[Time course of inhibition of caffeine elimination in response to the oral depot contraceptive agent Deposiston. Hormonal contraceptives and caffeine elimination]. / Zeitverlauf der Hemmung der Coffeinelimination unter dem Einfluss des oralen Depotkontrazeptivum Deposiston. Hormonale Kontrazeptiva und Coffeinelimination.

In the course of six months, the influence of the oral depot contraceptive, Deposiston (3 mg ethinylestradiol sulphonate and 10 mg norethisterone acetate per menstrual cycle) on the pharmacokinetics of caffeine as a model substance was studied in seven women in intraindividual comparison. The first examination began prior to administration of Deposition. The women were subjected to little challenge as saliva was used as the measuring compartment. Deposiston was found markedly delay the elimination half-life life of caffeine (p less than 0.05): t1/2 prior to therapy 4.9 +/- 2.6 h and, after as little as 2 mg ethinylestradiol sulphonate 8.0 +/- 3.5 h. In contrast to the effect observed for preparations containing less estrogen, these longer half-lives persisted throughout the trial. As expected, the AUC values were slightly elevated during this period, whereas clearance values were reduced.

[Intra-individual comparison of the long term effect of Non-Ovlon on caffeine pharmacokinetics]. / Langzeituntersuchung zum Einfluss von Non-Ovlon auf die Pharmakokinetik von Coffein im intraindividuellen Vergleich.

The effect of the oral contraceptive, Non-Ovlon, on the pharmacokinetics of the model substance, caffeine, was studied in an intraindividual comparison in the course of seven months, i.e. four and two weeks before as well as 0.5, one, three and six months after the women had begun to take the contraceptive. The study commenced in twelve women of which, after seven months, only five were involved. The measuring compartment chosen was saliva so as to minimize strain on the volunteers by this noninvasive approach. Non-Ovlon delayed the caffeine elimination of 4.0 +/- 1.7 hr to 9.0 +/- 4.5 hr and 11.0 +/- 10.4 hr at the end of the first and third intake cycle, respectively. Markedly successive decreases in clearance and an increase in AUC levels were seen in addition to longer half-lives. Interindividual variations were considerable, a finding that might be relevant to the therapy by other, similarly interacting, drugs. There were no differences observed between the initial phase and the median phase of normal menstrual cycle. In one smoker, the caffeine elimination was highly accelerated compared to the average, throughout the period of investigation.