Pharmacokinetics of an oral contraceptive containing oestradiol valerate and dienogest.

Full Abstract

OBJECTIVE: To evaluate the pharmacokinetics of a combined oral contraceptive (OC) containing oestradiol valerate/dienogest (E2V/DNG) administered according to a four-phasic dosing regimen with an oestrogen step-down and a progestin step-up over 26 days of active treatment. METHODS: This Phase I, open-label study included healthy women aged 18-50 years. Treatment consisted of the administration of E2V 3 mg for 2 days, E2V 2 mg/DNG 2 mg for 5 days, E2V 2 mg/DNG 3 mg for 17 days, E2V 1 mg for 2 days, and placebo for 2 days. RESULTS: Pharmacokinetic data were analysed in 15 women. Stable E2 concentrations were maintained throughout the study. Minimum mean serum E2 levels were 33.6-64.7 pg/ml during E2V administration. The ratio of oestrone:E2 in serum was approximately 5:1. Minimum mean serum DNG levels were 6.8-15.1 ng/ml during DNG administration. Minimum concentrations of DNG increased only slightly during each phase of the regimen during which DNG was being administered. On day 24 the geometric mean C(max), C(ave) and t((1/2)) of DNG were 82.9 ng/ml, 33.7 ng/ml and 12.2 hours, respectively; the median t(max) was 1.5 hours. Serum sex hormone-binding globulin concentrations increased by 40% (within the normal range). Cortisol binding-globulin levels remained almost unchanged. Treatment was well tolerated. CONCLUSIONS: Treatment with an OC containing E2V and DNG was well tolerated and was associated with stable E2 concentrations over 28 days. The pharmacokinetics of DNG were consistent with previous findings. Minimum serum concentrations of DNG increased only slightly during phases of the regimen during which DNG was administered.

Author information

Author/s: Zeun, Susan (S); Lu, Ming (M); Uddin, Alkaz (A); Zeiler, Brian (B); Morrison, Dennis (D); Blode, Hartmut (H);

Affiliation: Bayer Schering Pharma AG, Berlin 13342, Germany. susan.zeun(-atsign-)bayerhealthcare.com

Journal and publication information

Publication Type: Clinical Trial, Phase I; Journal Article; Research Support, Non-U.S. Gov't

Journal: The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception (Eur J Contracept Reprod Health Care), published in England. (Language: eng)

Reference: 2009-Jun; vol 14 (issue 3) : pp 221-32

Dates: Created 2009/06/30; Completed 2009/10/08;

PMID: 19565420, status: MEDLINE (last retrieval date: 10/8/2009, IMS Date: )

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Adolescent
Adult
Carrier Proteins - blood
Contraceptives, Oral - adverse effects; blood; pharmacokinetics
Drug Administration Schedule
Drug Combinations
Estradiol - adverse effects; analogs & derivatives; blood; pharmacokinetics
Female

Female
Headache - chemically induced
Humans
Middle Aged
Nandrolone - adverse effects; analogs & derivatives; blood; pharmacokinetics
Radioimmunoassay
Sex Hormone-Binding Globulin - analysis
Young Adult

Associated Chemicals: Carrier Proteins (0) ; Contraceptives, Oral (0) ; Drug Combinations (0) ; Sex Hormone-Binding Globulin (0) ; cortisol binding globulin (0) ; Nandrolone (434-22-0) ; Estradiol (50-28-2) ; dienogest (65928-58-7) ; estradiol valerate (979-32-8)

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