BIJUVA Dosage & Rx Info | Uses, Side Effects

Bijuva Generic Name & Formulations

Legal Class

General Description

Estradiol, progesterone; 0.5mg/100mg, 1mg/100mg; caps.

Pharmacological Class

Estrogen + progestin.

How Supplied

Caps—30

Manufacturer

TherapeuticsMD, Inc.

Generic Availability

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. Progesterone enhances cellular differentiation and generally opposes 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. Progesterone exerts its effects in target cells by binding to specific progesterone receptors that interact with progesterone response elements in target genes.

Bijuva Indications

Indications

Moderate to severe vasomotor symptoms due to menopause in women with a uterus.

Bijuva Dosage and Administration

Adult

Use lowest effective dose for the shortest duration. Take with food. Initially 0.5mg/100mg daily in the evening; adjust based on response. Attempt to taper or discontinue at 3–6 month intervals.

Children

Not applicable.

Bijuva Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Breast or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders.

Bijuva Boxed Warnings

Boxed Warning

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

Bijuva Warnings/Precautions

Warnings/Precautions

Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, stroke, MI, VTE); discontinue if occurs or suspected. Manage risk factors for cardiovascular disease and/or 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 endometrial cancer in women with intact uterus (adding progestins has been shown to reduce endometrial hyperplasia risk). 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. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Monitor conditions that may predispose to fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Perform yearly breast exams (including mammography). Reevaluate periodically. Elderly. Nursing mothers.

Bijuva Pharmacokinetics

Distribution

Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in blood largely bound to SHBG and albumin.

Plasma protein bound: ~96–99% (progesterone).

Metabolism

Hepatic.

Elimination

Renal. Half-life: ~26 hours (estradiol); ~10 hours (progesterone).

Bijuva 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).

Bijuva Adverse Reactions

Adverse Reactions

Breast tenderness, headache, nausea, vaginal bleeding, vaginal discharge, pelvic pain; thromboembolism, neoplasms.

Bijuva Clinical Trials

See Literature

Bijuva Note

Not Applicable

Bijuva Patient Counseling