Adult Dosing

Moderate to severe vasomotor symptoms, vulvar and vaginal atrophy associated with the menopause

• Usual dose: 10-20 mg IM q4wks

Hypoestrogenism due to hypogonadism, castration, or primary ovarian failure

• Usual dose: 10-20 mg IM q4wks

advanced androgen-dependent carcinoma of the prostate (for palliation only)

• Usual dose: 30 mg IM q1-2 wks

• Progestin should be initiated to reduce the risk of endometrial cancer
• Use lowest effective dose for the shortest duration

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Moderate to severe vasomotor symptoms associated with the menopause
• Moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause (local preparations preferred)
• Hypoestrogenism due to hypogonadism, castration, or primary ovarian failure
• Advanced androgen-dependent carcinoma of the prostate (palliative)

• Hypersensitivity to any of the ingredients of the product
• Undiagnosed abnormal vaginal bleeding
• Active or history of breast cancer
• Known or suspected estrogen-dependent neoplasia
• Active or history of deep vein thrombosis or pulmonary embolism
• Active or recent arterial thromboembolism
• 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: Caution advised, dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic impairment: Contraindicated

• Estrogen and estrogen/progestin therapy increases the risk of cardiovascular events like myocardial infarction, DVT and stroke, and also venous thrombosis and pulmonary embolism. Discontinue the drug immediately if any of these event suspected [US Black Box warning]
• Increased risk of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 yrs of age) during five years of treatment with oral conjugated equine estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo [US Black Box Warning]
• Unopposed use of estrogens in women with intact uteri increases the risk of endometrial cancer [US Black Box warning]
• Estrogen and estrogen/progestin therapy increases the risk of dementia in postmenopausal women 65 years of age and older. It should not be used for the prevention of dementia [US Black Box warning]
• Risk factors for arterial vascular disease, venous thromboembolism should be managed appropriately
• Hypercoagulability may occur and appears to be dose and duration dependent
• Estrogen causes fluid retention, use cautiously in patients with conditions like asthma, epilepsy, migraine, and cardiac or renal dysfunction
• May aggravate asthma, diabetes, epilepsy, migraine, porphyria, SLE, hepatic hemangiomas
• 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
• 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
• Increased risk factors of arterial vascular disease include: hypertension, diabetes mellitus, tobacco use, hypercholesterolemia amd obesity
• 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
• 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 use causes increases in blood pressure, monitor BP at regular interval
• 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
• Use of estrogen alone for 10 or more years increases the risk of ovarian cancer
• Estrogen alone therapy in exacerbate endometriosis in post-hysterectomy, consider addition of progestin to the therapy

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: Injectable estradiol valerate has been used to suppress lactation, usually in combination with testosterone. It should be avoided in mothers wishing to breastfeed. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 14 June 2011). As per manufacturer's data, detectable amounts of estrogens have been identified in the milk of mothers receiving this drug; caution should be advised in nursing mothers.

• CV: Myocardial infarction; stroke, increase in blood pressure, edema, hypertension, thrombophlebitis, thromboembolism, deep/superficial venous thrombosis, fluid retention
• CNS: Headache, migraine, dizziness, chorea, irritability, exacerbation of epilepsy, dementia
• PSYCHIATRIC: Depression, nervousness, mood disturbances
• GI: Nausea, vomiting; abdominal cramps, bloating, cholestatic jaundice, increased incidence of gallbladder disease, pancreatitis, enlargement of hepatic hemangiomas
• GU: Changes in vaginal bleeding pattern, abnormal withdrawal bleeding/flow, dysmenorrhea, vaginitis, vaginal candidiasis, change in amount of cervical secretion, changes in cervical ectropion, ovarian cancer, endometrial hyperplasia, endometrial cancer, breast tenderness/enlargement/pain, nipple discharge, galactorrhea, fibrocystic breast changes, breast cancer. ovarian CA
• HEMA: Aggravation of porphyria
• METABOLIC: Increase or decrease in weight, hypocalcemia
• DERM: Chloasma, melasma, erythema multiforme, erythema nodosum, hemorrhagic eruption, loss of scalp hair, hirsutism, pruritus, rash, urticaria
• EENT: Retinal vascular thrombosis, intolerance to contact lenses
• RESP: Pulmonary embolism, exacerbation of asthma
• REPRODUCTIVE: Changes in libido
• MUSC: Arthalgia, leg cramps
• HYPERSENSITIVITY: Angioedema, anaphylactoid/anaphylactic reactions

• 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)
• single intramuscular injection of estradiol cypionate is absorbed over several weeks
• Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Metabolized by liver; CYP450: 3A4. Also undergoes enterohepatic re-circulation
• Renally excreted as conjugates
• Half-life: Unknown

US Trade Name(s)

• Delestrogen

US Availability

estradiol valerate (generic)

• INJ: 10 mg/mL (5 mL vial)
• INJ: 20 mg/mL (5 mL vial)
• INJ: 40 mg/mL (5 mL vial)

Delestrogen

• INJ: 10 mg/mL (5 mL vial)
• INJ: 20 mg/mL (5 mL vial)
• INJ: 40 mg/mL (5 mL vial)

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]

Endocrine/Metabolic

Sex Hormones

Estrogens

Obstetrics/Gynecology

Sex Hormones

Estrogens

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

• Delestrogen 10 MG/ML OIL [Vial] (JHP PHARMACEUTICALS)
  5 ml = $85.99
  15 ml = $233.96
• Estradiol Valerate 20 MG/ML OIL [Vial] (SANDOZ)
  5 ml = $95.99
  15 ml = $255.98
• Delestrogen 40 MG/ML OIL [Vial] (JHP PHARMACEUTICALS)
  5 ml = $185.99
  15 ml = $519.96
• Delestrogen 20 MG/ML OIL [Vial] (JHP PHARMACEUTICALS)
  5 ml = $111.99
  15 ml = $315.97
• Estradiol Valerate 10 MG/ML OIL [Vial] (SANDOZ)
  5 ml = $75.99
  15 ml = $227.98

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.