Activella

Generic name: Estradiol and Norethindrone Acetate

Drug class: Sex hormone combinations

Dosage form: Film-coated tablets

Root of administration: Oral

Dose: 1 mg estradiol and 0.5 mg norethindrone acetate per tablet, taken once daily

Mechanism of action: Estradiol is a synthetic form of the primary female sex hormone estrogen, which helps alleviate menopausal symptoms by compensating for the decreased natural estrogen levels. Norethindrone acetate is a synthetic progestin that, when combined with estrogen, reduces the risk of endometrial hyperplasia and cancer, conditions that can be associated with estrogen therapy alone.

Drug usage cases:

• Treatment of moderate to severe vasomotor symptoms due to menopause
• Treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause
• Prevention of postmenopausal osteoporosis

Drug contraindications:

• Undiagnosed abnormal genital bleeding
• Known, suspected, or history of breast cancer
• Known or suspected estrogen-dependent neoplasia
• Active deep vein thrombosis (DVT), pulmonary embolism (PE), or history of these conditions
• Active arterial thromboembolic disease (e.g., stroke, myocardial infarction) or history of these conditions
• Known anaphylactic reaction or angioedema to estradiol, norethindrone acetate, or any component of the formulation
• Known or suspected pregnancy

Side effects:

• Headache
• Breast pain
• Back pain
• Irregular vaginal bleeding or spotting
• Stomach or abdominal cramps, bloating
• Nausea and vomiting
• Diarrhea
• Fluid retention
• Vaginal yeast infection

Warnings:

• Increased risk of cardiovascular events, including myocardial infarction, stroke, pulmonary embolism, and deep vein thrombosis
• Increased risk of breast and endometrial cancer in postmenopausal women
• Probable increased risk of dementia in women aged 65 years and older
• Potential for gallbladder disease
• Possible changes in vision, including sudden loss of vision or other visual disturbances
• Elevated blood pressure
• Elevated triglyceride levels
• Liver dysfunction
• Changes in thyroid hormone levels
• Swelling or fluid retention
• Enlargement of benign tumors (e.g., fibroids)
• Worsening of angioedema in women with a history of this condition
• Altered laboratory test results, such as increased bleeding time and elevated blood sugar levels

Use during pregnancy or breastfeeding: Activella is contraindicated during pregnancy due to potential harm to the developing fetus. It is also contraindicated during breastfeeding, as it may be excreted in breast milk and could affect the nursing infant. Women who are pregnant or breastfeeding should not use Activella.