Delestrogen

— THERAPEUTIC CATEGORIES —
  • Menopause and HRT
  • Prostate and other male cancers

Delestrogen Generic Name & Formulations

General Description

Estradiol valerate 10mg/mL (in a vehicle containing chlorobutanol 5mg and sesame oil), 20mg/mL (in a vehicle containing benzyl benzoate 224mg, benzyl alcohol 20mg, and castor oil), 40mg/mL (in a vehicle containing benzyl benzoate 447mg, benzyl alcohol 20mg, and castor oil); soln for IM inj.

Pharmacological Class

Estrogen.

How Supplied

Multi-dose vials (5mL)—1

Storage

Store between 20º to 25ºC (68º to 77ºF).

Mechanism of Action

Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.

Delestrogen Indications

Indications

Moderate to severe vasomotor symptoms of menopause. Moderate to severe symptoms of vulvar and vaginal atrophy of menopause. Hypoestrogenism due to hypogonadism, castration or primary ovarian failure.

Delestrogen Dosage and Administration

Adult

Give by deep IM inj into upper, outer quadrant of gluteal muscle. Vasomotor symptoms, vulvar, vaginal atrophy: 10–20mg every 4 weeks; attempts to discontinue or taper should be made at 3–6 month intervals. Hypoestrogenism: 10–20mg every 4 weeks.

Children

Not applicable.

Delestrogen Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Breast or other estrogen-dependent neoplasms. Active DVT, PE or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Pregnancy.

Delestrogen Boxed Warnings

Boxed Warning

Estrogens increase the risk of endometrial cancer. Cardiovascular disease and other risks.

Delestrogen Warnings/Precautions

Warnings/Precautions

Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Monitor conditions that may predispose to fluid retention. Endometriosis. Severe hypocalcemia. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers.

Delestrogen Pharmacokinetics

Distribution

Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in blood largely bound to SHBG and albumin.

Metabolism

Hepatic (CYP3A4).

Elimination

Renal.

Delestrogen Interactions

Interactions

May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John's wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

Delestrogen Adverse Reactions

Adverse Reactions

Nausea, vomiting, irregular bleeding, vaginitis, dysmenorrhea, headache, dizziness, edema, hypertension, mastodynia, chloasma, weight changes, intolerance to contact lenses; hypercoagulability, thromboembolism, neoplasms.

Delestrogen Clinical Trials

See Literature

Delestrogen Note

Not Applicable

Delestrogen Patient Counseling

See Literature

Delestrogen Generic Name & Formulations

General Description

Estradiol valerate 10mg/mL (in a vehicle containing chlorobutanol 5mg and sesame oil), 20mg/mL (in a vehicle containing benzyl benzoate 224mg, benzyl alcohol 20mg, and castor oil), 40mg/mL (in a vehicle containing benzyl benzoate 447mg, benzyl alcohol 20mg, and castor oil); soln for IM inj.

Pharmacological Class

Estrogen.

How Supplied

Multi-dose vials (5mL)—1

Storage

Store between 20º to 25ºC (68º to 77ºF).

Mechanism of Action

Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.

Delestrogen Indications

Indications

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

Delestrogen Dosage and Administration

Adult

Give by deep IM inj into upper, outer quadrant of gluteal muscle. 30mg or more every 1 or 2 weeks.

Children

Not applicable.

Delestrogen Contraindications

Contraindications

Thrombophlebitis. Thromboembolic disorders. Cerebrovascular disorders. Abnormal undiagnosed genital bleeding. Estrogen-depended neoplasias. Hepatic impairment or disease. Pregnancy.

Delestrogen Boxed Warnings

Boxed Warning

Estrogens increase the risk of endometrial cancer. Cardiovascular disease and other risks.

Delestrogen Warnings/Precautions

Warnings/Precautions

Cardiovascular disorders, arterial vascular disease, and risks factors (eg, hypertension, diabetes, obesity, SLE). Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. Hepatic dysfunction. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor BP, thyroid function. Monitor conditions that may predispose to fluid retention. Severe hypocalcemia. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. 

Delestrogen Pharmacokinetics

Distribution

Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in blood largely bound to SHBG and albumin.

Metabolism

Hepatic (CYP3A4).

Elimination

Renal.

Delestrogen Interactions

Interactions

May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John's wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

Delestrogen Adverse Reactions

Adverse Reactions

See full labeling. GI upset, headache, hypertension, edema, hypercalcemia, gallbladder or thromboembolic disease, gynecomastia, impotence, impaired glucose tolerance.

Delestrogen Clinical Trials

See Literature

Delestrogen Note

Not Applicable

Delestrogen Patient Counseling

See Literature