A. Balogh et al., INFLUENCE OF ETHINYLESTRADIOL-CONTAINING COMBINATION ORAL-CONTRACEPTIVES WITH GESTODENE OR LEVONORGESTREL, European Journal of Clinical Pharmacology, 48(2), 1995, pp. 161-166
In a controlled clinical trial, the elimination of caffeine was examin
ed in 20 healthy women prior to and during one cycle of treatment with
either of two oral contraceptive formulations, one containing 0.075 m
g gestodene and 0.03 mg ethinylestradiol and one containing 0.125 mg l
evonorgestrel and 0.03 mg ethinylestradiol. In addition, caffeine clea
rance was determined 1 month after the last intake of the oral contrac
eptives. Compared with pretreatment values, the clearance of caffeine
was reduced by about 54% and 55% after one treatment cycle with gestod
ene- and the levonorgestrel-containing oral contraceptive, respectivel
y. Other pharmacokinetic parameters of caffeine, such as t(max) and C-
max were not affected. Clearance values returned to pretreatment value
s 1 month after the last administration of the oral contraceptives. Th
ere was no difference in the reduction of caffeine clearance between c
ontraceptive formulations. A small, but significant difference in the
AUC(0-24 h) values of ethinylestradiol was noted between both preparat
ions. There was no correlation between the AUC(model) values of caffei
ne and the AUC(0-24 h) values of ethinylestradiol. In the present stud
y, a somewhat more pronounced effect on the elimination of caffeine wa
s observed than in previous investigations, where several contraceptiv
e steroids were administered only for a period of 2 weeks.