Estrogen Category

Estrogen (systemic) - Chlorotrianisene; Conjugated Estrogens; Diethylstibestrol; Esterified Estrogens; Estrone; Estropipate; Ethinyl Estradiol; Quinestrol.

Antineoplastic- Chlorotrianisene; Conjugatee Estrogens Tablets USP; Diethylstilbestrol; Esterified Estrogens; Estradiol; Estradiol Valerate; Estrone; Ethinyl Estradiol.

Osteoporosis Prophylactic- Conjugated Estrogens Tablets USP; Diethylstibestrol Tables USP; Diethylstibestrol Tables USP (Enteric-coated); Esterified Estrogens; Estradiol tables USP; Estradiol Transdermal System; Estropipate; Ethinyl Estradiol.

Indications

Note : Bracketed information in the Indications section refers to uses not included in U.S. product labeling.

Accepted

Bleeding, uterine, hormonal imbalance-induced (treatment)-Conjugate estrogens tablets, estradiol, estradio) valerate, esterified estrogens, estrone, estropipate, and quinestrol are indicated as estrogen replacement therapy in the treatment of atrophic vaginitis, female hypogonadism or castration, vulvar squamous hyperplasia, primary ovarian failure and moderate to severe vasomotor symptoms associated with menopause.

Chlorotrianisene is indicated as estrogen replacement therapy in the treatment of atrophic vaginitis, female hypogonadism, vulvar squamous hyperplasia, and moderate to severe vasomotor symptoms of menopause.

Conjugated estrogens for injection, [estradiol valerate], estrone, and [ethinyl estradiol] are indicated in the treatment of inorganic abnormal uterine bleeding caused by hormonal imbalance.

Estradiol cypionate' and ethinyl estradiol' are indicated as estrogen replacement therapy in the treatment of female hypogonadism and moderate to severe vasomotor symptoms of menopause.

Carcinoma, breast (treatment)-Conjugated estrogens tablets, diethyl-stilbestrol tablets and enteric-coated tablets, [estradiol valerate], esterified estrogens1, estradiol tablets, and [ethinyl estradiol] are indicated for treatment of metastatic breast carcinoma in selected men and postmenopausal women.

Carcinoma, prostatic (treatment)-Chlorotrianisene, conjugated estrogens tablets, diethylstilbestro), esterified estrogens1, estradiol, estradiol valerate, estrone, and [ethinyl estradiol] are indicated for treatment of advanced prostatic carcinoma.

Ospteoporosis, postmenopausal (prophylaxis)-Conjugated estrogens tablets, diethylstilbestrol tablets', diethylstilbestrol enteric-coated tablets, esterified estrogens1, estradiol tablets1 and transdermal system ethinyl estradiol1, and estropipate1 are indicated in post-menopausal women to retard bone loss and estrogen deficiency-induced osteoporosis. Estrogen replacement therapy can reduce the rate of bone loss and fractures in postmenopausal women. Proper diet, calcium supplementation, and physical activity should also be encouraged along with estrogen replacement therapy.

[Osteoporosis, premenopausal, estrogen deficiency-induced (prophylaxis)]1 -Conjugated estrogens tablets, diethylstilbestrol tablets, diethylstilbestrol enteric-coated tablets, esterified estrogens, estradiol tablets, ethinyl estradiol, and estropipate are also used in premenopausal women who are estrogen-deficient to protect them against bone loss.

[Atherosclerotic disease (prophylaxis)]'-Estrogens may be effective in the prevention of cardiovascular disease in postmenopausal women.

[Turner's yndrome (treatment)]'-Ethinyl estradiol is used in the treatment of Turner's syndrome (gonadal dysgenesis).

Chlorotrianisene, estropipate, and quinestrol are infrequently prescribed for estrogen replacement therapy. Also, there is very little use for estrogens administered parenterally.

Unaccepted

The use of estrogens to reduce postpartum breast engorgement recommended. In many patients, postpartum breast engorgement is a benign, self-limited condition that may respond to breast support and mild analgesics, such as acetaminophen and ibuprofen. Evidence supporting the efficacy of estrogens for this indication is lacking. Therefore, the questionable benefits of administering the large doses of estrogens required for this indication are outweighed by the risk of increasing the incidence of puerperal thromboembolism.

Ethinyl estradiol, conjugated estrogens, and diethylstilbestrol tablets have been used as postcoital contraceptives (the "morning-after pill), primarily in emergency care situations, such as the management of rape or incest victims. However, the combination oral contraceptive, norgestrel and ethinyl estradiol, is more commonly prescribed for this indication.

Pharmacology

Mechanism of action/Effect: At the cellular level, estrogens increase the synthesis of DNA, RNA, and various proteins in target tissues. Pituitary mass is also increased. Estrogens reduce the release of gonadotropin-releasing hormone from the hypothalamus, leading to a reduction in release of follicle-stimulating hormone and luteinizing hormone from the pituitary.

For estrogen replacement in healthy females, endogenous estrogens maintain genitourinary function and vasomotor stability. Estrogens are used as replacement therapy to alleviate or pre-vent symptoms caused by the decreased amounts of estrogens produced by the ovaries after natural or surgical menopause or other estrogen deficiency states.

For prevention of postmenopausal osteoporosis during periods of estrogen deficiency, the rate of bone resorption by osteo-clasts greatly exceeds the rate of bone formation by osteoblasts. Estrogen replacement therapy prevents this accelerated bone loss by inhibiting bone resorption to a level where the near equilibrium between bone resorption and formation is restored. However, estrogens do not replace previously lost bone or significantly increase total bone mass.

For prostatic carcinoma inhibition of pituitary secretion of luteinizing hormone and a possible rninor, direct effect on the testis, resulting in decreased serum concentrations of testosterone.

Precautions to Consider


Geriatrics

Studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of estrogens in the elderly.

Dental

Estrogens may predispose the patient to bleeding of the gingival tissues. In addition, gingival hyperplasia may occur during estrogen therapy, usually starting as gingivitis or gum inflammation. A strictly enforced program of teeth cleaning by a professional, combined with plaque control by the patient, will minimize growth rate and severity of gingival enlargement.

Drug Interactions and/or Related Problems

The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance possible mechanism in parentheses where appropriate)-not necessarily inclusive (>> = major clinical, significance):

Note: Combinations containing any of the following mediations, depending on the amount present, may also interact with this medication.

Adrenocorticoids, Glucocorticoid

(concurrent use with estrogens may alter the metafolism and protein binding of the glucocorticoids, leading to decreased clearance, increased elimination half-life, and increased therapeutic and toxic effects of the glucocorticoids; glucocorticoid dosage adjustment may be required during and following concurrent use)

Bromocriptine

(estrogens may cause amenorrhea, interfering with effects of bromocriptine; concurrent use is not recommended)

Calcium Supplements

(concurrent use with estrogens may increase calcium absorption; this can be used to therapeutic advantage)

Corticotropin (chronic therapeutic use)

(concurrent use with estrogens may potentiate the anti-inflammatory effects of endogenous cortisol induced by corticotropin)
Cyclosporine

(estrogens have been reported to inhibit cyclosporine metabolism and thereby increase plasma concentrations of cyclosporine. possibly increasing the risk of hepatotoxicity and nephrotoxicity; concurrent use is recommended only with great caution and frequent monitoring of blood cyclosporine concentrations and liver and renal function)
Hepatoloxic medications, especially dantrolene

(concurrent use of these medications with estrogens may increase the risk of hepatotoxicity; with use in females over 35 years of age, prolonged use, or use in patients with a history of liver disease, risk may be further increased)

Smoking Tobacco

(data from studies on tobacco smoking and the use of high-dose estrogen oral contraceptives indicate that there is an increased risk of serious cardiovascular side effects, including cerebrovascular accident, transient ischemic attacks, thromho-phlebitis, and pulmonary embolism; risk increases with in-creasing tobacco usage and with age, especially in women over 35 years of age; it is not known whether any elevation of risk occurs with tobacco smoking during the use of estrogen re-placement therapy) (metabolism of estrogens may also be increased by smoking. resulting in a decreased estrogenic effect)

Somatrem or Somatropin

(in prepubertal patients, concurrent use of estrogens with somatrem or somatropin may accelerate epiphyseal maturation)

Tamoxifen

(concurrent use may interfere with therapeutic effect of tamoxifen)

Contraindications/Medical problems

The contraindications/medical problems included have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate) -not necessarily inclusive ( major clinical significance).

Except under special circumstances, this medication should not be used when the/allowing medical problems exist:

Breast cancer, known or suspected, except in selected patients treated for metastatic diseases (possible promotion of tumor growth in breast cancer)

Vaginal Bleeding, Abnormal and Undiagnosed

(may indicate the presence ofendometrial hyperplasia or carcinoma, which may be exacerbated or promoted by the use of estrogens)

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