Activella

— THERAPEUTIC CATEGORIES —
  • Bone disorders
  • Menopause and HRT
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Activella Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Estradiol, norethindrone acetate; 1mg/0.5mg; tabs.

    Pharmacological Class

    Estrogen + progestin.

    How Supplied

    Packs (28 tabs)—1

    Manufacturer

    Amneal Pharmaceuticals

    Generic Availability

    YES

    Mechanism of Action

    Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH), and FSH through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women. Progestin compounds enhance cellular differentiation and generally oppose the actions of estrogens by decreasing estrogen receptor levels, increasing local metabolism of estrogens to less active metabolites, or inducing gene products that blunt cellular responses to estrogen. Progestins exert their effects in target cells by binding to specific progesterone receptors that interact with progesterone response elements in target genes.

    Activella Indications

    Indications

    Prevention of postmenopausal osteoporosis.

    Activella Dosage and Administration

    Adult

    1 tab (1mg/0.5mg) once daily.

    Children

    Not applicable.

    Activella Contraindications

    Contraindications

    Undiagnosed abnormal genital bleeding. Breast or other estrogen-dependent neoplasms. Thromboembolic disorders (eg, DVT, PE, stroke, MI). Protein C, protein S, or antithrombin deficiency, or other thrombophilias. Hepatic impairment or disease.

    Activella Boxed Warnings

    Boxed Warning

    Cardiovascular disorders. Probable dementia. Breast cancer. Endometrial cancer.

    Activella Warnings/Precautions

    Warnings/Precautions

    Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); immediately discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. History of hypertriglyceridemia or cholestatic jaundice. Discontinue if cholestatic jaundice, pancreatitis, or hypercalcemia occurs. Monitor thyroid function, conditions aggravated by fluid retention (discontinue if medically concerning). Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Pregnancy: not indicated. Nursing mothers.

    Activella Pharmacokinetics

    Absorption

    Peak plasma concentration: 5–8 hours (estradiol); 0.51.5 hours (norethindrone acetate). Bioavailability: 53% (estradiol); 100% (norethindrone acetate).

    Distribution

    Protein bound: 36–37% (SHBG); albumin (61%).

    Metabolism

    Hepatic.

    Elimination

    Renal. Half-life: 12–14 hours (estradiol); 8–11 hours (norethindrone acetate).

    Activella Interactions

    Interactions

    May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

    Activella Adverse Reactions

    Adverse Reactions

    Back pain, headache, pain in the extremity, nausea, diarrhea, gastroenteritis, insomnia, emotional lability, upper RTI, sinusitis, nasopharyngitis, weight increase, breast pain, post-menopausal bleeding, uterine fibroid, vaginal hemorrhage, ovarian cyst, endometrial thickening, viral infection, moniliasis genital, accidental injury; thromboembolism, neoplasms.

    Activella Clinical Trials

    See Literature

    Activella Note

    Not Applicable

    Activella Patient Counseling

    See Literature

    Activella Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Estradiol, norethindrone acetate; 1mg/0.5mg; tabs.

    Pharmacological Class

    Estrogen + progestin.

    How Supplied

    Packs (28 tabs)—1

    Manufacturer

    Amneal Pharmaceuticals

    Generic Availability

    YES

    Mechanism of Action

    Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH), and FSH through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women. Progestin compounds enhance cellular differentiation and generally oppose the actions of estrogens by decreasing estrogen receptor levels, increasing local metabolism of estrogens to less active metabolites, or inducing gene products that blunt cellular responses to estrogen. Progestins exert their effects in target cells by binding to specific progesterone receptors that interact with progesterone response elements in target genes.

    Activella Indications

    Indications

    Moderate to severe vasomotor symptoms of menopause. Moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.

    Activella Dosage and Administration

    Adult

    1 tab (1mg/0.5mg) once daily.

    Children

    Not applicable.

    Activella Contraindications

    Contraindications

    Undiagnosed abnormal genital bleeding. Breast or other estrogen-dependent neoplasms. Thromboembolic disorders (eg, DVT, PE, stroke, MI). Protein C, protein S, or antithrombin deficiency, or other thrombophilias. Hepatic impairment or disease.

    Activella Boxed Warnings

    Boxed Warning

    Cardiovascular disorders. Probable dementia. Breast cancer. Endometrial cancer.

    Activella Warnings/Precautions

    Warnings/Precautions

    Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); immediately discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. History of hypertriglyceridemia or cholestatic jaundice. Discontinue if cholestatic jaundice, pancreatitis, or hypercalcemia occurs. Monitor thyroid function, conditions aggravated by fluid retention (discontinue if medically concerning). Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Pregnancy: not indicated. Nursing mothers.

    Activella Pharmacokinetics

    Absorption

    Peak plasma concentration: 5–8 hours (estradiol); 0.51.5 hours (norethindrone acetate). Bioavailability: 53% (estradiol); 100% (norethindrone acetate).

    Distribution

    Protein bound: 36–37% (SHBG); albumin (61%).

    Metabolism

    Hepatic.

    Elimination

    Renal. Half-life: 12–14 hours (estradiol); 8–11 hours (norethindrone acetate).

    Activella Interactions

    Interactions

    May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

    Activella Adverse Reactions

    Adverse Reactions

    Back pain, headache, pain in the extremity, nausea, diarrhea, gastroenteritis, insomnia, emotional lability, upper RTI, sinusitis, nasopharyngitis, weight increase, breast pain, post-menopausal bleeding, uterine fibroid, vaginal hemorrhage, ovarian cyst, endometrial thickening, viral infection, moniliasis genital, accidental injury; thromboembolism, neoplasms.

    Activella Clinical Trials

    See Literature

    Activella Note

    Not Applicable

    Activella Patient Counseling

    See Literature

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