Classifications: hormone; estrogen; Therapeutic: estrogen; female hormone replacement therapy (hrt)
Pregnancy Category: X
0.02 mg, 0.05 mg, 0.5 mg tablets
Potent oral estrogen with actions similar to those of estradiol. Given cyclically for short-term use. Ethinyl estradiol is
not commonly used as a single agent, but most commonly found in combination oral contraceptives.
May be used to prevent osteoporosis and relieve symptoms associated with menopause.
Moderate to severe vasomotor symptoms associated with menopause; also postmenopausal osteoporosis, female hypogonadism, and
as palliation for inoperable, metastatic cancer of female breast (at least 5 y postmenopause) and of the prostate.
Breast, ovarian, cervical, or endometrial cancer; endometrial hyperplasia; uterine or vaginal cancer; abnormal vaginal bleeding;
hepatic disease or cancer; jaundice; MI; history of thromboembolic disease; heart failure; coagulopathies; lupus; known or
suspected pregnancy (category X), lactation.
Hypertension; gallbladder disease; diabetes mellitus; kidney dysfunction.
Route & Dosage
|Menopause, Postmenopausal Osteoporosis
Adult: PO 0.020.05 mg/d for 21 d each month, adjust to lowest level that gives symptom control
Adult: PO 0.05 mg 13 times/d for 2 wk, followed by 2 wk of progestin, continue this regimen for 36 mo
Adult: PO 1 mg t.i.d. for 23 mo
Prostatic Cancer Palliation
Adult: PO 0.152 mg/d
Adult: PO 5 mg/d for 5 consecutive days beginning within 72 h of coitus
- Morning-after pill: Start drug within 24 h and not later than 72 h after sexual exposure when used as an emergency postcoital
contraceptive. Perform a pregnancy test prior to dosing.
- Store at 15°30° C (59°86° F) in tight, light-resistant container.
Adverse Effects (≥1%)CNS:
Headache, dizziness, depression
, libido changes. CV: Thromboembolic disorders
, hypertension. GI: Nausea,
, anorexia, weight changes, bloating, cholestatic jaundice
Mastodynia, breakthrough bleeding, changes in menstrual flow, dysmenorrhea, amenorrhea; in men: impotence, gynecomastia, testicular
Reduced carbohydrate tolerance, fluid retention. Body as a Whole:
Leg cramps, edema, intolerance to contact lenses.
Interactions Drug: Carbamazepine, phenytoin, rifampin
decrease estrogen levels because they increase its metabolism
; may enhance steroid effects of corticosteroids
; may decrease anticoagulant effects of oral anticoagulants
83% absorbed. Metabolism:
Extensively metabolized in liver. Elimination:
In urine and feces. Half-Life:
Assessment & Drug Effects
- Check BP on a regular basis in patients with conditions that may be influenced by fluid retention (migraine, cardiac or kidney
dysfunction, asthma, epilepsy, hypertension).
- Supplement pyridoxine (vitamin B6) in patients on long-term therapy, especially if undernourished; levels are lowered by estrogens.
Patient & Family Education
- Be aware that risk of blood clot formation is high. Notify physician immediately of positive Homans' sign (calf pain upon
foot flexion) and the following symptoms of thromboembolic disorders: Tenderness, pain, swelling, and redness in extremity;
sudden, severe headache or chest pain, slurring of speech; change in vision; sudden shortness of breath. If physician is not
available, go to the nearest emergency room.
- Report severe abdominal pain and tenderness, or abdominal mass.
- Determine weight under standard conditions 1 or 2 times/wk and report sudden weight gain or other signs of fluid retention.
- Notify physician of yellow skin and sclera, pruritus, dark urine, and light-colored stools; history of jaundice in pregnancy
increases the possibility of estrogen-induced jaundice. Estrogen therapy is usually interrupted pending clinical investigation.
- Abrupt withdrawal of vitamin C may lead to breakthrough bleeding; high vitamin C intake (e.g., 1 g/d) may increase ethinyl
- Report symptoms of vaginal candidiasis (thick, white, curd-like secretions and inflamed congested introitus) to permit appropriate
- Note: Estrogen-induced feminization and impotence in male patients are reversible with termination of therapy.
- Decrease caffeine intake from sources such as tea, coffee, and cola; estrogenic depression of caffeine metabolism may cause