Intravaginal administration of RU 486 in humans and rats: Inadequate absorption in humans

O. Heikinheimo, H. Croxatto, A. M. Salvatierra, C. C. Chang, T. Luukkainen, P. Lähteenmäki

Resultado de la investigación: Article

11 Citas (Scopus)

Resumen

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.

Idioma originalEnglish
Páginas (desde-hasta)645-648
Número de páginas4
PublicaciónHuman Reproduction
Volumen2
N.º8
DOI
EstadoPublished - 1 ene 1987

Huella dactilar

Intravaginal Administration
Mifepristone
Suppositories
Oils
Serum
Area Under Curve
Oral Administration
Steroids
Pregnancy

ASJC Scopus subject areas

  • Reproductive Medicine
  • Rehabilitation
  • Obstetrics and Gynaecology

Citar esto

Heikinheimo, O. ; Croxatto, H. ; Salvatierra, A. M. ; Chang, C. C. ; Luukkainen, T. ; Lähteenmäki, P. / Intravaginal administration of RU 486 in humans and rats : Inadequate absorption in humans. En: Human Reproduction. 1987 ; Vol. 2, N.º 8. pp. 645-648.
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abstract = "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.",
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Heikinheimo, O, Croxatto, H, Salvatierra, AM, Chang, CC, Luukkainen, T & Lähteenmäki, P 1987, 'Intravaginal administration of RU 486 in humans and rats: Inadequate absorption in humans', Human Reproduction, vol. 2, n.º 8, pp. 645-648. https://doi.org/10.1093/oxfordjournals.humrep.a136608

Intravaginal administration of RU 486 in humans and rats : Inadequate absorption in humans. / Heikinheimo, O.; Croxatto, H.; Salvatierra, A. M.; Chang, C. C.; Luukkainen, T.; Lähteenmäki, P.

En: Human Reproduction, Vol. 2, N.º 8, 01.01.1987, p. 645-648.

Resultado de la investigación: Article

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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.

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