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Basic Drug Info
Drug Name:Estradiol
Manufacturer:Mylan Pharmaceuticals Inc.
Other Info:Mylan Pharmaceuticals Inc.Morgantown, WV 26505REV FEBRUARY 1999PL:ESTRT:R1



Clinical Trials:


Indications and Usage

Estradiol Tablets, USP are indicated in the:1.Treatment of moderate to severe vasomotor symptoms associated with the menopause.

There is no adequate evidence that estrogens are effective for nervous symptoms or depression which might occur during menopause and they should not be used to treat these conditions.2.Treatment of vulval and vaginal atrophy.3.Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.4.Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease.5.Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).6.Prevention of osteoporosis.Since estrogen administration is associated with risk, selection of patients should ideally be based on prospective identification of risk factors for developing osteoporosis.

Unfortunately, there is no certain way to identify those women who will develop osteoporotic fractures.

Most prospective studies of efficacy for this indication have been carried out in white menopausal women, without stratification by other risk factors, and tend to show a universally salutary effect on bone.

Thus, patient selection must be individualized based on the balance of risks and benefits.

A more favorable risk/benefit ratio exists in a hysterectomized woman because she has no risk of endometrial cancer (see BOXED WARNINGS).Estrogen replacement therapy reduces bone resorption and retards or halts postmenopausal bone loss.

Case-control studies have shown an approximately 60 percent reduction in hip and wrist fractures in women whose estrogen replacement was begun within a few years of menopause.

Studies also suggest that estrogen reduces the rate of vertebral fractures.

Even when started as late as 6 years after menopause, estrogen prevents further loss of bone mass for as long as the treatment is continued.

The results of a two-year, randomized, placebo-controlled, double-blind, dose-ranging study have shown that treatment with 0.5 mg estradiol daily for 23 days (of a 28 day cycle) prevents vertebral bone mass loss in postmenopausal women.

When estrogen therapy is discontinued, bone mass declines at a rate comparable to the immediate postmenopausal period.

There is no evidence that estrogen replacement therapy restores bone mass to premenopausal levels.At skeletal maturity there are sex and race differences in both the total amount of bone present and its density, in favor of men and blacks.

Thus, women are at higher risk than men because they start with less bone mass and, for several years following natural or induced menopause, the rate of bone mass decline is accelerated.

White and Asian women are at higher risk than black women.Early menopause is one of the strongest predictors for the development of osteoporosis.

In addition, other factors affecting the skeleton which are associated with osteoporosis include genetic factors (small build, family history), and endocrine factors (nulliparity, thyrotoxicosis, hyperparathyroidism, Cushing's syndrome, hyperprolactinemia, Type I diabetes), lifestyle (cigarette smoking, alcohol abuse, sedentary exercise habits) and nutrition (below average body weight, dietary calcium intake).The mainstays of prevention and management of osteoporosis are estrogen, an adequate lifetime calcium intake, and exercise.

Postmenopausal women absorb dietary calcium less efficiently than premenopausal women and require an average of 1500 mg/day of elemental calcium to remain in neutral calcium balance.

By comparison, premenopausal women require about 1000 mg/day and the average calcium intake in the USA is 400 to 600 mg/day.

Therefore, when not contraindicated, calcium supplementation may be helpful.Weight-bearing exercise and nutrition may be important adjuncts to the prevention and management of osteoporosis.

Immobilization and prolonged bed rest produce rapid bone loss, while weight-bearing exercise has been shown both to reduce bone loss and to increase bone mass.

The optimal type and amount of physical activity that would prevent osteoporosis have not been established, however in two studies an hour of walking and running exercise twice or three times weekly significantly increased lumbar spine bone mass.
Symptoms -- An indication that a person has a condition or disease. Some examples of symptoms are headache, fever, fatigue, nausea, vomiting, and pain.

Hypogonadism -- Condition resulting from deficient gonadal functions, such as GAMETOGENESIS and the production of GONADAL STEROID HORMONES. It is characterized by delay in GROWTH, germ cell maturation, and development of secondary sex characteristics. Hypogonadism can be due to a deficiency of GONADOTROPINS (hypogonadotropic hypogonadism) or due to primary gonadal failure (hypergonadotropic hypogonadism).

Breast Carcinoma -- (brest KAN-ser) Cancer that forms in tissues of the breast, usually the ducts (tubes that carry milk to the nipple) and lobules (glands that make milk). It occurs in both men and women, although male breast cancer is rare.

Malignant neoplasm of breast -- A primary or metastatic malignant neoplasm involving the breast. The vast majority of cases are carcinomas arising from the breast parenchyma or the nipple. Malignant breast neoplasms occur more frequently in females than in males. -- 2003

Neoplasm Metastasis -- The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.

Carcinoma -- A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm but is often wrongly used as a synonym for "cancer." (From Dorland, 27th ed)

Osteoporosis -- Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.

OSTEOPOROSIS FRACTURE --

Endometrial Carcinoma -- A malignant tumor arising from the epithelium that lines the cavity of the uterine body. The vast majority of endometrial carcinomas are adenocarcinomas; squamous cell and adenosquamous carcinomas represent a minority of the cases. Endometrioid adenocarcinoma is the most frequently seen variant of endometrial adenocarcinoma. Uterine bleeding is an initial clinical sign. The prognosis depends on the stage of the tumor, the depth of myometrial wall invasion, and the degree of differentiation. -- 2004

Uterine Corpus Cancer --

Osteoporosis, Postmenopausal -- Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.

Osteopenia -- decreased calcification, bone density, or bone mass due to inadequate osteoid synthesis.

Menopause, Premature -- The premature cessation of menses (MENSTRUATION) when the last menstrual period occurs in a woman under the age of 40. It is due to the depletion of OVARIAN FOLLICLES. Premature MENOPAUSE can be caused by diseases; OVARIECTOMY; RADIATION; chemicals; and chromosomal abnormalities.

Thyrotoxicosis -- A hypermetabolic syndrome caused by excess THYROID HORMONES which may come from endogenous or exogenous sources. The endogenous source of hormone may be thyroid HYPERPLASIA; THYROID NEOPLASMS; or hormone-producing extrathyroidal tissue. Thyrotoxicosis is characterized by NERVOUSNESS; TACHYCARDIA; FATIGUE; WEIGHT LOSS; heat intolerance; and excessive SWEATING.

Hyperparathyroidism -- WHAT: Hyperparathyroidism. Hyperparathyroidism: a condition due to an increase in the secretion of the parathyroids, causing generalized osteitis fibrosa cystica, elevated serum calcium, decreased serum phosphorus, and increased excretion of both calcium and phosphorus. WHY: Several rheumatological disorders are associated with hyperpara- thyroidism. First, hyperuricemia and gouty arthritis (which may mimic hyperparathyroidism with renal stone formation and colic) have an increased incidence in patients with hyperparathyroidism. Second, patients with primary hyperparathyroidism show an increased incidence of chondrocalcinosis with episodes of calcium pyrophosphate crystal induced synovitis. Approximately 25% of patients with hyperparathyroidism will show radiographic evidence of calcification of articular cartilage and joint capsules. Finally, there can be a synovial and cartilaginous lesion ("osteogenic synovitis") in patients with hyperparathyroidism which may mimic other primary rheumatic diseases such as rheumatoid arthritis. In osteogenic synovitis there is softening and collapse of subchondral bone. Eventually the cartilage overlying this area erodes and is replaced by an irregular fibrocartilage. Eventually the articular surface of the joint is destroyed and secondary degenerative arthritis may develop. REFS: 1) Zvaifler, NJ; Reefe, WE and Black, RL: Articular manifestations in primary hyperparathyroidism. Arthritis Rheum 5:237, 1962. 2) Scott, JT; Dixon, ASJ and Bywaters, EGL: Association of hyperuricemia and gout with hyperparathyroidism. Br Med J 1:1070, 1964. 3) Bywaters, EGL and Scott, JT : Joint lesions of hyperparathyroidism. Ann Rheum Dis 22:171-87, 1963.

Cushing Syndrome -- A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent.

Hyperprolactinemia -- Increased levels of PROLACTIN in the BLOOD, which may be associated with AMENORRHEA and GALACTORRHEA. Relatively common etiologies include PROLACTINOMA, medication effect, KIDNEY FAILURE, granulomatous diseases of the PITUITARY GLAND, and disorders which interfere with the hypothalamic inhibition of prolactin release. Ectopic (non-pituitary) production of prolactin may also occur. (From Joynt, Clinical Neurology, 1992, Ch36, pp77-8)

Diabetes Mellitus, Insulin-Dependent -- subtype of diabetes mellitus that is characterized by insulin deficiency; it is manifested by the sudden onset of severe hyperglycemia, rapid progression to diabetic ketoacidosis, and death unless treated with insulin; the disease may occur at any age, but is most common in childhood or adolescence.

SPONDYLOMETAEPIPHYSEAL DYSPLASIA, SHORT LIMB-HAND TYPE --

Contraindications

Estrogens should not be used in individuals with any of the following conditions:1.Known or suspected pregnancy (see BOXED WARNINGS).

Estrogens may cause fetal harm when administered to a pregnant woman.2.Undiagnosed abnormal genital bleeding.3.Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease.4.Known or suspected estrogen-dependent neoplasia.5.Active thrombophlebitis or thromboembolic disorders.
Neoplasm Metastasis -- The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.

Thrombophlebitis -- Inflammation of a vein associated with a blood clot (THROMBUS).

Thromboembolism -- Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.

Warnings

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.

In three studies, persistence of risk was demonstrated for 8 to over 15 years after cessation of estrogen treatment.

In one study a significant decrease in the incidence of endometrial cancer occurred six months after estrogen withdrawal.

Concurrent progestin therapy may offset this risk but the overall health impact in postmenopausal women is not known (see PRECAUTIONS).
Branded Drugs
The following US Branded drugs contain Estradiol


ANGELIQ -- BAYER HEALTHCARE PHARMACEUTICALS INC

ESTRACE -- WARNER CHILCOTT INC

ALORA -- WATSON LABORATORIES INC

CLIMARA -- BAYER HEALTHCARE PHARMACEUTICALS INC

ESCLIM -- WOMEN FIRST HEALTHCARE INC

ESTRADERM -- NOVARTIS PHARMACEUTICALS CORP

FEMPATCH -- PARKE DAVIS PHARMACEUTICAL RESEARCH DIV WARNER LAMBERT CO

MENOSTAR -- BAYER HEALTHCARE PHARMACEUTICALS INC

VIVELLE -- NOVARTIS PHARMACEUTICALS CORP

VIVELLE-DOT -- NOVARTIS PHARMACEUTICALS CORP

ELESTRIN -- AZUR PHARMA INTERNATIONAL II LTD

ESTROGEL -- ASCEND THERAPEUTICS INC

DIVIGEL -- UPSHER SMITH LABORATORIES INC

ESTRING -- PHARMACIA AND UPJOHN CO

EVAMIST -- KV PHARMACEUTICAL CO

ESTRACE -- BRISTOL MYERS SQUIBB CO

ESTRACE -- BRISTOL MYERS SQUIBB CO PHARMACEUTICAL RESEARCH INSTITUTE

GYNODIOL -- DURAMED PHARMACEUTICALS INC SUB BARR LABORATORIES INC

INNOFEM -- NOVO NORDISK INC

VAGIFEM -- NOVO NORDISK INC

CLIMARA PRO -- BAYER HEALTHCARE PHARMACEUTICALS INC

COMBIPATCH -- NOVARTIS PHARMACEUTICALS CORP

ACTIVELLA -- NOVO NORDISK INC

ESTRADIOL AND NORETHINDRONE ACETATE -- BRECKENRIDGE PHARMACEUTICAL INC

ESTRADIOL AND NORGESTIMATE -- BARR LABORATORIES INC

PREFEST -- DURAMED PHARMACEUTICALS INC


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