No

Estrogen Derivative

Atrophic vaginitis; hypogonadism; primary ovarian failure; vasomotor symptoms of menopause; prostatic carcinoma; osteoporosis prophylactic

X

Known or suspected cancer of the breast, except in appropriately selected patients being treated for metastatic disease; known or suspected estrogen-dependent neoplasia; known or suspected pregnancy; undiagnosed abnormal genital bleeding; active thrombophlebitis or thromboembolic disorders; past history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use except when used in the treatment of breast or prostatic malignancy

Use with caution in patients with asthma, epilepsy, migraine, diabetes, cardiac or renal dysfunction; estrogens may cause premature closure of the epiphyses in young individuals; safety and efficacy in children have not been established; estrogens have been reported to increase the risk of endometrial carcinoma, do not use estrogens during pregnancy

>10%:

Cardiovascular: Peripheral edema

Endocrine & metabolic: Enlargement of breasts, breast tenderness

Gastrointestinal: Nausea, anorexia, bloating

1% to 10%:

Central nervous system: Headache

Endocrine & metabolic: Increased libido

Gastrointestinal: Vomiting, diarrhea

<1%: Hypertension, thromboembolism, myocardial infarction, edema, stroke, depression, dizziness, anxiety, chloasma, melasma, rash, amenorrhea, alterations in frequency and flow of menses, decreased glucose tolerance, increased triglycerides and LDL, GI distress, cholestatic jaundice, intolerance to contact lenses, increased susceptibility to Candida infection, breast tumors

Symptoms of overdose include fluid retention, jaundice, thrombophlebitis

Toxicity is unlikely following single exposures of excessive doses, any treatment following emesis and charcoal administration should be supportive and symptomatic

Decreased effect: Rifampin decreases estrogen serum concentrations

Increased toxicity:

Hydrocortisone increases corticosteroid toxic potential

Anticoagulants: Increases potential for thromboembolic events with anticoagulants

Carbamazepine, tricyclic antidepressants, and corticosteroids; increased thromboembolic potential with oral anticoagulants

Primary effects on the interphase DNA-protein complex (chromatin) by binding to a receptor (usually located in the cytoplasm of a target cell) and initiating translocation of the hormone-receptor complex to the nucleus

Absorption: Readily absorbed from GI tract

Metabolism: Rapidly in the liver to less active metabolites

Elimination: In urine as unchanged compound and metabolites

Adults: Oral:

Female:

Hypogonadism: 2.5-7.5 mg of estrogen daily for 20 days followed by a 10-day rest period. Administer cyclically (3 weeks on and 1 week off). If bleeding does not occur by the end of the 10-day period, begin an estrogen-progestin cyclic regimen of 2.5-7.5 mg/day in divided doses for 20 days. During the last days of estrogen therapy, give an oral progestin. If bleeding occurs before this regimen is concluded, discontinue therapy and resume on the fifth day of bleeding.

Moderate to severe vasomotor symptoms: 1.25 mg/day administered cyclically (3 weeks on and 1 week off). If patient has not menstruated within the last 2 months or more, cyclic administration is started arbitrary. If the patient is menstruating, cyclical administration is started on day 5 of the bleeding. For short-term use only and should be discontinued as soon as possible. Re-evaluate at 3- to 6-month intervals for tapering or discontinuation of therapy.

Atopic vaginitis and kraurosis vulvae: 0.3 to greater than or equal to 1.25 mg/day, depending on the tissue response of the individual patient. Administer cyclically. For short-term use only and should be discontinued as soon as possible. Re-evaluate at 3- to 6-month intervals for tapering or discontinuation of therapy.

Breast cancer (inoperable, progressing): 10 mg 3 times/day for at least 3 months

Osteoporosis, in postmenopausal women: Initial: 0.3 mg/day and increase to a maximum daily dose of 1.25 mg/day; initiate therapy as soon as possible after menopause; cyclical therapy is recommended

Female castration and primary ovarian failure: 1.25 mg/day, cyclically. Adjust dosage up- or downward according to the severity of symptoms and patient response. For maintenance, adjust dosage to lowest level that will provide effective control.

Dosing adjustment in hepatic impairment:

Mild to moderate liver impairment: Dosage reduction of estrogens is recommended

Severe liver impairment: Not recommended

Should be administered with food at same time each day

Endocrine function test may be altered

Decreased serum folate concentration

Increased prothrombin and factors VII, VIII, IX, X

Increased platelet aggregability

Increased thyroid binding globulin

Increased total thyroid hormone (T₄)

Increased serum triglycerides/phospholipids

May rarely cause anxiety or depression

None reported

No information available to require special precautions

No effects or complications reported

Use this drug in cycles or term as prescribed. Take each day at the same time with food. Periodic gynecologic exam and breast exams are important. You may experience nausea or vomiting (small frequent meals may help); dizziness or mental depression (use caution when driving); rash; loss of scalp hair; enlargement/tenderness of breasts; or increased/decreased libido. Report significant swelling of extremities, sudden acute pain in legs or calves, chest, or abdomen; shortness of breath; severe headache or vomiting; weakness or numbness of arms or legs; or unusual vaginal bleeding. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Consult prescriber if breast-feeding.

Esterified estrogens are a combination of the sodium salts of the sulfate esters of estrogenic substances; the principal component is estrone, with preparations containing 75% to 85% sodium estrone sulfate and 6% to 15% sodium equilin sulfate such that the total is not <90%

Tablet: 0.3 mg, 0.625 mg, 1.25 mg, 2.5 mg

Winship KA, "Unopposed Oestrogens," Adverse Drug React Acute Poisoning Rev, 1987, 6(1):37-66.