Contraception. 1977 Mar;15(3):307-17.

Steroid contraceptives in non-human primates (II). Metabolic fate of synthetic estrogens in the baboon after exposure to oral contraceptives.

Abstract

PIP:

The metabolism of isotopically labeled ethinyl estradiol (EE) and mestranol (ME) was studied in 3 baboons before and after the simultaneous injection of a norethindrone-mestranol contraceptive formulation. 6 days after the administration of tritiated-EE and carbon-14-ME, the mean urinary excretion of labeled-EE was 38.3-40.8% of the dose, while the excretion of labeled-ME was 17.8-19.8% of the dose. Plasma levels of tritiated-EE did not differ markedly between the follicular and luteal phases of the cycle. 24 hours after injection, plasma levels of tritiated-EE remained at levels more than 7% of the dose, which was considerably higher than recorded before administration of norethindrone-mestranol. In contrast, carbon-14-ME levels 24 hours after injection did not differ markedly from those found before treatment with norethindrone-mestranol. The results suggest that orally administered ME is demethylated to EE in primates.

PMID:: 880810; [PubMed - indexed for MEDLINE]

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