Pharmacokinetic profile of nomegestrol acetate and 17β-estradiol after multiple and single dosing in healthy women

Background: The pharmacolcinefics of the monophasic oral contraceptive nomegestrol acetate (NOMAC) plus 17 beta-estradiol (E-2) were investigated after a single dose and multiple dosing. Study design: NOMAC/E-2 (2.5 mg/1.5 mg) was administered daily to healthy women (18-50 years, n=23) for 24 days; blood samples for pharmacokinetic analysis were obtained on Day 24 and again, after a 10-day pill-free interval, on Day 35 after a single dose. Results: NOMAC reached steady state after 5 days with mean +/- standard deviation (SD) trough NOMAC concentration (C-av) of 4.4 +/- 1.4 ng/mL. On Day 24, mean +/- SD peak NOMAC concentration (C-max, 12.3 +/- 3.5 ng/mL) was reached in mean 1.5 h (t(max)); the mean +/- SD elimination half-life (t(1/2)) was 45.9 +/- 15.3 h. After a single dose, NOMAC mean +/- SD C-max was 7.2 +/- 10 ng/mL and mean SD t1/2 was 41.9 +/- 16.2 h. On Day 24, E-2 mean +/- SD C, was 50.3 +/- 25.7 pg/mL; mean +/- SD C-max was 86.0 +/- 51.3 pg/mL. After a single dose, mean +/- SD E-2 C-max was 253 +/- 179 pg/mL. Conclusions: These data demonstrate that NOMAC/E-2 has a pharmacokinetic profile consistent with once-daily dosing. (C) 2013 Elsevier Inc. All rights reserved.