Depo® Estradiol Cypionate

(Commercial Product) Injection, USP

5 mg/mL

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Product Overview

Estradiol Cypionate Description1,2,3

Estradiol Cypionate is a long-acting injectable ester of 17β-estradiol, the primary estrogen produced by the ovaries in premenopausal women. It is formulated for intramuscular (IM) administration, usually in oil-based solutions that provide slow release and extended systemic activity.

References

  1. Clinical Pharmacology (Elsevier) – Estradiol Cypionate Monograph; accessed August 2025 through: https://www.clinicalkey.com/pharmacology/monograph/1330?n=Estradiol
  2. FDA Label – Depo-Estradiol (estradiol cypionate injection); accessed August 2025 through: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009747s037lbl.pdf
  3. MedlinePlus – Estradiol Injection (systemic) accessed August 2025 through: https://medlineplus.gov/druginfo/meds/a682750.html

Mechanism of Action1,2,3

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, which may lead to a broad range of systemic and local effects:

  • Endometrial proliferation in the absence of a progesterone or progestogen.
  • Negative feedback on the hypothalamic-pituitary axis (reduces FSH and LH)
  • Maintenance of bone density via inhibition of bone resorption
  • Thermoregulatory stabilization, reducing hot flashes and night sweats
  • Cardiovascular and lipid effects (e.g., improves HDL/LDL ratio)
  • Neurotransmitter modulation affecting mood and cognition

Common1,2,3

  • Breast tenderness
  • Nausea
  • Headache
  • Fluid retention
  • Bloating
  • Mood changes
  • Breakthrough vaginal bleeding or spotting
  • Injection site discomfort

Absolute Contraindications1,2,3

  • Known or suspected breast cancer or estrogen-dependent neoplasia
  • Undiagnosed abnormal genital bleeding
  • Active or history of thromboembolic disorders (e.g., DVT, PE, stroke)
  • Active liver dysfunction or disease
  • Known hypersensitivity to estradiol cypionate or its formulation components (e.g., sesame oil)

Precautions1,2,3

  • Women with a history of hormone-sensitive cancers
  • Hypertension or cardiovascular disease
  • Migraine with aura
  • Diabetes mellitus
  • Hypertriglyceridemia
  • In women with an intact uterus, a progestogen must be co-administered to reduce the risk of endometrial hyperplasia and cancer.
  • Routine monitoring of breast, pelvic, and cardiovascular health is advised during therapy.
  • Store at controlled room temperature (20°C to 25°C / 68°F to 77°F)
  • Protect from moisture and light
  • Keep in a tightly closed container
  1. Clinical Pharmacology (Elsevier) – Estradiol Cypionate Monograph; accessed August 2025 through: https://www.clinicalkey.com/pharmacology/monograph/1330?n=Estradiol
  2. FDA Label – Depo-Estradiol (estradiol cypionate injection); accessed August 2025 through: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009747s037lbl.pdf
  3. MedlinePlus – Estradiol Injection (systemic) accessed August 2025 through: https://medlineplus.gov/druginfo/meds/a682750.html
This information is for educational purposes only.
WP Pharma Labs distributes certain FDA-approved commercial products that are manufactured by third-party pharmaceutical companies. These products are not compounded or manufactured by WP Pharma Labs. Product availability at the time of dispensing may vary due to supply chain conditions.
This information is a summary. It may not cover all possible drug information about this product. For complete product information, refer to the manufacturer’s prescribing information and labeling. 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 WP Pharma Labs pharmacist will be happy to answer any questions. For consultation, please call 1-800-441-0048.

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