Patwardhan R V, Desmond P V, Johnson R F, Schenker S
J Lab Clin Med. 1980 Apr;95(4):603-8.
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 t1/2 (beta) was significantly prolonged in women on OCS (10.7 +/- 3.0 hr vs. 6.2 +/- 1.6) (p less than 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) that 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 less than 0.05). We conclude that OCS impair the elimination of caffeine.
研究了口服避孕药（OCS）对咖啡因代谢和消除的影响。给13名健康男性、9名未服用OCS的健康女性以及9名正在服用OCS的健康女性口服250毫克咖啡因。与未服用OCS的女性相比，正在服用OCS的女性咖啡因的消除半衰期（t1/2，β）显著延长（分别为10.7±3.0小时和6.2±1.6小时）（p<0.001）。正在服用OCS的女性总血浆清除率（分别为0.79±0.21毫升/分钟/千克和1.3±0.35）及游离清除率（分别为1.12±0.28毫升/分钟/千克和1.97±0.57）显著低于未服用OCS的女性。两组女性的分布容积和血浆结合率相似。将未服用OCS的女性与男性相比，除分布容积外，所有药代动力学参数均相似，女性的分布容积显著更大（p<0.05）。我们得出结论，OCS会损害咖啡因的消除。
