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Bioavailability and pharmacokinetics of cyproterone acetate after oral administration of 2.0 mg cyproterone acetate in combination with 50 micrograms ethinyloestradiol to 6 young women



Bioavailability and pharmacokinetics of cyproterone acetate after oral administration of 2.0 mg cyproterone acetate in combination with 50 micrograms ethinyloestradiol to 6 young women



Contraception 15(5): 579-588



The bioavailability and pharmokinetics of cyproterone acetate (CA) were studied in 6 healthy young women. The subjects received a single oral dose of 2 mg carbon-14-CA plus 50 mcg tritiated-ethinyl estradiol. Matimum plasma levels of CA were observed about 4 hours after administration. During the 4-10 hours following administration, carbon-14-CA in plasma disappeared with a half-life of 3 + or -1.6 hours. The half-life for the subsequent phase of disposition was 1.7 + or -.5 days. The apparent volume of distribution for CA was 1300 + or -580 liters. Although plasma equivalents of carbon-14-CA had higher absolute values, the course of their distribution was similar to those concentrations for the unchanged drug. 88 + or -11% of the dose was recovered and 30.4 + or -7.3 excreted in urine. The concentration of the primary metabolite of CA in plasma showed a decline which paralleled the terminal disposition phase of CA; the elmination half-life being 1.8 + or -.1 days. The apparent distribution volume for the primary metabolite was 95 + or -25 liters. CA, in comparison with its primary metabolite, had 10 times the apparent distribution volume. Approximately 90% of CA was present at all times following administration. In terms of total activity, the proportion of CA in plasma remained constant 1/2 day after administration. It is suggested that the transfer of CA from tissues determines the rate of metabolization of CA and the excretion of metabolites.

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Accession: 068537063

Download citation: RISBibTeXText

PMID: 880829

DOI: 10.1016/0010-7824(77)90108-1


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