Table 1

CLint values, bioavailability (f), and other pharmacokinetic parameters for selected progestins, determinedin vivo during clinical pharmacokinetic studies with healthy young women

CompoundIn Vivo CLHfu1-aIn Vivo CLintEfRefs.
liters/hr % liters/hr %
3-Keto-desogestrel8.71.85880.1876 Backet al., 1987b; Kuhnz et al., 1992c,e
9.51.86550.1962 Orme et al., 1991
Levonorgestrel5.81.35060.12100 Back et al., 1987a
7.11.36390.1487 Hümpelet al., 1987; Kuhnz et al., 1992a,b, 1994b
Gestodene3.41.32810.0787 Kuhnz et al., 1992d,e, 1993; Orme et al., 1991; Dibbelt et al., 1992; Heuner et al., 1995
2.71.32200.0699 Täuber et al., 1989
Norethisterone243.712710.4964 Back et al., 1977, 1978; Hammond et al., 1982
Dienogest3.410370.0791 Oettel et al., 1995
4.010440.0896 Oettel et al., 1995
  • If more than one study was published, the mean values for the parameters (f and in vivo CLint) were used for the in vitro-in vivo correlations (figs. 2, 3, and5).

  • 1-a fu, unbound fraction; E, extraction ratio.