The conversion of d-norgestrel-3-oxime-17-acetate to d-norgestrel in female rhesus monkeys

Add time:08/19/2019    Source:sciencedirect.com

Single intragastric 0.5 mg/kg doses of 14C-d-norgestrel-3-oxime-17-acetate were given to female rhesus monkeys. Rapid absorption was evidenced by peak concentrations of radioactivity in plasma and whole blood within three hours. A multiphasic decline in concentrations of radioactivity then followed. At three and six hours after drug administration, two major metabolites, d-norgestrel and d-norgestrel-3-oxime, and at least five minor metabolites were detected in plasma fractions containing unconjugated metabolites. These accounted for approximately 40% of the plasma radioactivity. d-Norgestrel was also found in plasma fractions containing conjugated metabolites although the major conjugated biotransformation product was a glucuronide of d-3α,5β-tetrahydronorgestrel, previously shown to be the major metabolite of d-norgestrel in humans and the African green monkey. The presence of d-norgestrel was confirmed by chemical ionization mass spectrometric analysis. No d-norgestrel-17-acetate or d-norgestrel-3-oxime-17-acetate was detected in any plasma specimen. d-Norgestrel-3-oxime-17-acetate thus appears to be a “pro drug” that is rapidly deacetylated to d-norgestrel-3-oxime, which is then hydrolyzed to d-norgestrel. Further metabolism of the d-norgestrel was indicated by comparing the plasma metabolite patterns obtained after administration of either d-norgestrel-3-oxime-17-acetate or d-norgestrel to female rhesus monkeys.

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