Division of Reproductive Infectious Diseases, Department of Obstetrics, Gynecology, and Reproductive Sciences, Magee-Women's Hospital, University of Pittsburgh Medical Center, Pittsburgh, PA, USA.
Am J Obstet Gynecol. 2011 Jun;204(6 Suppl 1):S84-8. doi: 10.1016/j.ajog.2011.03.002. Epub 2011 Mar 9.
We sought to delineate the pharmacokinetics (PK) of oseltamivir and its active metabolite oseltamivir carboxylate during pregnancy. Physiologic changes of pregnancy, including increased renal filtration and secretion, may increase the clearance of oseltamivir carboxylate. Sixteen pregnant women taking oseltamivir for prophylaxis or treatment of suspected/proven influenza infection were enrolled. Twenty-three nonpregnant reproductive-age females served as the control group. The primary PK endpoint was area under the plasma concentration time curve for oseltamivir carboxylate. Pregnancy did not alter the PK parameters of the parent compound, oseltamivir. However, for oseltamivir carboxylate the area under the plasma concentration time curve was significantly lower (P = .007) and the apparent clearance significantly higher (P = .006) in pregnant women compared with nonpregnant women. Pregnancy produces lower systemic levels of oseltamivir carboxylate. Increasing the dose and/or dosing frequency of oseltamivir during pregnancy may be necessary to achieve comparable exposure in pregnant and nonpregnant women.
我们旨在描述奥司他韦及其活性代谢物奥司他韦羧酸在妊娠期间的药代动力学（PK）。妊娠期间的生理变化，包括肾滤过和分泌增加，可能会增加奥司他韦羧酸的清除率。我们招募了 16 名因预防或治疗疑似/确诊流感感染而服用奥司他韦的孕妇。23 名未怀孕的育龄期女性作为对照组。主要 PK 终点是奥司他韦羧酸的血浆浓度时间曲线下面积。妊娠并未改变母体化合物奥司他韦的 PK 参数。然而，与非孕妇相比，奥司他韦羧酸的血浆浓度时间曲线下面积明显降低（P=0.007），表观清除率明显升高（P=0.006）。妊娠会导致奥司他韦羧酸的全身水平降低。在妊娠期间增加奥司他韦的剂量和/或给药频率可能是必要的，以在孕妇和非孕妇中实现可比的暴露。
