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The first uterine pass effect

D De Ziegler1, C Bulletti, B De Monstier

  • 1Columbia Laboratories, Paris, France.

Annals of the New York Academy of Sciences
|November 5, 1997
PubMed
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Vaginal progesterone reliably targets the uterus via direct vagina-to-uterus transport. This "first uterine pass effect" achieves higher uterine concentrations than systemic delivery, suggesting a physiological role in uterine function.

Area of Science:

  • Pharmacology
  • Reproductive Biology
  • Gynecology

Background:

  • Vaginal progesterone demonstrates reliable endometrial effects.
  • A direct vagina-to-uterus transport mechanism is suspected.
  • This pathway may explain targeted uterine delivery.

Purpose of the Study:

  • To investigate the mechanism of vaginal progesterone's endometrial effects.
  • To evaluate the 'first uterine pass effect' for vaginal drug delivery.
  • To explore the physiological role of this effect in uterine function.

Main Methods:

  • Comparison of uterine tissue and plasma progesterone concentrations after vaginal versus systemic administration.
  • Analysis of drug concentration ratios between systemic and uterine tissues.

Related Experiment Videos

  • Review of existing data on vaginal and oral danazol administration.

    • Main Results:

    • Vaginal progesterone administration resulted in uterine tissue concentrations over 10-fold higher than systemic administration.
    • Systemic levels were over 7-fold higher with systemic administration compared to vaginal.
    • Similar concentration differences were observed for danazol administered orally versus vaginally.

    Conclusions:

    • The 'first uterine pass effect' is a significant factor in the targeted delivery of vaginally administered progesterone to the uterus.
    • This mechanism offers a pharmacological advantage for uterine drug delivery.
    • The effect may play a physiological role in regulating uterine contractility via seminal prostaglandins.