estradiol cypionate
estradiol valerate (oestradiol valerate)
Pregnancy Risk Category X
How supplied
estradiol
Tablets (micronized): 0.5 mg, 1 mg, 2 mg
Transdermal: 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours; 0.075 mg/24 hours; 0.1 mg/24 hours; 4 mg/10 cm2 (delivers 0.05 mg/24 hours); 8 mg/20 cm2
Vaginal cream (in nonliquefying base): 0.1 mg/g
estradiol cypionate
Injection (in oil): 1 mg/ml, 5 mg/ml
estradiol valerate
Injection (in oil): 10 mg/ml, 20 mg/ml, 40 mg/ml
Action
Increases synthesis of DNA, RNA, and protein in responsive tissues. Also reduces release of follicle-stimulating and luteinizing hormones from the pituitary gland.
Indications & dosage
Vasomotor menopausal symptoms, female hypogonadism, female castration, primary ovarian failure--
Women: 0.5 to 2 mg P.O. (estradiol) daily in cycles of 21 days on and 7 days off; or cycles of 5 days on and 2 days off; or one transdermal system (Estraderm) delivering 0.05 mg/24 hours applied twice weekly; or as a system (Vivelle) delivering either 0.05 mg/24 hours or 0.0375 mg/24 hours applied twice weekly; or as a system (Climara) delivering either 0.05 mg/
24 hours or 0.1 mg/24 hours and applied once weekly, in cycles of 3 weeks on and 1 week off.
Note: Transdermal systems are sometimes used on a continuous basis (not cyclic). Or, 1 to 5 mg (cypionate) I.M. q 3 to 4 weeks; or 10 to 20 mg (valerate) I.M. q 4 weeks, p.r.n.
Atrophic vaginitis, kraurosis vulvae--
Women: 0.05 mg/24 hours (Estraderm) applied twice weekly in a cyclic regimen; or 0.05 mg/24 hours (Climara) applied weekly in a cyclic regimen; or 2 to 4 g intravaginal applications of cream daily for 1 to 2 weeks. When vaginal mucosa is restored, maintenance dose is 1 g one to three times weekly in a cyclic regimen. Or, 10 to 20 mg (valerate) I.M. q 4 weeks, p.r.n.
Palliative treatment of advanced, inoperable breast cancer--
Men and postmenopausal women: 10 mg P.O. (estradiol) t.i.d. for 3 months.
Palliative treatment of advanced, inoperable prostate cancer--
Men: 30 mg (valerate) I.M. q 1 to 2 weeks, or 1 to 2 mg P.O. (estradiol) t.i.d.
NEW INDICATION: Prevention of postmenopausal osteoporosis--
Adults: place a 6.5-cm2 (0.025 mg/day) Climara system once weekly on clean, dry skin area of lower abdomen or upper quadrant of buttock; press firmly in place for about 10 seconds, making sure contact is good, especially around edges.
Adverse reactions
CNS: headache, dizziness, chorea, depression, seizures.
CV: thrombophlebitis, thromboembolism, hypertension, edema; increased risk of CVA, pulmonary embolism, MI.
EENT: worsening myopia or astigmatism, intolerance of contact lenses.
GI: nausea, vomiting, abdominal cramps, bloating, increased appetite, pancreatitis, anorexia.
GU: breakthrough bleeding, altered menstrual flow, dysmenorrhea, amenorrhea, increased risk of endometrial cancer, cervical erosion, altered cervical secretions, enlargement of uterine fibromas, vaginal candidiasis in women; gynecomastia, testicular atrophy, impotence in men.
Hematologic: increased PT and clotting factors VII to X, and norepinephrine-induced platelet aggregation.
Hepatic: cholestatic jaundice, hepatic adenoma.
Metabolic: weight changes.
Skin: melasma, urticaria, erythema nodosum, dermatitis, hair loss.
Other: gallbladder disease; breast tenderness, enlargement, or secretion; possible increased risk of breast cancer.
Interactions
Drug-drug. Carbamazepine, phenobarbital, rifampin: decreased effectiveness of estrogen therapy. Monitor closely.
Corticosteroids: possible enhanced effects of corticosteroids. Monitor closely.
Cyclosporine: increased risk of toxicity. Use together with caution and monitor cyclosporine levels frequently.
Dantrolene, other hepatotoxic drugs: increased risk of hepatotoxicity. Monitor closely.
Oral anticoagulants: effect of anticoagulant may be decreased. Dosage adjustments may be needed. Monitor PT and INR, as ordered.
Tamoxifen: estrogens may interfere with effectiveness of tamoxifen. Avoid concomitant use.
Drug-food. Caffeine: may increase serum caffeine levels. Monitor effects.
Drug-lifestyle. Smoking: increased risk of adverse CV effects. If smoking continues, may need alternative therapy.
Effects on diagnostic tests
Glucose tolerance may be impaired. There may be a reduced response to metyrapone test.
Contraindications
Contraindicated in patients with thrombophlebitis or thromboembolic disorders, estrogen-dependent neoplasia, breast or reproductive organ cancer (except for palliative treatment), undiagnosed abnormal genital bleeding, or history of thrombophlebitis or thromboembolic disorders associated with previous estrogen use (except for palliative treatment of breast and prostate cancer); also contraindicated during pregnancy.
Nursing considerations
Patient teaching
*Liquid contains alcohol. **May contain tartrazine. †Canada ‡Australia §U.K. OTCOver the counter
Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE-THREATENING