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Impaired elimination of caffeine by oral contraceptive steroids

  • Rashmi V. Patwardhan
    Affiliations
    From the Department of Medicine, Vanderbilt University School of Medicine and Nashville Veterans Administration Medical Center, Nashville, Tenn., USA
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  • Paul V. Desmond
    Affiliations
    From the Department of Medicine, Vanderbilt University School of Medicine and Nashville Veterans Administration Medical Center, Nashville, Tenn., USA
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  • Raymond F. Johnson
    Affiliations
    From the Department of Medicine, Vanderbilt University School of Medicine and Nashville Veterans Administration Medical Center, Nashville, Tenn., USA
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  • Steven Schenker
    Correspondence
    Reprint requests: Steven Schenker, M.D., V. A. Medical Center, 1310 24th Avenue South, Nashville, Tenn. 37203.
    Affiliations
    From the Department of Medicine, Vanderbilt University School of Medicine and Nashville Veterans Administration Medical Center, Nashville, Tenn., USA
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      Abstract

      The effect of OCS on the disposition and elimination of caffeine was examined. Caffeine (250 mg) was administered orally to 13 healthy males, nine healthy females taking no OCS, and nine healthy females on OCS. The Math Eq was significantly prolonged in women on OCS (10.7 ± 3.0 hr vs. 6.2 ± 1.6) (p < 0.001) as compared to women taking no OCS. Women on OCS had a significantly lower total plasma clearance (0.79 ± 0.21 ml/min/kg vs. 1.3 ± 0.35) and free clearance (1.12 ± 0.28 ml/min/kg vs. 1.97 ± 0.57) than women not taking OCS. Volumes of distribution and plasma binding were similar in both groups of females. When women taking no OCS were compared with men, all pharmacokinetic parameters were similar except for volume of distribution, which was significantly larger in the women (p < 0.05). We conclude that OCS impair the elimination of caffeine.

      Abbreviations:

      oral contraceptive steroids (OCS), elimination half-life (t12(β)), aminopyrine breath test (ABT)
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