Estropipate (Piperazine Estrone Sulfate)(ess’ troe pi’ pate)
PREGNANCY CATEGORY X
Drug Classes
Estrogen
Hormone
Therapeutic Actions
Estrogens are endogenous female sex hormones important in the development of the female reproductive system and secondary sex characteristics. They cause capillary dilatation, fluid retention, protein anabolism, and thin cervical mucus; conserve calcium and phosphorus and encourage bone formation; inhibit ovulation and prevent postpartum breast discomfort. They are responsible for the proliferation of the endometrium; absence or decline of estrogen produces signs and symptoms of menopause on the uterus, vagina, breasts, cervix. Palliation with androgen-dependent prostatic carcinoma is attributable to competition with androgens for receptor sites, decreasing the influence of androgens.
Indications
Palliation of moderate to severe vasomotor symptoms, atrophic vaginitis, or kraurosis vulvae associated with menopause
Treatment of female hypogonadism, female castration, primary ovarian failure
Prevention of osteoporosis
Contraindications and Cautions
Contraindicated with allergy to estrogens, breast cancer (with exceptions), estrogen-dependent neoplasm, undiagnosed abnormal genital bleeding, active or past thrombophlebitis or thromboembolic disorders from previous estrogen use, pregnancy (serious fetal defects; advise women of childbearing age of the potential risks and suggest birth control measures).
Use cautiously with metabolic bone disease, renal or hepatic insufficiency, heart failure, lactation.
Available Forms
Tablets—0.75, 1.5, 3 mg
Dosages
Adults
Moderate to severe vasomotor symptoms, atrophic vaginitis, kraurosis vulvae associated with menopause: 0.75–6 mg/day PO given cyclically (3 wk on and 1 wk off). Use lowest possible dose.
Female hypogonadism, female castration, primary ovarian failure: 1.5–9 mg/day PO for the first 3 wk, followed by a rest period of 8–10 days. Repeat if bleeding does not occur at end of rest period.
Prevention of osteoporosis: 0.75 mg daily PO for 25 days of a 31-day cycle per month.
Pediatric patients
Safety and efficacy not established.
Pharmacokinetics
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