Estradiol(ess tra dye’ ole)
Estradiol
Oral: Estrace, Gynodiol
Transdermal system: Alora, Climara, Menostar, Minivelle, Vivelle, Vivelle Dot
Topical vaginal cream: Estrace
Vaginal ring: Estring
Topical emulsion: Estrasorb
Gel: Divigel, Elestrin, Estrogel
Topical spray: Evamist
Estradiol Acetate
Vaginal ring: Femring
Estradiol Cypionate
Injection in oil: Depo-Estradiol
Estradiol Hemihydrate
Vaginal tablet: Vagifem
Estradiol Valerate
Injection in oil: Delestrogen
PREGNANCY CATEGORY X
Drug Classes
Estrogen
Hormone
Therapeutic Actions
Estradiol is the most potent endogenous female sex hormone. Estrogens are important in the development of the female reproductive system and secondary sex characteristics; affect the release of pituitary gonadotropins; 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 proliferation of the endometrium; absence or decline of estrogen produces signs and symptoms of menopause on the uterus, vagina, breasts, cervix; relief in androgen-dependent prostatic carcinoma is attributable to competition with androgens for receptor sites, decreasing influence of the androgens.
Indications
Estrasorb, estradiol cypionate, estradiol valerate: Vasomotor symptoms
Estradiol acetate tablets (Femtrace), estradiol gel 0.1% (Divigel), estradiol spray (Evamist): Treatment of moderate to severe vasomotor symptoms associated with menopause
Vagifem, Estrace, Estring: Vaginal atrophy
Femring, tablets, transdermal (except Menostar), Estrogel: Vasomotor symptoms and vaginal atrophy
Estradiol oral, transdermal, estradiol valerate: Prevention of postmenopausal osteoporosis
Estradiol oral, transdermal, estradiol cypionate, valerate: Treatment of female hypogonadism, female castration, primary ovarian failure
Estradiol oral, estradiol valerate: Palliation of inoperable prostatic cancer
Estradiol oral: Palliation of inoperable, progressing breast cancer
Contraindications and Cautions
Contraindicated with allergy to estrogens, allergy to tartrazine (in 2-mg oral tablets), breast cancer (with exceptions), estrogen-dependent neoplasm, undiagnosed abnormal genital bleeding, active or past history of thrombophlebitis or thromboembolic disorders, pregnancy (potential serious fetal defects; women of childbearing age should be advised of risks and birth control measures suggested), history of breast cancer.
Use cautiously with metabolic bone disease, renal or hepatic insufficiency, heart failure, lactation.
Available Forms
Transdermal—release rates of 0.014, 0.025, 0.0375, 0.05, 0.06, 0.075, 0.1 mg/24 hr; tablets—0.5, 1, 2 mg; Femtrace—0.45, 0.9, 1.8 mg; injection—5, 10, 20, 40 mg/mL; vaginal cream—0.1 mg/g; vaginal ring—2 mg; Femring—0.05 mg/day, 0.1 mg/day; vaginal tablet—10, 25 mcg; topical emulsion—2.5 mg/g; gel—0.06%, 0.1%; topical spray—1.53 mg
Dosages
Adults
Moderate to severe vasomotor symptoms, atrophic vaginitis, kraurosis vulvae associated with menopause: 1–2 mg/day PO. Adjust dose to control symptoms. For gel, 0.25 g of 0.1% gel applied to right or left upper thigh on alternating days; may be increased to 0.5 or 1 g/day to control symptoms. For topical spray (Evamist), 1 spray once daily to forearm; may be increased to 2–3 sprays daily. Cyclic therapy (3 wk on/1 wk off) is recommended, especially in women who have not had a hysterectomy. 1–5 mg estradiol cypionate in oil IM every 3–4 wk. 10–20 mg estradiol valerate in oil IM, every 4 wk. The 0.014- to 0.05-mg system is applied to the skin weekly or twice weekly. If oral estrogens have been used, start transdermal system 1 wk after withdrawal of oral form. Given on a cyclic schedule (3 wk on/1 wk off). Attempt to taper or discontinue medication every 3–6 mo.
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