Research Article| Volume 40, ISSUE 4, P449-460, October 1989

Pharmacokinetic study of orally administered RU 486 in non-pregnant women

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      A method based on HPLC was devised for the estimation of RU 486 in blood and utilised to study the pharmacokinetics of a single dose of 50 mg RU 486 administered orally to 12 women on day 7 of the cycle. The dose was rapidly absorbed with peak plasma concentration between 1 and 2 hours. Distribution was also rapid (mean tMath Eqα: 1.4h), whereas elimination was slow (mean tMath Eqβ: 28.3 h). RU 486 was still detectable in some women at 72 h after administration. The plasma concentrations fitted the equation for a two-compartment open model from which the pharmacokinetic parameters were calculated. The mean total plasma clearance was 3.0 1/h, and the comparison of our data with those published studies suggests that the pharmacokinetics of RU 486 in Chinese women are similar to those of other populations.
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        • Baulieu EE
        RU 486: an antiprogestin steroid with contragestive activity in women.
        in: Baulieu EE Segal SJ The antiprogestin steroid RU 486 and human fertility control. Plenum Press, New York1985: 1-25
        • Herrmann W
        • Wyss R
        • Riondel A
        • et al.
        Effet d'unstéroide anti-progestérone chez la femme: interruption du cycle menstruel et de la grossesse au début.
        CR Acad Sci (Paris). 1982; 294: 933-938
        • Kovacs L
        • Sas M
        • Resch BA
        • et al.
        Termination of very early pregnancy by RU 486 -an antiprogestational compound.
        Contraception. 1984; 29: 399-410
        • Mishell Jr, DR
        • Shoupe D
        • Brenner PF
        • et al.
        Termination of early gestation with the anti-progestin steroid RU 486: medium versus low dose.
        Contraception. 1987; 35: 307-321
        • Birgerson L
        • Odlind V
        Early pregnancy termination with antiprogestins: a comparative clinical study of RU 486 given in two dose regimens and Epostane.
        Fertil Steril. 1987; 48: 565-570
        • Van Look PFA
        • Bygdeman M
        Antiprogestational steroids: a new dimension in human fertility regulation.
        in: 8 Aufl. Oxford Reviews of Reproductive Biology. Vol. 11. Oxford University Press, Oxford1989 (in press)
        • Ye Z
        • Zhang G
        • Bai X
        High performance liquid chromatographic determination of RU 486 in human plasma.
        Chin J Chromatogr. 1987; 3: 179-182
        • Deraedt R
        • Bonnat C
        • Busigny M
        • et al.
        Pharmacokinetics of RU 486.
        in: Baulieu EE Segal SJ The antiprogestin steroid RU 486 and human fertility control. Plenum Press, New York1985: 103-122
        • Swahn ML
        • Cekan S
        • Wang G
        • Lundstrom V
        • Bygdeman M
        Pharmacokinetic and clinical studies of RU 486 for fertility regulation.
        in: Baulieu EE Segal SJ The antiprogestin steroid RU 486 and human fertility control. Plenum Press, New York1985: 249-258
        • Heikinheimo O
        • Tevilin M
        • Shoupe D
        • Croxatto H
        • Lähteenmäki P
        Quantitation of RU 486 in human plasma by HPLC and RIA after column chromatography.
        Contraception. 1986; 34: 613-624
        • Heikinheimo O
        • Kontula K
        • Croxatto H
        • Spitz I
        • Luukkainen T
        • Lähteenmäki P
        Plasma concentrations and receptor binding of RU 486 and its metabolites in humans.
        J Steroid Biochem. 1987; 26: 279-284
        • Kawai S
        • Nieman LK
        • Brandon DD
        • Udelsman R
        • Loriaux DL
        • Chrousos GP
        Pharmacokinetic properties of the antiglucocorticoid and antiprogesterone steroid RU 486 in man.
        J Pharmacol Exp Ther. 1987; 241: 401-406
        • Lähteenmäki P
        • Heikinheimo O
        • Croxatto H
        • et al.
        Pharmacokinetics and metabolism of RU 486.
        J Steroid Biochem. 1987; 27: 859-863
        • Liu JH
        • Garzo VG
        • Yen SSC
        Pharmacodynamics of the antiprogesterone RU486 in women after oral administration.
        Fertil Steril. 1988; 50: 245-249
        • Heikinheimo O
        Pharmacokinetics of the antiprogesterone RU 486 in women during multiple dose administration.
        J Steroid Biochem. 1989; 32: 21-25
        • Gao J
        • Qiao G-M
        • Wu Y-M
        • et al.
        Pregnancy interruption with RU 486 in combination with dl-15-methyl-prostaglandin F methyl ester: the Chinese experience.
        Contraception. 1988; 38: 675-683
        • Heikinheimo O
        • Lähteenmäki PLA
        • Koivunen E
        • et al.
        Metabolism and serum binding of RU 486 in women after various single doses.
        Hum Reprod. 1987; 2: 379-385