Pharmacokinetic profile of nomegestrol acetate and 17β-estradiol after multiple and single dosing in healthy women.
BACKGROUND
The pharmacokinetics of the monophasic oral contraceptive nomegestrol acetate (NOMAC) plus 17β-estradiol (E(2)) were investigated after a single dose and multiple dosing.


METHODS
NOMAC/E2 (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 (Cmax, 12.3±3.5 ng/mL) was reached in mean 1.5 h (t(max)); the mean±SD elimination half-life (t(½)) was 45.9±15.3 h. After a single dose, NOMAC mean±SD C(max) was 7.2±2.0 ng/mL and mean±SD t(½) was 41.9±16.2 h. On Day 24, E2 mean±SD C(av) was 50.3±25.7 pg/mL; mean±SD Cmax was 86.0±51.3 pg/mL. After a single dose, mean±SD E2 Cmax was 253±179 pg/mL.


CONCLUSIONS
These data demonstrate that NOMAC/E2 has a pharmacokinetic profile consistent with once-daily dosing.
Merck Sharp & Dohme, 5340 BH Oss, The Netherlands. mireille.gerrits@merck.com
Mireille G F
MG
Gerrits
Peter G
PG
Schnabel
Teun M
TM
Post
Pierre A M
PA
Peeters
D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D003277:Contraceptives, Oral, Combined / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D004958:Estradiol / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D004970:Estrone / Q000097:blood; D005260:Female; D006801:Humans; D008535:Megestrol / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D008875:Middle Aged; D009649:Norpregnadienes / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*
D003277:Contraceptives, Oral, Combined; D009649:Norpregnadienes; D004970:Estrone; D004958:Estradiol; C038501:nomegestrol acetate; D008535:Megestrol