Schuhmann-Giampieri G, Krestin G
Schering AG, Berlin, Federal Republic of Germany.
Invest Radiol. 1991 Nov;26(11):975-9. doi: 10.1097/00004424-199111000-00009.
We investigated the pharmacokinetics of dimeglumine gadopentetate (Gd-DTPA), a contrast agent for magnetic resonance imaging (MRI), in 24 patients with chronic renal failure whose creatinine clearance ranged from 7.2 to 70.0 mL/minute (median 25.4 mL/minute). After single intravenous administration of 0.1 mmol/kg, the serum levels of Gd-DTPA were monitored up to five days and urine and feces were collected quantitatively up to two days. The pharmacokinetic parameters were calculated from the concentration-time profile in the serum and urine using an open two-compartment model. No changes in the volume of distribution (Vc and Varea) or in the half-life of distribution were found for patients with chronic renal failure as compared to patients with normal renal function. However, in correlation with the reduced glomerular filtration rate in patients with chronic renal failure, the half-life of elimination was prolonged and serum and renal clearance were decreased. The recovery of Gd-DTPA in urine was 92.1% +/- 12.1% of the dose administered, and extrarenal elimination was less than 0.4%, indicating that glomerular filtration remains the predominant route of elimination. Only for patients with highly impaired renal function (creatinine clearance less than 20 mL/minute) was the recovery in the urine less than complete.
我们对24例慢性肾衰竭患者进行了钆喷酸葡胺(Gd-DTPA,一种用于磁共振成像(MRI)的造影剂)的药代动力学研究,这些患者的肌酐清除率在7.2至70.0毫升/分钟之间(中位数为25.4毫升/分钟)。单次静脉注射0.1 mmol/kg后,监测Gd-DTPA的血清水平长达5天,并定量收集尿液和粪便长达2天。使用开放二室模型根据血清和尿液中的浓度-时间曲线计算药代动力学参数。与肾功能正常的患者相比,慢性肾衰竭患者的分布容积(Vc和Varea)或分布半衰期没有变化。然而,与慢性肾衰竭患者肾小球滤过率降低相关的是,消除半衰期延长,血清清除率和肾清除率降低。Gd-DTPA在尿液中的回收率为给药剂量的92.1%±12.1%,肾外消除率小于0.4%,这表明肾小球滤过仍然是主要的消除途径。仅对于肾功能严重受损(肌酐清除率小于20毫升/分钟)的患者,尿液中的回收率不完全。