ETHINYL ESTRADIOL

ETHINYL ESTRADIOL
(eth'in-il ess-tra-dye'ole)
Estinyl, Feminone
Classifications: hormone; estrogen;
Therapeutic: estrogen; female hormone replacement therapy (hrt)

Prototype: Estradiol
Pregnancy Category: X

Availability

0.02 mg, 0.05 mg, 0.5 mg tablets

Action

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.

Therapeutic Effect

May be used to prevent osteoporosis and relieve symptoms associated with menopause.

Uses

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.

Unlabeled Uses

Postcoital contraceptive.

Contraindications

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.

Cautious Use

Hypertension; gallbladder disease; diabetes mellitus; kidney dysfunction.

Route & Dosage

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

Administration

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.

Adverse Effects (≥1%)

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.

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.

Pharmacokinetics

Absorption: 83% absorbed. Metabolism: Extensively metabolized in liver. Elimination: In urine and feces. Half-Life: 3–27 h.

Nursing Implications

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 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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