Available Dosage Strengths
10 mg | 12.5 mg | 15 mg | 18 mg | 20 mg | 25 mg
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Micronized estradiol is a bioidentical form of 17β-estradiol, the primary estrogen produced by the ovaries in premenopausal women. It is used in a variety of hormone therapy (HT) regimens and can be considered one of the preferred estrogen formulations for menopausal women due to its bioidentical structure and favorable risk profile when appropriately prescribed. When applied topically and absorbed transdermally or implanted subcutaneously, micronized estradiol does not undergo first-pass metabolism through the liver, this leads to the favorable risk profile as the first pass-effect of estradiol causes the greatest increases in thromboembolic factors. Estradiol can be implanted subcutaneously through a compounded pellet to administer continuous estradiol over a period of typically 3 months. 1-7
Estradiol binds to estrogen receptors, which are widely distributed in reproductive tissues, the brain, bone, liver, and vasculature. Upon receptor binding, estradiol influences gene transcription, leading to a broad range of systemic and local effects: 1-7
– Endometrial stimulation: Promotes proliferation in the endometrial lining.
– Thermoregulatory effects: May relieve hot flashes by stabilizing hypothalamic activity.
– Bone preservation: May reduce osteoclast-mediated bone resorption, maintaining bone mineral density.
– Vaginal and urogenital health: Helps to maintain epithelial integrity, pH balance, and blood flow.
– Neuroprotection: Modulates neurotransmitter systems that affect mood, cognition, and sleep.
– Cardiovascular modulation: Promotes vasodilation and improves lipid profile, although the route of administration affects cardiovascular risk.
Common: 1-7
– Breast tenderness
– Nausea
– Headache
– Bloating or fluid retention
– Breakthrough vaginal bleeding
– Mood swings
Less Common / Serious Risks: 1-7
– Increased risk of venous thromboembolism (VTE) (primarily with oral use)
– Gallbladder disease
– Endometrial hyperplasia or cancer if unopposed by a progestogen in women with a uterus
Contraindications: 1-7
– Undiagnosed abnormal genital bleeding
– Active or history of estrogen-dependent cancer (e.g., breast, endometrial)
– Active or recent thromboembolic disorders (e.g., DVT, PE, stroke, heart attack)
– Active liver disease
– Known hypersensitivity to estradiol or formulation components
Precautions: 1-7
Use caution in women with:
– Controlled hypertension
– Migraine with aura
– Hypertriglyceridemia
– Diabetes mellitus
– History of gallbladder disease
– History of or active hormone-sensitive cancers (in remission)
*Use with Progesterone:
For women with an intact uterus, progesterone in some form should be included with systemic estradiol therapy to prevent endometrial hyperplasia or carcinoma.
Store in a cool, dry place, away from direct light and heat; Room temperature (20°C–25°C / 68°F–77°F) is ideal. Keep out of reach of children and pets.
This sheet is a summary. It may not cover all possible drug information about this product. Call your doctor for medical advice and/or about side effects. You may report side effects to the FDA at 1-800-FDA-1088. A Wells Pharmacy Network pharmacist will be happy to answer any questions. For consultation, please call 1-800-622-4510.
