Estradiol Pellets

Available Dosage Strengths

10 mg | 12.5 mg | 15 mg | 18 mg | 20 mg | 25 mg

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Product Overview

Description

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

Mechanism of Action

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.

Adverse Reactions

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 & Precautions

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.

Storage

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.

References

Cynthia A. Stuenkel, Susan R. Davis, Anne Gompel, Mary Ann Lumsden, M. Hassan Murad, JoAnn V. Pinkerton, Richard J. Santen, Treatment of Symptoms of the Menopause: An Endocrine Society Clinical Practice Guideline, The Journal of Clinical Endocrinology & Metabolism, Volume 100, Issue 11, 1 November 2015, Pages 3975–4011, accessed July 2025 through: https://doi.org/10.1210/jc.2015-2236
FDA Drug Label – Estradiol cream by Teva Pharmaceuticals accessed July 2025 through: https://fda.report/DailyMed/8cb31c7c-fba8-4201-833d-844ea1a8a4de
MedlinePlus Drug Information – Estradiol: https://medlineplus.gov/druginfo/meds/a605021.html
North American Menopause Society (NAMS) Position Statement (2022): “The 2022 Hormone Therapy Position Statement of The North American Menopause Society” https://www.menopause.org/docs/default-source/professional/2022-nams-ht-position-statement.pdf
Sobel TH, Shen W. Transdermal estrogen therapy in menopausal women at increased risk for thrombotic events: a scoping review. Menopause. 2022 Jan 14;29(4):483-490. doi: 10.1097/GME.0000000000001938. PMID: 35357370.
Canonico, M., Oger, E., Plu-Bureau, G., Conard, J., Meyer, G., Lévesque, H., … & Scarabin, P. Y. (2007). Hormone therapy and venous thromboembolism among postmenopausal women: impact of the route of estrogen administration and progestogens: the ESTHER study. Circulation, 115(7), 840-845.
Clinical Pharmacology estradiol clinical monograph accessed July 2025 through: https://www.clinicalkey.com/pharmacology/monograph/1330?n=Estradiol

Disclaimer

This information is for educational purposes only. This compounded product has not been reviewed, approved, or evaluated by the Food and Drug Administration for safety and effectiveness. This product is not intended to diagnose, treat, cure, or prevent any disease. No claims are made regarding treatment, cure, or prevention of any disease or condition.

This information 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.