What is Estreva (estradiol) Gel 0.1%?

What is Estreva Gel 0.1%?

Estreva Gel 0.1% is a transdermal estradiol formulation containing 0.1% estradiol (1 mg estradiol per 1 gram of gel) used primarily for treating menopausal vasomotor symptoms and vulvovaginal atrophy in postmenopausal women. 1

Formulation and Delivery

• The gel contains 0.1% (w/w) estradiol, with typical dosing ranging from 0.25 mg to 1.5 mg daily, delivering estimated daily estradiol amounts of 0.003 mg to 0.027 mg depending on the dose applied 1
• Transdermal estradiol gel formulations at 0.1% concentration demonstrate approximately 18% percutaneous penetration over 24 hours, equating to cumulative skin permeation of approximately 0.65 μg/cm² 2

Clinical Indications

Vasomotor Symptoms:

• Estradiol gel 0.1% at doses of 0.25 mg, 0.5 mg, and 1.0 mg daily produces statistically significant reductions in both frequency and severity of moderate to severe hot flashes as early as week 2 of treatment compared to placebo 1
• The lowest available dose (0.25 mg delivering 0.003 mg/day) remains effective for treating vasomotor symptoms, allowing individualized dose titration 1

Vulvovaginal Atrophy:

• All three doses (0.25 mg, 0.5 mg, 1.0 mg) significantly improve signs of vulvovaginal atrophy, including vaginal pH and percentage of superficial cells, compared to placebo 1

Route Preference and Safety Profile

Transdermal administration is strongly preferred over oral estradiol because it:

• Avoids hepatic first-pass metabolism, minimizing impact on hemostatic factors and clotting proteins 3, 4
• Provides more physiological serum estradiol concentrations that mimic natural hormone patterns 3, 4
• Demonstrates more favorable effects on lipid profiles compared to oral formulations 3

Oral estradiol (1-2 mg daily) should only be used when transdermal formulations are contraindicated or refused by the patient 3

Mandatory Progestin Co-Administration

• Any woman with an intact uterus receiving estradiol gel must receive concurrent progestin therapy to prevent endometrial hyperplasia and cancer 3
• First-line progestin: micronized progesterone 200 mg daily for 12-14 days every 28 days 3
• Alternative: medroxyprogesterone acetate 10 mg daily for 12-14 days per month 3

Critical Safety Limitations

Hormone therapy including estradiol gel should NOT be used for primary prevention of chronic conditions in postmenopausal women, as harms outweigh benefits 5, 3

Absolute contraindications include:

• Active or history of arterial thromboembolism, stroke, or myocardial infarction 3
• Current or history of breast cancer or estrogen-sensitive malignancies 3
• Undiagnosed genital bleeding 3
• Active liver disease 3
• Pregnancy 3

Prescribing Principles

• Use the lowest effective dose for the shortest duration consistent with treatment goals 3
• Baseline assessment must include blood pressure measurement and pregnancy status verification if applicable 3
• The formulation offers multiple dosing options (0.25 mg, 0.5 mg, 1.0 mg, 1.5 mg) to allow dose optimization based on symptom response 1