Pharmacokinetic profile of nomegestrol acetate and 17β-estradiol after multiple and single dosing in healthy women
| Autor: | Pierre A. M. Peeters, Peter G. Schnabel, Teun M. Post, Mireille Gerrits |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Nomegestrol acetate
Adult medicine.medical_specialty Norpregnadienes Adolescent Estrone Population Cmax Biological Availability Pharmacology Multiple dosing chemistry.chemical_compound Pharmacokinetics Internal medicine Medicine Humans Dosing education education.field_of_study Estradiol business.industry Obstetrics and Gynecology Half-life Megestrol Middle Aged Pharmacokinetic analysis Contraceptives Oral Combined Endocrinology Reproductive Medicine chemistry Female business |
| Zdroj: | Contraception. 87(2) |
| ISSN: | 1879-0518 |
| Popis: | BACKGROUND: The pharmacokinetics of the monophasic oral contraceptive nomegestrol acetate (NOMAC) plus 17beta-estradiol (E(2)) were investigated after a single dose and multiple dosing. STUDY DESIGN: 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((1/2))) 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((1/2)) 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. Copyright (c) 2013 Elsevier Inc. All rights reserved. |
| Databáze: | OpenAIRE |
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