Stacher G, Steinringer H, Schneider C, Vacariu-Granser G V, Castiglione F, Gaupmann G, Weber U, Stacher-Janotta G
Psychophysiology Unit, University of Vienna, Austria.
Dig Dis Sci. 1992 Feb;37(2):198-204. doi: 10.1007/BF01308172.
This crossover, double-blind study investigated the effects of single oral doses of the prodrug loperamide oxide, which is reduced gradually to loperamide in the intestine, and loperamide on jejunal motor activity in 12 fasting healthy men. Five minutes after a phase III of the migrating motor complex (MMC), 2 mg loperamide oxide, 4 mg loperamide oxide, 4 mg loperamide, or placebo were administered. Thereafter, motor activity 10-30 cm abroad the ligament of Treitz was recorded with five catheter orifices at 3-cm intervals over 4 hr. Number of contractions and area under curve increased significantly with 4 mg loperamide and 4 mg loperamide oxide, the increases with loperamide oxide occurring more gradually. Placebo and 2 mg loperamide oxide had no discernible effects. With both 4 mg loperamide and 4 mg loperamide oxide, phase I of the MMC was slightly prolonged and phase II and the time from drug administration to the onset of the first phase III slightly shortened. The percentage of aborally propagated contractions in phase II increased with all active treatments, whereas the occurrence of phases III was not altered.
这项交叉双盲研究调查了单次口服前体药物氧化洛哌丁胺（在肠道中逐渐还原为洛哌丁胺）和洛哌丁胺对12名空腹健康男性空肠运动活性的影响。在移行性运动复合波（MMC）的Ⅲ期后5分钟，给予2毫克氧化洛哌丁胺、4毫克氧化洛哌丁胺、4毫克洛哌丁胺或安慰剂。此后，在4小时内，用五个相距3厘米的导管孔记录屈氏韧带外10 - 30厘米处的运动活性。4毫克洛哌丁胺和4毫克氧化洛哌丁胺使收缩次数和曲线下面积显著增加，氧化洛哌丁胺的增加更为缓慢。安慰剂和2毫克氧化洛哌丁胺没有明显作用。4毫克洛哌丁胺和4毫克氧化洛哌丁胺均使MMC的Ⅰ期略有延长，Ⅱ期以及从给药到首个Ⅲ期开始的时间略有缩短。所有活性治疗均使Ⅱ期向口传播的收缩百分比增加，而Ⅲ期的出现没有改变。
