Adult Dosing

Severe vasomotor symptoms

estradiol

• 1-2 mg PO qd; administer in a cyclic regimen 3 wks on and 1 wk off
• Discontinue or taper medicine at 3-6 month interval
• Use lowest effective dose for maintenance therapy by titration

Femtrace (estradiol acetate)

• 0.45-1.8 mg PO qd, use lowest effective dose for maintenance therapy by titration
• Discontinue or taper medicine at 3-6 month interval
• Add progestin in postmenopausal women with intact uterus

Vulval and vaginal atrophy associated with the menopause

estradiol

• 1-2 mg PO qd; administer in a cyclic regimen 3 wks on and 1 wk off
• Discontinue or taper medicine at 3-6 month interval
• Use lowest effective dose for maintenance therapy by titration

Hypoestrogenism

estradiol

• Initial 1-2 mg PO qd
• Use lowest effective dose for maintenance therapy by titration

Palliative treatment of breast cancer

estradiol

• 10 mg PO tid x 3 months

Androgen-dependent prostate cancer

estradiol

• 1-2 mg PO tid

Prevention of osteoporosis

estradiol

• 0.5 mg PO qd in a cyclic regimen, the lowest effective dose has not been determined

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

Estradiol

• Moderate to severe vasomotor symptoms associated with the menopause
• Vulvar and vaginal atrophy associated with the menopause
• Hypoestrogenism due to hypogonadism, castration or primary ovarian failure
• Palliative treatment of breast cancer with metastatic disease
• Palliative treatment of advanced androgen-dependent prostate cancer
• Postmenopausal osteoporosis

Femtrace (estradiol acetate)

• Moderate to severe vasomotor symptoms associated with the menopause

• Hypersensitivity to any of the ingredients of the product
• Undiagnosed abnormal genital bleeding
• Active or history of breast cancer
• Estrogen-dependent neoplasia
• Active or history of deep vein thrombosis or pulmonary embolism
• Active or recent arterial thromboembolic diseases
• Liver dysfunction/diseases
• Known or suspected pregnancy

• Estrogen increases the risk of endometrial cancer. Monitor closely all the women taking estrogen therapy, use adequate diagnostic measures like endometrial sampling to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding
• Do not use estrogens with or without progestins for the prevention of cardiovascular disease. As per the study conducted by Women’s Health Initiative (WHI), oral conjugated estrogens 0.625 mg combined with medroxyprogesterone acetate 2.5 mg relative to placebo increases risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli and deep vein thrombosis in postmenopausal women (50 to 79 years of age) during 5 years of treatment. It also increases the risk of developing dementia in postmenopausal women 65 years of age or older during 4 years of treatment (WHIMS), other doses or estrogen/progestin combos not studied, but assume similar risk. Use lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic impairment: Contraindicated

• Estrogen and estrogen/progestin therapy increases the risk of cardiovascular events like myocardial infarction and stroke, discontinue the drug immediately if any of these event suspected [US Black Box warning]
• Unopposed use of estrogens in women with intact uteri increases the risk of endometrial cancer [US Black Box warning]
• Estrogens and progestins use in postmenopausal women increase the risk of breast cancer. Perform breast examination and mammogram yearly based on patient age, risk factors and prior mammogram results
• Estrogen and estrogen/progestin therapy increases the risk of dementia in postmenopausal women 65 years of age and older [US Black Box warning]
• Increases the risk of gallbladder diseases by 2 to 4 fold in postmenopausal women receiving estrogen therapy
• Estrogen therapy causes severe hypercalcemia in patients with breast cancer and bone metastases. Discontinue the therapy if hypercalcemia occurs, and provide appropriate measures
• Retinal vascular thrombosis occurs in patients receiving estrogens. Discontinue the drug if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia or migraine. Permanently discontinue if papilledema or retinal vascular lesions are seen on examination
• Estrogen use causes increases in blood pressure, monitor BP at regular interval
• Use of progestin with estrogen in continuous regimen lowers the incidence of endometrial hyperplasia, than would be induced by estrogen treatment alone. However there is possible increased risk of breast cancer associated with the use of progestins with estrogens compared to estrogen-alone regimens
• Estrogen therapy elevates the plasma triglycerides in patients with preexisting hypertriglyceridemia, leading to pancreatitis and other complications
• Use cautiously in patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy and in the case of recurrence discontinue the drug
• Estrogen administration causes increased thyroid-binding globulin (TBG) levels. Patients on thyroid hormone replacement therapy receiving estrogen require increased doses of their thyroid replacement therapy. Monitor thyroid function regularly to maintain free thyroid hormone levels in an acceptable range
• Estrogen causes fluid retention, use cautiously in patients with conditions like asthma, epilepsy, migraine, and cardiac or renal dysfunction
• Use of estrogen alone for 10 or more years increases the risk of ovarian cancer
• Topical vaginal products should be considered when prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy

Cautions: Use cautiously in

• Cardiovascular diseases
• Hypertension
• Hypertriglyceridemia
• History of Cholestatic Jaundice
• Hypothyroidism
• Asthma
• Diabetes mellitus
• Epilepsy
• Migraine
• Surgery or prolonged immobilization
• Porphyria
• Systemic lupus erythematosus
• Hepatic hemangiomas
• Endometriosis
• Severe hypocalcemia
• Gallbladder Disease
• Obesity
• Patients >65 yrs
• Tobacco use

Pregnancy Category:X

Breastfeeding: Limited data on the use of estradiol during breastfeeding indicates that the amount transferred into breastmilk is influenced by route of administration and dosage form. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 24 December 2010). Though this drug has found to be compatible with breastfeeding, withdrawal bleeding may occur after drug is withdrawn based upon data from AAP Policy Guidelines (available at http://aappolicy.aappublications.org/cgi/content/full/pediatrics;108/3/776)As per manufacturer's data, estrogen administration during breastfeeding interferes with lactation by decreasing the quantity and quality of the milk. Detectable amount is secreted in breast milk; use cautiously when estradiol is administered to a nursing woman.

• CV: Deep and superficial venous thrombosis, pulmonary embolism, thrombophlebitis, myocardial infarction, stroke, hypertension, increased triglycerides
• GI: Nausea, constipation, dyspepsia, vomiting, abdominal cramps, bloating, cholestatic jaundice, gallbladder disease, pancreatitis, enlargement of hepatic hemangiomas
• DERM: Chloasma or melasma, erythema multiforme, erythema nodosum, hemorrhagic eruption, hirsutism, pruritus, rash, hair loss, urticaria, angioedema
• EENT: Retinal vascular thrombosis, steepening of corneal curvature, intolerance to contact lenses, influenza, nasopharyngitis
• RESP: Sinusitis, URTI, bronchitis
• CNS: Headache, depression, insomnia, migraine, dizziness, mental depression, chorea, nervousness, mood disturbances, irritability, exacerbation of epilepsy, dementia
• MUSC: Arthralgia, back pain, neck pain, pain in limb, arthritis, myalgia
• METABOLIC: Hypocalcemia
• MISC: Weight gain, porphyria, carbohydrate intolerance, edema, anaphylactic reactions, infection, asthenia

• Estrogen; responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. By negative feedback mechanism regulates the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH)
• Metabolized by liver; CYP 450: 3A4. Also undergoes enterohepatic recirculation
• Renally excreted as conjugates
• Half-life: 1-2 hrs, estrone: 4-18 hrs

US Trade Name(s)

• Estrace (Discontinued)
• Femtrace

US Availability

estradiol (generic)

• TABS: 0.5, 1, 2 mg

Estrace (estradiol)

• TABS: 0.5, 1, 2 mg

Femtrace (estradiol acetate)

• TABS: 0.45, 0.9, 1.8 mg

Canadian Trade Name(s)

• Estrace

Canadian Availability

Estrace (estradiol)

• TABS: 0.5, 1, 2 mg

UK Trade Name(s)

• Climaval
• Elleste solo
• Progynova
• Zumenon

UK Availability

Climaval, Progynova (estradiol valerate)

• TABS: 1, 2 mg

Elleste solo(estradiol hemihydrate)

• TABS: 1, 2 mg

Zumenon

• TABS: 1, 2 mg

Australian Trade Name(s)

• Estrofem
• Progynova
• Zumenon

Australian Availability

Estrofem (estradiol hemihydrate)

• TABS: 1, 2 mg

Progynova (estradiol valerate)

• TABS: 1, 2 mg

Zumenon (estradiol)

• TABS: 2 mg

[Outline]

Obstetrics/Gynecology

Hormones

Estrogens

Pricing data from www.DrugStore.com in U.S.A.

• Femtrace 0.45 MG TABS [Bottle] (WARNER CHILCOTT PROF PROD DIV)
  100 mg = $224
  300 mg = $608.99
• Estrace 1 MG TABS [Bottle] (WARNER CHILCOTT PROF PROD DIV)
  30 mg = $75.99
  90 mg = $209.96
• Femtrace 0.9 MG TABS [Bottle] (WARNER CHILCOTT PROF PROD DIV)
  100 mg = $187
  200 mg = $370.95
• Femtrace 1.8 MG TABS [Bottle] (WARNER CHILCOTT PROF PROD DIV)
  100 mg = $236.98
  300 mg = $665.96
• Estrace 2 MG TABS [Bottle] (WARNER CHILCOTT PROF PROD DIV)
  30 mg = $95.99
  90 mg = $259.97

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

• Estrace 0.5 MG Oral Tablet (Bristol-Myers Squibb Co.)
• Estrace 0.5 MG Oral Tablet (Warner Chilcott (US), LLC)
• Estrace 1 MG Oral Tablet (Bristol-Myers Squibb Co.)
• Estrace 1 MG Oral Tablet (Warner Chilcott (US), LLC)
• Estrace 2 MG Oral Tablet (Bristol-Myers Squibb Co.)
• Estrace 2 MG Oral Tablet (Warner Chilcott (US), LLC)
• Estradiol 0.5 MG Oral Tablet (BARR LABORATORIES, INC.)
• Estradiol 0.5 MG Oral Tablet (Mylan Pharmaceuticals Inc.)
• Estradiol 0.5 MG Oral Tablet (Physicians Total Care, Inc.)
• Estradiol 0.5 MG Oral Tablet (Stat Rx USA)
• Estradiol 1 MG Oral Tablet (BARR LABORATORIES, INC.)
• Estradiol 1 MG Oral Tablet (Mylan Pharmaceuticals Inc.)
• Estradiol 1 MG Oral Tablet (Physicians Total Care, Inc.)
• Estradiol 2 MG Oral Tablet (BARR LABORATORIES, INC.)
• Estradiol 2 MG Oral Tablet (Caremark L.L.C.)
• Estradiol 2 MG Oral Tablet (Mylan Pharmaceuticals Inc.)
• Estradiol 2 MG Oral Tablet (Physicians Total Care, Inc.)
• Femtrace 0.45 MG Oral Tablet (Warner Chilcott (US), LLC)
• Femtrace 0.9 MG Oral Tablet (Warner Chilcott (US), LLC)
• Femtrace 1.8 MG Oral Tablet (Warner Chilcott (US), LLC)
• Innofem 0.5 MG Oral Tablet (NOVO NORDISK INC.)
• Innofem 1 MG Oral Tablet (NOVO NORDISK INC.)
• Innofem 2 MG Oral Tablet (NOVO NORDISK INC.)