estradiol (Rx)
Generic: Estradiol
Brand: Estrace
(ess-tra-dye'ole)
Pharmacological Action
Needed for adequate functioning of female reproductive system; affects release of pituitary gonadatropins, inhibits ovulation, promotes adequate calcium use in bone structure
Therapeutic outcome: Decreased tumor size in prostatic cancer; increased estrogen levels in menopause, female hypogonadism
Uses
Vasomotor symptoms associated with menopause, inoperable breast cancer (selected cases), prostatic cancer, atrophic vaginitis, kraurosis vulvae, hypogonadism, primary ovarian failure, prevention of osteoporosis, castration
Contraindications
Pregnancy X, breastfeeding, reproductive cancer, genital bleeding (abnormal, undiagnosed), protein C, S, antithrombin deficiency
BLACK BOX WARNING: Breast/endometrial cancer, thromboembolic disorders, MI, stroke
Precautions: Hypertension, asthma, blood dyscrasias, gallbladder disease, CHF, diabetes mellitus, bone disease, depression, migraine headache, seizure disorders, renal/hepatic disease, family history of cancer of breast or reproductive tract, history of smoking, uterine fibroids, vaginal irritation/infection, accidental exposure of topical products to children/pets, history of angioedema
BLACK BOX WARNING: Cardiac disease, dementia
Dosage & Routes
Hormone replacement/menopause symptoms
Adult: TD 1 patch delivering 0.025, 0.0375, 0.05, 0.075, or 0.1 mg/day 2-3/wk (Alora, Estraderm, Vivelle-Dot); 1 patch delivering 0.025, 0.0375, 0.05, 0.06, 0.075, or 0.1 mg/day replace q7 days (Climara); 1 patch delivering 0.025 mg/day replace q7 days, may increase to 2 patches after 4-6 wk; GEL apply entire unit dose packet to 5- x 7-inch area of upper thigh/day, alternate thighs; SPRAY (Evamist) 1 spray to inner surface of forearm/day in am Menopause/hypogonadism/castration/ovarian failure
Adult: PO 1-2 mg/day 3 wk on, 1 wk off or 5 days on, 2 days off; IM 1-5 mg q3-4 wk (cypionate), 1-5 mg q3-4 wk; 10-20 mg q4 wk (valerate); TOP Estraderm 0.05 mg/24 hr applied 2-3/wk, Climara 0.05 mg/hr applied 1-3/wk in a cyclic regimen; women with hysterectomy may use continuously Prostatic cancer
Adult: IM 30 mg q1-2 wk (valerate); PO 1-2 mg tid (oral estradiol) Breast cancer (palliative treatment)
Adult: PO 10 mg tid x 3 mo or longer Atropic vaginitis/kraurosis vulvae
Adult: VAG cream 2-4 g/day x 1-2 wk, then 1 g 1-3 x/wk cycled; VAG tab 1/day x 2 wk, maintenance 1 tab 2 x/wk; VAG ring inserted and left in place continuously for 3 mo Vasomotor symptoms
Adult: TOP after cleaning and drying skin on left thigh, calf, rub in contents of pouch using both hands until completely absorbed; wash hands
Available forms:
Estradiol: tabs 0.5, 1, 2 mg; valerate: inj 10, 20, 40 mg/ml; transdermal 0.025, 0.0375, 0.05, 0.06, 0.075, 0.1 mg/24-hr release rate; vag cream 100 mcg/g; vag ring 2 mg/90 days; vag tab 10 mcg; topical emulsion: 2.5 mg; gel 0.1% (Divigel); spray (Evamist) 1.53 mg/acuation
Implementation PO route - Give titrated dose, use lowest effective dose - Give with food or milk to decrease GI symptoms IM route - Administer deeply in large muscle mass; product is painful - Rotate syringe to mix oil and medication Transdermal route - May contain aluminum or other metals in backing of patch, can overheat in MRI scan and burn patients - Apply to area free of hair to ensure adhesion on trunk of body 2-3/wk; press firmly and hold in place for 10 sec to ensure good contact; do not apply to breasts - Start transdermal dose 7 days before last PO dose if routes are to be changed Topical route spray (Evamist) - Use daily; spray to inner upper arm; may increase to 2-3 x/day based on response; let dry for 2 min, avoid secondary exposure to children, pets, caregivers Vaginal route - Place cream in applicator by attaching tube to applicator; squeeze cream into tube to mark; insert with patient reclining - Use a new applicator daily
Adverse Effects
CNS: Dizziness, headache, migraine, depression, seizures
CV: Hypertension, thrombophlebitis, edema, thromboembolism, stroke, pulmonary embolism, MI, chest pain
EENT: Contact lens intolerance, increased myopia, astigmatism, throat swelling, eyelid edema
GI: Nausea, vomiting, diarrhea, anorexia, pancreatitis, cramps, constipation, increased appetite, increased weight, cholestatic jaundice, hepatic adenoma
GU: Amenorrhea, cervical erosion, breakthrough bleeding, dysmenorrhea, vaginal candidiasis, breast changes, gynecomastia, testicular atrophy, impotence; increased risk of breast, endometrial cancer, changes in libido; toxic shock, vaginal wall ulceration/erosion (vag ring)
INTEG: Rash, urticaria, acne, hirsutism, alopecia, oily skin, seborrhea, purpura, erythema, pruritus, melasma; site irritation (transdermal)
META: Folic acid deficiency, hypercalcemia, hyperglycemia
Pharmacokinetics
Absorption: Well absorbed
Distribution: Widely distributed, crosses placenta
Metabolism: Unknown
Excretion: Unknown
Half-life: Unknown
Pharmacodynamics
PO: Onset Rapid, Peak Unknown, Duration Unknown
IM: Onset Slow, Peak Unknown, Duration Unknown
IV: Onset Rapid, Peak Unknown, Duration Unknown
Interactions
Individual drugs Calcium, phenylbutazone, rifampin: decreased estradiol action CycloSPORINE, dantrolene: increased toxicity
Tamoxifen: decreased tamoxifen action
Drug classifications
Anticoagulants: decreased action of anticoagulants Anticonvulsants, barbiturates: decreased estradiol action
Corticosteroids: increased action of corticosteroids Hypoglycemics (oral): decreased action of hypoglycemics
Drug/herb Black cohosh,
DHEA: altered estrogen effect Saw palmetto, St. John’s wort: decreased estrogen effect
Drug/food Grapefruit juice: increased estrogen level
Drug/lab test
Increased: BSP retention test; PBI; T4; serum sodium; platelet aggregation; thyroxine-binding globulin (TBS); prothrombin; factors VII, VIII, IX, X; triglycerides
Decreased: serum folate, serum triglyceride, T3 resin uptake test, glucose tolerance test, antithrombin III, pregnanediol, metyrapone test False positive: LE prep, ANA titer
Nursing Considerations
Assessment
BLACK BOX WARNING: Assess for previous breast/endometrial cancer, thromboembolic disorders, MI, stroke, dementia - Monitor blood glucose in patient with diabetes; hyperglycemia may occur - Monitor B/P q4 hr; watch for increase caused by water and sodium retention - Monitor • I&O ratio; be alert for decreasing urinary output and increasing edema; monitor weight daily; notify prescriber if weekly weight gain is .5 lb; if increased, diuretic may be ordered - Obtain liver function tests baseline, periodically, including AST, ALT, bilirubin, alkaline phosphatase, periodic folic acid level - Assess edema, hypertension, cardiac symptoms, jaundice - Assess mental status: affect, mood, behavioral changes, aggression; depression may occur, product may need to be discontinued - Assess female patient for intact uterus; if so, progesterone should be added to estrogen therapy to decrease risk of endometrial cancer
Patient/family education - Tell patient to take exactly as prescribed; do not double doses - Advise patient that increased weight gain and symptoms of fluid retention should be reported to prescriber: edema of feet, ankles, sacral area; abnormal vaginal bleeding; breast lumps; hepatic disease (dark urine, clay-colored stools, jaundice of skin, sclera, pruritus); to report dermal rash with transdermal patch - Caution patient that thromboembolic symptoms should be reported: tenderness in legs, chest pain, dyspnea, headaches, blurred vision - Inform patient to use sunscreen and protective clothing because sunburns may occur - Advise patient to stop smoking; smokers have a greater chance of thromboembolic disorder - Tell patient to use nonhormonal birth control and to notify prescriber if pregnancy is suspected - Teach patient to avoid grapefruit or grapefruit juice (PO)
Evaluation
Positive therapeutic outcome: Reversal of menopausal symptoms; Decrease in tumor size in prostatic or breast cancer; Decrease in itching, inflammation of vagina; Absence of symptoms of osteoporosis
Reference
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