ANGELIQ 0.25/0.5 Dosage & Rx Info

Angeliq 0.25/0.5 Generic Name & Formulations

Legal Class

General Description

Drospirenone 0.25mg, estradiol 0.5mg; tabs.

Pharmacological Class

Progestin + estrogen.

How Supplied

Blister packs (28 tabs)—3

Manufacturer

Bayer Corporation

Generic Availability

Mechanism of Action

Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH), and follicle-stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated concentrations of these gonadotropins seen in postmenopausal women. Drospirenone is a synthetic progestin and spironolactone analog with antimineralocorticoid activity. In animals and in vitro, drospirenone has antiandrogenic activity, but no glucocorticoid, antiglucocorticoid, estrogenic, or androgenic activity. Progestins counter estrogenic effects by decreasing the number of nuclear estradiol receptors and suppressing epithelial DNA synthesis in endometrial tissue.

Angeliq 0.25/0.5 Indications

Indications

In women with an intact uterus: moderate to severe vasomotor symptoms of menopause; moderate to severe vulvar and vaginal atrophy due to menopause.

Angeliq 0.25/0.5 Dosage and Administration

Adult

Swallow whole. Give continuously. Vasomotor symptoms: 0.25mg/0.5mg or 0.5mg/1mg tab once daily. Vulvar and vaginal atrophy: 0.5mg/1mg tab once daily.

Children

Not applicable.

Angeliq 0.25/0.5 Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Breast cancer. Estrogen-dependent neoplasia. Thromboembolic disorders (eg, DVT, PE, stroke, MI). Protein C, protein S, or antithrombin deficiency, or other thrombophilias. Adrenal insufficiency. Renal impairment. Hepatic impairment or disease. Pregnancy.

Angeliq 0.25/0.5 Boxed Warnings

Boxed Warning

Cardiovascular disorders. Endometrial cancer and breast cancer. Probable dementia.

Angeliq 0.25/0.5 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, stroke, MI, DVT, PE); discontinue if occurs or is suspected. 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. Increased risk of hyperkalemia or hyponatremia in high-risk patients. 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. Discontinue if cholestatic jaundice, pancreatitis, or hypercalcemia occurs. Monitor thyroid function. Conditions aggravated by fluid retention. 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. Nursing mothers.

Angeliq 0.25/0.5 Pharmacokinetics

Absorption

Median Tmax: ~2 hours after administration. Mean absolute bioavailability ranges from 76–85%. Steady state for drospirenone observed after 10 days.

Distribution

Mean volume of distribution: 4.2 L/kg (drospirenone). Drospirenone does not bind to SHBG or CBG but binds ~97% to other serum proteins. Estradiol binds to SHBG (37%) and to albumin (61%).

Metabolism

Hepatic.

Elimination

Renal. Half-life: ~36–42 hours (drospirenone).

Angeliq 0.25/0.5 Interactions

Interactions

Monitor serum K⁺ during 1^st cycle with drugs that increase potassium (eg, ACEIs, ARBs, NSAIDs, K⁺-sparing diuretics, K⁺ supplements, heparin, aldosterone antagonists); consider monitoring in high-risk patients taking concomitant long-term strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, voriconazole, indinavir, boceprevir, clarithromycin). May be potentiated by CYP3A4 inhibitors (eg, azoles, verapamil, macrolides, diltiazem, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). May be affected by protease inhibitors, NNRTIs. Avoid alcohol. 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).

Angeliq 0.25/0.5 Adverse Reactions

Adverse Reactions

Abdominal pain, female genital tract bleeding, breast pain/discomfort, headache; thromboembolism, neoplasms.

Angeliq 0.25/0.5 Clinical Trials

See Literature

Angeliq 0.25/0.5 Note

Not Applicable

Angeliq 0.25/0.5 Patient Counseling