Activella Indications, Dosage, Storage, Stability - Estradiol/Norethindroneacetate

Activella Indications, Dosage, Storage, Stability - Estradiol/Norethindroneacetate

INDICATIONS

Activella^™ therapy is indicated in women with an intact uterus for the: 1. Treatment of moderate to severe vasomotor symptoms associated with the menopause. There is no adequate evidence that estrogens are effective for nervous symptoms or depression that might occur during menopause and they should not be used to treat these conditions. 2. Treatment of vulvar and vaginal atrophy.

3. Prevention of postmenopausal osteoporosis.

Most prospective studies of efficacy for the osteoporosis prevention indication have been carried out in white postmenopausal women, without stratification by other risk factors, and tend to show a universally beneficial effect on bone. Since estrogen administration is associated with risk, patient selection must be individualized based on the balance of risks and benefits.

Case-control studies have shown an approximately 60-percent reduction in hip and wrist fractures in women whose estrogen replacement was begun within a few years after menopause. Studies also suggest that estrogen reduces the rate of ver-tebral fractures. When estrogen therapy is discontinued, bone mass declines at a rate comparable to the immediate postmenopausal period. White and Asian women are at higher risk for osteoporosis than black women, and thin women are at a higher risk than heavier women, who generally have higher endogenous estrogen levels. Early menopause is one of the strongest predictors for the development of osteoporosis. Other factors associated with osteoporosis include genetic factors (small build, family history), lifestyle (cigarette smoking, alcohol abuse, sedentary exercise habits) and nutrition (below average body weight and dietary calcium intake).

The mainstays of prevention and management of osteoporosis are weight-bearing exercise, adequate calcium intake, and, when indicated, estrogen. Postmenopausal women absorb dietary calcium less efficiently than premenopausal women and require an average of 1500 mg/day of elemental calcium to remain in neutral calcium balance. The average calcium intake in the USA is 400-600 mg/day. Therefore, when not contraindicated, calcium supplementation may be helpful for women with suboptimal dietary intake.

DOSAGE AND ADMINISTRATION

Activella^™ (estradiol/norethindrone acetate tablets) therapy consists of a single tablet to be taken once daily. For the treatment of moderate to severe vasomotor symptoms associated with the menopause, treatment of vulvar and vaginal atrophy, and the prevention of postmenopausal osteoporosis - Activella^™ 1 mg E2 / 0.5 mg NETA daily. The doses of 17beta-estradiol and norethindrone acetate in Activella^™ may not be the lowest effective dose-combination for the prevention of osteoporosis.

Treated patients with an intact uterus should be monitored closely for signs of endometrial cancer, and appropriate diagnostic measures should be taken to rule out malignancy in the event of persistent or recurring abnormal vaginal bleeding.

HOW SUPPLIED

Activella^™, 1 mg estradiol and 0.5 mg norethindrone acetate, is a white, film-coated tablet, engraved with NOVO 288 on one side and the APIS bull on the other. It is round, 6 mm in diameter and bi-convex. Activella^™ is supplied as: 28 tablets in a calendar dial pack dispenser NDC 0009-5174-02. Store in a dry place protected from light. Store at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF). [See USP Controlled Room Temperature]

© May 2000

Activella^™ is a trademark owned by Novo Nordisk A/S, Revised May 2000

Manufactured for: Pharmacia & Upjohn Company , Kalamazoo, MI 49001, USA

By Novo Nordisk A/S 2880 Bagsværd, Denmark