Estradiol Tablet Dosing
For postmenopausal women with vasomotor symptoms or vulvovaginal atrophy, start with oral estradiol 1-2 mg daily, though transdermal formulations are strongly preferred over oral tablets when feasible. 1
Preferred Route of Administration
- Transdermal estradiol is the preferred route over oral tablets because it mimics physiological serum concentrations, avoids hepatic first-pass metabolism, provides a superior safety profile, and has more favorable effects on lipid profiles 2
- Oral estradiol tablets (1-2 mg daily) should only be used when transdermal formulations are contraindicated or refused by the patient 2
Standard Oral Dosing Regimens
For Vasomotor Symptoms and Vulvovaginal Atrophy
- Initial dose: 1-2 mg daily of estradiol, adjusted to control symptoms 1
- Administer cyclically (3 weeks on, 1 week off) 1
- Titrate to the minimal effective maintenance dose 1
- Use the lowest effective dose for the shortest duration consistent with treatment goals 1
For Female Hypoestrogenism
- Start with 1-2 mg daily, adjusted to control symptoms 1
- Determine minimal effective maintenance dose through titration 1
For Breast Cancer Palliation
- 10 mg three times daily for at least 3 months 1
For Prostate Cancer Palliation
- 1-2 mg three times daily 1
Mandatory Progestin Co-Administration
- For any woman with an intact uterus receiving estrogen therapy, progestin MUST be added to reduce endometrial cancer risk 2, 1
- First-line progestin: Micronized progesterone 200 mg daily for 12-14 days every 28 days 2
- Alternative: Medroxyprogesterone acetate 10 mg daily for 12-14 days per month 2
- Women without a uterus do not require progestin 1
Monitoring and Duration
- Reevaluate patients every 3-6 months to determine if treatment is still necessary 1
- Attempt to discontinue or taper medication at 3-6 month intervals 1
- For undiagnosed persistent or recurring abnormal vaginal bleeding, perform endometrial sampling to rule out malignancy before continuing therapy 1
Critical Safety Considerations
- Hormone therapy should NOT be used for primary prevention of chronic conditions (including osteoporosis prevention as primary indication), as harms outweigh benefits 2
- Use only for symptom management, not disease prevention 2
- Baseline assessment should include blood pressure and pregnancy status 2
Absolute Contraindications
- Active or history of arterial thromboembolism, stroke, or MI 2
- Breast cancer or estrogen-sensitive malignancies 2
- Undiagnosed genital bleeding 2
- Active liver disease 2
- Pregnancy 2
Common Pitfall to Avoid
The most critical error is prescribing estrogen to a woman with an intact uterus without concurrent progestin therapy, which significantly increases endometrial cancer risk. Always verify uterine status before initiating therapy and ensure appropriate progestin coverage throughout treatment 2, 1.