Pregnancy Category X
Estradiol is the most potent endogenous female sex hormone. Estrogens are important in the development of the female reproductive system and secondary sex characteristics; affect the release of pituitary gonadotropins; cause capillary dilatation, fluid retention, protein anabolism and thin cervical mucus; conserve calcium and phosphorus and 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; 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.
- Palliation of moderate to severe vasomotor symptoms, atrophic vaginitis or kraurosis vulvae associated with menopause (estradiol oral, transdermal, cream, estradiol valerate)
- Treatment of female hypogonadism, female castration, primary ovarian failure (estradiol oral, transdermal, estradioll cypionate, valerate)
- Palliation of inoperable prostatic cancer (estradiol oral, estradiol valerate)
- Palliation of inoperable, progressing breast cancer (estradiol oral)
- Prevention of postpartum breast engorgement (estradiol valerate)
Contraindicated in the presence of allergy to estrogens, allergy to
tartrazine (in 2-mg oral tablets), breast cancer (except in specific,
selected patients), estrogen-dependent neoplasm, undiagnosed abnormal
genital bleeding, active thrombophlebitis or thromboembolic disorders
history of such from previous estrogen use, pregnancy (associated with serious fetal defects; women of childbearing ageshould be advised of the potential risks and birth control measures suggested).
Use caution in the presence of metabolic bone disease, renal insufficiency, CHF, lactation.
- CNS: Steepening of the corneal curvature with a resultant change in visual acuity and intolerance to contact lenses, headache, migraine, dizziness, mental depression, chorea, convulsions
- GI: Gallbladder disease (in postmenopausal women), hepatic adenoma, nausea, vomiting, abdominal cramps, bloating, cholestatic jaundice, colitis, acute pancreatitis
- CV: Increased blood pressure, thromboembolic and thrombotic disease
- Hematologic: Hypercalcemia, decreased glucose tolerance
- GU: 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
- Dermatologic: Photosensitivity, peripheral edema, chloasma, erythema nodosum or multiforme, hemorrhagic eruption, loss of scalp hair, hirsutism, urticaria, dermatitis
- Local: Pain at injection site, sterile abscess, postinjection flare
- Other: Weight changes, reduced carbohydrate tolerance, aggravation of por-phyria, edema, changes in libido, breast tenderness
Topical Vaginal Cream
- Systemic absorption may cause uterine bleeding in menopausal women and may cause serious bleeding of remaining endometrial foci in sterilized women with endometriosis.
Are you a Doctor, Pharmacist, PA or a Nurse?
Join the Doctors Lounge online medical community
Editorial activities: Publish, peer review, edit online articles.
Ask a Doctor Teams: Respond to patient questions and discuss challenging presentations with other members.