estradiol


Also found in: Dictionary, Thesaurus, Acronyms, Encyclopedia, Wikipedia.
Related to estradiol: estradiol patch

estradiol

 [es″trah-di´ol, es-tra´de-ol]
1. the most potent naturally occurring ovarian and placental estrogen in mammals; it prepares the uterus for implantation of the fertilized ovum and promotes the maturation of and maintenance of the female accessory reproductive organs and secondary sex characters.
2. a preparation of this hormone used in estrogen replacement therapy for conditions such as female hypogonadism, ovariectomy, or primary ovarian failure, and in treatment of abnormal uterine bleeding, vasomotor menopausal symptoms, postmenopausal osteoporosis, atrophic vaginitis, and certain advanced breast or prostatic carcinomas. Used most often in the form of estradiol cypionate, estradiol valerate, or ethinyl estradiol.

estradiol

Bedol (UK), Elestrin, Elleste (UK), Elleste-Solo (UK), Estrace, Estring, Estrogel, Gynodiol, Innofem, Oestrogel (UK), Progynova (UK), Sandrena (UK), Vagifem, Zumenon (UK)

estradiol acetate

Femring, Femtrace

estradiol cypionate

Depo-Estradiol

estradiol hemihydrate

Estrasorb

estradiol transdermal system

Alora, Climara, Estraderm, Estradot (UK), Evorel (UK), Fematrix (UK), Femseven (UK), Menostar, Vivelle

estradiol valerate

Climaval (UK), Delestrogen, Femogex (CA)

Pharmacologic class: Estrogen

Therapeutic class: Hormone

Pregnancy risk category X

Action

Binds to nuclear receptors in responsive tissues (such as female genital organs, breasts, and pituitary gland), enhancing DNA, RNA, and protein synthesis. In androgen-dependent prostate cancer, competes for androgen receptor sites, inhibiting androgen activity. Also decreases pituitary release of follicle-stimulating hormone and luteinizing hormone.

Availability

Injection (cypionate in oil): 5 mg/ml

Injection (valerate in oil): 10 mg/ml, 20 mg/ml, 40 mg/ml

Tablets: 0.5 mg, 1 mg, 1.5 mg, 2 mg

Tablets (film-coated): 25.8 mcg estradiol hemidrate (equivalent to 25 mcg estradiol)

Transdermal system: 25 mcg/24-hour release rate, 37.5 mcg/24-hour release rate, 50 mcg/24-hour release rate, 75 mcg/24-hour release rate, 100 mcg/24-hour release rate

Vaginal cream: 100 mcg/g

Vaginal ring: 2 mg released over 90 days

Vaginal tablets: 10 mcg

Indications and dosages

Symptoms of menopause, atrophic vaginitis, female hypogonadism, ovarian failure, and osteoporosis

Adults: 0.5 to 2 mg (estradiol) P.O. daily continuously or cyclically. Or 1 to 5 mg (cypionate) or 10 to 20 mg (valerate) I.M. monthly. Or 50- or 100-mcg/24-hour transdermal patch applied twice weekly (Alora, Estraderm) or weekly (Climara). Or 25-mcg/24-hour patch applied q 7 days (FemPatch) or 37.5- to 100-mcg transdermal patch applied twice weekly (Vivelle). Or 2 to 4 g (0.2 to 0.4 mg) vaginal cream (estradiol) applied daily for 1 to 2 weeks, then decreased to 1 to 2 g/day for 1 to 2 weeks, then a maintenance dose of 1 g one to three times weekly for 3 weeks, then off for 1 week; repeat cycle once vaginal mucosa has been restored. Or 2-mg vaginal ring q 3 months or 10-mcg vaginal tablet once daily for 2 weeks, then twice weekly.

Postmenopausal breast cancer

Adults: 10 mg P.O. t.i.d. (estradiol)

Prostate cancer

Adults: 1 to 2 mg P.O. t.i.d. (estradiol) or 30 mg I.M. q 1 to 2 weeks (valerate)

Contraindications

• Hypersensitivity to drug or its components

• Thromboembolic disease (current or previous)

• Undiagnosed vaginal bleeding

• Breast or reproductive system cancer (except in metastatic disease)

• Estrogen-dependent neoplasms

• Pregnancy

Precautions

Use cautiously in:

• cardiovascular, hepatic, or renal disease

• breastfeeding patients.

Administration

• Inject I.M. dose deep into large muscle mass; rotate injection sites.

• If switching from oral to transdermal estrogen, apply patch 1 week after withdrawal of oral therapy.

Adverse reactions

CNS: headache, dizziness, lethargy, depression

CV: hypertension, myocardial infarction (MI), thromboembolism

EENT: contact lens intolerance, worsening of myopia or astigmatism

GI: nausea, vomiting, bowel obstruction with vaginal ring (rare)

GU: amenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosions, decreased libido, vaginal candidiasis, erectile dysfunction, testicular atrophy, gynecomastia, breast pain or tenderness

Hepatic: jaundice

Metabolic: sodium and fluid retention, hypercalcemia, hyperglycemia

Musculoskeletal: leg cramps

Skin: oily skin, acne, pigmentation changes, urticaria

Other: weight loss or gain, edema, increased appetite, toxic shock syndrome with vaginal ring (rare)

Interactions

Drug-drug. Insulin, oral hypoglycemics, warfarin: altered requirements for these drugs

Drug-diagnostic tests. Antithrombin III, folate, low-density lipoproteins, pyridoxine, total cholesterol, urine pregnanediol: decreased levels

Cortisol; factors VII, VIII, IX, and X; glucose; high-density lipoproteins; phospholipids; prolactin; prothrombin; sodium; triglycerides: increased levels

Metyrapone test: false decrease

Thyroid function tests: false interpretation

Drug-behaviors. Smoking: increased risk of adverse CV reactions

Patient monitoring

Monitor vital signs and cardiovascular status, especially for hypertension, thromboembolism, and MI.

• Be aware that a few cases of ring adherence to the vaginal wall have occurred, which may require evaluation of wall ulceration and erosion.

• Assess vision.

• In diabetic patient, monitor blood glucose level and watch for signs and symptoms of hyperglycemia.

Patient teaching

• Instruct patient to place transdermal patch on clean, dry skin area.

• Teach proper technique for use of vaginal tablet, ring, or cream, as appropriate.

• Tell patient drug may cause loss of libido (in women) or erectile dysfunction (in men). Encourage patient to discuss these issues with prescriber.

Teach patient to recognize and immediately report signs and symptoms of thromboembolism.

Caution patient not to take drug if she is or plans to become pregnant.

• Advise patient that drug may worsen nearsightedness or astigmatism and make contact lenses uncomfortable.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

es·tra·di·ol (E2),

(es-tră-dī'ol, es-tra'dē-ōl),
β-Estradiol; 17β-estradiol; the most potent naturally occurring estrogen in mammals, formed by the ovary, placenta, testis, and possibly the adrenal cortex; therapeutic indications for estradiol are those typical of an estrogen. α-Estradiol (17α-estradiol), exhibits considerably less biologic activity.

estradiol

/es·tra·di·ol/ (es″trah-di´ol) (es-tra´de-ol) the most potent estrogen in humans; pharmacologically, it is often used in the form of its esters (e.g., e. cypionate, e. valerate ) or as a semisynthetic derivative (ethinyl e.) . For properties and uses, see estrogen.

estradiol

(ĕs′trə-dī′ôl′, -ōl′, -ŏl′)
n.
An estrogenic hormone, C18H24O2, that is produced by the ovaries and is the dominant naturally occurring estrogen in women between puberty and menopause. It is used to treat menopausal symptoms and other conditions.

estradiol

[es′trədī′ôl]
the most potent naturally occurring human estrogen.

estradiol

E2 Endocrinology The most potent natural estrogen, produced chiefly by the ovary and in small amount by the testis; it is measured to evaluate postmenopausal status or suspected hypogonadism ↑ in Ovarian tumors, pregnancy, adrenal feminizing tumors, precocious puberty, liver disease, gynecomastia ↓ in OCs, ovarian failure, menopause, hypogonadism

es·tra·di·ol

(es-tră-dī'ol)
The most potent naturally occurring estrogen, formed by the ovary, placenta, testes, and possibly the cortex of the suprarenal gland.
Synonym(s): oestradiol.

es·tra·di·ol

(es-tră-dī'ol)
Most potent naturally occurring estrogen in mammals, formed by the ovary, placenta, testis, and possibly the cortex of the suprarenal gland.

estradiol

the female steroid hormone produced by the mature ovarian follicle and the adrenal cortex and responsible for sexual receptivity at the time of estrus. Is the dominant estrogenic hormone in the nonpregnant animal. In the pregnant animal the dominant hormone is estrone; called also estradiol-17β; commercial products include estradiol benzoate and the cyprionate.

estradiol cyclopentyl propionate
a pharmaceutical preparation used in dogs; recorded as a cause of hyperestrogenism.
References in periodicals archive ?
Among 68 evaluable women (mean age, 56 years), mean baseline estradiol levels were 20 pg/mL (range, <2 to 127 pg/mL); estradiol levels were above the postmenopausal range (>10 pg/mL) in 37% of participants.
Table III: Variance analysis of regression of BMI on level of estradiol in premenopausal and postmenopausal breast cancer patients and controls.
The differing neurobiology of estradiol versus CEE may be a major factor in these conflicting results.
5 pg/mL) nivel serico de estradiol se presentan en el Cuadro 1.
Also, there was a strongly negative and significant association between serum estradiol level and total cholesterol.
The authors wrote in the discussion section of the paper, "Testosterone and associated increases in estradiol may promote inflammation, coagulation, and platelet aggregation.
Regarding the combination's effect on lipid levels, total and LDL cholesterol levels also were lowered significantly in women taking drospirenone and estradiol, with a 13.
Not only are the doses many magnitudes lower than those considered in classic high-dose toxicity studies, but at extremely low doses both estradiol and bisphenol A demonstrate a response that disappears as the dose increases.
Estradiol, for example, is a popular choice in branded pharmaceutical drugs: it's available in pills (including Estrace[R], Gynodiol[R] and generics), patches (Climara[R], Alora[R], Estraderm[R], Vivelle[R] and generics), vaginal creams (Estrace[R] and generics), vaginal rings (Estring[R] and so on Promoting estradiol-containing products as alternative therapies is like decanting supermarket jam into gingham-topped canning jars and passing them off as homemade at the county fair.
Serum estradiol concentrations have long been used in conjunction with ultrasonography and other clinical indices to monitor ovarian stimulation by exogenous gonadotropin therapy during in vitro fertilization (IVF) procedures (1-3).
ALBUQUERQUE -- Transdermal estradiol appears to be an effective antidepressant in penmenopausal women with various forms of depression, Dr.