Company:

Kenwood Therapeutics

Estrogen

Estradiol 0.06%; gel; contains alcohol.

Moderate-to-severe vasomotor symptoms associated with menopause.

The addition of exogenous estrogens, such as Elestrin, helps to alleviate the vasomotor symptoms associated with declining estrogen levels. Elestrin contains 0.06% estradiol in a hydro-alcoholic gel base. One pump actuation delivers 0.87g, which provides systemic delivery of 0.0125mg of estradiol daily. The 1.7g dose, two pump actuations, provides systemic delivery of 0.0375mg daily. After applying Elestrin to the upper arm, steady state serum concentrations are achieved in about three days.

Application of sunscreen 10 minutes before application of Elestrin increased exposure to estradiol by 55%. Concomitant sunscreen application for seven days increased estradiol exposure by 2-fold, regardless of when sunscreen was applied.

The efficacy of Elestrin was evaluated in a 12-week double-blind, placebo-controlled trial involving 484 postmenopausal women 28–74 years of age who had at least 60 moderate-to-severe hot flushes per week at baseline. Patients applied Elestrin 0.87g (0.52mg estradiol), 1.7g (1.02mg estradiol), 2.6g (1.56mg), or placebo once daily to the upper arm. Reduction in both the frequency and severity of hot flushes was statistically significant at week 4 for the Elestrin 1.7g/day dose, and week 5 for the Elestrin 0.87g/day dose when compared to placebo. Both the 0.87g/day and 1.7g/day doses were statistically significant compared to placebo at week 12.

Prime pump before 1st use. Use lowest effective dose. Initially: Apply 1 pump (0.87g) daily to clean, dry, unbroken skin of upper arm. Reevaluate periodically.

Not applicable.

Undiagnosed abnormal genital bleeding. Thromboembolic disease (eg, stroke or MI within past year, DVT, pulmonary embolism). Thrombophlebitis. Breast or estrogen-dependent carcinoma. Liver dysfunction or disease. Pregnancy (Cat X).

Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Renal dysfunction. Gallbladder disease. Hypertriglyceridemia. Hypothyroidism. Conditions aggravated by fluid retention. Bone disease associated with hypercalcemia. Do initial complete physical; repeat annually (include BP, mammogram, PAP smear). Discontinue if jaundice occurs and during immobilization or 2 weeks before planned mammogram or surgery associated with thromboembolism. Product is flammable. Nursing mothers.

May be antagonized by CYP3A4 inducers. May be potentiated by CYP3A4 inhibitors. Avoid applying sunscreen to application site (increases estradiol absorption).

See literature. Breast tenderness, metrorrhagia, vaginal discharge, nausea, nasopharyngitis, upper respiratory tract infection. Long-term use may increase risk of estrogen-dependent cancers (eg, breast and/or endometrial), dementia, others. Increased risk of thromboembolic disorders, gallbladder disease.

Gel—144g (100 metered 0.87g doses)

For more information call (800) 929-9300.

5/25/07