Dosage Forms. Tablet: 0.5 mg, 1 mg, 2 mg
Common FDA Label Indication, Dosing, and Titration.
1. Abnormal vasomotor function (moderate to severe), menopause: 1-2 mg po daily for 21 d followed by 7 d off
2. Atrophic vulva or vagina (moderate-severe), menopause: Oral tablet, 1-2 mg po daily in a cyclical pattern (3 wk on, 1 wk off)
3. Breast cancer, metastatic, for palliation only: 10 mg po tid × 3 mo
4. Carcinoma of prostate, advanced, androgen-dependent, for palliation only: 1-2 mg po tid
5. Decreased estrogen level, secondary to hypogonadism, castration, or primary ovarian failure: 1-2 mg po daily
6. Postmenopausal osteoporosis, prophylaxis: 0.5 mg po daily for 23 d followed by 5 d off
Off-Label Uses. None
MOA. Estradiol (17β-estradiol; E2) is the most potent of the naturally occurring estrogens and the major estrogen secreted during the reproductive years. Estradiol and other estrogens produce characteristic effects on specific tissues (such as breast), cause proliferation of vaginal and uterine mucosa, increase calcium deposition in bone, and accelerate epiphyseal closure after initial growth stimulation.
Drug Characteristics: Estradiol Oral
Medication Safety Issues: Estradiol Oral
Drug Interactions: Estradiol Oral
Adverse Reactions: Estradiol Oral
Efficacy Monitoring Parameters. Improvement in menopause symptoms; improved bone mineral density for postmenopausal osteoporosis.
Toxicity Monitoring Parameters. Annual physical examination including cervical cytology (Pap smear) and breast exam (in addition to monthly self-exam).
Key Patient Counseling Points. Report abnormal vaginal bleeding or signs/symptoms of a thromboembolic disorder. Do not smoke during therapy, as this increases the risk of thromboembolic events.
Clinical Pearls. Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Increased risks of MI, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women have been reported. An increased risk of developing dementia in women 65 y or older has also been reported. Estrogens, with or without progestins, should be prescribed at the lowest effective doses and for the shortest duration possible. Also available in a variety of topical and vaginal formulations.