Bazedoxifeno

Bazedoxifeno Uses, Dosage, Side Effects, Food Interaction and all others data.

Bazedoxifeno 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.

Trade Name Bazedoxifeno
Generic Bazedoxifene
Bazedoxifene Other Names Bazedoxifene, Bazedoxifeno
Type
Formula C30H34N2O3
Weight Average: 470.613
Monoisotopic: 470.256942963
Protein binding

98-99%.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Bazedoxifeno
Bazedoxifeno

Uses

Bazedoxifeno is a selective estrogen receptor modulator (SERM) used to treat moderate to severe vasomotor symptoms in menopause and osteoporosis alone or in combination with conjugated estrogens.

Indicated for following conditions alone or in combination with conjugated estrogens in women with a uterus:

  • Treatment of moderate to severe vasomotor symptoms associated with menopause

  • Prevention of postmenopausal osteoporosis

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

How Bazedoxifeno works

Bazedoxifeno belongs to a class of compounds known as selective estrogen receptor modulators (SERMs). Bazedoxifeno acts as both an oestrogen-receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifeno 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. Bazedoxifeno functions primarily as an oestrogen-receptor antagonist in uterine and breast tissues.

Food Interaction

  • Administer calcium supplement. If calcium intake from food is inadequate administer calcium supplements to prevent hypocalcemia.
  • Administer vitamin supplements. If dietary intake of vitamin D is inadequate, then administer vitamin D supplements to avoid deficiency of vitamin D and calcium.
  • Take at the same time every day.
  • Take with or without food. Taking bazedoxifene with food may increase its AUC by 25% but does not impact the Cmax.

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

Bazedoxifeno 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.

Innovators Monograph

You find simplified version here Bazedoxifeno

*** Taking medicines without doctor's advice can cause long-term problems.
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