CLint values, bioavailability (f), and other pharmacokinetic parameters for selected progestins, determinedin vivo during clinical pharmacokinetic studies with healthy young women
| Compound | In Vivo CLH | fu1-a | In Vivo CLint | E | f | Refs. |
|---|---|---|---|---|---|---|
| liters/hr | % | liters/hr | % | |||
| 3-Keto-desogestrel | 8.7 | 1.8 | 588 | 0.18 | 76 | Backet al., 1987b; Kuhnz et al., 1992c,e |
| 9.5 | 1.8 | 655 | 0.19 | 62 | Orme et al., 1991 | |
| Levonorgestrel | 5.8 | 1.3 | 506 | 0.12 | 100 | Back et al., 1987a |
| 7.1 | 1.3 | 639 | 0.14 | 87 | Hümpelet al., 1987; Kuhnz et al., 1992a,b, 1994b | |
| Gestodene | 3.4 | 1.3 | 281 | 0.07 | 87 | Kuhnz et al., 1992d,e, 1993; Orme et al., 1991; Dibbelt et al., 1992; Heuner et al., 1995 |
| 2.7 | 1.3 | 220 | 0.06 | 99 | Täuber et al., 1989 | |
| Norethisterone | 24 | 3.7 | 1271 | 0.49 | 64 | Back et al., 1977, 1978; Hammond et al., 1982 |
| Dienogest | 3.4 | 10 | 37 | 0.07 | 91 | Oettel et al., 1995 |
| 4.0 | 10 | 44 | 0.08 | 96 | 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.