Estradiol
ESTRACE
What it isER-alpha, ER-beta, and GPER agonist; menopausal vasomotor and genitourinary symptoms.
Why this oneTransdermal estradiol avoids hepatic first-pass effects, while vaginal forms directly treat genitourinary symptoms.
What limits itSystemic use raises thrombotic and stroke risk; add a progestogen when the uterus is present to protect the endometrium.
FDA-approved for
- menopausal symptoms (~1975)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Moderate-severe vasomotor symptoms / vulvovaginal atrophy of menopause | Adults | 1-2 mg QD, cyclic (3 wk on, 1 wk off) | Lowest effective dose | Titrated to symptoms |
| Female hypoestrogenism (hypogonadism, castration, primary ovarian failure) | Adults | 1-2 mg QD | Lowest effective maintenance dose | Titrated to symptoms |
| Breast cancer palliation (selected metastatic disease) | Adults | 10 mg TID x >=3 months | 10 mg TID | 10 mg TID |
| Advanced androgen-dependent prostate carcinoma (palliation) | Adults | 1-2 mg TID | 1-2 mg TID | 1-2 mg TID |
| Prevention of postmenopausal osteoporosis | Adults | Lowest effective dose (not determined) | Lowest effective dose | Lowest effective dose |
Renal Undefined
Hepatic Contraindicated in hepatic impairment or disease
Instructions
- Use lowest effective dose for shortest duration consistent with treatment goals
- Add a progestin in women with an intact uterus to reduce endometrial cancer risk
- Reevaluate periodically (e.g., every 3-6 months)
Contraindications
- Undiagnosed abnormal genital bleeding
- Known, suspected, or history of breast cancer (except selected metastatic disease)
- Known or suspected estrogen-dependent neoplasia
- Active or history of DVT/pulmonary embolism
- Active or recent (within past year) arterial thromboembolic disease (e.g., stroke, MI)
- Liver dysfunction or disease
- Known or suspected pregnancy
Cautions
- Cardiovascular and thromboembolic events (stroke, MI, DVT/PE)
- Malignancies (endometrial, breast, ovarian)
- Gallbladder disease and pancreatitis
- Hypertriglyceridemia
- Elevated blood pressure
- Retinal vascular thrombosis / visual abnormalities
- Probable dementia (age >=65)
- Hypocalcemia; aggravation of porphyria, asthma, epilepsy
Adverse reactions
- Abnormal vaginal bleeding/spotting
- Breast tenderness/enlargement
- Nausea, abdominal cramps/bloating
- Headache/migraine
- Mood disturbances
- Thromboembolic events
- Weight change
Pregnancy Contraindicated; should not be used during pregnancy
Lactation Undefined
⚠ BOXED WARNINGS
- Endometrial cancer
- Cardiovascular disorders
- Breast cancer
- Probable dementia
Cost, est. cash$300–$5,000/dose or month
Generic entryPre-1982
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityVenous thromboembolism and hormone-related adverse effects; estrogen also lowers lamotrigine exposure.
Mechanism of action: Estradiol ballicule
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