Pharmacokinetics of etonogestrel released from the contraceptive implant Implanon.
Eight healthy women between 22 and 40 years of age participated in this prospective open study of 2 years' duration. Either on or between days 1 to 7 of a spontaneous menses, an intravenous bolus dose of 150 micrograms etonogestrel (3-ketodesogestrel) was given. During days 1-5 of a subsequent spontaneous cycle, the single-rod contraceptive implant (Implanon) was inserted in the upper arm of the volunteer. One year after placement of the implant, another intravenous bolus dose was given (implant in place), and a third bolus dose was given after 2 years, with the implant removed. Frequent serum sampling immediately after the intravenous dosings of etonogestrel was done to study the primary pharmacokinetic parameters, i.e., volume of distribution and clearance, allowing the calculation of the absorption rate and bioavailability of the implant, as a function of time. Results showed that etonogestrel released from Implanon has an absorption rate of approximately 60 micrograms/day after 3 months, which slowly decreases to 30 micrograms/day at the end of 2 years. The bioavailability over this period of time was constant and close to 100%. The clearance remained around 7.5 L/h. With a bioavailability and clearance that remained constant, it may be concluded that there is no accumulation of etonogestrel.
Wenzl
R
R
University of Vienna, General Hospital, Department of Obstetrics and Gynecology, Austria.
van Beek
A
A
Schnabel
P
P
Huber
J
J
D000042:Absorption; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D003271:Contraceptive Agents, Female / Q000493:pharmacokinetics*; D017135:Desogestrel; D004343:Drug Implants; D005260:Female; D006207:Half-Life; D006801:Humans; D011446:Prospective Studies; D011863:Radioimmunoassay; D014753:Vinyl Compounds / Q000493:pharmacokinetics*
D003271:Contraceptive Agents, Female; D004343:Drug Implants; D014753:Vinyl Compounds; C044815:etonogestrel; D017135:Desogestrel