Estradiol Hemihydrate

estradiol hemihydrate

Brand Name: Vagifem

Pregnancy Category X

Drug classes: Hormone, Estrogen

 

Therapeutic actions

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; relief in androgen-dependent prostatic carcinoma is attributable to competition with androgens for receptor sites, decreasing the influence of androgens.

 

Indications

· Palliation of moderate to severe vasomotor symptoms, atrophic vaginitis or kraurosis vulvae associated with menopause; prevention of postmenopausal osteoporosis (estradiol oral, transdermal, cream, estradiol valerate)

· Treatment of female hypogonadism, female castration, primary ovarian failure (estradiol oral, transdermal, estradiol cypionate, valerate)

· Palliation of inoperable prostatic cancer (estradiol oral, estradiol valerate)

· Palliation of inoperable, progressing breast cancer (estradiol oral)

 

Contraindications

· Contraindicated with allergy to estrogens, allergy to tartrazine (in 2-mg oral tablets), breast cancer (with exceptions), estrogen-dependent neoplasm, undiagnosed abnormal genital bleeding, active or past history of thrombophlebitis or thromboembolic disorders (potential serious fetal defects; women of childbearing age should be advised of risks and birth control measures suggested).

 

Adverse effects

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 postmenopausal endometrial cancer, 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 may cause serious bleeding of remaining endometrial foci in sterilized women with endometriosis.

 

Drug Interactions:

· Increased therapeutic and toxic effects of corticosteroids

· Decreased serum levels of estradiol with drugs that enhance hepatic metabolism of the drug: barbiturates, phenytoin, rifampin

Nursing considerations

· 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 of estrogen use, the need to prevent pregnancy during treatment, for frequent medical follow-up, and for periodic rests from drug treatment.

· Administer 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.

· Apply transdermal system to a clean, dry area of skin on the trunk of the body, preferably the abdomen; do not apply to breasts; rotate the site at least 1 wk between applications; avoid the waistline because clothing may rub the system off; apply immediately after opening and compress for about 10 sec to attach.

· Insert vaginal ring as deeply as possible into upper one-third of vagina. Ring will remain in place for 3 months. Then, remove and evaluate need for continued therapy. If a ring falls out during 3 mo, rinse with warm water and reinsert.

· Arrange for the concomitant use of progestin therapy during long-term estrogen therapy; this will mimic normal physiologic cycling and allow for a cyclic uterine bleeding that may decrease the risk of endometrial cancer.

· Administer parenteral preparations by deep IM injection only. Monitor injection sites and rotate with each injection to decrease development of abscesses.