TY - JOUR
T1 - Intravaginal administration of RU 486 in humans and rats
T2 - Inadequate absorption in humans
AU - Heikinheimo, O.
AU - Croxatto, H.
AU - Salvatierra, A. M.
AU - Chang, C. C.
AU - Luukkainen, T.
AU - Lähteenmäki, P.
PY - 1987/1/1
Y1 - 1987/1/1
N2 - Vaginal absorption of the antiprogesterone steroid RU 486 was studied in humans and rat. In rats, RU 486 was sufficiently absorbed to terminate early pregnancy following vaginal, oral or intramuscular administration. The quantitation of RU 486 in serum showed that the ratios of the areas under the coocentration curves per mg administered were 1:2.8:3.4 for the vaginal, intramuscular and oral routes, respectively. Female voluteers received RU 486 vaginally in polyethylene glycol (PEG) suppositories, In tampons and in oil solution. Following vaginal (PEG-suppository) and oral a administration of 100 mg of RU 486, the ratio of the areas under the serum concentration curves was 1:56, respectively. From tampons and oil, RU 486 was absorbed in a similar manner to that of the PEG-suppositories, resulting in nanomolar serum concentrations. In humans no biological effects were noted following vaginal administration of RU 486. These data suggest that vaginal release of RU 486 is not a successful route of administration in humans.
AB - Vaginal absorption of the antiprogesterone steroid RU 486 was studied in humans and rat. In rats, RU 486 was sufficiently absorbed to terminate early pregnancy following vaginal, oral or intramuscular administration. The quantitation of RU 486 in serum showed that the ratios of the areas under the coocentration curves per mg administered were 1:2.8:3.4 for the vaginal, intramuscular and oral routes, respectively. Female voluteers received RU 486 vaginally in polyethylene glycol (PEG) suppositories, In tampons and in oil solution. Following vaginal (PEG-suppository) and oral a administration of 100 mg of RU 486, the ratio of the areas under the serum concentration curves was 1:56, respectively. From tampons and oil, RU 486 was absorbed in a similar manner to that of the PEG-suppositories, resulting in nanomolar serum concentrations. In humans no biological effects were noted following vaginal administration of RU 486. These data suggest that vaginal release of RU 486 is not a successful route of administration in humans.
KW - Antiprogesterone RU 486
KW - Pharmacokinetics of RU 486
KW - Polyethylene glycol suppository
KW - Vaginal administration of RU 486
UR - http://www.scopus.com/inward/record.url?scp=0023542734&partnerID=8YFLogxK
U2 - 10.1093/oxfordjournals.humrep.a136608
DO - 10.1093/oxfordjournals.humrep.a136608
M3 - Article
C2 - 3437043
AN - SCOPUS:0023542734
SN - 0268-1161
VL - 2
SP - 645
EP - 648
JO - Human Reproduction
JF - Human Reproduction
IS - 8
ER -