The pharmacokinetics of a large (3 mg) oral dose of ethynylestradiol in women

D J BackA E Schindler


Plasma levels of ethynylestradiol (EE), EE sulphate (EES), EE glucuronide (EEG) and prolactin were measured in women up to 72 h following the oral administration of 3 mg of EE. The decline in plasma EE levels showed a sharp discontinuity at 10 h which is assumed to be due to the beginning of enterohepatic circulation (EHC). After this event, an apparently terminal monoexponential decline was eventually established with a half-life of 13.1 h. As a result of EHC, the volume of distribution was increased by 60% to 6.0 1.Kg-1 but it does not appear that any significant accumulation of EE would occur during multiple dosing. Plasma levels of EES were, on average, 22.5 times greater than those of EE and this circulating metabolite may act as a reservoir of EE. No circulating EEG could be detected. Comparing these results with those previously obtained with 50 microgram EE, there was no evidence of dose dependency in the pharmacokinetics of this steroid. Plasma prolactin levels were markedly enhanced by this single dose of oestrogen.


Oct 1, 1981·Journal of Steroid Biochemistry·D J BackP H Rowe
Jan 1, 1984·Journal of Steroid Biochemistry·H AdlercreutzJ T Korpela
Jan 1, 1989·Pharmacology & Therapeutics·M L OrmeS Ball
Jun 1, 1991·The Journal of Steroid Biochemistry and Molecular Biology·K Fotherby
Jan 27, 2007·Clinical Pharmacokinetics·Hongjian ZhangA David Rodrigues
May 1, 1989·American Journal of Obstetrics and Gynecology·J W Goldzieher
May 1, 1983·American Journal of Obstetrics and Gynecology·J NewburgerJ W Goldzieher
Sep 24, 2016·Journal of Neurosurgery·Harrison KimIrshad H Chaudry
Jul 1, 1985·Contraception·J Newburger, J W Goldzieher
Dec 19, 2013·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Maciej J Zamek-GliszczynskiAleksandra Galetin
Apr 3, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yong-Hae HanA David Rodrigues
Apr 3, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yong-Hae HanA David Rodrigues
Jun 29, 2011·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Maciej J Zamek-GliszczynskiDiane L Phillips
Jan 31, 2002·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Anja Wellejus, Steffen Loft

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