Ethinylestradiol/Progestogen Tables:
Pharmacokinetics
(E: Ethinylestradiol, L: Levonorgestrel*)
| Bioavailability |
Peak plasma level |
Plasma half-life |
Active metabolites |
Elimination |
E: great variability
L: variable |
in average 40%
> 90% |
E/L: 1 to 2 hours |
E: 6 to 20 hours
L: 11 to 45 hours |
E/L: none |
E/L: predominantly hepatic |
|
*Levonorgestrel as an example; desogestrel and norgestimate are biologically
nearly inactive 'prodrugs' and have (just like gestodene) a greater variability
in their bioavailability. Otherwise, their kinetics are nor significantly different.
Estrogens and progestogens mutually influence each others' kinetics.
Dose
| Indication |
Administration |
| Initial loading dose |
| Dose |
Interval |
|
|
| Maintenance dose |
| Dose |
Interval |
|
|
| contraception |
oral |
E: 20-35 µg*
L: 150 µg** |
24 hours*** |
E: 20-50 µg*
L: 150 µg** |
24 hours*** |
|
*Administration of smallest possible dose of ethinylestradiol should be targeted (not higher than 50 µg).
**Other progestogens: desogestrel 150 µg, gestogene 75 µg, norethisterone 500 µg, norgestimate 250 µg.
***Administration must be synchronized with the cycle for 21 days, then 7-day break.
Copyright © 1996 Infomed-Verlags
AG