ELESTRIN Dosage & Rx Info | Uses, Side Effects

Elestrin Generic Name & Formulations

Legal Class

General Description

Estradiol 0.06%; gel; contains alcohol.

Pharmacological Class

Estrogen.

How Supplied

Pump (35g)—1, 2

Storage

Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F).

Manufacturer

Mylan Inc.

Generic Availability

Mechanism of Action

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

Elestrin Indications

Indications

Moderate to severe vasomotor symptoms due to menopause.

Elestrin Dosage and Administration

Adult

Prime pump before 1^stuse. Use lowest effective dose. Initially: apply 1 pump (0.87g) once daily to clean, dry, unbroken skin of upper arm.

Children

Not applicable.

Elestrin Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Breast cancer or history of. Estrogen-dependent neoplasia. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders.

Elestrin Boxed Warnings

Boxed Warning

Endometrial cancer. Cardiovascular disorders. Probable dementia. Breast cancer.

Elestrin 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 disorders (eg, stroke, MI, VTE); discontinue if occurs or suspected. 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. Conditions aggravated by fluid retention. Hypocalcemia. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, BP). Flammable. Reevaluate periodically. Pregnancy: not indicated. Nursing mothers: not recommended.

Elestrin Pharmacokinetics

Absorption

Steady-state serum concentrations of estradiol are achieved in ~3 days.

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.

Elimination

Renal.

Elestrin Interactions

Interactions

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

Elestrin Adverse Reactions

Adverse Reactions

Breast tenderness, metrorrhagia, nasopharyngitis, upper respiratory tract infection; thromboembolism, neoplasms.

Elestrin Clinical Trials

See Literature

Elestrin Note

Not Applicable

Elestrin Patient Counseling