Estradiol vaginal
ESTRACE CREAM
What it isVaginal ER-alpha, ER-beta, and GPER agonist; menopausal vaginal dryness, irritation, and dyspareunia.
Why this oneIt restores local tissue and urinary comfort with much less systemic exposure than oral or transdermal estrogen.
What limits itLocal irritation or discharge can end treatment; unexplained vaginal bleeding still requires evaluation.
FDA label
Read the full label on DailyMed ↗
BOXED WARNING Estrogens: increased risk of endometrial cancer, cardiovascular disorders (stroke, DVT/PE, MI), invasive breast cancer, and probable dementia; not for prevention of cardiovascular disease or dementia.
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Moderate to severe vulvar and vaginal atrophy due to menopause | Postmenopausal women | 2–4 g intravaginally QD ×1–2 weeks | Then reduce to ½ initial dose for a similar period; maintenance 1 g 1–3×/week | 4 g/day |
Renal Undefined
Hepatic Undefined
Instructions
- Administer intravaginally with calibrated applicator
- Use lowest effective dose for shortest duration; taper to maintenance and discontinue as soon as possible
Contraindications
- Undiagnosed abnormal genital bleeding
- Known, suspected, or history of cancer of the breast
- Known or suspected estrogen-dependent neoplasia
- Active DVT, PE or history of these conditions
- Active arterial thromboembolic disease (for example, stroke, MI) or a history of these conditions
- Known liver dysfunction or disease
- Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
- Known or suspected pregnancy
Cautions
- Cardiovascular disorders: increased risk of stroke, DVT/PE, MI — discontinue if occurs
- Malignant neoplasms: endometrial, breast, and ovarian cancer
- Probable dementia in women ≥65
- Gallbladder disease
- Severe hypercalcemia in breast cancer with bone metastases
- Retinal vascular thrombosis / visual abnormalities
- Hypertriglyceridemia may lead to pancreatitis
- Hypothyroidism (increased thyroid-hormone requirement); fluid retention
- Anaphylaxis/angioedema; exacerbation of hereditary angioedema
Adverse reactions
- Abnormal uterine bleeding/spotting, vaginitis, vulvovaginal burning/irritation
- Breast tenderness/enlargement/pain
- Nausea, abdominal cramps, bloating
- Headache, migraine, dizziness, mood changes
- Venous/arterial thrombotic events; increased blood pressure
Pregnancy Contraindicated in pregnancy (should not be used).
Lactation Should not be used during lactation; estrogens can decrease quantity and quality of breast milk.
NO BOXED WARNINGS
Classes and tags
Clinical profile
Mechanism of action: Estradiol vaginal ballicule
