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Activella (Estradiol) - Summary

 
 



BOX WARNING

CARDIOVASCULAR AND OTHER RISKS

Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. (See CLINICAL STUDIES  and  WARNINGS , Cardiovascular disorders and Dementia.)

The estrogen plus progestin substudy of the Women’s Health Initiative (WHI) reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) during 5.6 years of treatment with oral conjugated estrogens (CE 0.625 mg) combined with medroxyprogesterone acetate (MPA 2.5 mg) per day, relative to placebo. (See CLINICAL STUDIES and WARNINGS, Cardiovascular disorders and Malignant neoplasms, Breast cancer.)

The estrogen-alone substudy of the WHI reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) during 6.8 years and 7.1 years, respectively, of treatment with oral conjugated estrogens (CE 0.625 mg) per day, relative to placebo. (See CLINICAL STUDIES and WARNINGS , Cardiovascular disorders.)

The Women’s Health Initiative Memory Study (WHIMS), a substudy of the WHI study, reported increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with CE 0.625 mg combined with MPA 2.5 mg and during 5.2 years of treatment with CE 0.625 mg alone, relative to placebo. It is unknown whether this finding applies to younger postmenopausal women. (See CLINICAL STUDIES, WARNINGS, Dementia and PRECAUTIONS, Geriatric Use.)

Other doses of oral conjugated estrogens with medroxyprogesterone acetate, and other combinations and dosage forms of estrogens and progestins were not studied in the WHI clinical trials and, in the absence of comparable data, these risks should be assumed to be similar. Because of these trials, estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.

 

ACTIVELLA SUMMARY

CARDIOVASCULAR AND OTHER RISKS

Activella® is a single tablet containing an estrogen, estradiol (E2), and a progestin, norethindrone acetate (NETA), for oral administration. Each tablet contains 1 mg estradiol and 0.5 mg norethindrone acetate and the following excipients: lactose monohydrate, starch (corn), copovidone, talc, magnesium stearate, hypromellose and triacetin.

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 vertebral 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.
See all Activella indications & dosage >>

NEWS HIGHLIGHTS

Media Articles Related to Activella (Estradiol)

In postmenopausal women at risk for dementia, estradiol preserves key brain regions
Source: Endocrinology News From Medical News Today [2014.03.14]
When initiated soon after menopause, hormone therapy with estradiol prevented degeneration in key brain regions of women who were at heightened dementia risk, according to a new study led by Stanford...

more news >>

Published Studies Related to Activella (Estradiol)

Effects of tibolone or continuous combined oestradiol/norethisterone acetate on glucose and insulin metabolism. [2013]
insulin metabolism in postmenopausal women... CONCLUSIONS: Tibolone reduces insulin sensitivity. Healthy postmenopausal women

An overview of four studies of a continuous oral contraceptive (levonorgestrel 90 mcg/ethinyl estradiol 20 mcg) on premenstrual dysphoric disorder and premenstrual syndrome. [2012]
and premenstrual syndrome (PMS)... CONCLUSIONS: These data, although not consistent, indicate that continuous LNG/EE

Blastocyst-stage versus cleavage-stage embryo transfer in women with high oestradiol concentrations: randomized controlled trial. [2011.12]
This prospective, randomized, controlled trial tested the hypothesis that delaying embryo transfer to the blastocyst stage can increase the probability of clinical pregnancy and live birth in women with high oestradiol concentrations on the day of human chorionic gonadotrophin (HCG) undergoing intracytoplasmic sperm injection using the long protocol...

Ethinyl estradiol and levonorgestrel pharmacokinetics with a low-dose transdermal contraceptive delivery system, AG200-15: a randomized controlled trial. [2011.11.29]
BACKGROUND: This study evaluated the ethinyl estradiol (EE) and levonorgestrel (LNG) pharmacokinetic profiles of AG200-15, a transdermal contraceptive delivery system, compared with a combination oral contraceptive (COC) containing EE 35 mcg and norgestimate 250 mcg... CONCLUSIONS: EE and LNG daily exposure during AG200-15 treatment was within the range reported for a low-dose COC. The daily EE dose with AG 200-15 was equivalent to a 30-mcg COC and was safe and well tolerated. Copyright (c) 2011 Elsevier Inc. All rights reserved.

Naproxen or estradiol for bleeding and spotting with the levonorgestrel intrauterine system: a randomized controlled trial. [2011.09.24]
OBJECTIVE: The purpose of this study was to evaluate whether oral naproxen or transdermal estradiol decreases bleeding and spotting in women who are initiating the levonorgestrel-releasing intrauterine system... CONCLUSION: The administration of naproxen resulted in a reduction in bleeding and spotting days compared with placebo. Copyright A(c) 2011 Mosby, Inc. All rights reserved.

more studies >>

Clinical Trials Related to Activella (Estradiol)

Efficacy and Tolerability Study of Progesterone Vaginal Tablets (Endometrin´┐Ż) in Menopausal Women Treated by Estrogen [Not yet recruiting]

A Study to Characterize Epidemiology, Clinical and Genetic Features of Kallmann Syndrome in Finland [Enrolling by invitation]

more trials >>

Reports of Suspected Activella (Estradiol) Side Effects

Breast Cancer Female (4)Product Substitution Issue (2)Night Sweats (1)Drug Ineffective (1)Haemorrhage (1)Wrong Drug Administered (1)Vaginal Haemorrhage (1)Hot Flush (1)Hypertrichosis (1)Depression (1)more >>


Page last updated: 2014-03-14

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