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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


estradiol hemihydrate


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


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.


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)


• 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


Use cautiously in:

• cardiovascular, hepatic, or renal disease

• breastfeeding patients.


• 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)


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.


A trademark for a drug preparation of estradiol.


a trademark for an estrogen (estradiol).
References in periodicals archive ?
With an expected launch in the Q2 of this year, the Estrace Cream will be marketed by the company's partner, Impax Laboratories Inc (NASDAQ:IPXL).
01%, the first generic version of Allergan's Estrace Cream, in the US, the company said.
We measured serum estrone because some women, when questioned about their use of exogenous estrogens, equate ERT with occasional use of preparations such as Estrace or Premarin or using transdermal estrogen patches and vaginal creams, which do not have the same effect as oral estrogens in raising serum estrone concentrations (17).
For menopausal women with vaginal thinning, dryness or insensitivity, your health care professional may prescribe an estrogen cream such as Estrace or Premarin, or a vaginal ring, such as Estring, Phadia (low-dose) or Femring (higher dose), to ease sexual discomfort.
Finally, I found a doctor who switched my hormone formulation to bio-identical hormones, Estrace and Prometrium.
The company currently has two marketed products: Estrace, for the symptomatic relief of menopausal symptoms, is commercialised in Canada; Natesto testosterone nasal gel, for testosterone replacement therapy in adult males diagnosed with hypogonadism, is commercialized in Canada and the US, and has been licensed for distribution in 30 countries worldwide.
According to the company, the 2013 revenue expectations reflect, amongst other things, the anticipated growth of certain of its promoted products, including LO LOESTRIN FE and ESTRACE CREAM, which it believes will be more than offset by the anticipated continued decline in ACTONEL revenues.
OSTEOPOROSIS DRUGS AT A GLANCE Oral bisphosphonates Actonel, Boniva, Fosamax Stops bone loss Intravenous Reclast Stops bone loss bisphosphonates Anabolic agent Forteo Builds bone Hormone Activella, Climara, therapies Estrace, Estraderm, Ortho-Est, Premarin, Prempro Selective estrogen Evista Slows bone loss receptor modulator DIETARY SOURCES OF CALCIUM * Plain nonfat yogurt, 8 ounces 452 mg Swiss cheese, 1 1/2 ounces 336 mg Provolone cheese, 1 1/2 ounces 321 mg Mozzarella cheese, 1 1/2 ounces 311 mg Skim milk, 1 cup 306 mg DIETARY SOURCES OF VITAMIN D ** Cod liver oil, 1 tablespoon 1,360 IU Salmon, 3 1/2 ounces cooked 345 IU Mackerel, 3 1/2 ounces cooked 320 IU Sardines, 1 3/4 ounces 250 IU Tuna, canned, in oil, 3 ounces 200 IU * IN MILLIGRAMS ** IN INTERNATIONAL UNITS
I'm now taking half the dose of Estrace and I'm much better.
Drug therapy for prevention and treatment of postmenopausal osteoporosis Drug Indication and dosage (trade name) Calcium and vitamin D Prevention and treatment: (generic, Tums, Citracal, 1200-1500 mg/day calcium and others) and 800 IU/day vitamin D Estrogen ([dagger]) Prevention: (Premarin, Ogen, Estrace, 0.