Yes

Estrogen Derivative

Hypogonadism; primary ovarian failure; vasomotor symptoms of menopause; prostatic carcinoma; inoperable breast cancer, kraurosis vulvae, abnormal uterine bleeding due to hormone imbalance

X

Thrombophlebitis, undiagnosed vaginal bleeding, hypersensitivity to estrogens or any component, pregnancy

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 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

Estrone is a natural ovarian estrogenic hormone that is available as an aqueous mixture of water insoluble estrone and water soluble estrone potassium sulfate; all estrogens, including estrone, act in a similar manner; there is no evidence that there are biological differences among various estrogen preparations other than their ability to bind to cellular receptors inside the target cells

Absorption: Readily absorbed from the GI tract

Adults: I.M.:

Female:

Senile vaginitis and kraurosis vulvae: 0.1-0.5 mg 2-3 times/week; cyclical (3 weeks on and 1 week off)

Breast cancer (inoperable, progressing): 5 mg 3 or more times/week

Primary ovarian failure, hypogonadism: 0.1-1 mg/week, up to 2 mg/week in single or divided doses; cyclical (3 weeks on and 1 week off)

Abnormal uterine bleeding: Brief courses of intensive therapy: 2-5 mg/day for several days

Dosing adjustment in hepatic impairment:

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

Severe liver impairment: Not recommended

Decreased antithrombin III

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

This drug can only be given I.M. It is important to maintain schedule of drug days and drug-free days. 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.

May also be administered intramuscularly; administer at bedtime to minimize occurrence of adverse effects; when administered I.V., drug should be administered slowly to avoid the occurrence of a flushing reaction

Injection: 2 mg/mL (10 mL, 30 mL); 5 mg/mL (10 mL)