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Related Experiment Videos

Can grapefruit juice influence ethinylestradiol bioavailability?

A Weber1, R Jäger, A Börner

  • 1Department of Clinical Pharmacology, Friedrich Schiller University of Jena, Germany.

Contraception
|January 1, 1996
PubMed
Summary

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Grapefruit juice significantly increases the bioavailability of 17 alpha-ethinylestradiol (EE2), a key component in many contraceptives. This finding suggests grapefruit may impact EE2 metabolism, warranting further clinical investigation.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Nutritional Science

Background:

  • 17 alpha-ethinylestradiol (EE2) is a synthetic estrogen commonly used in oral contraceptives.
  • The bioavailability of orally administered drugs can be influenced by co-ingested substances, including food and beverages.
  • Grapefruit juice is known to interact with various medications, primarily through inhibition of cytochrome P450 enzymes.

Purpose of the Study:

  • To investigate the effect of grapefruit juice on the bioavailability of 17 alpha-ethinylestradiol (EE2) following oral administration.
  • To compare the pharmacokinetic profile of EE2 when taken with grapefruit juice versus herbal tea.
  • To assess potential alterations in EE2 absorption and metabolism induced by grapefruit juice.

Main Methods:

Keywords:
BiologyContraceptionContraceptive AgentsContraceptive Agents, EstrogenContraceptive Agents, FemaleContraceptive MethodsDietEthinyl EstradiolFamily PlanningHealthMetabolic EffectsNutritionOral ContraceptivesPhysiologyResearch Report

Related Experiment Videos

  • An open-label, randomized, cross-over study design was employed.
  • Thirteen healthy volunteers participated in the study.
  • Participants received a single oral dose of 50 micrograms EE2, administered either with herbal tea or grapefruit juice (containing 887 mg/ml naringin).
  • Pharmacokinetic parameters, including peak plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC0-8), were measured.

    • Main Results:

    • Grapefruit juice significantly increased the peak plasma concentration (Cmax) of EE2 to 137% of the control value (p = 0.0088).
    • The area under the plasma concentration-time curve from 0 to 8 hours (AUC0-8) for EE2 was also significantly increased by grapefruit juice to 128% of the control value (p = 0.0186).
    • In contrast, herbal tea did not produce significant changes in EE2 pharmacokinetics.

    Conclusions:

    • Grapefruit juice significantly enhances the bioavailability of 17 alpha-ethinylestradiol (EE2) after oral administration.
    • The observed increase in EE2 bioavailability is likely due to grapefruit juice inhibiting the metabolic degradation of the drug.
    • Further long-term studies are recommended to determine the clinical significance of this interaction.