Estradiol

DEA Class; Rx

Common Brand Names; Estrace, Vivelle-Dot, Delestrogen, DepoEstradiol, Divigel, Elestrin, Alora, Estrace Cream, Estraderm Transdermal, estradiol topical, Estradot, Estrasorb, Estrogel, Evamist, Femtrace, Menostar, Minivelle, Vivelle, Climara

Indicated for treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae), whether menopause is natural or surgical (e.g., due to oophorectomy).

Documented hypersensitivity

Known anaphylactic reaction or angioedema with topical emulsion

Known protein C, protein S, or antithrombin deficiency or other known thrombophilic disorder

Active or previous breast cancer

Arterial thromboembolic disease (stroke, myocardial infarction [MI]), thrombophlebitis, DVT/PE, thrombogenic valvular disease

Estrogen-dependent neoplasia

Uncontrolled hypertension, diabetes mellitus with vascular involvement, jaundice with previous oral contraceptive (OC) use

Undiagnosed abnormal vaginal bleeding

Liver disease, liver tumors

Severe anaphylactic reactions including hives , pruritus, swollen lips-tong-face, respiratory compromise, abdominal pain, vomiting during transdermal treatment reported

Increased risks of stroke and DVT reported with estrogen-alone and estrogen plus progestin therapy; immediately discontinue estrogen with or without progestogen if any of these occur or are suspected

Use caution in patients with family history of breast cancer or DVT/PE; current or previous depression, endometriosis, diabetes mellitus, hypertension, bone mineral density changes, renal or hepatic impairment, bone metabolic disease, systemic lupus erythematosus; conditions exacerbated by fluid retention (eg, migraine, asthma, epilepsy)

Discontinue if the following develop: Jaundice, visual problems (may cause contact lens intolerance), any signs of venous thromboembolism, migraine with unusual severity, significang blood pressure increase, severe depression, increased risk of thromboembolic complications after surgery

Discontinue 4 weeks before major surgery or prolonged immobilization

Patients on warfarin or other oral anticoagulants (increase in anticoagulant dose may be warranted)

Some studies link OC use with increased risk of breast cancer, whereas other studies have not shown any change in risk; risk depends on conditions where naturally high hormone levels persist for long periods, including early-onset menstruation (<12 years), late-onset menopause (>55 years), first child after age 30 years, nulliparity

Increased risk of ovarian cancer reported in women who used hormonal therapy for menopausal symptoms

Increased risk of cervical cancer with OC use; however human papillomavirus (HPV) remains main risk factor for this cancer; evidence suggests long-term (≥5 years) use of OCs may be associated with increased risk

Increased risk of liver cancer with OC use; risk increases with longer duration of use

Hypercalcemia may occur in patients with breast cancer or bone metastases; discontinue therapy if hypercalcemia occurs, and take appropriate measures to reduce serum calcium level

Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema; consider whether benefits of estrogen therapy outweigh the risks in such women

Angioedema involving eye/eyelid, face, larynx, pharynx, tongue and extremity (hands, legs, ankles, and fingers) with or without urticaria reported; discontinue therapy permanently if angioedema occurs

Femring is more potent than Estring and should be used with progesterone therapy to prevent endometrial hyperplasia

Caution regarding unintentional exposure in children (see Black Box Warnings)

Clinical surveillance of all women using estrogen-alone or estrogen plus progestogen therapy important; perform adequate diagnostic measures, including directed or random endometrial sampling when indicated to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding with unknown etiology

Therapy not indicated for use in pregnancy; there are no data with use in pregnant women; however, epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to combined hormonal contraceptives (estrogen and progestins) before conception or during early pregnancy

Therapy not indicated for use in females of reproductive potential; estrogens present in human milk and can reduce milk production in breast-feeding females; reduction can occur at any time but is less likely to occur once breast-feeding is well- established