No

Estrogen Derivative

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

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 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

Crystalline estrone that has been solubilized as the sulfate and stabilized with piperazine. 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: Estrone is not orally active due to enzymatic degradation in the gut and liver; addition of piperazine moiety increases oral absorption

Adults: Female:

Hypogonadism or primary ovarian failure: Oral: 1.5-9 mg/day for the first 3 weeks, followed by a rest period of 8-10 days. Repeat if bleeding does not occur by the end of the rest period. The duration of therapy necessary to product the withdrawal bleeding will vary according to the responsiveness of the endometrium. If satisfactory withdrawal bleeding does not occur, give an oral progestin in addition to estrogen during the third week of the cycle.

Osteoporosis prevention: Oral: 0.625 mg/day for 25 days of a 31-day cycle

Atrophic vaginitis or kraurosis vulvae: Vaginal: Instill 2-4 g/day 3 weeks on and 1 week off

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

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.

Patients should inform their physicians if signs or symptoms of any of the following occur: Thromboembolic or thrombotic disorders including sudden severe headache or vomiting, disturbance of vision or speech, loss of vision, numbness or weakness in an extremity, sharp or crushing chest pain, calf pain, shortness of breath, severe abdominal pain or mass, mental depression or unusual bleeding; patients should discontinue taking the medication if they suspect they are pregnant or become pregnant. Patient package insert is available; insert product high into the vagina.

Cream, vaginal: 0.15% [estropipate 1.5 mg/g] (42.5 g tube)

Tablet: 0.625 mg [estropipate 0.75 mg]; 1.25 mg [estropipate 1.5 mg]; 2.5 mg [estropipate 3 mg]; 5 mg [estropipate 6 mg]