the addition of progestin should be considered.

Exacerbation of other conditions

Estrogens may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine or porphyria, systemic lupus erythematosus, and hepatic hemangiomas and should be used with caution in women with these conditions.

Patient Information

Physicians are advised to discuss the PATIENT INFORMATION leaflet with patients for whom they prescribe ESTRACE (estradiol vaginal cream, USP, 0.01%).

Laboratory Tests

Estrogen administration should be initiated at the lowest dose approved for the indication and then guided by clinical response rather than by serum hormone levels (e.g., estradiol, FSH).

Carcinogensis, Mutagenesis, And Impairment Of Fertility

Long-term continuous administration of estrogen, with and without progestin, in women with and without a uterus, has shown an increased risk of endometrial cancer, breast cancer, and ovarian cancer. (See BOXED WARNINGS, WARNINGS and PRECAUTIONS.)

Long-term continuous administration of natural and synthetic estrogens in certain animal species increases the frequency of carcinomas of the breast, uterus, cervix, vagina, testis, and liver.

Pregnancy

ESTRACE (estradiol vaginal cream, USP, 0.01%) should not be used during pregnancy. (See CONTRAINDICATIONS.)

Nursing Mothers

Estrogen administration to nursing mothers has been shown to decrease the quantity and quality of the milk. Detectable amounts of estrogens have been identified in the milk of mothers receiving this drug. Caution should be exercised when ESTRACE (estradiol vaginal cream, USP, 0.01%) is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Large and repeated doses of estrogen over an extended period of time have been shown to accelerate epiphyseal closure, resulting in short adult stature if treatment is initiated before the completion of physiologic puberty in normally developing children. In patients in whom bone growth is not complete, periodic monitoring of bone maturation and effects on epiphyseal centers is recommended.

Estrogen treatment of prepubertal children also induces premature breast development and vaginal cornification, and may potentially induce vaginal bleeding in girls. In boys, estrogen treatment may modify the normal pubertal process. All other physiological and adverse reactions shown to be associated with estrogen treatment of adults could potentially occur in the pediatric population, including thromboembolic disorders and growth stimulation of certain tumors. Therefore, estrogens should only be administered to pediatric patients when clearly indicated and the lowest effective dose should always be utilized.

Geriatric Use

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.)

There have not been sufficient numbers of geriatric patients involved in studies utilizing ESTRACE (estradiol vaginal cream, USP, 0.01%) to determine whether those over 65 years of age differ from younger subjects in their response to ESTRACE (estradiol vaginal cream, USP, 0.01%).

 

Estrace Vaginal Cream


Estrace Vaginal Cream Overdosage & Contraindications


OVERDOSE

Serious ill effects have not been reported following acute ingestion of large doses of estrogen-containing drug products by young children. Overdosage of estrogen may cause nausea and vomiting, and withdrawal bleeding may occur in females.

CONTRAINDICATIONS

ESTRACE (estradiol vaginal cream, USP, 0.01%) should not be used in women with any of the following conditions:

  1. Undiagnosed abnormalgenital bleeding.
  2. Known, suspected, or history of cancer of the breast.
  3. Known or suspected estrogen-dependent neoplasia.
  4. Active deep vein thrombosis, pulmonary embolism or history of these conditions.
  5. Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).
  6. Liverdysfunction or disease.
  7. 7 ESTRACE (estradiol vaginal cream, USP, 0.01%) should not be used in patients with known hypersensitivity to its ingredients.
  8. Known or suspected pregnancy. There is no indication for ESTRACE (estradiol vaginal cream, USP, 0.01%) in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy. (See PRECAUTIONS.)

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Clinical Pharmacology


CLINICAL PHARMACOLOGY

Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol at the receptor level.

The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. After menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.

Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. To date, two estrogen receptors have been identified. These vary in proportion from tissue to tissue.

Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.

Pharmacokinetics

Absorption

Estrogen drug products are absorbed through the skin, mucous membranes, and the gastrointestinal tract after release from the drug formulation.

Distribution

The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to sex hormone binding globulin (SHBG) and albumin.

Metabolism

Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.

Excretion

Estradiol, estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates.

Special Populations

No pharmacokinetic studies were conducted in special populations, including patients with renal or hepatic impairment.

Drug Interactions

In vitro and in vivo studies have shown that estrogens are metabolized partially by cytochrome P450 3A4 (CYP3A4). Therefore, inducers or inhibitors of CYP3A4 may affect estrogen drug metabolism. Inducers of CYP3A4 such as St. John's Wort preparations (Hypericum perforatum), phenobarbital, carbamazepine, and rifampin may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile. Inhibitors of CYP3A4 such as erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice may increase plasma concentrations of estrogens and may result in side effects.

Clinical Studies

Women's Health Initiative Studies

The Women's Health Initiative (WHI) enrolled a total of 27,000 predominantly healthy postmenopausal women to assess the risks and benefits of either the use of oral 0.625 mg conjugated estrogens (CE) per day alone or the use of oral 0.625 mg conjugated estrogens plus 2.5 mg medroxyprogesterone acetate (MPA) per day compared to placebo in the prevention of certain chronic diseases. The primary endpoint was the incidence of coronary heart disease (CHD) (nonfatal myocardial infarction and CHD death), with invasive breast cancer as the primary adverse outcome studied. A “global index” included the earliest occurrence of CHD, invasive breast cancer, stroke, pulmonary embolism (PE), endometrial cancer, colorectal cancer, hip fracture, or death due to other cause. The study did not evaluate the effects of CE or CE/MPA on menopausal symptoms.

The CE/MPA substudy was stopped early because, according to the predefined stopping rule, the increased risk of breast cancer and cardiovascular events exceeded the specified benefits included in the “global index”. Results of the CE/MPA substudy, which included 16,608 women (average age of 63 years, range 50 to 79; 83.9% White, 6.5% Black, 5.5% Hispanic), after an average follow-up of 5.2 years are presented in Table 1 below:

Table 1. RELATIVE AND ABSOLUTE RISK SEEN IN THE CE/MPA SUBSTUDY OF WHIa

Eventc Relative Risk CE/MPA vs placebo at 5.2 Years (95% CI*) Placebo
n = 8102
CE/MPA
n = 8506
Absolute Risk per 10,000 Women-years
CHD events 1.29 (1.02 - 1.63) 30 37
Non-fatal MI 1.32 (1.02 - 1.72) 23 30
CHD death 1.18 (0.70 - 1.97) 6 7
Invasive breast cancerb 1.26 (1.00 - 1.59) 30 38
Stroke 1.41 (1.07 - 1.85) 21 29
Pulmonary embolism 2.13 (1.39 - 3.25) 8 16
Colorectal cancer 0.63 (0.43 - 0.92) 16 10
Endometrial cancer 0.83 (0.47 - 1.47) 6 5
Hip fracture 0.66 (0.45 - 0.98) 15 10
Death due to causes other than the events above 0.92 (0.74 - 1.14) 40 37
Global Indexc 1.15 (1.03 - 1.28) 151 170
Deep vein thrombosisd 2.07 (1.49 - 2.87) 13 26
Vertebral fracturesd 0.66 (0.44 - 0.98) 15 9
Other osteoporotic fracturesd 0.77 (0.69 - 0.86) 170 131
a adapted from JAMA, 2002; 288:321-333
b includes metastatic and non-metastatic breast cancer with the exception of in situ breast cancer
c a subset of the events was combined in a “global index”, defined as the earliest occurrence of CHD events, invasive breast cancer, stroke, pulmonary embolism, endometrial cancer, colorectal cancer, hip fracture, or death due to other causes
d not included in Global Index
* nominal confidence intervals unadjusted for multiple looks and multiple comparisons

For those outcomes included in the "global index”, the absolute excess risks per 10,000 women-years in the group treated with CE/MPA were 7 more CHD events, 8 more strokes, 8 more PEs, and 8 more invasive breast cancers, while the absolute risk reductions per 10,000 women-years were 6 fewer colorectal cancers and 5 fewer hip fractures. The absolute excess risk of events included in the “global index” was 19 per 10,000 women-years. There was no difference between the groups in terms of all-cause mortality. (See BOXED WARNINGS, WARNINGS, and PRECAUTIONS.)

Women's Health Initiative Memory Study

The Women's Health Initiative Memory Study (WHIMS), a substudy of WHI, enrolled 4,532 predominantly healthy postmenopausal women 65 years of age and older (47% were age 65 to 69 years, 35% were 70 to 74 years, and 18% were 75 years of age and older) to evaluate the effects of CE/MPA (0.625 mg conjugated estrogens plus 2.5 mg medroxyprogesterone acetate) on the incidence of probable dementia (primary outcome) compared with placebo.

After an average follow-up of 4 years, 40 women in the estrogen/progestin group (45 per 10,000 women-years) and 21 in the placebo group (22 per 10,000 women-years) were diagnosed with probable dementia. The relative risk of probable dementia in the hormone therapy group was 2.05 (95% CI, 1.21 to 3.48) compared to placebo. Differences between groups became apparent in the first year of treatment. It is unknown whether these findings apply to younger postmenopausal women. (See BOXED WARNINGS and WARNINGS, Dementia.)

 

Estrace Vaginal Cream


Estrace Vaginal Cream Medication Guide


PATIENT INFORMATION

NOTE: The number of doses per tube will vary with dosage requirements and patient handling.

Read this PATIENT INFORMATION before you start using ESTRACE® Vaginal Cream and read what you get each time you refill ESTRACE Vaginal Cream (estradiol vaginal cream) . There may be new information. This information does not take the place of talking with your healthcare provider about your medical condition or your treatment.

WHAT IS THE MOST IMPORTANT INFORMATION I SHOULD KNOW ABOUT ESTRACE VAGINAL CREAM (AN ESTROGEN HORMONE)?

  • Estrogens increase the chances of getting cancer of the uterus.

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.

  • Do not use estrogens with or without progestins to prevent heart disease, heart attacks, or strokes.

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 ESTRACE Vaginal Cream (estradiol vaginal cream) .

What is ESTRACE Vaginal Cream (estradiol vaginal cream) ?

ESTRACE Vaginal Cream (estradiol vaginal cream) is a medicine that contains estrogen hormones.

What is ESTRACE Vaginal Cream (estradiol vaginal cream) used for?

ESTRACE Vaginal Cream (estradiol vaginal cream) is used to:

  • treat moderate to severe dryness, itching, and burning in and around the vagina due to menopause. You and your healthcare provider should talk regularly about whether you still need treatment with ESTRACE Vaginal Cream (estradiol vaginal cream) to control these problems.

Who should not use ESTRACE Vaginal Cream (estradiol vaginal cream) ?

Do not start using ESTRACE Vaginal Cream (estradiol vaginal cream) if you:

  • have unusual vaginal bleeding
  • currently have or have had certain cancers

Estrogens may increase the chances of getting certain types of cancers, including cancer of the breast or uterus. If you have or have had cancer, talk with your healthcare provider about whether you should use ESTRACE Vaginal Cream (estradiol vaginal cream) .

  • had a stroke or heart attack in the past year
  • currently have or have had blood clots
  • currently have or have had liver problems
  • are allergic to ESTRACE Vaginal Cream (estradiol vaginal cream) or any of its ingredients

See the end of this leaflet for a list of ingredients in ESTRACE Vaginal Cream (estradiol vaginal cream)

  • think you may be pregnant

Tell your healthcare provider:

  • if you are breastfeeding

The hormone in ESTRACE Vaginal Cream (estradiol vaginal cream) 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 ESTRACE Vaginal Cream (estradiol vaginal cream) works. ESTRACE Vaginal Cream (estradiol vaginal cream) 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 use ESTRACE Vaginal Cream (estradiol vaginal cream) ?

  1. Remove cap from tube. (There is no seal on tube)
  2. Do not separate plunger from applicator.
  3. Screw threaded end of applicator onto the opened tube until secure.
  4. Position upright in order to view the calibrated gram amounts.
  5. Gently squeeze tube from the bottom to expel the prescribed amount of ESTRACE Vaginal Cream into the applicator. As cream is squeezed out, plunger will rise to indicate amount of grams.
  6. Unscrew applicator from tube.
  7. Replace cap onto tube.
  8. Lie on back with knees drawn up. To deliver medication, gently insert applicator deeply into the vagina and press plunger downward to its original position.
  9. To cleanse applicator: Pull plunger to remove it from barrel. Wash with mild soap and warm water. DO NOT BOIL OR USE HOT WATER.

ESTRACE Vaginal Cream (estradiol vaginal cream) 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 ESTRACE Vaginal Cream (estradiol vaginal cream) .

What are the possible side effects of ESTRACE Vaginal Cream (estradiol vaginal cream) ?

Although ESTRACE Vaginal Cream (estradiol vaginal cream) is only used in and around the vagina, the risks associated with oral estrogens should be taken into account.

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 serious side effects:

  • Breast lumps
  • Unusual vaginal bleeding
  • Dizziness and faintness
  • Changes in speech
  • Severe headaches
  • Chest pain
  • Shortness of breath
  • Pains in your legs
  • 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 tenderness
  • Irregular vaginal bleeding or spotting
  • Stomach/abdominal cramps, bloating
  • Nausea and vomiting
  • Hair loss
  • Vaginal burning, irritation, and itching

Other side effects include:

  • High blood pressure
  • Liver problems
  • High blood sugar
  • Fluid retention
  • Enlargement of benign tumors of the uterus (“fibroids”)
  • Vaginal yeast infection
  • Allergic Reactions

These are not all the possible side effects of ESTRACE Vaginal Cream (estradiol vaginal cream) . For more information, ask your healthcare provider or pharmacist.

What can I do to lower my chances of a serious side effect with ESTRACE Vaginal Cream?

Talk with your healthcare provider regularly about whether you should continue using ESTRACE Vaginal Cream (estradiol vaginal cream) . See your healthcare provider right away if you get vaginal bleeding while using ESTRACE Vaginal Cream (estradiol vaginal cream) . 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, you may need to have breast exams more often. 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.

General information about safe and effective use of ESTRACE Vaginal Cream (estradiol vaginal cream)

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use ESTRACE Vaginal Cream (estradiol vaginal cream) for conditions for which it was not prescribed. Do not give ESTRACE Vaginal Cream (estradiol vaginal cream) to other people, even if they have the same symptoms you have. It may harm them.

Keep ESTRACE Vaginal Cream (estradiol vaginal cream) out of the reach of children.

This leaflet provides a summary of the most important information about ESTRACE Vaginal Cream (estradiol vaginal cream) . If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about ESTRACE Vaginal Cream (estradiol vaginal cream) that is written for health professionals. You can get more information by calling the toll free number 1-800-521-8813.

What are the ingredients in ESTRACE Vaginal Cream (estradiol vaginal cream) ?

Each gram of ESTRACE Vaginal Cream contains 0.1 mg estradiol in a nonliquefying base containing purified water, propylene glycol, stearyl alcohol, white ceresin wax, mono- and di-glycerides, hypromellose 2208 (4000 cps), sodium lauryl sulfate, methylparaben, edetate di-sodium and tertiary-butylhydroquinone.

 

Estrace Vaginal Cream


Estrace Vaginal Cream Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

ESTROGENS CREAM - VAGINAL

 

(ESS-trow-jens)

 

COMMON BRAND NAME(S): Premarin

 

WARNING: Estrogens, either used alone or with another hormone (progestin), have rarely caused very serious side effects. Discuss the risks and benefits of hormone treatment with your doctor. Estrogens should not be used to prevent heart disease or dementia.

Estrogens can increase the risk of cancer of the uterus (endometrial cancer). Taking a progestin as directed by your doctor can help decrease this risk. Tell your doctor right away if you have any unusual vaginal bleeding.

In postmenopausal women, estrogens can increase the risk of cancer of the ovaries, stroke, dementia, and serious blood clots in the legs. Estrogens alone do not appear to increase the risk of breast cancer when used for up to 7 years. Estrogen, when used with a progestin, can increase the risk of heart disease (such as heart attacks), stroke, serious blood clots in the lungs/legs, dementia, and cancer of the breast/ovaries.

The risk for serious side effects may depend on the dose of estrogen and the length of time it is used. Therefore, this medication should be used at the lowest effective dose and for the shortest amount of time. Discuss the use of this medication with your doctor and check with him/her regularly (for example, every 3 to 6 months) to see if you still need to use this medication. If you will be using this medication long-term, you should have regular complete physical exams (for example, once a year) as directed by your doctor. See also Notes section.

 

USES: This medication is a female hormone. It is used by women to help reduce vaginal symptoms of menopause (such as vaginal dryness/burning/itching). These symptoms are caused by the body making less estrogen. When treating only vaginal symptoms of menopause, products applied directly inside the vagina (such as this medication) should be used first. Estrogens that are taken by mouth, absorbed through the skin, or injected may have greater risks of side effects due to more estrogen being absorbed.

 

HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using this medication and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Use this medication as directed by your doctor. Fill the applicator with the medication according to the directions. Insert the applicator high into the vagina and press the plunger to release the medication. Clean the applicator with warm soapy water and rinse well. Do not boil or use hot water to clean the applicator.

The dosage is based on your medical condition and response to treatment.

Use this medication regularly to get the most benefit from it. Follow your dosing schedule carefully. Do not increase your dose or use this medication more often or for a longer time than directed.

Tell your doctor if your condition does not improve or if it worsens.

 

Estrace Vaginal Cream


Estrace Vaginal Cream Consumer (continued)

SIDE EFFECTS: See also Warning section.

Nausea/vomiting, bloating, breast tenderness, headache, or weight changes may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression, memory loss), breast lumps, unusual vaginal bleeding (such as spotting, breakthrough bleeding, prolonged/recurrent bleeding), increased or new vaginal irritation/itching/odor/discharge, severe stomach/abdominal pain, persistent nausea/vomiting, yellowing eyes/skin, dark urine, swelling hands/ankles/feet, increased thirst/urination.

This medication may rarely cause serious problems from blood clots (such as heart attacks, strokes, deep vein thrombosis, pulmonary embolism). Get medical help right away if you have any serious side effects, including: chest/jaw/left arm pain, unusual sweating, sudden/severe headache, weakness on one side of the body, confusion, slurred speech, sudden vision changes (such as partial/complete blindness), pain/redness/swelling of legs, tingling/weakness/numbness in the arms/legs, trouble breathing, coughing up blood, sudden dizziness/fainting.

A very serious allergic reaction to this product is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

PRECAUTIONS: Before using this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: vaginal bleeding of unknown cause, certain cancers (such as breast cancer, cancer of the uterus/ovaries), blood clots, stroke, heart disease (such as heart attack), liver disease, kidney disease, family medical history (especially breast lumps, cancer, blood clots, angioedema), blood clotting disorders (such as protein C or protein S deficiency), high blood pressure, diabetes, high cholesterol/triglyceride levels, obesity, lupus, underactive thyroid (hypothyroidism), mineral imbalance (low or high level of calcium in the blood), a certain hormone problem (hypoparathyroidism), uterus problems (such as fibroids, endometriosis), gallbladder disease, asthma, seizures, migraine headaches, mental/mood disorders (such as dementia, depression), certain blood disorder (porphyria).

Do not smoke or use tobacco. Estrogens combined with smoking further increases your risk of stroke, blood clots, high blood pressure, and heart attack, especially in women older than 35.

Tell your doctor if you just had or will be having surgery, or if you will be confined to a chair or bed for a long time (such as a long plane flight). These conditions increase your risk of getting blood clots, especially if you are using an estrogen product. You may need to stop this medication for a time or take special precautions.

This drug may cause blotchy, dark areas of the skin on the face (melasma). Sunlight may worsen this effect. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.

If you are nearsighted or wear contact lenses, you may develop vision problems or trouble wearing your contact lenses. Contact your eye doctor if these problems occur.

Some estrogen products contain mineral oil which can weaken rubber products such as latex condoms, cervical caps, and diaphragms and lead to their failure. Consult your pharmacist if you are unsure if your product contains mineral oil. If it does, talk to your doctor about other birth control products (such as polyurethane condoms) while you are using this medication.

This medication must not be used during pregnancy. If you become pregnant or think you may be pregnant, tell your doctor immediately.

This medication passes into breast milk. It may reduce the quality and amount of breast milk produced. Consult your doctor before breast-feeding.

 

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Consumer (continued)

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Some products that may interact with this drug include: aromatase inhibitors (such as anastrozole, exemestane, letrozole), fulvestrant, raloxifene, tamoxifen, toremifene.

This medication may interfere with certain laboratory tests (including metyrapone test), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

 

OVERDOSE: This medicine may be harmful if swallowed. If swallowing or overdose is suspected, contact a poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe nausea/vomiting, unusual vaginal bleeding.

 

NOTES: Do not share this medication with others.

Keep all regular medical and laboratory appointments. You should have regular complete physical exams (for example, once a year) which include laboratory and medical tests (such as blood pressure, breast exam/mammogram, pelvic exam, pap smear) to monitor your progress and check for side effects. Follow your doctor's instructions for examining your own breasts, and report any lumps right away. Consult your doctor for more details.

Preventing or controlling high blood pressure, high cholesterol, and diabetes can help to reduce your chances of heart disease and stroke. Lifestyle changes that can help to control or prevent these diseases include reducing stress, eating a low fat/salt diet, losing weight if overweight, exercising regularly, and stopping smoking. Keep your mind active with mental exercises (such as reading, solving crossword puzzles) to help prevent dementia. Talk to your doctor about lifestyle changes that might benefit you.

 

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

STORAGE: Store at room temperature. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

 

Estrace Vaginal Cream


Estrace Vaginal Cream Patient Information Including Side Effects

Brand Names: Estrace Vaginal Cream, Estring

Generic Name: estradiol (topical) (Pronunciation: ess tra DYE ole)

 

  • What is estradiol (Estrace Vaginal Cream)?
  • What are the possible side effects of estradiol (Estrace Vaginal Cream)?
  • What is the most important information I should know about estradiol (Estrace Vaginal Cream)?
  • What should I discuss with my healthcare provider before using estradiol (Estrace Vaginal Cream)?
  • How should I use estradiol (Estrace Vaginal Cream)?
  • What happens if I miss a dose (Estrace Vaginal Cream)?
  • What happens if I overdose (Estrace Vaginal Cream)?
  • What should I avoid while using estradiol (Estrace Vaginal Cream)?
  • What other drugs will affect estradiol (Estrace Vaginal Cream)?
  • Where can I get more information?

 

What is estradiol (Estrace Vaginal Cream)?

Estradiol (a form of estrogen) is a female sex hormone necessary for many processes in the body. Estradiol vaginal products release estrogen that is absorbed directly through the skin of the vaginal wall.

Estradiol topical is used to treat certain symptoms of menopause such as dryness, burning, and itching of the vaginal area and urgency or irritation with urination.

Estradiol may also be used for purposes other than those listed in this medication guide.

What are the possible side effects of estradiol (Estrace Vaginal Cream)?

Estradiol increases the risk of developing a condition (endometrial hyperplasia) that may lead to cancer of the lining of the uterus. Taking progestins, another hormone drug, while using estradiol lowers the risk of developing this condition. Therefore, if your uterus has not been removed, your doctor may prescribe a progestin for you to take together while using estradiol. Visit your doctor regularly and report any unusual vaginal bleeding right away.

Treatment with estradiol long-term may increase the risk of stroke. Because of this risk, you should contact your doctor or healthcare provider to discuss your individual risks and benefits before taking estradiol long-term. You should also talk to your doctor or healthcare provider on a regular basis (for example, every 3-6 months) about whether you should continue this treatment.

If you experience any of the following serious side effects, stop using estradiol and seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives);
  • shortness or breath or pain in the chest;
  • a painful, red, swollen leg;
  • abnormal vaginal bleeding;
  • pain, swelling, or tenderness in the abdomen;
  • severe headache or vomiting, dizziness, faintness or changes in vision or speech;
  • yellowing of the skin or eyes; or
  • a lump in a breast.

Other, less serious side effects may be more likely to occur. Continue to use estradiol and talk to your doctor if you experience

  • decreased appetite, nausea, or vomiting;
  • swollen breasts;
  • acne or skin color changes;
  • decreased sex drive;
  • migraine headaches or dizziness;
  • vaginal pain, dryness, or discomfort;
  • water retention (swollen hands, feet, or ankles);
  • depression; or
  • changes in your menstrual cycle or break-through bleeding.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

What is the most important information I should know about estradiol (Estrace Vaginal Cream)?

Estradiol increases the risk of developing a condition (endometrial hyperplasia) that may lead to cancer of the lining of the uterus. Taking progestins, another hormone drug, while using estradiol lowers the risk of developing this condition. Therefore, if your uterus has not been removed, your doctor may prescribe a progestin for you to take together while using estradiol. Visit your doctor regularly and report any unusual vaginal bleeding right away.

Treatment with estradiol long-term may increase the risk of stroke. Because of this risk, you should contact your doctor or healthcare provider to discuss your individual risks and benefits before taking estradiol long-term. You should also talk to your doctor or healthcare provider on a regular basis (for example, every 3-6 months) about whether you should continue this treatment.

Have yearly physical exams and examine your breasts for lumps on a monthly basis while using estradiol.

Do not use this medication if you are pregnant.

The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5 years of treatment with oral conjugated estrogens combined with medroxyprogesterone acetate.

The Women's Health Initiative Memory Study (WHIMS) found that postmenopausal women 65 years of age or older who were treated with oral conjugated estrogens plus medroxyprogesterone acetate had an increased risk of developing dementia. It is unknown whether this finding applies to younger postmenopausal women or to women using estrogen only therapy.

Related Drug Centers
  • Estrace Vaginal Cream
  • Estring

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Patient Information including How Should I Take

In this Article

  • What is estradiol (Estrace Vaginal Cream)?
  • What are the possible side effects of estradiol (Estrace Vaginal Cream)?
  • What is the most important information I should know about estradiol (Estrace Vaginal Cream)?
  • What should I discuss with my healthcare provider before using estradiol (Estrace Vaginal Cream)?
  • How should I use estradiol (Estrace Vaginal Cream)?
  • What happens if I miss a dose (Estrace Vaginal Cream)?
  • What happens if I overdose (Estrace Vaginal Cream)?
  • What should I avoid while using estradiol (Estrace Vaginal Cream)?
  • What other drugs will affect estradiol (Estrace Vaginal Cream)?
  • Where can I get more information?

What should I discuss with my healthcare provider before using estradiol (Estrace Vaginal Cream)?

Do not use estradiol without first talking to your doctor if you have

  • a circulation, bleeding, or blood-clotting disorder;
  • undiagnosed, abnormal vaginal bleeding; or
  • any type of breast, uterine, or hormone-dependent cancer.

Using estradiol may be dangerous in some cases if you have any of the conditions listed above.

Before using estradiol, tell your doctor if you have

  • high blood pressure, angina, or heart disease;
  • high levels of cholesterol or triglycerides in your blood;
  • liver disease;
  • kidney disease;
  • asthma;
  • epilepsy;
  • migraines;
  • diabetes;
  • depression;
  • gallbladder disease;
  • uterine fibroids;
  • had a hysterectomy (uterus removed);
  • a narrow, short, or prolapsed vagina;
  • vaginal irritation; or
  • a vaginal infection.

You may not be able to use estradiol, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Treatment with estradiol long-term may increase the risk of stroke. Because of this risk, you should contact your doctor or healthcare provider to discuss your individual risks and benefits before taking estradiol long-term. You should also talk to your doctor or healthcare provider on a regular basis (for example, every 3-6 months) about whether you should continue this treatment.

The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5 years of treatment with oral conjugated estrogens combined with medroxyprogesterone acetate.

The Women's Health Initiative Memory Study (WHIMS) found that postmenopausal women 65 years of age or older who were treated with oral conjugated estrogens plus medroxyprogesterone acetate had an increased risk of developing dementia. It is unknown whether this finding applies to younger postmenopausal women or to women using estrogen only therapy.

Estradiol is in the FDA pregnancy category X. This means that estradiol will cause birth defects in an unborn baby. Do not use estradiol if you are pregnant or are planning a pregnancy.

Estradiol may decrease milk flow and have other effects on milk composition. Do not use estradiol without first talking to your doctor if you are breast-feeding a baby.

How should I use estradiol (Estrace Vaginal Cream)?

Use estradiol exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

To use the Estring vaginal ring:

  • Squeeze the sides of the ring together and insert it into the vagina as far as possible (into the upper 1/3 of the vagina). You should not be able to feel the ring once it is in position. If you can feel it, use a finger to push it further into the vagina. It is not possible for the ring to go too far in or become lost.
  • The ring should remain in place for 90 days. It should then be removed and replaced by a new ring, if prescribed by your doctor. If at any time the ring falls out, rinse it with warm water and reinsert it. If it slides down into the lower part of the vagina, use a finger to reinsert it.
  • The ring does not need to be removed during sexual intercourse. It should not be felt by either partner. If it is bothersome, it can be removed, rinsed with warm water, and reinserted following intercourse.
  • To remove the ring, loop a finger through the ring and gently pull it from the vagina.

To use the estradiol vaginal cream:

  • Using the marked applicator provided, measure the prescribed dose of cream.
  • Lie on your back with your knees drawn up, sit, or stand in a position that allows you comfortable access to the vaginal area. To deliver the medication, gently insert the applicator deeply into your vagina and press the plunger downward to its original position.
  • Clean the applicator by pulling the plunger to remove it from the barrel. Wash it with mild soap and warm water.

Have yearly physical exams and examine your breasts for lumps on a monthly basis while using estradiol.

Store the vaginal rings and cream at room temperature away from moisture and heat.

Related Drug Centers
  • Estrace Vaginal Cream
  • Estring

 

 

Estrace Vaginal Cream


Estrace Vaginal Cream Patient Information including If I Miss a Dose

In this Article

  • What is estradiol (Estrace Vaginal Cream)?
  • What are the possible side effects of estradiol (Estrace Vaginal Cream)?
  • What is the most important information I should know about estradiol (Estrace Vaginal Cream)?
  • What should I discuss with my healthcare provider before using estradiol (Estrace Vaginal Cream)?
  • How should I use estradiol (Estrace Vaginal Cream)?
  • What happens if I miss a dose (Estrace Vaginal Cream)?
  • What happens if I overdose (Estrace Vaginal Cream)?
  • What should I avoid while using estradiol (Estrace Vaginal Cream)?
  • What other drugs will affect estradiol (Estrace Vaginal Cream)?
  • Where can I get more information?

What happens if I miss a dose (Estrace Vaginal Cream)?

Insert the next dose of cream or ring as soon as you remember. Continue to follow your regular schedule. Do not use two doses simultaneously unless your doctor directs otherwise.

If at any time the ring falls out, rinse it with warm water and reinsert it. If it slides down into the lower part of the vagina, use a finger to reinsert it.

What happens if I overdose (Estrace Vaginal Cream)?

An overdose of estradiol is unlikely to occur and is not likely to threaten life. If you do suspect an overdose, or if the medication has been ingested, call an emergency room or poison control center for advice.

What should I avoid while using estradiol (Estrace Vaginal Cream)?

There are no restrictions on food, beverages, or activity while using estradiol unless your doctor directs otherwise.

What other drugs will affect estradiol (Estrace Vaginal Cream)?

Before using estradiol, tell your doctor if you are taking any of the following medicines:

  • an anticoagulant (blood thinner) such as warfarin (Coumadin);
  • a thyroid medication such as levothyroxine (Synthroid, Levoxyl, Levothroid, and others);
  • insulin or an oral diabetes medicine such as glipizide (Glucotrol), glyburide (Diabeta, Micronase), and others; or
  • tamoxifen (Nolvadex).

A dosage adjustment or special monitoring may be required during treatment if you are taking any of the medicines listed above.

Do not use other vaginal products at the same times as estradiol without first talking to your doctor.

Drugs other than those listed here may also interact with estradiol. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including vitamins, minerals, and herbal products.

Where can I get more information?

Your pharmacist has additional information about estradiol written for health professionals that you may read.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Last Updated on Wednesday, 11 January 2012 14:47
 
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