Activella is an estrogen and progestin combination indicated in a woman with a uterus for the:

Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause

Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause

When prescribing solely for the prevention of postmenopausal osteoporosis, first consider the use of non-estrogen medications. Consider estrogen therapy only for women at significant risk of osteoporosis.

Prevention of Postmenopausal Osteoporosis

When prescribing solely for the prevention of postmenopausal osteoporosis, first consider the use of non estrogen medications. Consider estrogen therapy only for women at significant risk of osteoporosis.

Prescribe estrogens with or without progestogens at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.

Do not use estrogen-alone therapy for the prevention of cardiovascular disease or dementia.

Estrogen Plus Progestin Therapy:

• Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease or dementia
• There is increased risk of deep vein thrombosis (DVT), pulmonary embolism (PE), stroke and myocardial infarction (MI) in postmenopausal women (50 to 79 years of age) during 5.6 years of treatment with daily oral conjugated estrogen (CE) [0.625 mg] combined with medroxyprogesterone acetate (MPA) [2.5 mg], relative to placebo
• There is increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily CE (0.625 mg) combined with MPA (2.5 mg), relative to placebo. It is unknown whether this finding applies to younger postmenopausal women
• Estrogen plus progestin substudy also demonstrated an increased risk of invasive breast cancer

Estrogen-Alone Therapy:

• There is increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding
• Estrogen-alone therapy should not be used for the prevention of cardiovascular disease or dementia
• There is increased risk of stroke and DVT in postmenopausal women (50 to 79 years of age) during 7.1 years of treatment with daily oral CE (0.625 mg)-alone, relative to placebo
• There is increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 5.2 years of treatment with daily CE (0.625 mg)-alone, relative to placebo. It is unknown whether this finding applies to younger postmenopausal women

Activella is contraindicated in patients with:

• Undiagnosed abnormal genital bleeding
• Known, suspected, or history of breast cancer
• Known, past or suspected estrogen-dependent neoplasia
• Active DVT, PE, or history of these conditions
• Active arterial thromboembolic disease (for example stroke and MI), or a history of these conditions
• Known anaphylactic reaction or angioedema or hypersensitivity to Activella
• Known liver impairment or disease
• Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
• Known or suspected pregnancy 

A 2- to 4-fold increase in the risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens has been reported.

Estrogen administration may lead to severe hypercalcemia in patients with breast cancer and bone metastases.

Retinal vascular thrombosis has been reported in patients receiving estrogens.

In a small number of case reports, substantial increases in blood pressure have been attributed to idiosyncratic reactions to estrogens.

In women with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis.

Estrogen therapy should be used with caution in women with hypoparathyroidism as estrogen-induced hypocalcemia may occur.

Estrogen therapy may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas and should be used with caution in women with these conditions.

Inducers of CYP3A4 such as St. John’s wort (Hypericum perforatum) preparations, phenobarbital, carbamazepine, and rifampin may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile. Inhibitors of CYP3A4 such as erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice may increase plasma concentrations of estrogens and result in side effects.

Drugs or herbal products that induce or inhibit cytochrome P-450 enzymes, including CYP3A4, may decrease or increase the serum concentrations of norethindrone.

Activella should not be used during pregnancy.

Activella should not be used during lactation.

GoToSource

• Decrease dementia. GoToSource

• Reduction of peripheral arterial disease. GoToSource

• Decrease intraocular pressure, delay cataract formation and decrease aging macular degeneration in post-menopausal women. GoToSource

• Use in patients under the age of 18. GoToSource

Increased risk of myocardial infarction, stroke, pulmonary embolism and deep vein thrombosis.. GoToSource

Increased risk of gallbladder disease. GoToSource

Increased risk of breast, ovarian and endometrial cancer. GoToSource

Postmenopausal bleeding. GoToSource

Increased risk of dementia. GoToSource

Retinal vascular thrombosis. GoToSource

Pancreatitis (inflammation of pancreas). GoToSource

Lawsuits filed for breast and ovarian cancer.