Estrasorb

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.

Estrasorb®

Geriatrics A topical cream–17ß estradiol for ERT in symptomatic menopausal ♀
References in periodicals archive ?
Estradiol gel (EstroGel) is a transdermal gel; Estrasorb is a transdermal estradiol lotion.
the first topical product, Estrasorb developed by Novavax, a topical estrogen using its micellar nanoparticulate system, reached the market in 2004;
Novavax will continue to operate its manufacturing facility, located outside Philadelphia, where the company makes Estrasorb under a licensing agreement with Esprit Pharma.
Women should not apply Estrasorb and sunscreen at the same time because this could affect the amount of estradiol that is absorbed.
Estrasorb uses oil and water nanoemulsions that encapsulate and deliver 17[beta]-estradiol through the skin.
Estrasorb is distributed in pouches, each containing 1.
Studies showed that vigorous rubbing of a man's forearm for 2 minutes across a leg where Estrasorb had been applied resulted in a 25% increase in the man's estradiol levels, but the level remained within the normal range.
Novavax received $20 million on December 19, 2000, and will receive an additional $5 million when Novavax files a New Drug Application for its topical transdermal estrogen replacement therapy, ESTRASORB, expected to be filed in the first half of 2001.
There are two main types of bioidentical hormones: those that are FDA-approved and commercially available with a prescription, such as Estrace, Climara, Vivelle, EstroGel, Divigel and Estrasorb, and those that are produced on an individual basis for women, in compounding pharmacies.
Novavax has several product candidates in pre-clinical and human clinical trials, including ESTRASORB, a topical cream for estrogen replacement therapy which has entered Phase III clinical testing.
There are two main types of bioidentical hormones: those that are FDA-approved and commercially available with a prescription, such as Estrace, Climara, Vivelle, EstroGel, Divigel, and Estrasorb, and those that are produced on an individual basis for women in compounding pharmacies.