Impact of Menopause on Pharmacokinetics of Rosuvastatin Compared with Premenopausal Women

Abstract

Background and objective: Rosuvastatin is used to treat dyslipidemia and its use is quite frequent among postmenopausal women. Menopause significantly affects the pharmacokinetics of drugs, and altered drug response and therapeutic efficacy may be anticipated in postmenopausal women compared with premenopausal women. The current study is based on assessment of differences in pharmacokinetics of rosuvastatin between pre- and postmenopausal women of Asian ethnicity.

Methods: Volunteers were administered a single oral dose of rosuvastatin 40 mg in an open-label and non-controlled pharmacokinetic study. A reversed-phase HPLC method was applied for quantification of rosuvastatin in plasma samples. Student's t test was used to compare the pharmacokinetic parameters of rosuvastatin between pre- and postmenopausal women at the 95 % confidence interval.

Results: The C max (premenopausal = 58.2 ± 29.1, postmenopausal = 12.2 ± 3.1 ng/ml), [Formula: see text] (premenopausal = 272.6 ± 107.3 ng·h/ml, postmenopausal = 58.8 ± 16.6 ng·h/ml), and [Formula: see text] (premenopausal = 366.1 ± 169, postmenopausal = 66.4 ± 12.9 ng·h/ml) of rosuvastatin were significantly higher (p < 0.05) in premenopausal compared with postmenopausal women. The Vd/F of rosuvastatin was significantly higher (p < 0.05) in postmenopausal women compared with women, and CL/F was also significantly (p < 0.05) faster in postmenopausal women when compared at the 95 % confidence interval.

Conclusion: Rosuvastatin plasma level was significantly higher in premenopausal compared with postmenopausal women, which raises the question whether the latter are getting due therapeutic results, as after the menopause women experience more frequent cardiovascular problems and dyslipidemia.