ETHINYL ESTRADIOL
(eth'in-il ess-tra-dye'ole)
Estinyl, Feminone
Classifications: hormones and synthetic substitutes; estrogen
Prototype: Estradiol
Pregnancy Category: X
|
0.02 mg, 0.05 mg, 0.5 mg tablets
Oral estrogen with actions similar to those of estradiol. Given cyclically for short-term use.
Binds to intracellular receptors that stimulate DNA and RNA to synthesize proteins responsible for effects of estrogen.
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.
Postcoital contraceptive.
Breast cancer; known or suspected pregnancy (category X), lactation.
Hypertension; gallbladder disease; diabetes mellitus; heart failure; liver or kidney dysfunction, history of thromboembolic
disease.
Menopause, Postmenopausal Osteoporosis
Adult: PO 0.02–0.05 mg/d for 21 d each month, adjust to lowest level that gives symptom control
Female Hypogonadism
Adult: PO 0.05 mg 1–3 times/d for 2 wk, followed by 2 wk of progestin, continue this regimen for 3–6 mo
Breast Cancer
Adult: PO 1 mg t.i.d. for 2–3 mo
Prostatic Cancer Palliation
Adult: PO 0.15–2 mg/d
Postcoital Contraceptive
Adult: PO 5 mg/d for 5 consecutive days beginning within 72 h of coitus
|
Oral
- 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.
CNS: Headache, dizziness, depression, libido changes. CV: Thromboembolic disorders, hypertension. GI: Nausea, vomiting, diarrhea, anorexia, weight changes, bloating, cholestatic jaundice. Urogenital: Mastodynia, breakthrough bleeding, changes in menstrual flow, dysmenorrhea, amenorrhea; in men: impotence, gynecomastia, testicular
atrophy. Metabolic: Reduced carbohydrate tolerance, fluid retention. Body as a Whole: Leg cramps, edema, intolerance to contact lenses.
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.
Absorption: 83% absorbed. Metabolism: extensively metabolized in liver. Elimination: excreted in urine and feces. Half-Life: 3–27 h.
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 Homan's 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
estradiol levels.
- Report symptoms of vaginal candidiasis (thick, white, curd-like secretions and inflamed congested introitus) to permit appropriate
treatment.
- 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
caffeinism.
- Do not breast feed while taking this drug.
1%)
Canadian drug name; 
Prototype drug