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Conjugated Estrogen + Bazedoxifene

Generic Medicine
Indications

This medication is used to treat moderate to severe hot flashes related to menopause and to help prevent osteoporosis after menopause.

Pharmacology

Conjugated estrogens and bazedoxifene work by binding to and activating estrogen receptors (ER) alpha and beta. Bazedoxifene acts as both an estrogen agonist and antagonist—stimulating estrogen effects in some tissues while blocking them in others, such as the uterus.

Dosage Administration

Take Bestron once daily, without regard to meals. Tablets should be swallowed whole. Women taking Bestron for prevention of postmenopausal osteoporosis should add supplemental calcium and/or vitamin-D to their diet if daily intake is inadequate. Use in Children: Bestron is not indicated for use in children

Interactions

No formal drug interaction studies have been conducted with this tablet. Estrogens are partly metabolized by the CYP3A4 enzyme. Using this medication together with CYP3A4 inhibitors may increase the levels of conjugated estrogens in the body, which could raise the risk of endometrial hyperplasia.

Contraindications

Bestron should not be used in women who have unexplained abnormal uterine bleeding, or who have a known, suspected, or previous history of breast cancer. It is also contraindicated in those with known or suspected estrogen-dependent tumors, active or past deep vein thrombosis (DVT) or pulmonary embolism, or other active arterial thromboembolic diseases.

It must not be used in patients with hypersensitivity (such as anaphylaxis or angioedema) to estrogens, bazedoxifene, or any of the tablet’s ingredients. It is also contraindicated in women with known liver impairment or other known blood clotting (thrombophilic) disorders.

Side Effects

Possible side effects include high blood pressure, blood clots, liver disorders, and thyroid problems. Other effects may include fluid retention, low calcium levels (hypocalcemia), and risk of dementia.

Some patients may also experience breast lumps, abnormal vaginal bleeding, severe headache, muscle cramps, weakness, fatigue, nausea, diarrhea, throat pain, and dizziness.

Pregnancy & Lactation

Bestron is classified as Pregnancy Category X and must not be used during pregnancy or in women who may become pregnant. It is also not recommended for use during breastfeeding. It is unknown whether the drug passes into human breast milk. However, estrogen therapy in nursing mothers has been shown to reduce both the amount and quality of breast milk.

Precautions & Warnings

Estrogen therapy should not be used to prevent cardiovascular disease or dementia. In women who still have a uterus, using estrogen without adequate opposition increases the risk of endometrial cancer.

Overdose Effects

There is no specific antidote for overdose. Treatment should be supportive and based on symptoms. Overdose of estrogen-containing medicines may cause nausea, vomiting, breast tenderness, dizziness, abdominal pain, and fatigue. Withdrawal bleeding may also occur.

Therapeutic Class

Female Sex hormones

Storage Conditions

Keep out of reach of children. Store below 30°C and protect from light. After opening the foil pouch, the product should be used within 60 days.

Common Questions

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