Ell C, Braun J, König H J, Domschke S, Domschke W
Klin Wochenschr. 1985 Jun 18;63(12):572-4. doi: 10.1007/BF01733203.
The pharmacokinetics of high-dose metoclopramide (10 mg/kg body wt. in five infusions of 2 mg/kg body wt. each) was studied in 11 patients (5 females, 6 males) in two groups: group A with and group B (consisting of five patients) without forced diuresis. When the drug was infused, forced diuresis had no influence on the pharmacokinetics of metoclopramide (serum level after the 1st infusion was 851 +/- 361 ng/ml in group A versus 840 +/- 348 ng/ml in group B; after the 5th infusion it was 2,005 +/- 588 ng/ml in group A versus 2,463 +/- 1,350 ng/ml in group B). There were significant differences in the 24-h serum levels (582 +/- 308 ng/ml in group A versus 379 +/- 170 ng/ml in group B; P less than 0.05) and in the elimination half life (8.5 +/- 2.6 h in group A versus 6.1 +/- 1.1 h in group B; P less than 0.05). The results demonstrate that the dosage regimen originally suggested by Gralla for cytostatic drugs, with forced diuresis for high-dose metoclopramide therapy, may also be applied, with no dosage reduction, with to other cytostatic drugs which do not require forced diuresis.
在11名患者（5名女性，6名男性）中，分两组研究了大剂量甲氧氯普胺（每次2mg/kg体重，共五次输注，总量10mg/kg体重）的药代动力学：A组进行强制利尿，B组（由5名患者组成）不进行强制利尿。当输注药物时，强制利尿对甲氧氯普胺的药代动力学没有影响（A组第一次输注后的血清水平为851±361ng/ml，B组为840±348ng/ml；第五次输注后，A组为2005±588ng/ml，B组为2463±1350ng/ml）。24小时血清水平（A组为582±308ng/ml，B组为379±170ng/ml；P<0.05）和消除半衰期（A组为8.5±2.6小时，B组为6.1±1.1小时；P<0.05）存在显著差异。结果表明，格拉拉最初为细胞毒性药物建议的给药方案，即大剂量甲氧氯普胺治疗时进行强制利尿，也可在不减量的情况下应用于其他不需要强制利尿的细胞毒性药物。
