W. Kuhnz et B. Lofberg, URINARY-EXCRETION OF 6-BETA-HYDROXYCORTISOL IN WOMEN DURING TREATMENTWITH DIFFERENT ORAL-CONTRACEPTIVE FORMULATIONS, Journal of steroid biochemistry and molecular biology, 55(1), 1995, pp. 129-133
The measurement of the urinary excretion ratio of 6 beta-hydroxycortis
ol (6 beta-OHC)/cortisol was used as a non-invasive method to investig
ate possible changes in the activity of drug-metabolizing enzymes in w
omen receiving different oral contraceptive formulations for 1 up to 3
treatment cycles. The contraceptive preparations were either levonorg
estrel, gestodene or cyproterone acetate, each in combination with eth
inyl estradiol, or only the progestogens levonorgestrel or gestodene.
There was either no or only a small decrease in the 6 beta-OHC/cortiso
l ratio. Thus, only a minor inhibitory effect, if any, can be ascribed
to the investigated contraceptive steroids in vivo. Previously observ
ed differences between selected contraceptive steroids in vitro were n
ot observed in the same way in vivo. This may be due either to the abs
ence of a marked inhibitory activity in vivo or to the insufficient se
nsitivity of the marker 6 beta-OHC/cortisol to detect these changes. A
nother possible reason may be the considerably higher drug concentrati
ons used in the in vitro studies as compared to those present in the s
erum of women under oral contraceptive therapy.