Breiby M, Aarbakke J, Sundsfjord J, Goussius G, Pape J
Br J Clin Pharmacol. 1983 Dec;16(6):691-4. doi: 10.1111/j.1365-2125.1983.tb02242.x.
Differences in drug kinetics between supine rest and ambulation have been reported, but the relative contribution of postural changes and changes in the level of physical activity has not been evaluated. Ampicillin pharmacokinetics, glomerular filtration rate (GFR) and renal plasma flow (RPF) were studied in six male volunteers at rest in the sitting and lying position with an interval of 1 week. After intravenous administration ampicillin kinetics, analyzed according to a two-compartment open model, demonstrated significant changes in drug distribution when the position was changed from lying to sitting: alpha-increased by 50%, V1 and V beta increased by 19% and 22% respectively. Ampicillin clearance, the fraction of dose recovered from urine, GFR and RPF were, however, not influenced by the change in posture. Our data on effects of posture in resting subjects suggest that previously reported differences in drug elimination and RPF between lying and ambulatory subjects are largely due to differences in the level of physical activity.
已有报道称仰卧休息和走动时药物动力学存在差异,但体位变化和身体活动水平变化的相对贡献尚未得到评估。对6名男性志愿者在坐位和卧位休息时(间隔1周)的氨苄西林药代动力学、肾小球滤过率(GFR)和肾血浆流量(RPF)进行了研究。静脉注射氨苄西林后,根据二室开放模型分析其动力学,结果显示,当体位从卧位变为坐位时,药物分布出现显著变化:α增加50%,V1和Vβ分别增加19%和22%。然而,氨苄西林清除率、从尿液中回收的剂量分数、GFR和RPF不受体位变化的影响。我们关于休息状态下受试者体位影响的数据表明,先前报道的卧位和走动受试者之间药物消除和RPF的差异很大程度上是由于身体活动水平的差异。