Estradiol (es-tra-dye-ole)

Brand Names: Estrace, Gynodiol

Estradiol acetate

Brand Names: Femtrace

Estradiol cypionate

Brand Names: depGynogen, Depo-Estradiol, Depogen, Dura-Estrin, E-Cypionate, Estragyn LA5, Estro-Cyp, Estrofem, Estroject-LA, Estro-LA

Estradiol valerate

Brand Names: Clinagen LA, Delestrogen, Dioval, Duragen, Estra-L, Estro-Span, Femogex, Gynogen LA, Menaval, Valergen

Estradiol topical emulsion

Brand Names: Estrasorb

Estradiol topical gel

Brand Names: Divigel, Elestrin, EstroGel

Estradiol transdermal spray

Brand Names: EvaMist

Estradiol transdermal system

Brand Names: Alora, Climara, Esclim, Estraderm, Fern Patch, Menostar, Vivelle

Estradiol vaginal tablet

Brand Names: Vagifem

Estradiol vaginal ring

Brand Names: Femring, Estring

Estradiol Classification

(The therapeutic classification, which categorizes drugs by the disease state they are used to treat, appears first, followed by the pharmacologic classification, which is based on the drug’s mechanism of action.)

Therapeutic class: hormones

Pharmacologic class of Estradiol: estrogens

Pregnancy Category (pregnancy categories (A, B, C, D, and X) provide a basis for determining a drug’s potential for fetal harm): X

Estradiol Indications

(Medications are approved by the FDA for specific disease states. This section identifies the diseases or conditions for which the drug is commonly used and includes significant unlabeled uses as well.)

PO (by mouth, orally), intramuscular (IM), Topical, Transdermal: Replacement of estrogen (HRT) to diminish moderate to severe vasomotor symptoms of menopause and of various estrogen deficiency states including: Female hypogonadism, Ovariectomy, Primary ovarian failure. Treatment and prevention of postmenopausal osteoporosis (not vaginal dose forms). Per Os/By Mouth: Inoperable metastatic postmenopausal breast or prostate carcinoma. Vaginal: Management of atrophic vaginitis that may occur with menopause (low dose), bothersome systemic symptoms of menopause (higher dose). Concurrent use of progestin is recommended during cyclical therapy to decrease the risk of endometrial carcinoma in patients with an intact uterus.

Estradiol Action

(This section contains a concise description of how the Estradiol produces the desired therapeutic effect.)

Estrogens promote growth and development of female sex organs and the maintenance of secondary sex characteristics in women. Metabolic effects include reduced blood cholesterol, protein synthesis, and sodium and water retention.

Therapeutic Effects of Estradiol: Restoration of hormonal balance in various deficiency states, including menopause. Treatment of hormone-sensitive tumors.

Pharmacokinetics

(Pharmacokinetics refers to the way the body processes a medication by absorption, distribution, metabolism, and excretion. Also includes information on the drug’s half-life.)

Absorption: Well absorbed after oral administration. Readily absorbed through skin and mucous membranes.

Distribution: Widely distributed. Crosses the placenta and enters breast milk.

Metabolism and Excretion: Mostly metabolized by the liver and other tissues. Enterohepatic recirculation occurs, and more absorption may occur from the gastrointestinal tract.

Half-life: Gel: 36 hours.

Time/Action Profile (the table provides the onset of Estradiol action, its peak effect, and its duration of activity) (estrogenic effects)

Route

Onset

Peak

Duration

PO unknown unknown unknown
IM unknown unknown unknown
TD unknown unknown 3-4 days (Estraderm), 7 days (Climara)
Topical unknown unknown uknown
Vaginal ring unknown unknown 90 days
Vaginal tablet unknown unknown 3-4 days

Contraindications/Precautions

(Situations in which Estradiol use should be avoided or alternatives strongly considered are listed as contraindications. In general, most drugs are contraindicated in pregnancy or lactation. The precautions portion includes disease states or clinical situations in which drug use involves particular risks or in which dosage modification may be necessary.)

Contraindicated in: Thromboembolic disease; Undiagnosed vaginal bleeding; Obstetric Pregnancy (may result in harm to the fetus); Lactation.

Use Cautiously in: Underlying cardiovascular disease; Severe hepatic or renal disease; May increase the risk of endometrial carcinoma; History of porphyria.

Adverse Reactions/Side Effects of Estradiol

(Although it is not possible to include all reported reactions, major side effects for all drugs are included.)

Central Nervous System (CNS): headache, dizziness, lethargy. Eye, Ear, Nose, and Throat: intolerance to contact lenses, worsening of myopia or astigmatism. Cardiovascular: myocardial infarction, thromboembolism, edema, hypertension. Gastrointestinal (GI): nausea, weight changes, anorexia, increased appetite, jaundice, vomiting. Genitourinary: women — amenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosions, loss of libido, vaginal candidiasis; men — impotence, testicular atrophy. Dermatologic: oily skin, acne, pigmentation, urticaria. Endocrine: gynecomastia (men), hyperglycemia. Fluid and Electrolyte: hypercalcemia, sodium and water retention. Musculoskeletal: leg cramps. Misc: breast tenderness.

Interactions

(Estradiol interactions are a significant risk for patients. As the number of medications a patient receives increases, so does the likelihood of drug-drug interactions. This section provides the most important drug-drug interactions and their physiological effects.)

Estradiol-Drugs: May alter requirement for warfarin, oral hypoglycemic agents, or insulins. Barbiturates or rifampin Estradiol may reduce effectiveness. Smoking reduce risk of adverse CV reactions.

Estradiol Dosage / Route

(Routes of administration are grouped together and include recommended doses for adults, children, and other. Dosage units are expressed in the terms in which they are usually prescribed. Dosing intervals also are provided in the manner in which they are frequently ordered.)

Estrogens should be used in the lowest doses for the shortest period of time consistent with desired therapeutic outcome.

Symptoms of Menopause, Atrophic Vaginalinitis, Female Hypogonadism, Ovarian Failure/Osteoporosis PO (Adults): 0.45-2 mg daily or in a cycle. intramuscular (Adults): 1-5 mg monthly (estradiol cypionate) or 10-20 mg (estradiol valerate) monthly.

Topical: Emulsion (Estrasorb) (Adults): Apply two 1.74 g pouches (4.35 mg estradiol) daily.

Gel (Adults): Apply contents of one packet (Divigel) or one actuation from pump (EstroGel, Elestrin) daily.

Spray EvaMist (Adults): 1 spray daily, maybe increased to 2-3 sprays daily. Transdermal (Adults) : Alora, Estraderm — 50-or 100-mcg/24-hrtransdermal patch applied twice weekly. Climara — 50-100-mcg/24-hr patch applied weekly. FemPatch — 25-mcg/24-hr patch applied every 7 days. Vivelle — 37.5-100-mcg/24 hours transdermal patch applied twice weekly. Menostar — 14-mcg/24-hr patch applied every 7 days. Progestin may be admin-isteredfor 10-14days of each month. Vaginal (Adults): Cream — 2-4 g (0.2-0.4 mg estradiol) daily for 1-2 wk, then decrease to 1-2 g/day for 1-2 wk; then maintenance dose of 1 g 1-3 times weekly for 3 wk, then off for 1 wk; then repeat cycle once vaginal mucosa has been restored; Vaginal ring (Estring) — 2-mg (releases 7.5 meg estradiol/24 hours)q 3 month; Vaginal ring (Femring) — 12.4 mg (releases 50meg estradiol/24 hours)q 3 month or 24.8 mg (releases 100 meg estradiol/24 hours) q 3 month (Femring requires concurrent progesterone) Vaginal tablet — 25-mcg once daily for 2 wk, then twice weekly.

Postmenopausal Breast Carcinoma PO (Adults): 10 mg 3 times daily.

Prostate Carcinoma

PO (by mouth, orally) (Adults): 1-2 mg 3 times daily.

IM (Adults): 30 mg every 1-2 week (estradiolvalerate).

Package & Price of Estradiol in Pharmacies of the US

(This lists the strengths and concentrations of available dose forms. Such information is useful in planning more convenient regimens (fewer tablets / capsules, less injection volume). General availability and average wholesale prices of commonly prescribed drugs have also been added as an aid to nurses with prescriptive authority.)

Estradiol Tablets: 0.45 mg, 0.5 mg, 0.9 mg, 1 mg, 1.8 mg, 2 mg. Estradiol Cost: Generic ― 0.5 mg of Estradiol cost $22.17/100, 1 mg of Estradiol cost $15.52/100, 2 mg of Estradiol cost $33.30/100. Injection (valerate in oil): 10 mg/ml, 20 mg/ml, 40 mg/ml. Injection (cypionate in oil): 5 mg/ml. Topical emulsion: 4.35 mg/1.74 g pouch in boxes of 14 pouches in a one-month supply carton of 56 pouches. Topical gel packet: 0.25 g packet, 0.5 g packet, 1 g packet. Topical gel pump (0.06%): 0.87 g/actuation, 1.25 g/actu-ation. Transdermal Spray: metered dose pump contains 8.1 mL, delivers 56 sprays of 1.53 mg each. Transdermal system: 14 meg/24-hr release rate, 25 mcg/24-hr release rate, 37.5 mcg/24-hr release rate, 50 mcg/24-hr release rate, 60 mcg/24-hr release rate, 75 meg/24-hr release rate, 100 mcg/24-hr release rate. Estradiol Cost: Generic — 25 mcg/24-hr release rate of Estradiol cost $36.99/4 patches, 37.5 mcg/24-hr release rate of Estradiol cost $39-35/4 patches, 50 mcg/24-hr release rate of Estradiol cost $29-97/4 patches, 60 mcg/24-hr release rate of Estradiol cost $39.99/4 patches, 75 mcg/24-hr release rate of Estradiol cost $35.99/4 patches, 100 mcg/24-hr release rate of Estradiol cost $31.46/4 patches. Vaginal cream: 100 meg/g. Vaginal ring (Estring): 2 mg (releases 7.5 meg/day over 90 days). Vaginal ring (Femring): 12.4 mg (releases 50 meg/day over 90 days), 24.8 mg (releases 100 meg/day over 90 days). Vaginal tablet: 25 meg. Estradiol Cost: of Estradiol cost $75.81/18 tablets.

Nursing Implications for Estradiol

(This section helps the nurse apply the nursing process to pharmacotherapeutics. The subsections provide a step-by-step guide to clinical assessment, implementation (Estradiol administration), and evaluation of the outcomes of pharmacologic therapy.)

Assessment

(This section includes guidelines for assessing patient history and physical data before and during drug therapy. Assessments specific to the drug’s various indications are also included.)

• Assess blood pressure before and periodically during therapy.

• Monitor intake and output ratios and weekly weight. Report significant discrepancies or steady weight gain.

• Menopause: Assess frequency and severity of vasomotor symptoms.

Lab Test Considerations: Estradiol may cause increase high-density lipoproteins (HDL), phospholipids, and triglycerides and reduce serum low-density lipoproteins (LDL) and total cholesterol concentrations.

• Estradiol may cause increase serum glucose, sodium, cortisol, prolactin, prothrombin, and factor VII, VIII, K, and X levels. Estradiol may reduce serum folate, pyridoxine, antithrombin III, and urine pregnanediol concentrations.

• Monitor hepatic function before and periodically during therapy.

• May cause false interpretations of thyroid function tests, false increase in norepinephrine platelet-induced aggregability, and false reduce in metyrapone tests.

• May cause hypercalcemia in patients with metastatic bone lesions.

Potential Nursing Diagnoses

(The two or three most pertinent NANDA diagnoses that potentially apply to a patient receiving the Estradiol are listed. Each diagnosis includes the pharmacologic effect from which the diagnosis has been derived.)

Sexual dysfunction (Indications)

Estradiol Implementation

(Guidelines specific for Estradiol administration)

• Do not confuse Estraderm (estradiol) with Testaderm (testosterone).

Per Os/By Mouth: Administer with or immediately after food to reduce nausea.

Vaginal: Manufacturer provides applicator with cream. Dose is marked on the applicator. Wash applicator with mild soap and warm water after each use.

• Transdermal: When switching from PO form, begin transdermal therapy 1 week after the last dose or when symptoms reappear.

Topical: In a comfortable position, apply Estrasorb to clean, dry skin of thighs each morning. Open each foil pouch individually. Cut or tear the first pouch at the notches near the top of the pouch. Apply the contents of the pouch to the top of the left thigh; push entire contents from bottom through neck of pouch. Using one or both hands rub the emulsion into the thigh and calf for 3 min until completely absorbed. Rub any excess remaining on hands into buttocks. Repeat procedure with second pouch on right leg. Allow application sites to dry completely before covering with clothing to prevent transfer. Wash hands with soap and water to remove residual estradiol.

• Apply Divigel individual-use once-daily packets of quick drying gel to an area measuring 5 inches by 7 inches (size of 2 palm prints) on the thigh. Do not wash area for at least 1 hour after gel has dried.

• Spray EvaMist on inside of forearm at the same time each day. Do not massage or rub the spray into the skin. Allow to dry for 2 min before dressing and 30 min before washing. Never spray EvaMist around breast or vagina Do not use more than 56 doses, even if fluid remains in pump.

Intramuscular (IM): Injection has oil base. Roll syringe to ensure even dispersion. Administer deep IM. Avoid intravenous (IV) administration.

Estradiol: Patient/Family Teaching

(This section includes information that should be taught to patients. Side effects that should be reported, information on minimizing and managing side effects of Estradiol, details on administration, and follow-up requirements are presented. Home Care Issues discusses aspects to be considered for medications taken in the home setting.)

• Instruct patient on correct method of administration. Instruct patient to take medication as directed. Take missed doses as soon as remembered as long as it is not just before next dose. If a dose of EvaMist is missed, apply if more than 12 hours before next dose; if less than 12 hourss, omit dose and return to regular schedule. Do not double doses.

• Explain dose schedule and maintenance routine. Discontinuing medication suddenly may cause withdrawal bleeding.

• If nausea becomes a problem, advise patient that eating solid food often provides relief.

• Advise patient to report signs and symptoms of fluid retention (swelling of ankles and feet, weight gain), thromboembolic disorders (pain, swelling, tenderness in extremities, headache, chest pain, blurred vision), mental depression, or hepatic dysfunction (yellowed skin or eyes, pruritus, dark urine, light-colored stools) to health care professional.

• Instruct patient to stop taking medication and notify health care professional if pregnancy is suspected.

• Advise patient to notify health care professional of medication regimen before treatment or surgery.

• Caution patient that cigarette smoking during estrogen therapy may cause increased risk of serious side effects, especially for women over age 35.

• Caution patient to use sunscreen and protective clothing to prevent increased pigmentation.

• Advise patient treated for osteoporosis that exercise has been found to arrest and reverse bone loss. The patient should discuss any exercise limitations with health care professional before beginning program.

• Inform patient that estrogens should not be used to decrease risk of cardiovascular disease. Estrogens may increase risk of cardiovascular disease and breast cancer.

• Emphasize the importance of routine follow-up physical exams, including blood pressure; breast, abdomen, and pelvic examinations; Papanicolaou smears every 6-12 month; and mammogram every 12 month or as directed. Health care professional will evaluate possibility of discontinuing medication every 3-6 month. If on continuous (not cyclical) therapy

or without concurrent progestins, endometrial biopsy may be recommended, if uterus is intact.

Vaginal: Instruct patient in the correct use of applicator. Patient should remain recumbent for at least 30 min after administration. May use sanitary napkin to protect clothing, but do not use tampon. If a dose is missed, do not use the missed dose, but return to regular dosing schedule.

• Instruct patient to use applicator provided with vaginal tablet. Insert as high up in the vagina as comfortable, without using force.

• Vaginal Ring: Instruct patient to press ring into an oval and insert into the upper third of the vaginal vault. Exact position is not critical. Once ring is inserted, patient should not feel anything. If discomfort is felt, ring is probably not in far enough; gently push farther into vagina. Leave in place continuously for 90 days. Ring does not interfere with sexual intercourse. If straining at defecation makes ring move to lower vagina, push up with finger. If expelled totally, rinse ring with lukewarm water and reinsert. To remove, hook a finger through the ring and pull it out.

• Transdermal: Instruct patient to wash and dry hands first. Apply disc to intact skin on hairless portion of abdomen (do not apply to breasts or waistline). Press disc for 10 sec to ensure contact with skin (especially around edges). Avoid areas where clothing may rub disc loose. Change site with each administration to prevent skin irritation. Do not reuse site for 1 wk; disc may be reapplied if it falls off.

Estradiol: Evaluation / Desired Outcomes

(Outcome criteria for determination of the effectiveness of Estradiol are provided.)

• Resolution of menopausalvasomotor symptoms.

• Decreased vaginal and vulvar itching, inflammation, or dryness associated with menopause.

• Normalization of estrogen levels in patients with ovariectomy or hypogonadism.

• Control of the spread of advanced metastatic breast or prostate cancer.

• Prevention of osteoporosis.

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