ESTROGEL Dosage & Rx Info | Uses, Side Effects

Estrogel Generic Name & Formulations

Legal Class

General Description

Estradiol 0.06%; topical gel; contains alcohol.

Pharmacological Class

Estrogen.

How Supplied

Metered-dose pump (50g)—1

Manufacturer

Ascend Therapeutics

Generic Availability

Mechanism of Action

Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretions 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.

Estrogel Indications

Indications

Moderate to severe vasomotor symptoms of menopause. Vulvar and vaginal atrophy due to menopause.

Estrogel Dosage and Administration

Adult

Prime pump before 1^st use. Apply 1 pump (1.25g) daily to clean, dry, intact skin over one arm; allow to dry for 5mins.

Children

Not applicable.

Administration

Prime pump before 1^st use. Depress pump twice for 93g pump or 3 times for 50g and 25g pump. Apply at the same time each day to clean, dry, unbroken skin. Apply after bath, shower, or sauna. Be sure skin is completely dry before applying. Wash hands after applying. Do not apply directly to breast. Missed dose: if next dose <12hrs away, wait and apply the next day; if >12hrs away, apply missed dose, then resume normal schedule.

Nursing Considerations

Prime pump before 1^st use. Depress pump twice for 93g pump or 3 times for 50g and 25g pump. Apply at the same time each day to clean, dry, unbroken skin. Apply after bath, shower, or sauna. Be sure skin is completely dry before applying. Wash hands after applying. Do not apply directly to breast. Avoid fire, flame or smoking until the gel has dried. Missed dose: if next dose <12hrs away, wait and apply the next day; if >12hrs away, apply missed dose, then resume normal schedule.

Estrogel 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 history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency or other thrombophilic disorders.

Estrogel Boxed Warnings

Boxed Warning

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

Estrogel 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, stroke, MI, VTE); discontinue if these occur or are 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. Monitor conditions that may predispose to fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Flammable. Reevaluate periodically. Pregnancy: not indicated. Nursing mothers.

Estrogel Pharmacokinetics

Absorption

Estradiol is transported across intact skin and into the systemic circulation by a passive diffusion process. The rate of diffusion across the stratum corneum is the rate-limiting factor. When EstroGel is applied to the skin, it dries in 2–5 minutes.

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. Half-life: ~36 hours.

Estrogel 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. May be affected by application of topical lotion (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).

Estrogel Adverse Reactions

Adverse Reactions

Headache, flatulence, breast pain, rash, pruritus; thromboembolism, neoplasms.

Estrogel Clinical Trials

See Literature

Estrogel Note

Not Applicable

Estrogel Patient Counseling