Conjugated Estrogen + Bazedoxifene

Conjugated Estrogen + Bazedoxifene Uses, Dosage, Side Effects, Food Interaction and all others data.

Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. It is approved in the European Union (marketed in Italy and Spain) and Japan as monotherapy. In 2013, the combination product containing conjugated estrogens and bazedoxifene was approved by the FDA for the treatment of moderate to severe vasomotor symptoms associated with menopause, as well as the prevention of postmenopausal osteoporosis in women.

Conjugated Estrogen + Bazedoxifene
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Conjugated Estrogen + Bazedoxifene
Generic	Conjugated Estrogen + Bazedoxifene
Type
Therapeutic Class	Female Sex hormones
Manufacturer
Available Country	Bangladesh
Last Updated:	September 24, 2024 at 5:38 am

Uses

This is a combination of conjugated estrogens with an estrogen agonist/antagonist indicated for treatment of the following conditions in women with a uterus: Treatment of moderate to severe vasomotor symptoms associated with menopause Prevention of postmenopausal osteoporosis

Conjugated Estrogen + Bazedoxifene is also used to associated treatment for these conditions: Postmenopausal Osteoporosis, Moderate Menopausal Vasomotor Symptoms, Severe Vasomotor Symptoms Associated With Menopause

How Conjugated Estrogen + Bazedoxifene works

Bazedoxifene belongs to a class of compounds known as selective estrogen receptor modulators (SERMs). Bazedoxifene acts as both an oestrogen-receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifene decreases bone resorption and reduces biochemical markers of bone turnover to the premenopausal range. These effects on bone remodelling lead to an increase in bone mineral density (BMD), which in turn contributes to a reduction in the risk of fractures. Bazedoxifene functions primarily as an oestrogen-receptor antagonist in uterine and breast tissues.

Side Effects

In four prospective, randomized, placebo-controlled trials the common adverse reactions (incidence ≥5%) were muscle spasms, nausea, diarrhea, dyspepsia, abdominal pain upper, oropharyngeal pain, dizziness, and neck pain.

Precaution

Women taking this tablet should not take progestins, additional estrogens or additional estrogen agonist/antagonists Cardiovascular disorders, including venous thromboembolism, pulmonary embolism, stroke, and retinal vascular thrombosis Malignant neoplasms, including endometrial cancer, breast cancer, and ovarian cancer Estrogens increase the risk of gallbladder disease Discontinue estrogen if loss of vision, severe hypertriglyceridemia or cholestatic jaundice occurs Monitor thyroid function in women on thyroid replacement therapy

Interaction

No drug interaction studies were conducted with This tablet. Estrogens are metabolized partially by CYP3A4. Concomitant use of this tablet with CYP3A4 inhibitors may increase the exposure of conjugated estrogens and thereby may increase the risk of endometrial hyperplasia.

Volume of Distribution

Following intravenous administration of a 3 mg dose of bazedoxifene, the volume of distribution is 14.7 ± 3.9 l/kg.

Elimination Route

Bazedoxifene is rapidly absorbed with a tmax of approximately 2 hours and exhibits a linear increase in plasma concentrations for single doses from 0.5 mg up to 120 mg and multiple daily doses from 1 mg to 80 mg. The absolute bioavailability of bazedoxifene is approximately 6%.

Half Life

~30 hours.

Clearance

The apparent oral clearance of bazedoxifene is approximately 4 to 5 l/h/kg.

Elimination Route

The major route of elimination of radio-labelled bazedoxifene is the faeces, and less than 1% of the dose is eliminated in urine.

Pregnancy & Breastfeeding use

Pregnancy Category X. This tablet must not be used in women who are or may become pregnant. No studies were performed on animals to evaluate the effects on reproduction with conjugated estrogens/bazedoxifene. This tablet should not be used by lactating women. It is not known whether this drug is excreted in human milk. Detectable amounts of estrogens have been identified in the milk of mothers receiving conjugated estrogens. Estrogen administration to nursing mothers has been shown to decrease the quantity and quality of the milk

Contraindication

Undiagnosed abnormal uterine bleeding Known, suspected, or past history of breast cancer Known or suspected estrogen-dependent neoplasia Active or past history of venous thromboembolism Active or past history of arterial thromboembolism Hypersensitivity (angioedema, anaphylaxis) to estrogens, bazedoxifene, or any ingredients Known hepatic impairment or disease Known protein C, protein S, or antithrombin deficiency or other known thrombophilic disorders Pregnancy, women who may become pregnant, and nursing mothers

Special Warning

Pediatric Use: This tablet is not indicated for use in children.Geriatric Use: This tablet was not studied in women aged 75 or older; use in this population is not recommended. An increased risk of probable dementia in women over 65 years of age was reported in the Women’s Health Initiative Memory ancillary studies of the Women’s Health Initiative.Renal Impairment: This tablet was not studied in women with renal impairment; use in this population is not recommended.Body Mass Index: Women with BMI >27 kg/m 2 may have an increased risk of endometrial hyperplasia.

Acute Overdose

In case of overdosage, there is no specific antidote, and the treatment should be symptomatic. Symptoms of overdosage of estrogen-containing products in adults and children may include nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness/fatigue; withdrawal bleeding may occur.