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Estradiol ER

Class
Sex hormones
Subclass
Estrogens
Substance name
Estradiol ER
Common formulations
Patch
See also
Estradiol (Estrace®, Yuvafem®, Estrogel®)
Estradiol cypionate (Depo-Estradiol®)
Estradiol valerate (Delestrogen®)
Dosage and administration
Adults patients
Treatment
Hypoestrogenism in females • Due to hypogonadism, due to primary ovarian failure, due to castration
•
0.025 mg TD daily patch applied to the skin × 1 weekly
Taper at 3-6-month intervals.
Prevention
Prevention of osteoporosis in postmenopausal females
•
0.025 mg TD daily patch applied to the skin × 1 weekly
Taper at 3-6-month intervals.
Other off-label uses
•
Treatment of gender dysphoria
Indications for use
Labeled indications
Adults
•
Treatment of hypoestrogenism in females (due to hypogonadism, due to primary ovarian failure, due to castration)
•
Treatment of vasomotor symptoms (moderate-to-severe)
•
Treatment of vulvovaginal atrophy
•
Prevention of osteoporosis in postmenopausal females
Off-label indications
Adults
•
Treatment of gender dysphoria
Safety risks
Boxed warnings
Breast cancer, ovarian cancer, endometrial cancer
DVT, PE, stroke
Contraindications
Hypersensitivity to estradiol or its components
Hereditary angioedema
Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
Recent or active arterial thromboembolic disease
Undiagnosed abnormal uterine bleeding
Warnings and precautions
Dementia
•
Use caution in all patients especially healthy postmenopausal women.
Exacerbation of hypertriglyceridemia
•
Use caution in patients with pre-existing hypertriglyceridemia.
Fluid retention
•
Use caution in patients with a condition(s) that might predispose her to fluid retention, such as cardiac or renal impairment.
Gallbladder disease
•
Use caution in all patients especially postmenopausal women.
Increased serum calcium
•
Use caution in patients with breast cancer and bone metastases.
Retinal vascular thrombosis
•
Use caution in all patients.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
No guidance available. Monitor for fluid retention.
Renal replacement therapy
Any modality
•
No guidance available.
Hepatic impairment
Any severity
•
Do not use.
Pregnancy and breastfeeding
Breastfeeding
Use only if benefits outweigh potential risks.
Very low levels in breastfed infants (< 5%).
May potentially cause adverse effects in breastfed infants.
Significant adverse effects on lactation reported.
Adverse reactions
Very common > 10%
•
Breast tenderness, edema, osteoarthritis, osteoarthritis, raynaud's phenomenon, abdominal pain, breast pain, headache, pain, sinusitis, skin erythema, upper respiratory tract infections
Common 1-10%
•
Dry eye disease, dry eye disease, leukorrhea, pharyngitis, anxiety, back pain, depression, diarrhea, flatulence, generalized pruritus, nausea, weight gain, rhinitis
Unknown frequency
•
Anaphylaxis, angioedema, asthma exacerbation, breast cancer, candidiasis, cerebrovascular accident, coagulation disorder, cognitive impairment, corneal pathology, dementia, endometrial cancer, endometrial hyperplasia, endometriosis, erythema multiforme, fibrocystic breast changes, fluid retention, gynecomastia, hepatic hemangioma, hepatitis, hirsutism, hypertension, ↑ serum calcium, ↑ serum triglycerides, influenza, jaundice, leukorrhea, meningioma, migraine, myocardial infarction, ovarian cancer, pulmonary embolism, pharyngitis, porphyria, pulmonary lymphangioleiomyomatosis, arthralgia, bloating, galactorrhea, generalized pruritus, hair loss, menstrual irregularity, vaginal irritation, vomiting, retinal vein thrombosis, systemic lupus erythematosus, silent myocardial ischemia, sinusitis, thrombocytopenia purpura, thrombophlebitis, upper respiratory tract infections, venous thromboembolism
Interactions
Drug(s)
Check Interactions
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