No

Estrogen Derivative

Hypogonadism; primary ovarian failure; vasomotor symptoms of menopause; prostatic carcinoma; breast cancer

X

Thrombophlebitis, undiagnosed vaginal bleeding, hypersensitivity to ethinyl estradiol or any component, pregnancy, estrogen-dependent neoplasia

Use with caution in patients with asthma, seizure disorders, migraine, cardiac, renal or hepatic impairment, cerebrovascular disorders or history of breast cancer, past or present thromboembolic disease, smokers >35 years of age

>10%:

Cardiovascular: Peripheral edema

Endocrine & metabolic: Enlargement of breasts, breast tenderness, bloating

Gastrointestinal: Nausea, anorexia

1% to 10%:

Central nervous system: Headache

Endocrine & metabolic: Increased libido

Gastrointestinal: Vomiting, diarrhea

<1%: Hypertension, thromboembolism, myocardial infarction, edema, stroke, depression, dizziness, anxiety, chloasma, melasma, rash, breast tumors, amenorrhea, alterations in frequency and flow of menses, decreased glucose tolerance, increased triglycerides and LDL, GI distress, cholestatic jaundice, intolerance to contact lenses, increased susceptibility to Candida infection

Symptoms of overdose include fluid retention, jaundice, thrombophlebitis, nausea

Toxicity is unlikely following single exposures of excessive doses, any treatment following emesis and charcoal administration should be supportive and symptomatic

CYP3A3/4 and 3A5-7 enzyme substrate; CYP1A2 enzyme inhibitor

Carbamazepine, tricyclic antidepressants, and corticosteroids

Increased thromboembolic potential with oral anticoagulants

Decreased efficacy:

Nelfinavir decreases ethinyl estradiol concentrations

Increases the synthesis of DNA, RNA, and various proteins in target tissues; reduces the release of gonadotropin-releasing hormone from the hypothalamus; reduces FSH and LH release from the pituitary

Absorption: Absorbed well from GI tract

Protein binding: 50% to 80%

Metabolism: Inactivated by liver

Elimination: By the kidneys

Adults: Oral:

Female:

Hypogonadism: 0.05 mg 1-3 times/day during the first 2 weeks of a theoretical menstrual cycle. Follow with a progesterone during the last half of the arbitrary cycle. Continue for 3-6 months. The patient should not be treated for the following 2 months.

Vasomotor symptoms: Usual dosage range: 0.02-0.05 mg/day; give cyclically for short-term use only and use the lowest dose that will control symptoms. Discontinue as soon as possible and administer cyclically (3 weeks on and 1 week off). Attempt to discontinue or taper medication at 3- to 6-month intervals.

Breast cancer (inoperable, progressing): 1 mg 3 times/day for palliation

Dosing adjustment in hepatic impairment:

Mild to moderate liver impairment: Dosage reduction of estrogens is recommended

Severe liver impairment: Not recommended

Decreased antithrombin III

Decreased serum folate concentration

Increased prothrombin and factors VII, VIII, IX, X

Increased platelet aggregability

Increased thyroid binding globulin

Increased total thyroid hormone (T₄)

Increased serum triglycerides/phospholipids

May rarely cause anxiety or depression

None reported

No information available to require special precautions

No effects or complications reported

Take according to recommended schedule. It is important to maintain schedule of drug days and drug-free days. Periodic gynecologic exam and breast exams for females are important. You may experience nausea or vomiting (small frequent meals may help); dizziness or mental depression (use caution when driving); rash; loss of scalp hair; enlargement/tenderness of breasts; or increased/decreased libido. Report significant swelling in extremities, sudden acute pain in legs or calves, chest, or abdomen; shortness of breath; severe headache or vomiting; weakness or numbness of arms or legs; or unusual vaginal bleeding. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Consult prescriber if breast-feeding.

Administer at bedtime to minimize occurrence of adverse effects

Tablet: 0.02 mg, 0.05 mg, 0.25 mg, 0.5 mg

American College of Physicians, "Guidelines for Counseling Postmenopausal Women About Preventive Hormone Therapy," Ann Intern Med, 1992, 117(12):1038-41.

Belchetz PE, "Hormonal Treatment of Postmenopausal Women," N Engl J Med, 1994, 330 (15): 1062-71.

Collins P, Rosano GM, Sarrel PM, et al, "17 b-Estradiol Attenuates Acetylcholine-Induced Coronary Arterial Constriction in Women but Not Men With Coronary Heart Disease," Circulation, 1995, 92(1):24-30.

Ettinger B, Friedman GD, Bush T, et al, "Reduced Mortality Associated with Long-Term Postmenopausal Estrogen Therapy," Obstet Gynecol, 1996, 87(1):6-12.

Goldzieher JW and Brody SA, "Pharmacokinetics of Ethinyl Estradiol and Mestranol," Am J Obstet Gynecol, 1990, 163(6 Pt 2):2114-9.

The Writing Group for the PEPI Trial, "Effects of Estrogen or Estrogen/Progestin Regimens on Heart Disease Risk Factors in Postmenopausal Women," JAMA, 1995, 273(3):199-208.