Pregnancy Category X
Drug classes: Hormone, Estrogen
Estrogens are endogenous female sex hormones important in the development of the female reproductive system and secondary sex characteristics. They affect the release of pituitary gonadotropins; cause capillary dilatation, fluid retention, protein anabolism, and thin cervical mucus; conserve calcium and phosphorus; encourage bone formation; inhibit ovulation and prevent postpartum breast discomfort. They are responsible for the proliferation of the endometrium; absence or decline of estrogen produces signs and symptoms of menopause on the uterus, vagina, breasts, cervix. Their efficacy as palliation in male patients with androgen-dependent prostatic carcinoma is attributable to their competition with androgens for receptor sites, thus decreasing the influence of androgens.
· Oral palliation of moderate to severe vasomotor symptoms, atrophic vaginitis, or kraurosis vulvae associated with menopause
· Treatment of female hypogonadism; female castration; primary ovarian failure
· Osteoporosis: to retard progression
· Palliation of inoperable prostatic cancer
· Palliation of mammary cancer
· Treatment of moderate to severe vasomotor symptoms associated with menopause (Cenestin)
· Unlabeled use: postcoital contraceptive
· Parenteral: treatment of uterine bleeding due to hormonal imbalance in the absence of organic pathology
· Vaginal cream: treatment of atrophic vaginitis and kraurosis vulvae associated with menopause
· Contraindicated with allergy to estrogens, breast cancer (with exceptions), estrogen-dependent neoplasm, undiagnosed abnormal genital bleeding, active or past thrombophlebitis or thromboembolic disorders from previous estrogen use, pregnancy (serious fetal defects; women of childbearing age should be advised of risks and birth control measures suggested).
Steepening of the corneal curvature with a resultant change in visual acuity and intolerance to contact lenses, headache, migraine, dizziness, mental depression, chorea, convulsions
Increased blood pressure, thromboembolic and thrombotic disease
Photosensitivity, peripheral edema, chloasma, erythema nodosum or multiforme, hemorrhagic eruption, loss of scalp hair, hirsutism, urticaria, dermatitis
Gallbladder disease (in postmenopausal women), hepatic adenoma, nausea, vomiting, abdominal cramps, bloating, cholestatic jaundice, colitis, acute pancreatitis
Increased risk of endometrial cancer in postmenopausal women, breakthrough bleeding, change in menstrual flow, dysmenorrhea, premenstrual-like syndrome, amenorrhea, vaginal candidiasis, cystitis-like syndrome, endometrial cystic hyperplasia
Hypercalcemia, decreased glucose tolerance
Pain at injection site, sterile abscess, postinjection flare
Weight changes, reduced carbohydrate tolerance, aggravation of porphyria, edema, changes in libido, breast tenderness
Topical vaginal cream
Systemic absorption may cause uterine bleeding in menopausal women and serious bleeding of remaining endometrial foci in sterilized women with endometriosis.
· Increased therapeutic and toxic effects of corticosteroids
· Decreased serum levels of estrogen with drugs that enhance hepatic metabolism of the drug: barbiturates, phenytoin, rifampin
· Arrange for pretreatment and periodic (at least annual) history and physical, which should include BP, breasts, abdomen, pelvic organs, and a Pap smear.
· Caution patient of the risks involved with estrogen use, the need to prevent pregnancy during treatment, for frequent medical follow-up, and periodic rests from drug treatment.
· Give cyclically for short term only when treating postmenopausal conditions because of the risk of endometrial neoplasm; taper to the lowest effective dose, and provide a drug-free week each month.
· Refrigerate unreconstituted parenteral solution; use reconstituted solution within a few hours.
· Refrigerated reconstituted solution is stable for 60 days; do not use solution if darkened or precipitates have formed.
· Arrange for the concomitant use of progestin therapy during long-term estrogen therapy in women; this will mimic normal physiologic cycling and allow for cyclic uterine bleeding, which may decrease the risk of endometrial cancer.