Bateman D N, Kahn C, Davies D S
Br J Clin Pharmacol. 1980 Apr;9(4):371-7. doi: 10.1111/j.1365-2125.1980.tb01064.x.
1 The pharmacokinetics of metoclopramide have been studied in eight normal male volunteers. 2 The mean plasma beta half-life was 156.7 min after i.v. administration of 10 mg metoclopramide. 3 After oral dosing of 10 mg the mean half-life was 196.6 min and after 20 mg 317.5 min (P less than 0.05). 4 Bioavailability of a 10 mg oral dose of metoclopramide varied between 32 and 97%. 5 A major urinary metabolite was metoclopramide-N-4-sulphate and the amounts of conjugates appearing in urine to 24 h correlated significantly with the bioavailability. 6 In the dog the metabolic fate of metoclopramide is different to man with conjugation being a minor metabolic pathway. The half-life in the dog does not appear to be dose dependent. 7 The wide differences in bioavailability of metoclopramide in man may contribute to the unpredictable occurrence of side effects.
已在8名正常男性志愿者身上研究了甲氧氯普胺的药代动力学。
静脉注射10毫克甲氧氯普胺后，血浆β半衰期的平均值为156.7分钟。
口服10毫克后，平均半衰期为196.6分钟，口服20毫克后为317.5分钟（P小于0.05）。
口服10毫克剂量的甲氧氯普胺的生物利用度在32%至97%之间变化。
主要的尿液代谢产物是甲氧氯普胺-N-4-硫酸盐，24小时内出现在尿液中的结合物量与生物利用度显著相关。
在狗身上，甲氧氯普胺的代谢命运与人不同，结合是次要的代谢途径。狗的半衰期似乎不依赖于剂量。
甲氧氯普胺在人体内生物利用度的广泛差异可能导致副作用的不可预测发生。
