Disposition of norgestimate in the presence and absence of ethinyl estradiol after oral administration to humans.
The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4 muCi, 0.50 mg) or in combination (73.5 muCi, 0.49 mg) with 3H-ethinyl estradiol (103 muCi, 0.14 mg) in polyethylene glycol 400. Peak levels of radioactivity due to carbon-14 and tritium in plasma occurred within 2 hr after drug administration, followed by distribution and elimination phases. The mean apparent elimination half-life and mean cumulative elimination of radioactivity in the urine and feces following 14C-norgestimate administration were not significantly different than those following administration of the combination dose. Approximately 50% of the administered radioactivity due to carbon-14 was excreted in the urine following administration of 14C-norgestimate both in the presence and absence of coadministered 3H-ethinyl estradiol.
D000284:Administration, Oral; D004338:Drug Combinations; D004347:Drug Interactions; D004997:Ethinyl Estradiol / Q000494:pharmacology*; D005260:Female; D006801:Humans; D007408:Intestinal Absorption; D007700:Kinetics; D009644:Norgestrel / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism
D004338:Drug Combinations; D009644:Norgestrel; D004997:Ethinyl Estradiol; C017576:norgestimate