REMS
Contraindicated in:
Thromboembolic disease (e.g., deep vein thrombosis, pulmonary embolism, MI, stroke)
;Protein C, protein S, or antithrombin deficiency or other thrombophilic disorder
;History of breast cancer
;History of estrogen-dependent cancer
;Undiagnosed vaginal bleeding
;Use Cautiously in:
Long-term use (more than 4–5 yr); may ↑ risk of MI, stroke, invasive breast cancer, pulmonary emboli (PE), deep vein thrombosis (DVT), and dementia in postmenopausal women
;Underlying cardiovascular disease
;CV: edema, hypertension, DVT, MI
Derm: oily skin, acne, pigmentation, urticaria
EENT: intolerance to contact lenses, worsening of myopia or astigmatism
Endo: gynecomastia (men), hyperglycemia
F and E: hypercalcemia, sodium and water retention
GI: nausea, weight changes, anorexia, jaundice, vomiting
GU: womenamenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosions, loss of libido, vaginal candidiasis;, menerectile dysfunction, testicular atrophy.
MS: leg cramps
Neuro: headache,
dementia
, dizziness, lethargy, STROKEResp: PE
Misc: breast tenderness, MALIGNANCY (BREAST, ENDOMETRIAL, OVARIAN)
Drug-drug:
Estradiol
Estradiol Cypionate
Estradiol Transdermal Preparations
Estradiol Vaginal Preparations
Estradiol Valerate
Estrogens should be used in the lowest doses for the shortest period of time consistent with desired therapeutic outcome. Concurrent use of progestin is recommended during cyclical therapy to ↓ the risk of endometrial carcinoma in patients with an intact uterus.
Symptoms of Menopause, Atrophic Vaginitis, Moderate to Severe Dyspareunia, Female Hypogonadism, Ovarian Failure/Osteoporosis
Postmenopausal Breast Cancer
Prostate Cancer
estradiol cypionate: Depo-Estradiol,
estradiol tablets: Estrace,
estradiol transdermal gel: Divigel, Elestrin, EstroGel,
estradiol transdermal spray: EvaMist,
estradiol transdermal system : Alora, Climara, Dotti, Estraderm, Lyllana, Menostar, Minivelle, Vivelle-Dot,
estradiol vaginal cream: Estrace,
estradiol vaginal insert: Imvexxy,
estradiol vaginal ring: Estring, Femring,
estradiol vaginal tablet: Vagifem, Yuvafem,
estradiol valerate: Delestrogen
Absorption: Well absorbed after oral administration. Readily absorbed through skin and mucous membranes.
Distribution: Widely distributed to tissues.
Half-Life: Gel: 36 hr.
(estrogenic effects)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | unknown | unknown | unknown |
| IM | unknown | unknown | unknown |
| Transdermal | unknown | unknown | 3–4 days (Estraderm), 7 days (Climara) |
| Topical | unknown | unknown | unknown |
| Vaginal insert | unknown | unknown | 3–4 days |
| Vaginal ring | unknown | unknown | 90 days |
Advise patient to report signs and symptoms of thromboembolic disorders (pain, swelling, tenderness in extremities, headache, chest pain, blurred vision).
Inform postmenopausal women that long-term use may ↑ risk of MI, stroke, invasive breast cancer, PE, DVT, and dementia.
Emphasize the importance of routine follow-up physical exams, including BP check; breast, abdomen, and pelvic examinations; Papanicolaou smears every 6–12 mo; and mammogram every 12 mo or as directed. Health care provider will evaluate possibility of discontinuing medication every 3–6 mo. If on continuous (not cyclical) therapy or without concurrent progestins, endometrial biopsy may be recommended, if uterus is intact.
Inform patient that estrogens should not be used to ↓ risk of cardiovascular disease or dementia. Estrogens may ↑ risk of cardiovascular disease (MI, stroke), dementia, and breast cancer.
NDC Code