Bazedoxifene Acetate Dose Proportionality in Healthy, Postmenopausal Women

Abstract

Clinical Pharmacology & Therapeutics (2003) 73, P46–P46; doi:

Bazedoxifene + conjugated estrogens in HT for the prevention of osteoporosis and treatment of vasomotor symptoms associated with the menopause

“…Steady state concentrations were achieved by day 7. After intravenous administration of BZA, plasma clearance was 0.4 L/h/kg [19]. Plasma concentrations of BZA increased in a linear fashion with single doses of between 0.5 and 120 mg, and multiple daily doses of between 1 and 80 mg. With once-daily BZA dosing, steady-state concentrations of the drug were reached at the second week, with an accumulation of » 2-fold [19].…”

“…Oral BZA 20 mg was rapidly absorbed in healthy postmenopausal women (n = 23), with t max of » 2 h (range » 1 --4 h) and a mean oral absolute bioavailability of 6% [19]. After administration of multiple doses of once-daily BZA 20 mg, a mean maximum plasma concentration (C max ) of 6.2 ng/ml and a mean area under the plasma concentration-time curve (AUC) of 82 ng·h/ml were reached.…”

“…The absorption of BZA was influenced by food, although this was not considered to be clinically relevant [19]. Following administration of BZA 20 mg with a high-fat meal, C max and AUC were increased by 28 and 22%.…”

Current pharmacotherapy of osteoporosis

“…Dodatkowo stwierdzono u objętych badaniem kobiet brak wpływu leku na grubość endometrium oraz objętość jajników [19]. Skuteczność działania bazedoxifenu została przeanalizowana w randomizowanym, kontrolowanym badaniu z placebo z udziałem 494 zdrowych kobiet po menopauzie [20].…”

“…doses of 20 mg [18]. Moreover, there was no influence of the drug on the thickness of endometrium and on the volume of the ovaries [19]. Efficacy of bazedoxifene was analysed in a randomized, placebo-controlled study including 494 healthy women after menopause [20].…”